What question did this study set out to answer?

To identify and characterize A-1331852, a first-in-class, potent, and orally bioavailable small-molecule inhibitor of the anti-apoptotic protein BCL-XL.

March 30, 2020ACS Medicinal Chemistry LettersOpen Access

Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor

View Full Paper

Ask AI

Bookmark

To identify and characterize A-1331852, a first-in-class, potent, and orally bioavailable small-molecule inhibitor of the anti-apoptotic protein BCL-XL.
Structure-guided chemical design and optimization targeting the BCL-2 family protein BCL-XL.
Pharmacological and biochemical evaluation of compound potency, selectivity, and oral bioavailability.
Identified A-1331852 as a first-in-class, potent, and orally bioavailable BCL-XL inhibitor.
Demonstrated utility of A-1331852 as a critical chemical tool for interrogating BCL-2 family biology and initiating therapeutic drug discovery.

Implication

Preclinical study demonstrates potent BCL-XL inhibition by A-1331852 in preclinical models, highlighting its utility as an orally bioavailable tool compound.

Abstract

. A-1331852 has since been used as a critical tool molecule for further exploring BCL-2 family protein biology, while also representing an attractive entry into a drug discovery program.

Discussion

No takes yet. Share an insight, caveat, or question.

Cite This Study

Wang et al. (2020) studied this question.

synapsesocial.com/papers/6a0f502e8090e499da5faba5 https://doi.org/10.1021/acsmedchemlett.9b00568

View Full Paper

Ask AI

Bookmark

Implication

Preclinical study demonstrates potent BCL-XL inhibition by A-1331852 in preclinical models, highlighting its utility as an orally bioavailable tool compound.

Abstract

. A-1331852 has since been used as a critical tool molecule for further exploring BCL-2 family protein biology, while also representing an attractive entry into a drug discovery program.

Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor

Key Points

Implication

Abstract

Discussion

Cite This Study

Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor

Key Points

Implication

Abstract

Discussion

Cite This Study

Keep reading

Keep reading