Evans Lindsay E, Jones Keith, Cheeseman Matthew D
Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London SW7 3RP, UK.
Chem Commun (Camb). 2017 May 4;53(37):5167-5170. doi: 10.1039/c7cc01376k.
Proteins typically carry out their biological functions as multi-protein complexes, which can significantly affect the affinity of small-molecule inhibitors. HSP70 is an important target in oncology, so to study its chemical biology and the drug discovery potential of the HSP70/BAG1 complex, we designed a high-affinity non-nucleotide fluorescence polarisation probe.
蛋白质通常以多蛋白复合物的形式发挥其生物学功能,这会显著影响小分子抑制剂的亲和力。热休克蛋白70(HSP70)是肿瘤学中的一个重要靶点,因此为了研究其化学生物学以及HSP70/BAG1复合物的药物发现潜力,我们设计了一种高亲和力的非核苷酸荧光偏振探针。