Professor Matthias Gehringer
University of Tubingen
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Talk title: TBC
Biography: Matthias studied chemistry at the Karlsruhe Institute of Technology (KIT; Germany), the Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM; France), and the University of Heidelberg (Germany). He obtained his doctorate from the University of Tübingen (Germany) where he worked in the group of Prof. Stefan Laufer on reversible and irreversible inhibitors of the protein kinase JAK3. As a postdoc at the Swiss Federal Institute of Technology (ETH) Zürich (with Prof. Karl-Heinz Altmann), he focused on the total synthesis of complex natural products from the mycolactone family. In 2019, he was appointed as Assistant Professor for Medicinal Chemistry at the Institute of Pharmaceutical Sciences, University of Tübingen. In May 2024, he was appointed as Full Professor and head of the Division for Medicinal Chemistry at the Institute of Biomedical Engineering of the Faculty of Medicine, University of Tübingen. Matthias is a Principal Investigator (PI) in the Cluster of Excellence "Image Guided and Functionally Instructed Tumor Therapies (iFIT)".
His research focuses primarily on covalent protein kinase inhibitors and novel approaches for the covalent targeting of cysteine and other amino acids. He received a variety of awards including the Young Investigator Award of the German Pharmaceutical Society (DPhG) and the Phil Portoghese Lectureship Award of the American Chemical Society (ACS) MEDI division. Notably, Matthias is currently heading a European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practices initiative on covalent drug modalities.
Dr Stephan Hacker
University of Leiden
Tentative talk title: Profiling the proteome-wide selectivity of diverse electrophiles
Biography: Dr. Stephan Hacker performed his PhD studies with Prof. Andreas Marx at the University of Konstanz, Germany, and his postdoctoral research with Prof. Benjamin Cravatt at The Scripps Research Institute in La Jolla, USA. Afterwards, he moved to the Technical University of Munich, Germany, to work as an independent group leader. In 2021, he became an Assistant Professor at the Leiden Institute of Chemistry. Stephan Hacker’s group develops chemistries for novel covalent protein ligands targeting diverse amino acids as well as chemoproteomic technologies to study their target engagement with resolution of the modified amino acid residue in proteome-wide studies. His group focuses on the application of these compounds and technologies to identify new druggable target proteins in bacteria.
Abstract: Patrick R. A. Zanon, Fengchao Yu, Patricia Musacchio, Lisa Lewald, Michael Zollo, Kristina Krauskopf, Dario Mrdović, Patrick Raunft, Thomas E. Maher, Marko Cigler, Christopher Chang, Kathrin Lang, F. Dean Toste, Alexey I. Nesvizhskii, Stephan M. Hacker
Targeted covalent inhibitors are powerful entities in drug discovery to expand the druggable proteome. Nevertheless, their application has so far mainly been limited to addressing cysteine residues. The development of cysteine-directed covalent inhibitors has largely profited from determining their proteome-wide selectivity using competitive residue-specific proteomics. Several probes have recently been described to monitor other amino acids using this technology and many more electrophiles exist to modify proteins. Nevertheless, a direct, proteome-wide comparison of the selectivity of diverse probes is still entirely missing. Here, we developed a completely unbiased workflow to analyse electrophile selectivity proteome-wide and applied it to directly compare 54 alkyne probes containing diverse reactive groups. In this way, we verified and newly identified probes to monitor a total of nine different amino acids as well as the N terminus proteome-wide. This selection includes the first probes to globally monitor tryptophans, histidines and arginines as well as novel tailored probes for methionines, aspartates and glutamates.
Dr Louise Walport
Imperial College London
Talk title: Adventures in Covalency with mRNA display
Biography: Louise is an Associate Professor in the Department of Chemistry at Imperial College London and a Group Leader at the Francis Crick Institute. She obtained her doctorate from the University of Oxford in 2014 under the supervision of Prof. Chris Schofield and Prof. Christina Redfield, focussing on mechanistic studies of histone demethylases. Following further postdoctoral work in Oxford, she was awarded a Marie Skłodowska-Curie Global Fellowship to work in the group of Prof. Hiroaki Suga at the University of Tokyo, where she developed her interest in cyclic peptides. She established her independent group in late 2018, where she continues to be interested in understanding enzyme-catalysed post-translational modifications and developing new approaches to probe these with cyclic peptide-based tools. He group has pioneered ways to expand the target scope of mRNA display including through screening proteins in cell lysates and introducing covalent warheads into cyclic peptide libraries.
Dr Megan Wright
Imperial College London
Talk title: Chemical probes for target identification and protein labelling in cells
Biography: Megan graduated with an MSci from the University of Cambridge in 2008 in Natural Sciences (Chemistry), then went on to study for an MRes-PhD with Prof. Ed Tate at the Institute of Chemical Biology at Imperial College London, working on chemical biology approaches to protein lipidation. After receiving her PhD in 2013, she undertook postdoctoral research, first as an EPSRC Doctoral Prize Fellow in the Tate group, and then as a Marie Curie Fellow with Prof. Stephan Sieber at the TU Munich where she developed activity- and affinity-based probes for protein targets. She joined Leeds on a tenure-track University Academic Fellowship in 2016 and was promoted to Associate Professor in 2022. The Wright group works in the field of chemical biology, exploiting covalent chemistry to develop chemical tools to probe dynamic protein function and the mode of action of small molecules in live cells and at the molecular level.
Dr Matthew Bilyard
Roche
Talk title: TBC
Biography: Matt completed his PhD at the University of Oxford under Prof. Ben Davis (2013-2017), researching site-selective covalent modification of enzymes and its application to study mechanisms of glycogen biosynthesis. Following postdoctoral research with Prof. Sir Shankar Balasubramanian (University of Cambridge), he joined AstraZeneca’s Mechanistic Biology and Profiling team in 2021. In 2023, Matt moved to F. Hoffmann-La Roche in Basel, where he is currently a Senior Scientist in Mass Spectrometry and Biochemistry within the Lead Discovery department.
Matt’s work focuses on the development of diverse MS-based assays to support hit-to-lead activities across multiple therapeutic areas. Throughout his time at Roche and AstraZeneca, he has specialized in covalent drug discovery, from designing and running high-throughput MS-based covalent screens to developing new approaches to accelerate and simplify hit follow-up. In collaboration with external partners, he is leading the implementation of fast, automated data analysis pathways for covalent screening, while additionally helping to shape Roche’s broader covalent strategy as a member of a dedicated “covalents focus team”.
Dr Elena De Vita
Lecturer in Synthetic Biology and Biotechnology
Tentative talk title: Covalent ligand development to tackle challenging targets
Biography: Elena De Vita graduated in Pharmaceutical Chemistry and Technologies from the University of Pisa in 2014, where she developed novel carboxylic acid–based inhibitors of matrix metalloproteases during her Master’s thesis (Prof Armando Rossello). She then joined the Cancer Drug Development group at the German Cancer Research Center (DKFZ, Heidelberg) as a DKFZ-MOST funded PhD student (German-Israeli collaboration) to develop of covalent inhibitors of a secreted serine protease (KLK6) under the supervision of Dr Aubry Miller.
Following a short EMBO-funded visit to Imperial College, Elena joined the Tate group as a CRUK Research associate to work on the development of covalent inhibitors for the small GTPase Rab27A. In 2020, she was awarded a Marie Skłodowska Curie Fellow and successively she was funded by Worldwide Cancer Research as a Co-investigator (2022). Alongside her research, Elena has been active in scientific innovation and recognition initiatives, including participation in the winning team of the Merck Innovation Cup in 2021 and being shortlisted for the L’Oréal–UNESCO UK For Women in Science programme in 2022.
Currently, Elena is a Lecturer in Synthetic Biology and Biotechnology within the Centre for Molecular and Cellular Biology at Queen Mary University of London.
Professor Ed Tate
Imperial College London
Tentative talk title: Chemoproteomic discovery of druggable targets and pathways
Biography: Ed holds the GSK Chair in Chemical Biology at Imperial College London, and he is a Group Leader at the Francis Crick Institute. Following his PhD (2000) with Steve Ley in Cambridge and postdoctoral research in Paris as an 1851 Fellow and Howard Trust Fellow, he was awarded a BBSRC David Phillips Fellowship in 2006 to start his group at Imperial College. He sits on the advisory boards of several international research institutes and biotechs, and develops new drug discovery technologies with companies including Pfizer, GSK and AstraZeneca. His research has been recognised by awards and Fellowships, most recently the 2019 Sir David Cooksey Translation Prize, the 2020 Corday-Morgan Prize of the RSC, a 2022 Cancer Research UK Programme Award, and the 2024 RSC Horizon Prize. In 2023 he was appointed to the GSK Endowed Chair in Chemical Biology at Imperial College. Ed is also academic founder of several companies developing his lab’s research toward clinical applications, including Siftr Bio and Myricx Bio, which in 2024 raised one of the largest Series A rounds to date for a European biotech.
Steven Gygi
Harvard Medical School
Talk title: Covalent Breakers in Drug Discovery: Disrupting Protein-Protein Interactions
Biography: Steven Gygi, Ph.D., received his Ph.D. from the University of Utah in Pharmacology and Toxicology performing small molecule mass spectrometry. He went on to pursue postdoctoral work with Ruedi Aebersold at the University of Washington in 1996. A revolution in biological mass spectrometry was occurring which allowed for the measurement of protein expression levels, and a new field, Proteomics, was born. In 2000, Dr. Gygi moved to Harvard Medical School and joined the Department of Cell Biology. Currently, he is the faculty director of two MS core facilities (Taplin Biological MS Facility, and the Thermo Fisher Center for Multiplexed Proteomics).
Research in the Gygi lab centers around developing and applying new technologies in the field of mass spectrometry-based proteomics. These include the systematic and proteome-wide measurements of many protein properties including their expression levels, modification states, structure, localization, function, and interactions. For example, the Gygi lab, together with the Harper lab at HMS, is creating a genome-scale map of the protein-protein interaction landscape in cells (termed BioPlex). In addition, sample multiplexing techniques like Tandem Mass Tags (TMT) are being improved to allow up to 32 proteomics samples to be analyzed simultaneously using high-resolution mass spectrometry. One growing application area for TMT is in fragment-based drug discovery where entire libraries can be profiled for reactivity towards thousands of cysteines in cells.
Dr Matthew Boygo
Stanford University
Talk title: Making it stick: applications for covalent probes in drug discovery, diagnostics and imaging
Biography: Dr. Bogyo is a Professor of Pathology and Microbiology and Immunology at Stanford University. He received his bachelor’s degree in Chemistry from Bates College in 1993 and a doctorate in Chemistry from Massachusetts Institute of Technology in 1997. Dr. Bogyo established an independent scientific career as a Faculty Fellow at the University of California, San Francisco in 1998. In 2001, Dr. Bogyo established the Chemical Proteomics Department at Celera Genomics focused on applying small molecule probes to the field of drug discovery. Dr. Bogyo then joined the Department of Pathology at Stanford University in July 2003 and was promoted to Associate Professor in 2009 and to full professor in 2013. Dr. Bogyo has published over 300 primary research publications and currently serves on the Editorial Board of several journals. Dr. Bogyo is also a member of Stanford’s Comprehensive Cancer Center, the Molecular Imaging Program at Stanford (MIPS) and is a consultant for several biotechnology and pharmaceutical companies in the Bay Area. He is the recipient of numerous awards including the Searle Scholar Award, The Terman Fellowship and the Burroughs Wellcome Investigators in Pathogenesis award. He is the co-founder of Akrotome Imaging, a company developing imaging contrast agents for detection of surgical margins.
Dr Scott Lovell
University of Bath
Talk title: Screening Approaches for the Identification of Covalent Peptide Inhibitors
Biography: Scott Lovell is a Future Leaders Fellow and Senior Lecturer of Chemical Biology in the Department of Life Sciences. Before joining the University of Bath in 2022, he was a postdoctoral researcher and Dean’s fellow in the lab of Prof. Matt Bogyo in the School of Medicine at Stanford University. Prior to this Scott acquired his PhD in Chemical Biology at Imperial College in the group of Prof. Ed Tate where he was also an EPSRC Doctoral Prize Fellow. Scott has worked in research labs around the world including in the UK, US, Australia, and Canada and has significant industry experience having worked for AstraZeneca and Pfizer as a synthetic chemist.
Abstract: The identification of selective covalent peptide ligands enables high-affinity and durable engagement of challenging protein targets, particularly within highly homologous enzyme families. In this work, we describe an integrated platform for the identification of targeted covalent macrocycles (TCMs) - peptide based ligands that combine the structural and selectivity advantages of macrocyclic peptides with the sustained target engagement of covalent inhibitors. Our approach uniquely integrates peptide phage display, systematic electrophile scanning, and direct-to-biology screening to enable the discovery of selective covalent binders without reliance on extensive target engineering or in vitro optimisation. We apply this covalent peptide discovery strategy to the kallikrein-related peptidases (KLKs), a family of 15 secreted serine proteases that form a tightly regulated proteolytic network (the KLK activome) with essential roles in extracellular proteolysis and signalling.2 Dysregulation of KLK activity is implicated in tumour growth, invasion, metastasis, and therapeutic resistance, and several family members - including KLK3/prostate-specific antigen (PSA) - exhibit highly restricted expression patterns and established clinical relevance. These features make KLKs an ideal system for evaluating the ability of TCMs to discriminate between closely related enzymes. Overall, this work demonstrates how covalent macrocyclic peptide discovery can be leveraged to generate highly selective chemical tools for probing protease biology and highlights the broader potential of this strategy for cancer imaging and targeted payload delivery.
Dr David Heppner
The State University of New York at Buffalo
Talk title: Profiling and Characterizing Covalent Inhibitors
Biography: David E. Heppner is the J. Solo Assistant Professor of Medicinal Chemistry in the Department of Chemistry at the State University of New York at Buffalo. He earned his B.S. in Chemistry from the University of Minnesota and completed his Ph.D. in Chemistry under the mentorship of Edward I. Solomon at Stanford University.
Dr. Heppner received interdisciplinary training in biomedical research as an NIH postdoctoral fellow with Albert van der Vliet at the University of Vermont, followed by advanced postdoctoral research in medicinal chemistry, cancer biology, and structural biology with Michael J. Eck at the Dana-Farber Cancer Institute and Harvard Medical School.
The Heppner Laboratory integrates structural insights with medicinal chemistry to advance drug discovery, with an emphasis on the design and development of novel small-molecule therapeutics relevant to multiple disease areas. Prof. Heppner currently serves as an Associate Editor for the Journal of Medicinal Chemistry and was the recipient of the 2025 Philip S. Portoghese Lectureship Award.
More information about our speakers will be available soon.
