WebSMTIN-C10 was found to bind to an allosteric binding site at E115 in the N-terminal domain of TRAP1, in addition to binding to the ATP pocket, resulting in TRAP1 adopting a closed … WebIn addition to tight binding with the ATP binding site through the PU-H71 moiety, SMTIN-C10 interacts with the E115 residue in the N-terminal domain through the TPP moiety, and subsequently induces structural transition of TRAP1 to a tightly packed closed form. The data indicate the existence of a druggable allosteric site neighboring the ...
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WebDownload scientific diagram SMTIN-C10 effects on TRAP1. (a) ATPase activity of E93Q, E115Q, and E394Q mutants. Activities of TRAP1 mutants were analyzed in the presence … WebTo allow the flexible SMTIN-C10 alkyl-TPP chain to freely move into the binding site, the apo-form of the crystallographic structure was refined for residues 201-204 belonging to the … increased bile acid in pregnancy
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Web1 Nov 2024 · The compound with a 10-carbon linker (SMTIN-C10) established both orthosteric and allosteric interactions with TRAP1, inducing structural changes in the … Web2 Sep 2024 · The pathogenesis of -associated gastric cancer is dependent on delivery of CagA into host cells through a type IV secretion system (T4SS). The Cag T4SS includes a large membrane-spanning core complex containing five proteins, organized into an outer membrane cap (OMC), a periplasmic ring (PR) and a stalk. Web19 Nov 2024 · From these, the compound with a 10-carbon linker (SMTIN-C10) presented stronger inhibition of TRAP1 than SMTIN-P01 [106]. Shepherdin is a cell-penetrating … increased bile secretion