The Broad Stroke of Hsp90 Inhibitors: Painting over the RAF Inhibitor Paradox.
The Broad Stroke of Hsp90 Inhibitors: Painting over the RAF Inhibitor Paradox.
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Hsp90 抑制剂的大范围：打破 RAF 抑制剂悖论。
DOI：
10.1038/jid.2015.239
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发表时间：
2015
期刊：
影响因子：
--
通讯作者：
Aplin,AndrewE
中科院分区：
文献类型：
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作者：
Vido,MichaelJ;Aplin,AndrewE
新型Hsp90抑制剂XL888正在进行临床研究，用于与快速加速纤维肉瘤（RAF）激酶抑制剂vemurafenib联合治疗不可切除的黑色素瘤。将XL888添加到当前的治疗方案中，可以通过阻断RAF抑制剂悖论来达到额外的目的。这种活性可以减少患者的不良事件，并为成功抑制Hsp90靶蛋白提供生物标志物。
The novel Hsp90 inhibitor XL888 is undergoing clinical investigation for use in conjunction with the rapidly accelerated fibrosarcoma (RAF) kinase inhibitor vemurafenib to treat unresectable melanoma. The addition of XL888 to current regimens may serve an additional purpose by blocking the RAF inhibitor paradox. Such activity could reduce adverse events in patients and provide a biomarker for the successful inhibition of Hsp90 target proteins.