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- Title
Allosteric modulators of MEK1: drug design and discovery.
- Authors
Shang, Jialin; Lu, Shaoyong; Jiang, Yongjun; Zhang, Jian
- Abstract
Mitogen-activated protein kinase kinase (MAPKK, MEK) mediates signal transduction, controlling cell proliferation and survival. MEK occupies a key downstream position in the Ras-Raf-MEK-ERK signaling pathway, implying that inhibition of MEK will potently suppress tumor cell growth, with potential applications in cancer therapy. Based on the promising therapeutic effects of MEK modulators, continued efforts have been made in this class. Here, we review the discovery and development of MEK1 allosteric modulators, classifying them into four structural groups. The allosteric mechanisms and recent clinical progress involving these modulators are also reviewed.
- Subjects
MITOGEN-activated protein kinases; ALLOSTERIC regulation; CELL proliferation; CANCER treatment; CELLULAR signal transduction; RAS oncogenes; PREVENTION
- Publication
Chemical Biology & Drug Design, 2016, Vol 88, Issue 4, p485
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12780