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TAK-243 is a potent ubiquitin activating enzyme inhibitor with antitumor efficacy in vivo. Medicilon performed the experiment using the HCC70 model

2023-07-11

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The ubiquitin–proteasome system (UPS) comprises a network of enzymes that is responsible for maintaining cellular protein homeostasis. TAK-243 is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE), the primary mammalian E1 enzyme that regulates the ubiquitin conjugation cascade. TAK-243 has UAE-specific antitumor efficacy in vivo. Medicilon performed the experiment using the HCC70 (triple-negative breast cancer) model.

Reference:

Marc L Hyer, et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat Med. 2018 Feb;24(2):186-193. doi: 10.1038/nm.4474.

ubiquitin–proteasome-system antitumor triple-negative-breast-cancer Pharmacology Pharmacodynamics Model

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