Subasumstat TAK-981: SUMO Activating Enzyme Inhibitor
Discover Subasumstat (TAK-981), a small molecule that selectively inhibits SUMO-activating enzyme, blocking SUMOylation of target proteins. Learn about its mechanism of action and …
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO ... - PubMed
Mar 11, 2021 · Here, we describe the identification of TAK-981, a mechanism-based inhibitor of SAE which forms a SUMO-TAK-981 adduct as the inhibitory species within the enzyme …
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO …
Feb 25, 2021 · In mouse syngeneic tumor models, TAK-981 was shown to promote an innate immune response capable of bridging to an adaptive antitumor immune response, …
Phase 1/2 study of the novel SUMOylation inhibitor TAK-981 in …
May 28, 2021 · TAK-981 is a first-in-class, small-molecule inhibitor of SUMO-activating enzyme subunit 2 (SAE2). Inhibition of SAE2 by TAK-981 disrupts SUMOylation, thereby allowing …
TAK-981-1502 | Clinical Trial Summary - Takeda Pharmaceutical …
TAK-981 is being tested in combination with pembrolizumab to treat participants who have select advanced or metastatic solid tumors. The study aims are to evaluate the safety, tolerability, …
TAK-981, a SUMOylation inhibitor, suppresses AML growth …
Jul 11, 2023 · TAK-981, a first-in-class SUMOylation inhibitor currently under clinical trials for solid tumors, showed antileukemic effects with apoptosis induction, cell-cycle arrest, and induction …
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO …
Mar 11, 2021 · Here, we describe the identification of TAK-981, a mechanism-based inhibitor of SAE which forms a SUMO–TAK-981 adduct as the inhibitory species within the enzyme …
TAK-981, a SUMOylation inhibitor, suppresses AML growth …
Jul 3, 2023 · TAK-981, a first-in-class SUMOylation inhibitor currently under clinical trials for solid tumors, showed antileukemic effects with apoptosis induction, cell-cycle arrest, and induction …
TAK-981, a First-in-Class SUMO-Activating Enzyme Inhibitor, …
Nov 5, 2021 · The ability of TAK-981 to promote activation of macrophages and NK cells and increase their cytotoxic/phagocytic activity provides a mechanistic rationale for its use in …
The SUMOylation inhibitor TAK-981 (Subasumstat) triggers IFN-I ...
Feb 21, 2024 · TAK-981, a first-in-class inhibitor of SUMOylation undergoing phase I/II clinical trials for cancer, is emerging as an immunomodulatory drug. Here, we demonstrate that TAK …