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Azaindoles as Zinc-Binding Small-Molecule Inhibitors of the JAMM Protease CSN5

Altmann, Eva and Erbel, Paulus and Renatus, Martin and Schaefer, Michael and Schlierf, Anita and Druet, Adelaide and Kieffer, Laurence and Sorge, Mickael and Pfister, Keith and Hassiepen, Ulrich and Ostermeier, Daniela and Martoglio, Bruno and Jefferson , Anne B. and Ruedisser, Simon (2017) Azaindoles as Zinc-Binding Small-Molecule Inhibitors of the JAMM Protease CSN5. Chimia., 71 (4). p. 241. ISSN 10.2533/chimia2017.241

Abstract

Cullin-RING ligases (CRLs) represent the largest family of E3 ubiquitin ligases. CSN5 is the zinc metalloprotease subunit of the COP9 signalosome, an important regulator of CRLs. Elevated expression of CSN5 has been found in several types of cancers. Altmann and coworkers describe the discovery of azaindoles as a new class of CSN5 inhibitors, which interact with the active-site zinc ion through an unprecedented binding mode. Nanomolar inhibitors led to degradation of the substrate recognition subunit Skp2 and reduced the viability of HCT116 cells. The study provides a proof-of-concept for the potential of CSN5 inhibitors as anticancer agents.

Item Type: Article
Keywords: Azaindole CSN5 Inhibitor
Date Deposited: 18 Jul 2017 00:45
Last Modified: 18 Jul 2017 00:45
URI: https://oak.novartis.com/id/eprint/32275

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