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《Molecular cell》2021,81(16):3386-3399.e10
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Koen Bartholomeeusen Yanhui Xiang Koh Fujinaga B. Matija Peterlin 《The Journal of biological chemistry》2012,287(43):36609-36616
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Dr. Rongkun Lin Jie Yang Ting Liu Mingyu Wang Chongrong Ke Prof. Dr. Cheng Luo Dr. Jin Lin Dr. Jiacheng Li Prof. Dr. Hua Lin 《化学与生物多样性》2023,20(8):e202300769
Direct modulation of the non-kinase functions of cyclin and CDK-cyclin complexes poses challenges. We utilize hydrophobic tag (HyT) based small-molecule degraders induced degradation of cyclin T1 and its corresponding kinase partner CDK9. LL-CDK9-12 demonstrated the most potent and selective degradation ability, with DC50 values of 0.362 μM against CDK9 and 0.680 μM against cyclin T1. In prostate cancer cells, LL-CDK9-12 showed enhanced anti-proliferative activity than its parental molecule SNS032 and LL-K9-3, the previous reported CDK9-cyclin T1 degrader. Moreover, LL-CDK9-12 suppressed the downstream signaling of CDK9 and AR efficiently. Altogether, LL-CDK9-12 was an effective dual degrader of CDK9-cyclin T1 and helped study the unknown function of CDK9-cyclin T1. These results suggest that HyT-based degraders could be used as a strategy to induce the degradation of protein complexes, providing insights for the design of protein complexes′ degraders. 相似文献
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《Molecular cell》2021,81(15):3096-3109.e8