The rational design of ARUK2007145, a dual inhibitor of the α and γ isoforms of the lipid kinase phosphatidylinositol 5-phosphate 4-kinase (PI5P4K)-Reference-Cited by-同舟云学术

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The rational design of ARUK2007145, a dual inhibitor of the α and γ isoforms of the lipid kinase phosphatidylinositol 5-phosphate 4-kinase (PI5P4K)

Published:2023 Issue:10 Volume:14 Page:2035-2047
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Aldred Gregory G.¹^ORCID,Rooney Timothy P. C.¹^ORCID,Willems Henriette M. G.¹^ORCID,Boffey Helen K.¹^ORCID,Green Christopher¹^ORCID,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

We report the rational design of PI5P4Kα/γ dual inhibitors. ARUK2007145 (39) is disclosed as a potent, cell-active probe molecule with ADMET properties amenable to conducting experiments in cells.

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/D3MD00355H

Reference38 articles.

1. Phosphoinositides: Tiny Lipids With Giant Impact on Cell Regulation

2. Novel roles of phosphoinositides in signaling, lipid transport, and disease

3. Phosphoinositides as membrane organizers

4. Nuclear Phosphoinositides as Key Determinants of Nuclear Functions

5. Inositol phosphates and cell signalling

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