molecules of the month

compound 13

DCAF1 binder

preclinical, applied to targeted protein degradation

from HTS + optimization

ACS Med. Chem. Lett. June 2, 2023

Novartis, Basel, CH

compound 13, DCAF1 ligand, DCAF1 binder preclinical, applied to targeted protein degradation, from HTS + optimization, ACS Med. Chem. Lett. June 2, 2023, NOVARTIS, BASEL, CH
6 mins read

A DCAF1 Ligand Designed for Targeted Protein Degradation Targeted protein degraders continue to show differentiation from traditional small molecules in terms of both efficacy and safety. To expand the scope of targeted protein degradation (TPD), there has been significant interest throughout the industry in leveraging new E3 ligases beyond CRBN, VHL, MDM2, cIAP, and SCF. In 2022, the Cravatt lab published proof-of-concept work showing that covalent acrylamides could be used to recruit DCAF1 to mediate protein degradation via the Cullin4-RING E3 ubiquitin ligase complex. This year, the team at Novartis published a tour de force campaign to rationally identify novel DCAF1 ligands and develop non-covalent DCAF1-based PROTACs that differentiate from existing CRBN-based PROTACs. The rational lead generation campaign is particularly…

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