Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode-Reference-Cited by-同舟云学术

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Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode

Published:2021-09-11 Issue:18 Volume:64 Page:13780-13792
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Down Kenneth¹^ORCID,Amour Augustin¹,Anderson Niall A.¹^ORCID,Barton Nick¹,Campos Sebastien¹,Cannons Edward P.¹,Clissold Cole²,Convery Maire A.¹,Coward John J.¹,Doyle Kevin²,Duempelfeld Birgit³,Edwards Christopher D.¹,Goldsmith Michael D.²,Krause Jana³,Mallett David N.¹,McGonagle Grant A.¹,Patel Vipulkumar K.¹,Rowedder James¹,Rowland Paul¹,Sharpe Andrew²,Sriskantharajah Srividya¹,Thomas Daniel A.¹,Thomson Douglas W.³,Uddin Sorif¹,Hamblin J. Nicole¹,Hessel Edith M.¹

Affiliation:

1. Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K.

2. Charles River Discovery, Chesterford Research Park, Saffron Walden CB10 1XL, U.K.

3. Cellzome GmbH, A GlaxoSmithKline Company, Meyerhofstraße 1, Heidelberg 69117, Germany

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c01102

Reference34 articles.

1. The Phosphoinositide 3-Kinase Pathway

2. The emerging mechanisms of isoform-specific PI3K signalling

3. Inhibition of PI3K Signaling Spurs New Therapeutic Opportunities in Inflammatory/Autoimmune Diseases and Hematological Malignancies

4. Signalling by PI3K isoforms: insights from gene-targeted mice

5. Targeting phosphoinositide 3-kinase δ for allergic asthma

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2. Targeting the PI3K/AKT/mTOR Signaling Pathway in the Treatment of Human Diseases: Current Status, Trends, and Solutions;Journal of Medicinal Chemistry;2022-12-12

3. fastDRH: a webserver to predict and analyze protein–ligand complexes based on molecular docking and MM/PB(GB)SA computation;Briefings in Bioinformatics;2022-05-18

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