Preclinical evaluation of the selective small-molecule UBA1 inhibitor, TAK-243, in acute myeloid leukemia
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DOI: 10.1038/s41375-018-0167-0
Abstract: Acute myeloid leukemia (AML) is an aggressive hematologic malignancy for which new therapeutic approaches are required. One such potential therapeutic strategy is to target the ubiquitin-like modifier-activating enzyme 1 (UBA1), the initiating enzyme in the… read more here.
Keywords: tak 243; myeloid leukemia; uba1 inhibitor; acute myeloid ... See more keywords
Differential Inhibition of Human and Trypanosome Ubiquitin E1S by TAK-243 Offers Possibilities for Parasite Selective Inhibitors
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DOI: 10.1038/s41598-019-52618-3
Abstract: Novel strategies to target Trypanosoma brucei, Trypanosoma cruzi and Leishmania are urgently needed to generate better and safer drugs against Human African Trypanosomiasis, Chagas disease and Leishmaniasis, respectively. Here, we investigated the feasibility of selectively… read more here.
Keywords: tak 243; differential inhibition; inhibition human; human trypanosome ... See more keywords
Abstract 3476: TAK-243 increases tumor immunogenicity enhancing systemic anti-tumor immune response and tumor regression in combination with immune checkpoint inhibition in a syngeneic model of lymphoma
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DOI: 10.1158/1538-7445.am2023-3476
Abstract: Agents that induce a shift in the activity state of the immune tumor microenvironment (TME) from “cold-to-hot” may increase response to immune checkpoint inhibitors. Here we examined whether TAK-243, a small molecule inhibitor of the… read more here.
Keywords: anti tumor; tumor; combination; tak 243 ... See more keywords
UBA1 inhibition contributes radiosensitization of glioblastoma cells via blocking DNA damage repair
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DOI: 10.3389/fphar.2023.1073929
Abstract: Glioblastoma multiforme (GBM) is a brain tumor with high mortality and recurrence rate. Radiotherapy and chemotherapy after surgery are the main treatment options available for GBM. However, patients with glioblastoma have a grave prognosis. The… read more here.
Keywords: glioblastoma; uba1 inhibition; radiation; gbm ... See more keywords