Literature summary for 2.2.1.1 extracted from

Thomas, A.A.; De Meese, J.; Le Huerou, Y.; Boyd, S.A.; Romoff, T.T.; Gonzales, S.S.; Gunawardana, I.; Kaplan, T.; Sullivan, F.; Condroski, K.; Lyssikatos, J.P.; Aicher, T.D.; Ballard, J.; Bernat, B.; DeWolf, W.; Han, M.; Lemieux, C.; Smith, D.; Weiler, S.; Wright, S.K.; Vigers, G.; Brandhuber, B.
Non-charged thiamine analogs as inhibitors of enzyme transketolase (2008), Bioorg. Med. Chem. Lett., 18, 509-512.

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Application

Application	Comment	Organism
drug development	non-permanently charged thiamine mimetics (thiamine analogs possessing B-rings unable to participate in the cycle) are competent substrates for thiamine pyrophosphokinase, and the resulting pyrophosphates antagonize the activity of transketolase in vitro. Despite remarkable potencies in enzymatic assays, cellular potencies are modest to poor. Inhibition of the thiamine-utilizing enzyme transketolase is linked with diminished tumor cell proliferation	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
deazathiamine	retains thiamine pyrophosphokinase activity. Despite improvements in binding to transketolase in enzymatic assays, cell potency relative to the thiazolones and charged thiamine mimetics decrease	Homo sapiens
N3P-TT	an aminopyridine, which possesses low micromolar cellular potency against transketolase	Homo sapiens
thiamine thiazolone	retains thiamine pyrophosphokinase activity, is a significantly better binder to transketolase than thiamine	Homo sapiens
thiamine thiazolone diphosphate	is a significantly better binder to transketolase than thiamine	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
HCT-116 cell	-	Homo sapiens	-

Cofactor

Cofactor	Comment	Organism	Structure
thiamine diphosphate	thiamine B-ring is an essential component of catalysis	Homo sapiens

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Release 2023.1 (January 2023)