Discovery of new benzhydrol biscarbonate esters as potent and selective apoptosis inducers of human melanomas bearing the activated ERK pathway: SAR studies on an ERK MAPK signaling modulator, ACA-28
The recent discovery that an ERK signaling modulator [ACA-28 (2a)] preferentially kills human melanoma cell lines by inducing ERK-dependent apoptosis has generated significant interest in the field of anti-cancer therapy. In the first SAR study on 2a, here, we successfully developed candidates (2b, 2c) both of which induce more potent and selective apoptosis towards ERK-active melanoma cells than 2a, thus revealing the structural basis for inducing the ERK-dependent apoptosis and proposing the therapeutic prospect of these candidates against ERK-dependent cancers represented by melanoma.
APOPTOSIS INDUCERS AND THERAPEUTIC AGENTS FOR CANCER
PROBLEM TO BE SOLVED: To provide novel molecular target agents to overcome the problems of current molecular target agents which are designed to inhibit activated genes or products thereof in cancer cells but have a number of clinically serious problems s
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Paragraph 0031; 0032; 0033; 0034; 0035; 0036
(2019/07/25)
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