Identification of ARUK2002821 as an isoform-selective PI5P4Kα inhibitor-Reference-Cited by-同舟云学术

Identification of ARUK2002821 as an isoform-selective PI5P4Kα inhibitor

Published:2023 Issue:5 Volume:14 Page:934-946
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Willems Henriëtte M. G.¹^ORCID,Edwards Simon¹,Boffey Helen K.¹^ORCID,Chawner Stephen J.¹^ORCID,Green Christopher¹^ORCID,Romero Tamara¹,Winpenny David¹,Skidmore John¹^ORCID,Clarke Jonathan H.¹^ORCID,Andrews Stephen P.¹^ORCID

Affiliation:

1. The ALBORADA Drug Discovery Institute, University of Cambridge, Island Research Building, Cambridge Biomedical Campus, Hills Road, Cambridge, CB2 0AH, UK

Abstract

The PI5P4Ks play a central role in regulating cell signalling pathways. ARUK2002821 is reported as a potent and selective PI5P4Kα inhibitor (pIC50 = 8.0). ADMET and target engagement data are provided, with a ligand-protein X-ray structure, optimised to deliver ARUK2002821.

Funder

Alzheimer’s Research UK

Alborada Trust

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2023/MD/D3MD00039G

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