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通过BH3模拟物释放致癌激酶抑制剂的力量。

Unleashing the power of inhibitors of oncogenic kinases through BH3 mimetics.

作者信息

Cragg Mark S, Harris Claire, Strasser Andreas, Scott Clare L

机构信息

The Walter and Eliza Hall Institute of Medical Research, Parkville, Melbourne, Victoria, Australia.

出版信息

Nat Rev Cancer. 2009 May;9(5):321-6. doi: 10.1038/nrc2615. Epub 2009 Apr 3.

Abstract

Therapeutic targeting of tumours on the basis of molecular analysis is a new paradigm for cancer treatment but has yet to fulfil expectations. For many solid tumours, targeted therapeutics, such as inhibitors of oncogenic kinase pathways, elicit predominantly disease-stabilizing, cytostatic responses, rather than tumour regression. Combining oncogenic kinase inhibitors with direct activators of the apoptosis machinery, such as the BH3 mimetic ABT-737, may unlock potent anti-tumour potential to produce durable clinical responses with less collateral damage.

摘要

基于分子分析对肿瘤进行治疗性靶向是癌症治疗的一种新范式,但尚未达到预期效果。对于许多实体瘤而言,靶向治疗药物,如致癌激酶途径抑制剂,主要引发疾病稳定、细胞生长抑制反应,而非肿瘤消退。将致癌激酶抑制剂与凋亡机制的直接激活剂,如BH3模拟物ABT - 737联合使用,可能释放强大的抗肿瘤潜力,以产生持久的临床反应且附带损害更小。

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