Non-charged thiamine analogs as inhibitors of enzyme transketolase

AA Thomas, J De Meese, Y Le Huerou, SA Boyd…

文献索引：Thomas, Allen A.; De Meese; Le Huerou; Boyd, Steven A.; Romoff, Todd T.; Gonzales, Steven S.; Gunawardana, Indrani; Kaplan, Tomas; Sullivan, Francis; Condroski, Kevin; Lyssikatos, Joseph P.; Aicher, Thomas D.; Ballard, Josh; Bernat, Bryan; DeWolf, Walter; Han, May; Lemieux, Christine; Smith, Darin; Weiler, Solly; Wright, S. Kirk; Vigers, Guy; Brandhuber, Barb Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 2 p. 509 - 512

全文：HTML全文

被引用次数: 23

摘要

Inhibition of the thiamine-utilizing enzyme transketolase (TK) has been linked with diminished tumor cell proliferation. Most thiamine antagonists have a permanent positive charge on the B-ring, and it has been suggested that this charge is required for diphosphorylation by thiamine pyrophosphokinase (TPPK) and binding to TK. We sought to make neutral thiazolium replacements that would be substrates for TPPK, while not ...