Chemistry:Subasumstat
From HandWiki
Subasumstat (TAK-981) is a drug that acts as a SUMOylation inhibitor. By preventing cellular proteins from being stabilised by conjugation with SUMO proteins, it makes it more difficult for cancer cells to maintain genomic stability during repeated cell divisions. It has been researched for the treatment of leukemia, as well as other forms of cancer.[1][2][3][4][5][6][7][8]
References
- ↑ "The SUMOylation inhibitor subasumstat potentiates rituximab activity by IFN1-dependent macrophage and NK cell stimulation". Blood 139 (18): 2770–2781. May 2022. doi:10.1182/blood.2021014267. PMID 35226739.
- ↑ "SUMOylation inhibition overcomes proteasome inhibitor resistance in multiple myeloma". Blood Advances 7 (4): 469–481. February 2023. doi:10.1182/bloodadvances.2022007875. PMID 35917568.
- ↑ "T Cell-intrinsic Immunomodulatory Effects of TAK-981 (Subasumstat), a SUMO-activating Enzyme Inhibitor, in Chronic Lymphocytic Leukemia". Molecular Cancer Therapeutics 22 (9): 1040–1051. September 2023. doi:10.1158/1535-7163.MCT-22-0762. PMID 37420267.
- ↑ "SUMOylation inhibitor TAK-981 (subasumstat) synergizes with 5-azacytidine in preclinical models of acute myeloid leukemia". Haematologica 109 (1): 98–114. January 2024. doi:10.3324/haematol.2023.282704. PMID 37608777.
- ↑ "Phase I/II Study of Subasumstat (TAK-981) in Combination With Rituximab in Relapsed/Refractory Non-Hodgkin Lymphoma". Clinical Lymphoma, Myeloma & Leukemia 25 (11): 788–799.e11. November 2025. doi:10.1016/j.clml.2025.04.020. PMID 40467383.
- ↑ "A First-In-Human Study of the SUMOylation Inhibitor Subasumstat in Patients with Advanced/Metastatic Solid Tumors or Relapsed/Refractory Hematologic Malignancies". Cancer Research Communications 5 (11): 2025–2038. November 2025. doi:10.1158/2767-9764.CRC-25-0243. PMID 41134690.
- ↑ "Targeting SUMOylation Triggers IFN-β-dependent Activation of Patient and Allogenic NK Cells in Preclinical Models of Acute Myeloid Leukemia". Molecular Cancer Therapeutics 25 (1): 125–139. January 2026. doi:10.1158/1535-7163.MCT-25-0504. PMID 40661051.
- ↑ "Targeting Mutual Dependence of Phosphatidylinositol-3-Kinase α/δ and Small Ubiquitin-Like Modifier Signaling in Pancreatic Cancer.". Gastroenterology 170 (2): 315–329. February 2026. doi:10.1053/j.gastro.2025.08.018. PMID 41143762.
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