Drugging RAS: Know the enemy

被引：290

作者：

Papke, Bjoern ^{[1
]}

Der, Channing J. ^{[1
]}

机构：

[1] Univ North Carolina Chapel Hill, Lineberger Comprehens Canc Ctr, Chapel Hill, NC 27599 USA

来源：

SCIENCE | 2017年 / 355卷 / 6330期

关键词：

K-RAS; PLASMA-MEMBRANE; SMALL MOLECULES; CANCER; INHIBITION; BRAF; ERK; ASSOCIATION; DISCOVERY; ONCOGENES;

D O I：

10.1126/science.aam7622

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

The three RAS oncogenes make up the most frequently mutated gene family in human cancer. The well-validated role of mutationally activated RAS genes in driving cancer development and growth has stimulated comprehensive efforts to develop therapeutic strategies to block mutant RAS function for cancer treatment. Disappointingly, despite more than three decades of research effort, clinically effective anti-RAS therapies have remained elusive, prompting a perception that RAS may be undruggable. However, with a greater appreciation of the complexities of RAS that thwarted past efforts, and armed with new technologies and directions, the field is experiencing renewed excitement that mutant RAS may finally be conquered. Here we summarize where these efforts stand.

引用

页码：1158 / 1163

页数：6

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