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以PROTAC為代表的靶向蛋白質(zhì)降解是藥物發(fā)現(xiàn)的新興策略,研究人員設(shè)計并合成了多種PROTAC,此研究中所有PK研究均通過美迪西進(jìn)行

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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