GOT1inhibitor-1(compound2c)是一种戊酸衍生物，是一种新型的、有效的、非共价的谷氨酸草酰乙酸转氨酶1(GOT1)抑制剂，IC50为8.2uM。GOT1inhibitor-1可用于胰腺导管腺癌(PDAC)的研究。
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC)[1].
PDAC tumors are dependent upon a metabolic pathway involving aspartate aminotransferase 1 (glutamate-oxaloacetate transaminase 1 (GOT1)), for the maintenance of redox homeostasis and sustained proliferation. Small molecule inhibitors targeting this metabolic pathway may provide a novel way for cancer research.In the MDH coupled GOT1 enzymatic assay, GOT1 inhibitor-1 shows an inhibitory effect on GOT1 activity with an IC50 value of 8.2 uM[1].
[1]. Justin Anglin, et al. Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2675-2678
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