Cellular mechanisms underlying response and resistance to CDK4/6 inhibitors in the treatment of hormone receptor-positive breast cancer.
Cellular mechanisms underlying response and resistance to CDK4/6 inhibitors in the treatment of hormone receptor-positive breast cancer.
复制标题
激素受体阳性乳腺癌治疗中CDK 4/6抑制剂应答和耐药的细胞机制
DOI：
10.1186/s13058-022-01510-6
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发表时间：
2022-03-05
期刊：
影响因子：
--
通讯作者：
Goel S
中科院分区：
文献类型：
--
作者：
Watt AC;Goel S
细胞周期蛋白依赖性激酶4和6（CDK 4/6）的药理学抑制剂现在是晚期激素受体阳性乳腺癌患者的既定标准治疗。CDK 4/6抑制剂活性的典型机制是抑制视网膜母细胞瘤肿瘤抑制蛋白的磷酸化，其用于防止癌细胞增殖。最近的数据表明，这些药物在肿瘤和间质隔室中诱导其他不同的作用，这有助于解释其临床活性的各个方面。在这里，我们回顾了这些现象，并讨论了如何利用它们开发新的CDK 4/6通道的组合治疗。我们还简要回顾了各种已知的机制，获得性耐药的临床设置。
Pharmacological inhibitors of cyclin-dependent kinases 4 and 6 (CDK4/6) are now an established standard of care for patients with advanced hormone receptor-positive breast cancer. The canonical mechanism underlying CDK4/6 inhibitor activity is the suppression of phosphorylation of the retinoblastoma tumor suppressor protein, which serves to prevent cancer cell proliferation. Recent data suggest that these agents induce other diverse effects within both tumor and stromal compartments, which serve to explain aspects of their clinical activity. Here, we review these phenomena and discuss how they might be leveraged in the development of novel CDK4/6 inhibitor-containing combination treatments. We also briefly review the various known mechanisms of acquired resistance in the clinical setting.
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影响因子：
7.3
作者：
Gao J;Aksoy BA;Dogrusoz U;Dresdner G;Gross B;Sumer SO;Sun Y;Jacobsen A;Sinha R;Larsson E;Cerami E;Sander C;Schultz N
通讯作者：
Schultz N
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50.3
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Anders L;Ke N;Hydbring P;Choi YJ;Widlund HR;Chick JM;Zhai H;Vidal M;Gygi SP;Braun P;Sicinski P
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Sicinski P
影响因子：
5.3
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Fingar, DC;Richardson, CJ;Blenis, J
通讯作者：
Blenis, J
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64.5
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Ciriello G;Gatza ML;Beck AH;Wilkerson MD;Rhie SK;Pastore A;Zhang H;McLellan M;Yau C;Kandoth C;Bowlby R;Shen H;Hayat S;Fieldhouse R;Lester SC;Tse GM;Factor RE;Collins LC;Allison KH;Chen YY;Jensen K;Johnson NB;Oesterreich S;Mills GB;Cherniack AD;Robertson G;Benz C;Sander C;Laird PW;Hoadley KA;King TA;TCGA Research Network;Perou CM
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Perou CM
影响因子：
5.7
作者：
Chen, Ping;Lee, Nathan V.;Murray, Brion W.
通讯作者：
Murray, Brion W.