Honey, I shrunk the lead discovery process

Molecular Horizons Seminar: Professor Joel Mackay
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Wollongong Campus
35-G20
Small molecules and antibodies are the two prevalent classes of therapeutic molecules on the market today. However, new technologies are opening the door to other modalities, including cyclic peptides isolated from massive library screens as well as proteins hallucinated by artificial intelligence. In this talk, I will describe recent efforts in my lab to discover lead molecules that target proteins involved in the regulation of gene transcription – a class of proteins that are emerging as desirable therapeutic targets for various disorders.
Our work with cyclic peptides demonstrates that this class of molecules can obtain unparalleled specificity through surprising mechanisms of action, and our fledgling efforts with AI suggest that this strategy can yield inhibitors that successfully target protein domains that are unlikely to be amenable to traditional small-molecule strategies. Most pleasingly, both of these approaches are readily accessible to labs that don’t have an army of medicinal chemists at their disposal.