WEHI Special ACRF Chemical Biology Seminar hosted by Professor Isabelle Lucet

Paul Brennan PhD FRSC

Professor Medicinal Chemistry

Director – Centre for Medicines Discovery

Nuffield Department of Medicine – University of Oxford

Chemical Probes in Target Discovery

Davis Auditorium / Bundoora Large Boardroom

Join via TEAMS

Including Q&A session

Target Discovery and validation are the earliest steps in the long process of drug discovery. With a wealth of new protein targets discovered by omics techniques such as GWAS, eQTL and proteomics studies, prioritising targets for biological relevance and tractability via computational and high-throughput cellular methods is critical before major investment in drug discovery takes place. Chemical probes are potent and selective small molecule inhibitors that can be used in cellular assays to induce a phenotype and uncover novel targets for drug discovery. Epigenetics is the study of heritable changes in phenotype that are not encoded in an organism’s DNA. Epigenetic effects due to persistent changes in gene transcription have been linked to chemical modification of DNA and the proteins that package and regulate DNA in the nucleus, histones. Two of the major post-translational modifications of histones are acetylation and methylation of lysine residues prevalent in histone tails. By screening a library of epigenetic chemical probes in cellular assay from patient tissue, we have discovered novel targets and lead compounds for developing treatments for two rare diseases: Dupuytren’s contracture and Friedreich’s ataxia.

Paul Brennan received his PhD in organic chemistry from UC Berkeley. Following post-doctoral research at Cambridge University, Paul spent eight years working in the pharmaceutical industry at Amgen and Pfizer. After leaving Pfizer in 2011, Paul joined the Structural Genomics Consortium at the University of Oxford and led the chemical probes discovery effort on epigenetic targets. After leaving the SGC in 2019, Paul was Head of Chemistry and then Chief Scientific Officer of the Alzheimer’s Research UK Oxford Drug Discovery Institute where his research was focused on finding new treatments for dementia. In addition to dementia, Paul has worked on discovering new medicines for cancer, incontinence, pain, rare diseases, and inflammation. Paul is currently Professor of Medicinal Chemistry and Director of the Centre for Medicines Discovery at the University of Oxford and a scientific advisor to the biotech and pharmaceutical industries. His research centre is focused on early medicines discovery for poorly treated diseases.

All Welcome!