Flipped Out: Structure-guided Design of Selective Pyrazolylpyrrole Erk Inhibitors.
From: Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge, Massachusetts 02139-4242, USA. alex_aronov@vrtx.com
Journal of medicinal chemistry
- Publish Date: Mar 2007
- ISSN: 0022-2623
- Volume: 50
- Issue: 6
- Pages: 1280-7
- Medium: Print
- Language: English
- Citation (JAMA): Aronov Alex M, Baker Christopher, Bemis Guy W, et al. Flipped Out: Structure-guided Design of Selective Pyrazolylpyrrole Erk Inhibitors.. J. Med. Chem. Mar 2007;50:1280-7
Abstract
The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.
Mesh Headings (Keywords): Binding Sites, Crystallography, X-Ray, Mitogen-Activated Protein Kinase 1, Mitogen-Activated Protein Kinase 3, Models, Molecular, Molecular Structure, Protein Binding, Pyrazoles, Pyrroles, Quantitative Structure-Activity Relationship, Stereoisomerism
Check for Full Text / PubMed Unique Identifier (PMID): 17300186
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