Ontology highlight
ABSTRACT:
SUBMITTER: Kump KJ
PROVIDER: S-EPMC8024114 | biostudies-literature | 2020 Mar
REPOSITORIES: biostudies-literature
Kump Karson J KJ Miao Lei L Mady Ahmed S A ASA Ansari Nurul H NH Shrestha Uttar K UK Yang Yuting Y Pal Mohan M Liao Chenzhong C Perdih Andrej A Abulwerdi Fardokht A FA Chinnaswamy Krishnapriya K Meagher Jennifer L JL Carlson Jacob M JM Khanna May M Stuckey Jeanne A JA Nikolovska-Coleska Zaneta Z
Journal of medicinal chemistry 20200214 5
Anti-apoptotic Bcl-2 family proteins are overexpressed in a wide spectrum of cancers and have become well validated therapeutic targets. Cancer cells display survival dependence on individual or subsets of anti-apoptotic proteins that could be effectively targeted by multimodal inhibitors. We designed a 2,5-substituted benzoic acid scaffold that displayed equipotent binding to Mcl-1 and Bfl-1. Structure-based design was guided by several solved cocrystal structures with Mcl-1, leading to the dev ...[more]