Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders
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https://figshare.com/articles/dataset/Discovery_of_the_First_Examples_of_Threonine_Tyrosine_Kinase_PROTAC_Degraders/19077371
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资源简介：
The
first examples of threonine tyrosine kinase (TTK) PROTACs were
designed and synthesized. Two of the most potent molecules, 8e and 8j, demonstrated strong TTK degradation
in COLO-205 human colorectal cancer cells with DC50 values
of 1.7 and 3.1 nM, respectively. Proteasome-mediated degradation by
the compounds could last for approximately 8 h after washout. The
degraders 8e and 8j demonstrated improved
antiproliferative activities comparing with the structurally similar
inhibitor counterparts 8q and 8r. Degraders 8e and 8j also demonstrated reasonable PK profiles
and exhibited potent target degradation and in vivo anticancer efficacy in a xenograft mouse model of COLO-205 human
colorectal cancer cells upon i.p. administration.
创建时间：
2022-01-27
