Emergence of irreversible modulation in drug discovery




Call for abstracts closed

The call for abstracts is now closed. We will let abstract authors know if their abstracts have been accepted soon.

About the event

Irreversible covalent modulation is a crucial part of the drug discovery toolbox and is an important strategy for finding tractable equity against less druggable targets. However, understanding the binding kinetics, mechanistic PK/PD relationship and SAR of compounds is critical to success as is employing best practice in hit identification and lead optimisation.

Join us in Cambridge on 16-17 October 2024, where we will bring together established leaders and emerging investigators exploring the use of irreversible covalent modulators in drug discovery. Targeting of both cysteine and other amino acid residues will be considered as will in depth analysis of the kinetics of irreversible inhibition. Irreversible modulation as a strategy for targeted protein degradation and the identification of covalent chemical equity through proteomic approaches will also be covered.

Learning outcomes:
Our expectation is that the meeting may serve to:

1). Build a network amongst research interested in irreversible modulation in drug discovery
2). Establish the framework for understanding kinetics in drug discovery for irreversible binders
3). Enable researchers to better understand and optimise chemical tools, leads and drug candidates

Session recordings will also be made available to registrants.


                             Day 1: In vitro approaches to irreversible modulation
 
09:00 –10.15    Registration and coffee
10.15 – 10:30 Welcome and introduction
Bharath Srinivasan, Principal Scientist, AstraZeneca 
                                                          Session one
                                                Chair: Dr Maria Flocco 

    Vice President, Global Head of Mechanistic & Structural Biology, AstraZeneca
10:30 – 11.00 David Mann, Imperial College London
"Identifying and developing covalent fragment hits for targeted therapeutics"
11.00 – 11.15 OC1: Fangyuan Cao 
"Discovery of Small Molecule Activity-Based Probes (ABPs) for the Deubiquitinating Enzymes (DUBs)"
11:15 – 11.45 Ivan Cornella, Covant Therapeutics
 “Leaving a mark: Harnessing covalency to target native disease         proteoforms”
11.45 – 12.05 Fidabio - Partner session
Speaker: Henrik Jensen, CSO
"In-solution binding kinetics with 1st principle technology FIDA"
12.05 - 13:30 Lunch & Poster session
                                                           Session two
                                                    Chair: Dr Jacob Bush
                                                Director, GlaxoSmithKline
13:30 –14:00 Nir London, Weizman Institute of Science
“New functions for covalent binders”
14:00 –14:15 OC2: Julian Chesti
"High-Throughput Modular Syntheses and Biological Evaluation of Structurally-Diverse Reactive Fragment Libraries"
14:15 – 14:45 Andrea Gohlke, AstraZeneca
“Electrophile first lead generation for an intractable target”
14.45 – 15.05  Enzymlogic - Partner session 
Speaker: Ana Corrionero
“Decoding Irreversible Drug Kinetics: COVALfinder® case studies”
15.05 - 15:30 Coffee break
                                               Session 3: Beyond cysteine
                                                   Chair: Susan Critchlow
                                             Executive Director, AstraZeneca
15:30 – 16:00 Emma Grant, GlaxoSmithKline
“Reactive fragment platforms for covalent hit ID”
16:00 – 16:15 OC3: Tao Sun 
"DCAF16-based Covalent Molecular Glues for Targeted Protein Degradation of Histone Deacetylases (HDACs)"
16:15 -  16:45  Lyn Jones, Dana-Farber Cancer Institute
"Covalent Drug Development - Targeting Cysteine and Beyond"
16:45 – 17:00 Closing remarks
17:00 – 19:30 Drinks and networking reception
 
                           Day 2: Cellular approaches to irreversible inhibition
 
09:30 – 09:55 Registration and coffee
09:55 – 10:10 Welcome and introduction
                                                          Session one
                                               Chair: David Wilson, PhD
                       VP & Global Head, Oncology Chemistry, Astra Zeneca 
10:10–10:30   Pelago Bioscience – Partner Session
  Speaker: Isabel Martin Caballero
  “The Cellular Thermal Shift Assay, How assessment of target       engagement helps identify early liabilities”
10:30 –11:00 Megan Matthews, University of Pennsylvania 
"The revolution and evolution of activity-based protein profiling"
11:00 – 11:30 Dr Peter Cossar, Eindhoven University of Technology
"
Reversible Dual-Covalent Molecular Locking of the 14-3-3/ERRγ Protein-Protein Interaction as a Molecular Glue Drug Discovery Approach"
11:30– 11:45 OC4: George Hughes 
"Expanding “electrophile-first” hit ID into 10K+ lead-like covalent libraries"
11:45 – 12:05  OmicScouts - Partner session
Speaker: Christin Zasada, Head of Computational Biology
“Cellular Turnover of Covalent Drug Targets”
12:05 - 13:05 Lunch & Poster session
                                                            Session two
                                                     Chair: Richard Ward
         Executive Director, Oncology Search & Evaluation Group, AstraZeneca
13:05 – 13:35    Matt Patricelli, Vividion Therapeutics
"Lessons and learnings from 8 years of chemoproteomics-centered drug discovery"
13:35 – 14:05 Bradley Pentelute, MIT Chemistry
"Advancing Covalent Peptide Inhibitors through ReAct-ASMS"
14:05 – 14:20 OC5: Hugues Lemoine
"Design, synthesis and reactivity profiling of novel covalent libraries for chemical biology and drug discovery"
14:20 – 14:40 WuXi AppTec - Partner session
Speaker: Dr. David Dai, Head of Medicinal Chemistry of the WuXi AppTec Early Discovery Platform
“Utilizing DNA-Encoded Library Technology for Novel Covalent Hits Identification”
14:40 - 15:00 Promega – Partner Session
Speaker: Craig Malcolm, Business Manager, Emerging Technologies
“NanoBRET® Target engagement assays for irreversible inhibitors and
 reversible covalent kinase inhibitors with tunable residence time   kinetics”
15:00 - 15:30 Break & refreshments
                                                             Session three
                                                        Chair: Dr Ian Storer
                                           Head of Hit Discovery, AstraZeneca 
15:30 – 15:45   OC6: Yong Xu
  "How to Successfully Prosecute Large Covalent Library (>10K) Hit   Finding Campaigns Employing Mass Spectrometry Endpoints"
15:45 – 16:05   Kevin Beaumont 
  "
The Discovery of Osimertinib"
16:05 – 16:35 Brent Martin, Scorpion therapeutics
“Streamlined live cell covalent ligand discovery”
16:35 – 17:05 Daniel K. Nomura, University of California, Berkley
“Reimagining Druggability using Chemoproteomic Platforms”
17:05 – 17:30 Concluding remarks & Awards
Michael Spedding 
                                                       Conference close
 

 

Professor Daniel Nomura 



Speaker: Professor Daniel Nomura, The University of California, Berkeley

Talk title: Reimagining Druggability using Chemoproteomic Platforms 

Biography: Dan Nomura is a Professor of Chemical Biology and Molecular Therapeutics in the Department of Chemistry and the Department of Molecular and Cell Biology in the Division of Molecular Therapeutics at the University of California, Berkeley and an Investigator at the Innovative Genomics Institute. He is an Adjunct Professor in the Department of Pharmaceutical Chemistry at UCSF. Since 2017, he has been the Director of the Novartis-Berkeley Translational Chemical Biology Institute focused on using chemoproteomic platforms to tackle the undruggable proteome. He is Co-Founder of Frontier Medicines, a start-up company focused on using chemoproteomics and machine learning approaches to tackle the undruggable proteome. He is also the Founder of Vicinitas Therapeutics based on his group’s discovery of the Deubiquitinase Targeting Chimera (DUBTAC) platform for targeted protein stabilization. He is on the Scientific Advisory Boards for Frontier Medicines, Vicinitas Therapeutics, Photys Therapeutics, Apertor Pharma, Ecto Therapeutics, and Oerth Bio. Nomura is also on the scientific advisory boards of The Mark Foundation for Cancer Research and the MD Anderson Cancer Center. He is also an Investment Advisory Partner at a16z Bio+Health, an Investment Advisory Board member at Droia Ventures, and an iPartner with The Column Group. He earned his B.A. in Molecular and Cell Biology in 2003 and Ph.D. in Molecular Toxicology in 2008 at UC Berkeley with Professor John Casida and was a postdoctoral fellow at Scripps Research with Professor Benjamin F. Cravatt before returning to Berkeley as a faculty member in 2011. Among his honors include the National Cancer Institute Outstanding Investigator Award, Searle Scholar, and the Mark Foundation for Cancer Research ASPIRE award.

Professor Nir London



Speaker: Professor Nir London, Weizmann Institute of Science, Rehovot, Israel

Talk title: New functions for covalent binders

Biography: Prof. Nir London completed his PhD in computational structural biology at the Hebrew University in 2012. He then pursued a post-doctoral fellowship with Brian Shoichet at UCSF. In 2015 Dr. London joined the Weizmann Institute of Science. Dr. London’s lab is focused on covalent chemical biology and is developing new technologies to discover and functionalize covalently acting compounds. His honors include amongst others, the 2021 EFMC award for young medicinal chemist in academia and the 2021 ISCB award for young chemical biologist. He is currently the president of the Medicinal Chemistry Section of the Israel Chemical Society.

Emma Grant 



Speaker: Emma Grant, GlaxoSmithKline

Talk title: Reactive fragment platforms for covalent hit ID

Biography: Emma conducted her PhD studies on the collaborative programme between the University of Strathclyde and GlaxoSmithKline. Her research primarily focussed on photoaffinity labelling and the development of a reactive fragment screening platform, known as the PhABits, to identify tool compounds for target validation. Since graduating in 2020 and being awarded the SCI Young Chemist in Industry Prize, Emma’s work has focussed on the expansion of reactive fragment screening platforms for covalent drug discovery. She now leads the application of these technologies in covalent hit ID and to assess target tractability in the Chemical Biology group within GSK. She was recently awarded a 2023 TechWomen100 prize for her research.

Brent Martin


 

Speaker: Brent Martin, Scorpion Therapeutics

Talk title: Streamlined live cell covalent ligand discovery 

Biography: Brent Martin received his Ph.D. in Pharmacology at the University of California in San Diego followed by postdoctoral studies at the Scripps Research Institute. As faculty member in the Chemistry Department at the University of Michigan in Ann Arbor, his research expanded the scope of activity-based profiling methods, developed new bioconjugation reactions to identify redox modifications and lipid modifications, and introduced tunable electrophiles for cysteine profiling. Brent left academics to lead the Chemical Biology team at Janssen. He is currently Vice President and Head of Chemical Biology at Scorpion Therapeutics.

Dr Andrea Gohlke


 

Speaker: Dr Andrea Gohlke, AstraZeneca PLC, Cambridge, UK

Talk title: Electrophile first lead generation for an intractable target

Biography: Dr. Andrea Gohlke is an Associate Director in Biophysics leading a team within the Mechanistic and Structural Biology department at AstraZeneca in Cambridge, UK. She joined AstraZeneca in 2019 and is using Biophysics in early- stage cancer drug discovery providing essential information about binding kinetics and the mode of action. In addition, she is a project leader including new capability developments. Starting her scientific career, she studied Molecular Life Science and obtained her PhD in Biophysical Chemistry at TU Dortmund in Germany in conjunction with the Max Planck Institute for Molecular Physiology in 2010. Here, she biophysically characterised the interaction of amyloids and small GTPases with model membranes and cells and how these can be modified. After that, she worked as postdoc in the group of Nobel laureate James Rothman at Yale University (USA) as well as at the École Normale Supérieure (France) studying SNARE-mediated membrane fusion using model membranes. Her work has been acknowledged with a postdoctoral fellowship from the German Research foundation. In 2015 she joined the Drug Discovery Programme at the CRUK Beatson institute (UK) where she used Biophysics in early-stage cancer drug discovery as well as lead collaborations with academic institutions. Her general scientific focus is the biophysical characterisation of protein/ligand interactions using a range of spectroscopic and microscopic methods. She is also a member of the publication committee of the Biophysical Journal. 

Dr David Mann 



Speaker: Dr David Mann, Imperial College London, UK

Talk title: Identifying and developing covalent fragment hits for targeted therapeutics

Biography: PhD Sheffield on developmental gene expression
Post doc in the MRC Protein Phosphorylation Unit headed by Prof Sir Philip Cohen in Dundee
Postdoctoral fellow at Imperial Cancer Research Fund (became London Research Institute of CRUK) on cell cycle dependent phosphorylation with Prof Nic Jones
Research Lecturer at Brunel Univeristy
Current post at Imperial College (started 2000) focussing on molecular/chemical biology of cancer

Matt Patricelli



Speaker: Matt Patricelli, Vividion Therapeutics, USA

Talk title: Lessons and learnings from 8 years of chemoproteomics-centered drug discovery

Biography: Obtained PhD from The Scripps Research Institute under Prof. Benjamin Cravatt (was his first student). More than 20 years of experience in the fields of enzymology, chemical biology, chemical proteomics, and drug discovery. Developed cutting edge chemical proteomics methodologies that formed the foundation of the ActivX activity-based proteomics platforms used for both internal drug development and a successful fee-for-service business (KiNativ). Biology lead for the KRAS-G12C program at Wellspring biosciences leading to the first demonstration of selective KRAS-G12C inhibition in cells and in vivo. 1st Employee and founding scientist of Vividion therapeutics. Built initial team, established chemoproteomics screening platform and early results leading to Series A financing. Subsequently led all early discovery efforts to build deep pipeline of first in class small molecule inhibitor programs. Vividion was acquired by Bayer Pharmaceuticals in 2021 for $2B, in recognition of its uniquely valuable platform and pipeline. Promoted to CSO of Vividion in early 2023.  Vividion was responsible for 3 small molecule clinical entries in 2023, two internally run trials (STAT3, and Keap1 activator/NRF2 inhibitor) and on partnered trials (Roche, WRN), and continues to grow and advance a deep pipeline of novel small molecule discovery and development programs. Author or co-author of more than 40 scientific publications, and 6 issued patents.

Lyn Jones



Speaker: Lyn Jones, Dana-Farber Cancer Institute

Talk title: Covalent Drug Development - Targeting Cysteine and Beyond

Biography: Lyn Jones completed PhD studies in synthetic organic chemistry at the University of Nottingham, before starting his postdoctoral research at The Scripps Research Institute, California in chemical biology. He joined Pfizer Sandwich (UK) as a medicinal chemistry team leader, eventually becoming Head of Chemical Biology and Lead Discovery Technologies. He transferred to Pfizer Cambridge (USA) to become Head of Rare Disease Chemistry and Head of Chemical Biology. He then helped establish Jnana Therapeutics as Head of Chemistry and Chemical Biology, before moving to his current roles as Director of the Center for Protein Degradation, Institute Scientist, and Principal Investigator at the Dana-Farber Cancer Institute in Boston. His research interests include the creation and application of chemistry-based technologies, such as covalent protein labeling modalities and induced-proximity pharmacology, with the objective of expanding the druggable proteome.

Monique Mulder 



Speaker: Monique Mulder, Leiden University Medical Center 

Talk title: Unveiling the Ubiquitin System through Covalent Enzyme Inhibition

Biography: Monique Mulder earned her PhD in Medicinal Chemistry at Utrecht University in 2012. Subsequently, she embarked on a trajectory that integrates chemical principles with cutting-edge biological techniques. She now leads the Mulder lab at Leiden University Medical Center, where her research is centered on elucidating the intricate mechanisms governing post-translational modifications of substrate proteins by ubiquitin and ubiquitin-like proteins. Her focus extends to understanding how dysregulation in these processes contributes to the pathogenesis of diseases like neurodegeneration and cancer, striving to illuminate the pathogenesis at a molecular level. The lab specializes in crafting tailored covalent small molecule inhibitors and chemical probes essential for unraveling the complexities of protein (de)ubiquitination. 

Megan Matthews


Speaker: Megan Matthews, University of Pennsylvania, USA

Talk title: The revolution and evolution of activity-based protein profiling

Biography: Megan received her BA in Chemistry from Miami University and her PhD from Penn State University under Marty Bollinger and Carsten Krebs. Her PhD work led to an understanding for how iron- and 2-oxoglutarate dependent oxygenases suppress hydroxylation to allow for halogenation and other outcomes important in natural product biosynthesis. Upon graduation, she performed postdoctoral studies at Scripps Research in the chemical biology laboratory of Ben Cravatt as a Helen Hay Whitney Fellow. Matthews investigated the prevalence of undiscovered protein-bound electrophiles and the (dys)functions that the unknown electrophiles impart, uncovering evidence for their involvement in cancer and diseases of the central nervous system. Her program is tracking down these and a host of other leads to novel disease biology and therapeutics.

Professor Bradley Pentelute 



Speaker: Professor Bradley Pentelute, Professor of Chemistry at Massachusetts Institute of Technology

Talk title: Advancing Covalent Peptide Inhibitors through ReAct-ASMS

Biography: Bradley L. Pentelute is a Professor of Chemistry at MIT (https://pentelutelabmit.com). He is also an Associate Member, Broad Institute of Harvard and MIT, an Extramural Member of the MIT Koch Cancer Institute, and Member, Center for Environmental Health Sciences MIT. He received his undergraduate degree in Psychology and Chemistry from the University of Southern California, and his M.S and Ph.D. in Organic Chemistry from the University of Chicago with Prof. Steve Kent.  He was a postdoctoral fellow in the laboratory of Dr. R. John Collier at Harvard Medical School, Microbiology.  Bradley L. Pentelute has been recognized with several prestigious awards since 2013, including the Damon Runyon-Rachleff Innovation Award (2013), the Young Chemical Biologist Award from the International Chemical Biology Society (2013), the Sontag Distinguished Scientist Award (2013), the NSF CAREER Award (2014), the Sloan Research Fellowship in Chemistry (2015), the Novartis Early Career Award in Organic Chemistry (2015), the Amgen Young Investigator Award (2016), the Eli Lilly Award in Biological Chemistry (2018), and the Rao Makineni Lectureship from the American Peptide Society (2021).

Dr Peter Cossar 



Speaker: Dr Peter Cossar, Eindhoven University of Technology

Talk title: Reversible Dual-Covalent Molecular Locking of the 14-3-3/ERRγ Protein-Protein Interaction as a Molecular Glue Drug Discovery Approach

Biography: Peter Cossar completed his PhD in synthetic medicinal chemistry at the University of Newcastle, Australia. In 2018, he began a Marie Curie Postdoctoral Fellowship at the Technical University of Eindhoven in the Netherlands, where he trained as a chemical biologist. During this time, he pioneered a novel aldehyde-based covalent drug discovery approach, which is now licensed by Ambagon Therapeutics. In 2021, he was awarded the prestigious Veni Fellowship from the Dutch Science Foundation and was recognized as a future research leader by the EFMC Young Investigator Committee. In 2023, Peter was appointed Assistant Professor at the Technical University of Eindhoven. And in October 2024, he moved his research group to the University of Dundee’s Centre for Targeted Protein Degradation. His research group focuses on developing new fragment-based drug discovery approaches and molecular glue stabilizers for intrinsically disordered biomolecular complexes. 

Isabel Martin Caballero



Speaker: Isabel Martin Caballero, Pelago Bioscience, Project Advisor

Talk Title: The Cellular Thermal Shift Assay, How assessment of target engagement helps identify early liabilities

Biography: Isabel obtained her PhD in Stem Cell Biology from University of Edinburgh, followed by diverse research positions in industry and academia working on epigenetics, cell fate decisions and iPS disease modelling.  

With more than 20 years of research experience, Isabel is a Project Advisor at Pelago Bioscience, working at the interface between the client and the scientist teams. Isabel joined Pelago in 2017 as a senior scientist and has worked in a wide variety of projects in all the CETSA® formats, as well as being involved in developing the CETSA technology forward.

Craig Malcom 



Speaker: Craig Malcolm, Business Manager, Emerging Technologies

Talk Title: NanoBRET® Target engagement assays for irreversible inhibitors and reversible covalent kinase inhibitors with tunable residence time kinetics

Biography: After completing his PhD in Neurochemistry from St Andrews University in 1995, Dr Malcolm joined the pharmaceutical industry working for seven years as a Team Leader in Molecular Pharmacology (Vernalis Ltd.), developing cell-based assays and supporting drug discovery screening projects across a variety of therapeutic areas. After several more years in product development as a Senior Cell Biologist (PerkinElmer), and various other commercially-focused roles in several other UK-based Life Sciences companies (Scientifica, Roche Applied Science), Craig joined Promega UK in 2012 and is currently Business Manager – Emerging Technologies & Bioassays, with a focus on new and emerging technology platforms for small molecule & biologics discovery.

Ivan Cornella



Speaker: Ivan Cornella, Covant Therapeutics

Talk title: Leaving a mark: Harnessing covalency to target native disease proteoforms

Biography: Ivan is the co-founder and Chief Scientific Officer of Covant Therapeutics, a Boston-based start-up aimed at unleashing the power of covalency to transform the way we drug human biology, treating diseases with transformative therapeutics. In previous roles, at Roivant Sciences, Cedilla Therapeutics, Merck, AstraZeneca, Sanofi, and Novartis, Ivan contributed to establish and managed teams supporting drug discovery initiatives across disease areas, target classes, and modalities. Throughout his career, Ivan has consulted on target discovery and enablement, omics, lead finding, and drug mechanism of action for various start-ups and biotech firms.
Ivan holds a Ph.D. in organic chemistry from the Universidade da Coruña, Spain, and earned an Executive Certificate in innovation from MIT Sloan School of Management. He completed postdoctoral work at the Institute of Chemistry & Cell Biology of Harvard Medical School, as National Cancer Institute Initiative for Chemical Genetics Research Fellow, and at Boston College chemistry department. 

Ana Corrionero



Speaker: Ana Corrionero, Co-Founder and CEO of Enzymlogic and Professor of Pharmaceutical Biotechnology at UPM

Talk title: Decoding Irreversible Drug Kinetics: COVALfinder® case studies

Biography: Ana, Co-Founder and CEO of Enzymlogic and Professor of Pharmaceutical Biotechnology at UPM, has over 20 years of experience in the pharmaceutical industry, including roles at Novartis, GSK, and the Spanish National Cancer Research Centre (CNIO). At GSK, she contributed to research on drugs targeting Malaria and Tuberculosis, while at CNIO and Novartis her focus shifted to cancer research, where she specialized in assay development, binding kinetics and molecular profiling.

In 2013, Ana founded Enzymlogic, a company that has since grown to become the global leader in kinetic profiling for drug discovery. Under her leadership, Enzymlogic has pioneered two innovative platforms: KINETICfinder® and COVALfinder®, both of which provide high-throughput kinetic screening of reversible and irreversible drugs. 

Alongside her work as CEO, Ana remains deeply committed to academia. As a professor, she shares her expertise with students and enjoys inspiring the next generation of researchers.

Henrik Jensen



Speaker: Henrik Jensen, CSO, Fidabio

Talk title: "In-solution binding kinetics with 1st principle technology FIDA"

Biography: Henrik Jensen, Ph.D. is the inventor of FIDA technology (Flow Induced Dispersion Analysis), a former professor at Copenhagen University and current Chief Scientific Officer at Fida Biosystems. Thus, his scientific areas of interest span form academic and industrial pharmaceutical physical chemistry to development of novel research methodologies.  Henrik has over 100 peer reviewed papers and issued patents (Citations > 2500 and H-index = 28 according to web of science (October, 2016)). His recent invention is a method for studying in-solution binding kinetics. 

Christin Zasada 



Speaker: Christin Zasada, Head of Bioinformatics, OmicScouts

Talk title: “Cellular Turnover of Covalent Drug Targets”

Biography: Inspired by her studies of Biosystems Engineering at the University of Marburg, Christin early on developed a strong interest in mass spectrometry-driven proteomics and metabolomics, which she further pursued during her PhD at the Max Delbrück Center Berlin, exploring the metabolic reprogramming of cancer and stem cells.
A major reoccurring challenge during this time was the aggregation of complex data to allow for their deeper understanding. For this reason, Christin´s focus shifted from the experimental side to bioinformatic analysis: Crafting pipelines for robust data processing, advancing analytical algorithms and enhancing data visualization, one of her strongest passions.
She has since been using her expertise as a bioinformatician and team lead at Evotec Toulouse, and now as the Head of Bioinformatics at OmicScouts, to make proteomics data accessible to non-experts and to create ready-to-use data solutions such as the ProteinTurnoverAtlas™.

Dr David Dai




Speaker: Dr David Dai, Head of Medicinal Chemistry of the WuXi AppTec Early Discovery Platform

Talk title: “Utilizing DNA-Encoded Library Technology for Novel Covalent Hits Identification”

Biography: Dr. Dongcheng (David) Dai received his Ph.D. degree in organic chemistry from the State University of New York at Binghamton under the guidance of Professor Olivier Martin and was a postdoctoral fellow in the lab of Nobel Laureate Professor E. J. Corey at Harvard University. He has rich experience in medicinal chemistry. He has been working in drug discovery and development for 20+ years and is experienced in leading successful drug discovery program from inception to clinical trial. His research interests span from oncology, metabolic, neurological, cardiovascular, infectious to rare diseases. He discovered and synthesized two (2) FIC drug candidates that entered Phase I clinical trials and developed an FDA-approved drug [TPOXX® (tecovirimat)] from discovery to Phase II clinical trial. He also contributed to the development of the FDA-approved drug EXONDYS 51 (eteplirsen) injection. On technology development he led the establishment of DNA-encoded Library (DEL) platform and utilization of the technology in multiple companies and discovered potent hits for an extremely difficult and high value target. He is well educated in patent laws and experienced in all aspects of patent practice. He has 85 papers, patents, and patent applications. Dr. Dai joined WuXi AppTec in 2024 and is now leading the chemistry to identify novel hits, including those as targeted covalent inhibitors by using different technologies.







 


Dr Maria Flocco


 

Chair: Dr Maria M Flocco  VP, Mechanistic and Structural Biology, Discovery Sciences, Biopharmaceuticals R&D  

Biography: Maria joined AstraZeneca in 2015 as head of Structure and Biophysics moving to her current role in 2021. Previous to joining AstraZeneca, she held various positions of increasing responsibility in Pfizer and Pharmacia. She was Senior Director and Head of External R&D Innovation Europe, Sr Dir Head of Internal Medicine Chemistry, Sr Dir Head of Lead Discovery, and Director Head of Structural Biology and Biophysics at Pfizer, and Head of Structural Chemistry at Pharmacia. Prior to her career in the pharmaceutical industry, Maria was a Lecturer at the Karolinska Institute, Stockholm, and a researcher at the Uppsala Biomedical Centre, Sweden. Maria received a PhD in Physical Chemistry from the City University of New York, and  postdoctoral training in X-ray crystallography at the Fox Chase Cancer Centre, Philadelphia,  and the Uppsala Biomedical Centre. Maria has established successful external collaborations and is currently a member of the  scientific advisory panel of the Rosalind Franklin Institute, Oxford. She has been a member of  the MRC Molecular and Cellular Medicine Board, the SAB of INSTRUCT EU, the SAB of the  Chemical Biology Institute of Imperial College London and the SAB of INSERM Transfert Initiative, a seed funding organisation of INSERM in France.


David Wilson PhD


 

Chair: David Wilson, PhD, VP & Global Head, Oncology Chemistry, AstraZeneca 

Biography: 
David is Vice President and Global Head of Oncology Discovery Chemistry & DMPK at AstraZeneca. He received his PhD from the University of Leeds, and completed a postdoctoral fellowship in the US before starting his pharma career at GlaxoSmithKline. He has accumulated over 27 years’ experience of small molecule drug discovery and has held senior leadership roles at GlaxoSmithKline, Johnson & Johnson and AstraZeneca. During his  career, David has worked across multiple therapeutic areas including neurosciences, infectious diseases, immunology and oncology, and has been closely involved with the discovery of numerous drug candidates that have progressed into clinical phase development. David is a is a member of the Cambridge Discovery Centre site leadership group and represents early oncology on both the UK and Cambridge leadership teams.   


Richard Ward 



Chair: Richard Ward, Executive Director, Oncology Search & Evaluation Group, AstraZeneca

Biography: Richard Ward is a Executive Director in the Oncology Search & Evaluation Group in AstraZeneca. In this role, he is responsible for the identification and evaluation of innovative targets, programs, technologies and collaborations to enhance the company’s oncology pipeline. Richard moved into the Business Development team in January 2020 after working as a Computational Medicinal Chemist in drug discovery projects within Oncology R&D at AstraZeneca for almost 20 years. Most notably he was co-proposer and co-inventor of the approved EGFR mutant-selective covalent inhibitor osimertinib (Tagrisso). As part of this discovery work he was awarded the Heroes of Chemistry award by the ACS, the Malcolm Campbell Memorial Prize by the RSC and has also been the awarded the 8th Capps Green Zomaya Award by the Biological and Medical Chemistry sector of the RSC. Before starting his research career at AstraZeneca, Richard gained a First Class BSc in Chemistry and Bio-organic Chemistry and a PhD in Computational Chemistry at The University of Birmingham, UK.


Susan Critchlow



Chair: Susan Critchlow, Executive Director at AstraZeneca

Biography: Susan Critchlow, Ph.D. is an Executive Director in the Early Oncology group based in Cambridge, UK.  A member of Early Oncology Discovery leadership team, Susan leads the UK bioscience group delivering pre-clinical data to support taking novel Oncology drugs into the clinic. Since joining AstraZeneca, Susan has delivered across the drug discovery pipeline from Target Identification to Candidate Drug nomination and supported drug projects in clinical development.  Her department play a key role in discovering and developing new precision medicines and have delivered key pre-clinical data supporting progression of established and emerging Oncology medicines including osimertinib, olaparib, capivasertib, camizestrant, ceralasertib, and suraparib and are focussed on delivering wave of innovative Oncology medicines.


Dr Ian Storer




Chair: Ian Storer, Head of Hit Discovery at AstraZeneca

Biography: Dr Ian Storer is currently Vice President, Head of Hit Discovery in Global Research and Development at AstraZeneca Pharmaceuticals in the UK where he leads a department that deploys the latest high throughput and pooled screening technologies, robotic automation, chemistry and data AI to aid the discovery of the next generation of medicines. This work covers the discovery of traditional small molecule hits but also the latest modalities including covalent, bifunctional, and molecular glue molecules. Prior to joining AstraZeneca in 2016, Dr Storer spent 10 years at Pfizer working as a medicinal chemist and pre-clinical project leader across several disease areas, leading to multiple clinical-stage medicines. Before entering the pharmaceutical industry, he studied Natural Sciences then completed his Ph.D. in organic chemistry with Professor Steven V. Ley CBE at the University of Cambridge on the application of novel methods to natural product synthesis, followed by postdoctoral research at Caltech working with Professor Sir David W. C. MacMillan on asymmetric organocatalysis. 


Tickets


Affiliate and Retired Non Member Ticket Non-Member Ticket £400.00
AstraZeneca Member Ticket Non-Member Ticket £310.00
Full and Retired Member Ticket Member Ticket £310.00
Journal Author, Fellow, Retired Fellow, Honorary Fellow Member Ticket Member Ticket £310.00
Journal Author, Fellow, Retired Fellow, Honorary Fellow Non Member Ticket Non-Member Ticket £400.00
Undergraduate, Postgraduate, Affiliate, ECR and Diploma Student Member Registration Member Ticket £160.00
Undergraduate, Postgraduate, ECR and Diploma Student Non-Member Registration Non-Member Ticket £240.00

 
Poster presentation no.  Author and presentation title
PP1 Charlotte Griffiths-Jones
“X-ray Screening of an Electrophilic Fragment Library and Application towards the Development of a Novel ERK 1/2 Covalent Inhibitor”

 
PP2 Chloe Oxford 
“High Throughput Reactive Fragment Screening by MALDI-TOF MS”
 
PP3 Michael Spedding
“An assessment of enzyme-activated irreversible inhibition, as applied by the Merrell Research Centre at Strasbourg”
 
PP4 Maria Rodriguez-Rios
“The next generation BromoTAG”
 
PP5 Anna Hopkins
“Covalent Drug Discovery at Domainex: Curation of a covalent fragment library and fast follow-up via D2B screening”
 
PP6 Jemima Brimacombe
“Chemical biology tools to promote immune clearance of microbial infections”

 
PP7 Chris Pedder
“Developing integrated biochemical and mass-spectrometry cascades for covalent hit finding”
 
PP8 Dr David Dai 
"Discovery of a Novel Covalent Inhibitor using DNA Encoded Library"

 
PP9 Alfred Doherty 
“The Development of Next-Generation Reactive Electrophiles for Beyond Cysteine Covalent Drug Discovery”
 
PP11 Scott Martin
“Search for Transglutaminase 2 (TG2) covalent inhibitors using Domainex’s covalent fragment library and a LC-MS based covalent fragment screening platform”
 
PP12  Dominika Kowalczyk
“From screening to validation: a comprehensive approach to identifying covalent inhibitors for challenging targets”
 
PP13 Christin Zasada 
"A comprehensive protein turnover atlas for drug discovery"

 
PP14 Diana Zindel
“In Vitro Data Integration for PKPD Modelling of Irreversible TKIs”
 
PP15 Henrik Jensen
“Removing surface-related constrains in binding kinetics studies” 
 
PP16 Isabel Caballero
“The Cellular Thermal Shift Assay, How assessment of target engagement helps identify early liabilities”
 
PP17 Michael Zollo
“Cell-based Reactive Cysteine Profiling of an Electrophile”

 

 

 

We're excited to unveil our partnership opportunities! For more information on how to participate please download our - Partnership Prospectus 

If you have any questions or wish to connect with a member of the events team, please contact meetings@bps.ac.uk.
 


Fidabio assist you realizing the full potential of your complex biology beyond current technologies. We offer a completely new way to quantify and characterize complex biology in native conditions.  

Flow Induced Dispersion Analysis (FIDA) is a revolutionary, first principle technology for in solution, accurate and reproducible measurement of hydrodynamic radius of biomolecules in complex matrices leading to a wide range of orthogonal biophysics assays. 

It has been developed for quantification and characterization of proteins (including biologics) and particles with diameter from 0.5 to 1000 nm, including complex interactions, stoichiometry, oligomeric states etc. 

The FIDA technology is characterized by: 

•    Being fast (minutes)
•    Requiring very small sample amounts (nl-μl) 
•    Being exceptionally tolerant to the sample matrix. 

Contrary to most other procedures, the FIDA methodology is based on binding in homogenous solution; complications related to non-specific surface adsorption and challenging assay development is therefore avoided. 

The unique features of FIDA enable characterization and quantification in native (biorelevant) environments. In-built assay quality control ensures high data reliability and walk-away automation sets free resources for other tasks. 



Applied Photophysics of Leatherhead, Surrey, UK, is a leading provider of solutions for the biophysical characterisation of biomolecules and has been providing spectroscopy to the research community for over 50 years. Chirascan™ systems use the phenomenon of circular dichroism (CD) to characterise changes in the higher-order structure of proteins. These systems are used in cutting-edge research and to support the development of innovator drugs and biosimilars in the biopharmaceutical industry.

The company’s SX range of stopped-flow spectrometers is acknowledged globally as the gold standard for kinetic studies of fast biochemical reactions. Through a joint venture with Fluorescence Innovations Inc of Minneapolis, MN, USA, operating as Protein Stable, they have also introduced easy-to-use protein stability screening with microplate-based intrinsic fluorescence thermal ramping and chemical melt plate readers.


OmicScouts facilitates next generation drug discovery with its expertise in chemical proteomics. We provide end-to-end solutions and tailored projects integrating quantitative mass spectrometry and bioinformatics with biochemical and cell culture expertise. Our technologies enable comprehensive drug target deconvolution (target ID, selectivity, engagement), mode of action analyses and biomarker discovery. Founded by leading proteomics researchers, the company has a track record in delivering significant collaborations with top pharmaceutical and biotechnology companies.

Selvita is a preclinical Contract Research Organization providing multidisciplinary support in resolving the unique challenges of research within the areas of drug discovery and drug development studies. Selvita was established in 2007 and currently employs almost 900 professionals, of which over 40% hold a PhD degree. The Company research sites are located in Krakow (HQ) and Poznan, Poland, as well as Zagreb, Croatia. Selvita’s international offices are located in Cambridge, MA, and San Francisco Bay Area, in the U.S., as well as in Cambridge, the UK. 

Selvita Group has broad expertise and track record in oncology, inflammation, fibrosis, anti-infectives, respiratory diseases and CNS. The company offers drug discovery support at every stage of the early discovery phase up to the preclinical development. Selvita specializes in a variety of drug discovery processes from in silico drug design and synthesis of a target-focused library, SAR and ADME-driven lead optimization and toxicity prediction, followed by complex preclinical in vitro and in vivo pharmacology, structural biology, all tailored to the customer’s needs.


Genedata transforms data into intelligence with innovative software solutions that incorporate extensive biopharma R&D domain knowledge. Multinational biopharmaceutical organizations and cutting-edge biotechs around the globe rely on Genedata to digitalize and automate data-rich and complex R&D processes. From early discovery all the way to the clinic, Genedata solutions help maximize the ROI in R&D expenditure. Founded in 1997, Genedata is headquartered in Basel, Switzerland with additional offices in Boston, London, Munich, San Francisco, Singapore, and Tokyo.

Enzymlogic is a specialist CRO, providing kinetic profiling services for small molecule drug discovery with unparalleled speed and efficiency. We facilitate the screening of reversible and irreversible inhibitors in early discovery to iterate Med Chem, understand PK PD disconnects and build better models to define therapeutic windows.



Published by the Royal Society of Chemistry, RSC Medicinal Chemistry is home to publishes significant research in medicinal chemistry and related drug discovery science and RSC Chemical Biology is dedicated to publishing exceptionally significant findings from the broadly understood chemical biology community.

As a global company with operations across Asia, Europe, and North America, WuXi AppTec provides a broad portfolio of R&D and manufacturing services that enable the pharmaceutical and healthcare industry around the world to advance discoveries and deliver groundbreaking treatments to patients. Through its unique business models, WuXi AppTec’s integrated, end-to-end services include chemistry drug CRDMO (Contract Research, Development and Manufacturing Organization), biology discovery, preclinical testing and clinical research services, and cell and gene therapies CTDMO (Contract Testing, Development and Manufacturing Organization), helping customers improve the productivity of advancing healthcare products through cost effective and efficient solutions. WuXi AppTec received AA ESG rating from MSCI in 2023 and its open-access platform is enabling more than 6,000 customers from over 30 countries to improve the health of those in need – and to realize the vision that "every drug can be made and every disease can be treated."



Pelago Bioscience is a CRO, supporting early phase drug discovery, with expertise in target engagement in biologically relevant assay systems. 
Pelago Bioscience’s core technology, CETSA® (Cellular Thermal Shift Assay), is a keystone in gaining early confidence in decision-making in the early stages of the drug discovery pipeline.
CETSA holds multiple assay formats, from confirming target engagement to strengthening target validation and understanding the mechanism of action of compounds.


Promega are world leaders in providing innovative solutions and technical support to life science research. Over 4,000 products enable scientists to advance their knowledge in cellular analysis, genomics and proteomics, promoting understanding of the molecular basis of life and potential mechanisms of disease, as well as identifying targets for drug development.
 

Bharath Srinivasan

Principal Scientist, AstraZeneca, UK  

 

Bharath Srinivasan studied the structure-function relationship in members of the Haloacid Dehalogenase superfamily of enzymes as part of his PhD studies. He pursued an NIH-sponsored postdoctoral fellowship at the Centre for the Study of Systems Biology, Georgia Institute of Technology, working at the interface between biochemistry/biophysics, computational sciences and medicinal chemistry. Subsequently, he was awarded the prestigious Marie Skłodowska-Curie Actions fellowship to study the substrate specificity of deaminases acting on double-stranded RNA at the Instituto Gulbenkian de Ciencia, Portugal. Currently, Bharath is a Principal Scientist at the Mechanistic and Structural Biology Division at AstraZeneca, contributing actively to several oncology projects deducing the Mechanism of Action of small-molecule leads. Bharath has published around 40 peer-reviewed publications, 1 patent and several science outreach articles. He is an editor with two prominent pharmacology journals (British Journal of Pharmacology and Current opinion in Pharmacology), a faculty with facultyopinions and on the editorial advisory board of FEBS J. He is also an Honorary Associate Professor of Pharmacy and Life Sciences at the Robert Gordon University, Aberdeen. Further, he serves on the industrial committees of Biochemical Society and British Pharmacological Society. He is passionate about biophysical and kinetic characterization of enzymes with particular emphasis on studying the spatio-temporal evolution of kinetic systems, steady state kinetics, pre-steady state kinetics, single turnover kinetics, non-Michaelian kinetics and equilibrium/non-equilibrium modalities of enzyme inhibition. Bharath is also invested heavily in optimizing methods for in-cellulo kinetics and label-free detection methods. You can connect with him @ https://www.linkedin.com/in/bharath-srinivasan-b1716b3b/ or @ https://twitter.com/bharath_IGC.

Simon Lucas 

Associate Principal Scientist, AstraZeneca, UK 



Simon is a Medicinal Chemist with experience working on drug discovery projects at all stages. He obtained his PhD from the University of Strathclyde in 2019 through the GSK/Strathclyde Industrial PhD scheme where he worked in the Epigenetics group on the development of chemical tools for Bromodomain targets. He joined AstraZeneca in 2019 as a medicinal chemist in the Hit Discovery group where he has worked extensively on fragment-based lead generation and covalent hit identification projects delivering multiple lead series to project teams.

Mark McAlister 

Director, Mechanistic and Structural Biology, AstraZeneca, UK 



Mark McAlister is Director of Biophysics at AstraZeneca Cambridge UK. He obtained his PhD in 1993 from University of Aberdeen on the biochemistry of the complement C1, followed by postdocs at Oxford University and UCL on NMR structure and interactions of leukocyte cell-adhesion proteins. He then led the protein engineering lab at Bloomsbury Centre for Structural Biology (UCL/Birkbeck) contributing to 12 novel crystal structures and spin-out of Domainex Ltd. He joined AstraZeneca in 2002 to establish the protein engineering group, which he led until 2010 before moving to leadership roles in protein structure and biophysics. 
He is expert in protein biochemistry, biophysics and early drug discovery and has worked across a range of disease therapy areas, but with a focus on small-molecule cancer drug discover over the last 10 years, including project leadership and externalization. He leads the molecular biophysics group responsible for biomolecular NMR, structural mass spectrometry and biophysics and leads the AZ covalent hit discovery capability. He currently focusses on strategies to enable drug discovery for intractable or challenging oncology drug targets, including affinity-based screening, molecular glue strategies and electrophile-first covalent lead generation. 
 

Sarah Hewitt 

Associate Principal Scientist, AstraZeneca, UK 



Sarah is a biochemist in the Mechanistic and Structural Biology group at AstraZeneca. This follows a PhD at the University of Leeds within the general remit of supramolecular chemical biology, and postdoc at Loughborough University developing real-time enzyme monitoring assays before moving to industry. She started at Vertex Pharmaceuticals in Oxford prior to moving to AstraZeneca in 2020. Sarah now focusses on using mass spectrometry for covalent hit finding and covalent hit to lead studies at AstraZeneca, developing the platform and contributing to many projects.  
 

We are excited to announce our partnership with Mice Concierge, a dedicated team ready to provide personalised assistance with all your accommodation needs. Whether you have questions about booking a room or need guidance on hotel options, Mice Concierge is here to help ensure your stay is comfortable and hassle-free. Don't hesitate to reach out to them for any accommodation queries you may have.

The following conveniently located hotels are now open for booking:

Hilton Cambridge City Centre
Distance: 3.8km from The Discovery Centre

IBIS Cambridge Central Station HQ Hotel
Distance: 2.8km from The Discovery Centre

To finalise your accommodation booking for this event, please click the 'Book Now' button below.
 
Book Now

If you need group accommodation for over six rooms, feel free to contact the dedicated team at MICE Concierge, who will be delighted to assist you.


Immerse yourself in a world of discovery at the renowned Discovery Centre in Cambridge! Join us for an exclusive event that celebrates innovation and exploration. Explore cutting-edge ideas and connect with industry leaders in this dynamic space known for fostering ground breaking discoveries. Mark your calendar for an unforgettable experience at the Discovery Centre in Cambridge!



Venue
The Discovery Centre
Biomedical Campus
1 Francis Crick Ave
Trumpington
Cambridge
CB2 0AA
From
16 October 2024
To
17 October 2024
Venue
The Discovery Centre, Biomedical Campus, 1 Francis Crick Ave, Trumpington, Cambridge, CB2 0AA




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© 2021 British Pharmacological Society, The Schild Plot, 16 Angel Gate, City Road, London EC1V 2PT, United Kingdom

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