Remediating cancer via splicing modulation

Butler, Mark S. (2013) Remediating cancer via splicing modulation. Journal of Medicinal Chemistry, 56 17: 6573-6575. doi:10.1021/jm401289z

Author Butler, Mark S.
Title Remediating cancer via splicing modulation
Journal name Journal of Medicinal Chemistry   Check publisher's open access policy
ISSN 0022-2623
Publication date 2013-09-12
Year available 2013
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1021/jm401289z
Volume 56
Issue 17
Start page 6573
End page 6575
Total pages 3
Place of publication Washington, DC United States
Publisher American Chemical Society
Collection year 2014
Language eng
Subject 1313 Molecular Medicine
3002 Drug Discovery
Abstract The identification of three distinct but structurally related classes of microbial-derived spliceosome modulators has provided an exciting opportunity for the development of mechanistically new cancer treatments. A team at UC San Diego has undertaken a SAR study on the spliceosome modulator FD-895 that focused on improving compound stability, while retaining potent antiproliferative and splicing activity. This led to the identification of a more potent and stable analog, (17S)-FD-895 (1), and a less active but extremely stable cyclopropane analog 2, which is currently undergoing preclinical evaluation. These analogs will serve as templates for next generation spliceosome modulating anticancer drugs.
Q-Index Code CX
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
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Created: Thu, 28 Nov 2013, 19:44:31 EST by System User on behalf of Institute for Molecular Bioscience