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以PROTAC为代表的靶向蛋白质降解是药物发现的新兴战术,钻研人员设计并合成了多种PROTAC,此钻研中所有PK钻研均通过JDB电子进行

Targeted protein deg

2023-07-06
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Targeted protein degradation (TPD) exemplified by PROTACs is an emerging strategy for next generation drug discovery. Threonine tyrosine kinase (TTK) is a dual-specific protein kinase that catalyzes phosphorylation of both serine/threonine and tyrosine residues. Researchers designed and synthesized TTK PROTACs, which demonstrated reasonable pharmacokinetic profiles. All the pharmacokinetic studies were carried out by Medicilon, according to the protocols and guidelines of the institutional care and use committee.

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Reference:

Jibu Lu, et al. Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. J Med Chem. 2022 Feb 10;65(3):2313-2328. doi: 10.1021/acs.jmedchem.1c01768. 

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