Targeted protein degradation exemplified by PROTACs is an emerging strategy for drug discovery

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Targeted protein degradation exemplified by PROTACs is an emerging strategy for drug discovery

2023-07-11

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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.

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.