Targeting mutant fibroblast growth factor receptors in cancer.
Targeting mutant fibroblast growth factor receptors in cancer.
复制标题
DOI：
10.1016/j.molmed.2011.01.012
复制
发表时间：
2011-05
影响因子：
13.6
通讯作者：
Pollock PM
中科院分区：
文献类型：
--
作者：
Greulich H;Pollock PM
成纤维细胞生长因子受体（FGFR）在控制细胞增殖、细胞分化、血管生成和发育中发挥多种作用。长期以来，已知生殖系中FGFR的激活突变会导致各种骨骼发育障碍，但直到最近才发现类似的体细胞FGFR突变谱与人类癌症相关。这些体细胞突变中的许多是功能获得性和致癌性的，并且在携带此类突变的肿瘤细胞系中产生依赖性。临床前模型中的敲除研究和药物抑制相结合，进一步证实了基因组改变的FGFR作为癌症的治疗靶点，肿瘤学界正在通过临床试验来评估具有抗FGFR活性的多激酶抑制剂和新一代特异性泛FGFR抑制剂。
Fibroblast growth factor receptors (FGFRs) play diverse roles in control of cell proliferation, cell differentiation, angiogenesis, and development. Activating mutations of FGFRs in the germline have long been known to cause a variety of skeletal developmental disorders, but it is only recently that a similar spectrum of somatic FGFR mutations has been associated with human cancers. Many of these somatic mutations are gain-of-function and oncogenic and create dependencies in tumor cell lines harboring such mutations. A combination of knock-down studies and pharmaceutical inhibition in preclinical models has further substantiated genomically-altered FGFR as a therapeutic target in cancer, and the oncology community is responding with clinical trials evaluating multi-kinase inhibitors with anti-FGFR activity and a new generation of specific pan-FGFR inhibitors.
登录
查看更多内容
DOI：
10.1158/1541-7786.mcr-08-0021
发表时间：
2009-01
期刊：
Molecular cancer research : MCR
影响因子：
--
作者：
Gartside MG;Chen H;Ibrahimi OA;Byron SA;Curtis AV;Wellens CL;Bengston A;Yudt LM;Eliseenkova AV;Ma J;Curtin JA;Hyder P;Harper UL;Riedesel E;Mann GJ;Trent JM;Bastian BC;Meltzer PS;Mohammadi M;Pollock PM
通讯作者：
Pollock PM
影响因子：
64.8
作者：
通讯作者：
--
影响因子：
20.3
作者：
Chesi, M;Brents, LA;Bergsagel, PL
通讯作者：
Bergsagel, PL
影响因子：
9.3
作者：
Bakkar, AA;Quach, V;Grandchamp, B
通讯作者：
Grandchamp, B
影响因子：
9.8
作者：
Bellus, GA;Spector, EB;Francomano, CA
通讯作者：
Francomano, CA