Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders
Brett L. Roberts, Zhi‐Xiong Ma, Ang Gao, Eric D. Leisten, Dan Yin, Wei Xu, Weiping Tang
Abstract
= 69%) in MCF-7. This proof-of -concept study demonstrates that the two-stage strategy can significantly facilitate the development of PROTACs against ER without the tedious process of making large numbers of PROTACs one by one. It has the potential to be expanded to many other targets.
Topics & Concepts
Ubiquitin ligaseLinkerEstrogen receptorHydrazideSmall moleculeLigand (biochemistry)ChemistryTarget proteinDrug discoveryDNA ligaseUbiquitinReceptorBiochemistryCombinatorial chemistryBiologyCell biologyCancerGeneticsGeneOrganic chemistryEnzymeOperating systemComputer scienceBreast cancerProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysMultiple Myeloma Research and Treatments