Quick Search:

uzh logo
Browse by:
bullet
bullet
bullet
bullet

Zurich Open Repository and Archive

Permanent URL to this publication: http://dx.doi.org/10.5167/uzh-34628

Melkko, S; Mannocci, L; Dumelin, C E; Villa, A; Sommavilla, R; Zhang, Y; Grütter, M; Keller, N; Jermutus, L; Jackson, R H; Scheuermann, J; Neri, D (2010). Isolation of a small-molecule inhibitor of the antiapoptotic protein Bcl-xL from a DNA-encoded chemical library. ChemMedChem, 5(4):584-590.

[img] PDF - Registered users only
935kB

View at publisher

Abstract

Bcl-xL is an antiapoptotic member of the Bcl-2 protein family and an attractive target for the development of anticancer agents. Here we describe the isolation of binders to Bcl-xL from a DNA-encoded chemical library using affinity-capture selections and massively parallel high-throughput sequencing of >30,000 sequence tags of library members. The most potent binder identified, compound 19/93 [(R)-3-(amido indomethacin)-4-(naphthalen-1-yl)butanoic acid], bound to Bcl-xL with a dissociation constant (K(d)) of 930 nM and was able to compete with a Bak-derived BH3 peptide, an antagonist of Bcl-xL function.

Citations

13 citations in Web of Science®
13 citations in Scopus®
Google Scholar™

Altmetrics

Downloads

0 downloads since deposited on 06 Jul 2010
0 downloads since 12 months

Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:04 Faculty of Medicine > Department of Biochemistry
07 Faculty of Science > Department of Biochemistry
DDC:570 Life sciences; biology
Language:English
Date:6 April 2010
Deposited On:06 Jul 2010 08:27
Last Modified:12 Jan 2014 16:47
Publisher:Wiley-Blackwell
ISSN:1860-7179
Publisher DOI:10.1002/cmdc.200900520

Users (please log in): suggest update or correction for this item

Repository Staff Only: item control page