Drug Target Strategies

Targeted Protein Degradation via Redirecting the Action of CRL4 E3 Ligases

Wednesday, February 7
3:00 PM - 3:30 PM
Location: 6D

Discovery of the mechanism of action of the multiple myeloma drug lenalidomide opens a new chapter in drug discovery. Distinct cereblon binding molecules evoke different phenotypic responses yet bind the same target. Solution of the ligand bound CRBN complex provides a rationale for distinguishing “gain of function” targeting of key substrates including the transcription factors Aiolos and Ikaros, the protein kinase CK1alpha, or the translation termination factor GSPT1. Is it possible to harness the action of a single E3 ligase and direct its actions toward new and different substrates? Are other ligases able to be co-opted in a similar fashion? The presentation will explain distinctions amongst existing drugs and point to the therapeutic power of harnessing protein homeostatic mechanisms via redirecting the action of E3 ligases.

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Brian E. Cathers

Exec. Director
Celgene

Dr. Cathers is Executive Director and Head of Drug Discovery for the Protein Homeostasis Thematic Center of Excellence at Celgene. Dr. Cathers joined Celgene in 2004 and has led multiple Discovery Projects to successful candidate nominations and IND filings. Prior to Celgene, Dr. Cathers was Director of Enzymology & Biophysical Chemistry at NewBiotics. He generated and led several discovery projects in oncology and infectious diseases. Prior to NewBiotics, Dr. Cathers was a scientist at Axys Pharmaceuticals where he specialized in protease targets (e.g. cathepsins S, B and K) for inflammatory and oncology indications. Dr. Cathers earned his Ph.D. in Medicinal Chemistry from the University of Kansas synthesizing and characterizing novel transition state mimics as inhibitors of HIV protease and was a post-doctoral fellow at the University of Texas in Austin where he trained with Laurence Hurley and Dan Von Hoff working in the areas of G-quadruplex DNA and telomerase.

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Targeted Protein Degradation via Redirecting the Action of CRL4 E3 Ligases



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