期刊
PIGMENT CELL & MELANOMA RESEARCH
卷 23, 期 6, 页码 820-827出版社
WILEY-BLACKWELL
DOI: 10.1111/j.1755-148X.2010.00763.x
关键词
PLX4032; RG7204; B-Raf; melanoma; therapy; V600E
资金
- NIH [PO1CA114046]
P>Targeted intervention of the B-Raf V600E gene product that is prominent in melanoma has been met with modest success. Here, we characterize the pharmacological properties of PLX4032, a next-generation inhibitor with exquisite specificity against the V600E oncogene and striking anti-melanoma activity. PLX4032 induces potent cell cycle arrest, inhibits proliferation, and initiates apoptosis exclusively in V600E-positive cells in a variety of in vitro experimental systems; follow-up xenograft studies demonstrate extreme selectivity and efficacy against melanoma tumors bearing the V600E oncoproduct. The collective data support further exploration of PLX4032 as a candidate drug for patients with metastatic melanoma; accordingly, validation of PLX4032 as a therapeutic tool for patients with melanoma is now underway in advanced human (Phase III) clinical trials.
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