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Discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1

Winkler, Sebastiaan; Jadhav, Gopal P.; Kaur, Ishwinder; Maryati, Maryati; Airhihen, Blessing; Fischer, Peter M.

Authors

Sebastiaan Winkler

Gopal P. Jadhav

Ishwinder Kaur

Maryati Maryati

Blessing Airhihen

Peter M. Fischer

Abstract

Eukaryotic mRNA contains a 3′ poly(A) tail, which plays important roles in the regulation of mRNA stability and translation. Well-characterized enzymes involved in the shortening of the poly(A) tail include the multi-subunit Ccr4-Not deadenylase, which contains the Caf1 (Pop2) and Ccr4 catalytic components, and poly(A)-specific ribonuclease (PARN). Two Mg2+ ions present in the active sites of these ribonucleases are required for RNA cleavage. Here, we report the discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as (sub)micromolar inhibitors of Caf1.

Journal Article Type Article
Publication Date Oct 1, 2015
Electronic ISSN 1464-3405
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 25
Issue 19
Pages 4219-4224
DOI https://doi.org/10.1016/j.bmcl.2015.07.095
Publisher URL https://www.sciencedirect.com/science/article/pii/S0960894X15008148
PMID 26299350
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