Discovery, development and application of drugs targeting BCL-2 pro-survival proteins in cancer | Zendy

Erinna F. Lee | Zendy; W. Douglas Fairlie | Zendy

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Discovery, development and application of drugs targeting BCL-2 pro-survival proteins in cancer

Author(s) -

Erinna F. Lee,

W. Douglas Fairlie

Publication year - 2021

Publication title -

biochemical society transactions

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.562

H-Index - 144

eISSN - 1470-8752

pISSN - 0300-5127

DOI - 10.1042/bst20210749

Subject(s) - cancer , drug discovery , cancer drugs , computational biology , cancer research , chemistry , biology , bioinformatics , genetics

The discovery of a new class of small molecule compounds that target the BCL-2 family of anti-apoptotic proteins is one of the great success stories of basic science leading to translational outcomes in the last 30 years. The eponymous BCL-2 protein was identified over 30 years ago due to its association with cancer. However, it was the unveiling of the biochemistry and structural biology behind it and its close relatives' mechanism(s)-of-action that provided the inspiration for what are now known as 'BH3-mimetics', the first clinically approved drugs designed to specifically inhibit protein-protein interactions. Herein, we chart the history of how these drugs were discovered, their evolution and application in cancer treatment.

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