WebDec 11, 2014 · Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatment of human African trypanosomiasis (HAT). From … WebAug 12, 2014 · Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatment of human African trypanosomiasis (HAT). From previous studies, we identified pyrazole sulfonamide, DDD85646 (1), a potent inhibitor of TbNMT.

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WebAug 6, 2024 · DDD85646, a potent pan-NMT inhibitor, drastically reduces CVB3 titers in various host cells. The NMT1 KO resulted in a substantially decreased production of … Web130 DDD85646 (Fig. 2B), indicating that DDD85646 inhibits Nmt activity. 131 Next, we tested whether the Nmt inhibitor facilitates the conversion of the 132 primed-state mEpiSCs derived from post-implantation embryos into the mESC-like 133 naive-state cells (Fig. 2C). There are distinct differences in the gene expression profile chimney caps that prevent downdrafts

DDD85646-mediated inhibition of cellular N-myristoylation

WebDec 18, 2014 · Encouragingly, analogues of DDD85646 show improved translation of enzyme to cellular activity. In testing the high-throughput L. donovani hits, we observed macrophage cytotoxicity with compounds from two of the four NMT-selective series identified, while all four series displayed low enzyme to cellular translation, also seen … WebJan 10, 2024 · In DDD85646, this allows comparing compounds that form a hydrogen bond (unprotonated DDD85646) to compounds that form a salt bridge (protonated DDD85646). However, considering the pKa of the IMP-1088 and DDD85646, the unprotonated forms may rarely exist under the physiological pH, and thus the interaction between unprotonated … WebDDD85646, the previously published T. brucei NMT inhibitor. Source publication +8 Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of... chimney cap wind deflector