Discovery of C19-9 as a novel non-RGD inhibitor of αvβ3 to overcome enzalutamide resistance in castration-resistant prostate cancer  

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作  者:Xiaocong Pang Xiaojiao Sun Yanlun Gu Xu He Kan Gong Song Song Jixin Zhang Jie Xia Zhenming Liu Yimin Cui 

机构地区:[1]Peking University First Hospital,Xishiku Street,Xicheng District,100034 Beijing,China [2]School of Pharmaceutical Sciences,Peking University,Xueyuan Road 38,Haidian District,100191 Beijing,China [3]Institute of Materia Medica,Chinese Academy of Medical Sciences,Nanwei Road,Xicheng District,100050 Beijing,China

出  处:《Signal Transduction and Targeted Therapy》2023年第3期891-894,共4页信号转导与靶向治疗(英文)

基  金:This research was funded by National High Level Hospital Clinical Research Funding(Scientific and Technological Achievements Transformation Incubation Guidance Fund Project of Peking University First Hospital)(No.2022CX11,No.2022RT01);National Key R&D Program of China(No.2020YFC2008304);National Natural Science Foundation of China(No.81973320 and No.81903714).Thanks to Dr.Qian Wang in the State Key Laboratory of Natural and Biomimetic Drugs,Peking University for the experimental assistance of SPR.Thanks to K2 Oncology Co.Ltd.for experimental assistance with patient-derived organoids.

摘  要:Dear Editor,The integrinαvβ3 receptor is a promising target for anticancer therapy.1,2 However,there are no effective marketed treatments targetingαvβ3.One possible limitation of Arginine-Glycine-Aspartic(RGD)-mimeticαvβ3 antagonists has been shown to cause partial agonism,which could induce major conformational changes that trigger paradoxical cell adhesion and angiogenesis.

关 键 词:ΑVΒ3 OVERCOME RESISTANCE 

分 类 号:R737.25[医药卫生—肿瘤]

 

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