Identifying ligands for the PHD1 finger of KDM5A through high-throughput screening-Reference-Cited by-同舟云学术

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Identifying ligands for the PHD1 finger of KDM5A through high-throughput screening

Published:2024 Issue: Volume: Page:
ISSN:2633-0679
Container-title:RSC Chemical Biology
language:en
Short-container-title:RSC Chem. Biol.

Author:

Ortiz Gloria¹^ORCID,Longbotham James E.¹,Qin Sophia L.¹,Zhang Meng Yao¹,Lee Gregory M.²³^ORCID,Neitz R. Jeffrey²³,Kelly Mark J. S.³,Arkin Michelle R.²³^ORCID,Fujimori Danica Galonić¹³^ORCID

Affiliation:

1. Department of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, CA 94158, USA

2. Small Molecule Discovery Center (SMDC), University of California San Francisco, San Francisco, CA 94158, USA

3. Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, USA

Abstract

To identify ligands for the regulatory PHD1 domain of KDM5A, high-throughput screening and biophysical validation were conducted and led to the identification of benzofuran ligands. This work offers a starting point for further optimization of PHD1 ligands.

Funder

National Cancer Institute

Publisher

Royal Society of Chemistry (RSC)

Subject

Biochemistry, Genetics and Molecular Biology (miscellaneous),Molecular Biology,Biochemistry,Chemistry (miscellaneous)

Link

http://pubs.rsc.org/en/content/articlepdf/2024/CB/D3CB00214D

Reference38 articles.

1. Many keys to push: diversifying the ‘readership’ of plant homeodomain fingers

2. Atypical histone targets of PHD fingers

3. PHD Fingers: Epigenetic Effectors and Potential Drug Targets

4. Handpicking epigenetic marks with PHD fingers

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