肿瘤药学
腫瘤藥學
종류약학
ANTI-TUMOR PHARMACY
2013年
1期
2-6
,共5页
李代洪%艾俊涛%谢欣%胡高云%李乾斌*
李代洪%艾俊濤%謝訢%鬍高雲%李乾斌*
리대홍%애준도%사흔%호고운%리건빈*
血小板衍生生长因子%血小板衍生生长因子受体%小分子抑制剂%肿瘤
血小闆衍生生長因子%血小闆衍生生長因子受體%小分子抑製劑%腫瘤
혈소판연생생장인자%혈소판연생생장인자수체%소분자억제제%종류
PDGF%PDGFR%Small molecule inhibitors%Tumor
血小板衍生生长因子(platelet-derived growth factor, PDGF)是一种重要的促有丝分裂因子,与多种疾病的发生有关,PDGF发挥其生理作用是通过血小板衍生生长因子受体(platelet-derived growth factor receptor, PDGFR)介导的细胞信号传导实现的,PDGFR是一种酪氨酸蛋白激酶受体,已成为肿瘤等多种疾病的治疗靶点.目前已开发了喹喔啉、喹唑啉、吲哚酮等多种结构的PDGFR抑制剂,并有伊马替尼、苏尼替尼等多种抑制剂上市或进入临床实验研究阶段.本文旨在对PDGF的结构与功能以及PDGFR抑制剂的研究进展进行综述.
血小闆衍生生長因子(platelet-derived growth factor, PDGF)是一種重要的促有絲分裂因子,與多種疾病的髮生有關,PDGF髮揮其生理作用是通過血小闆衍生生長因子受體(platelet-derived growth factor receptor, PDGFR)介導的細胞信號傳導實現的,PDGFR是一種酪氨痠蛋白激酶受體,已成為腫瘤等多種疾病的治療靶點.目前已開髮瞭喹喔啉、喹唑啉、吲哚酮等多種結構的PDGFR抑製劑,併有伊馬替尼、囌尼替尼等多種抑製劑上市或進入臨床實驗研究階段.本文旨在對PDGF的結構與功能以及PDGFR抑製劑的研究進展進行綜述.
혈소판연생생장인자(platelet-derived growth factor, PDGF)시일충중요적촉유사분렬인자,여다충질병적발생유관,PDGF발휘기생리작용시통과혈소판연생생장인자수체(platelet-derived growth factor receptor, PDGFR)개도적세포신호전도실현적,PDGFR시일충락안산단백격매수체,이성위종류등다충질병적치료파점.목전이개발료규악람、규서람、신타동등다충결구적PDGFR억제제,병유이마체니、소니체니등다충억제제상시혹진입림상실험연구계단.본문지재대PDGF적결구여공능이급PDGFR억제제적연구진전진행종술.
Platelet-derived growth factor (PDGF) is a significant mitogen, which has been proved to be related to many diseases. PDGF physiological function works through the signal transduction mediated by platelet-derived growth factor re-ceptor (PDGFR). PDGFR, a tyrosine kinase receptor, has become therapy targets of many diseases, such as cancer. So far many PDGFR inhibitors have been developed of various chemical structures such as quinoxaline, quinazoline and indolone. Several inhibitors like imatinib and sunitinib have come to market or gotten into clinical trials. This article is aimed to introduce the structure and function of PDGF as well as the research progress on platelet-derived growth factor receptor inhibitors.