Prof. Nir London
Covalent inhibitors have many advantages as chemical probes and drug candidates, discovery of new covalent inhibitors remains challenging, however. Our lab is interested in covalent molecular recognition, the development of technologies to design and discover such covalent inhibitors and their application to shed new light on biology. We have several leading technologies for covalent probe discovery. One example is DOCKovalent, a software that computationally screens huge libraries of putative covalent binders. Another is a complementary, empirical, electrophile fragment-based approach. Through both, we were able to rapidly discover covalent fragment hits for several protein targets. Some of which progressed to show efficacy in animal models, and were even licensed for development by biotechs. We now develop additional approaches related to targeted protein degradation, proteomic target identification and new screening modalities.