Non-charged thiamine analogs as inhibitors of enzyme transketolase.

Non-charged thiamine analogs as inhibitors of enzyme transketolase. Research Abstract Details 

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Non-charged thiamine analogs as inhibitors of enzyme transketolase. Abstract Text:

Allen A Thomas,J De Meese,Y Le Huerou,Steven A Boyd,Todd T Romoff,Steven S Gonzales,Indrani Gunawardana,Tomas Kaplan,Francis Sullivan,Kevin Condroski,Joseph P Lyssikatos,Thomas D Aicher,Josh Ballard,Bryan Bernat,Walter DeWolf,May Han,Christine Lemieux,Darin Smith,Solly Weiler,S Kirk Wright,Guy Vigers,Barb Brandhuber,Allen A Thomas,J De Meese,Y Le Huerou,Steven A Boyd,Todd T Romoff,Steven S Gonzales,Indrani Gunawardana,Tomas Kaplan,Francis Sullivan,Kevin Condroski,Joseph P Lyssikatos,Thomas D Aicher,Josh Ballard,Bryan Bernat,Walter Dewolf,May Han,Christine Lemieux,Darin Smith,Solly Weiler,S Kirk Wright,Guy Vigers,Barb Brandhuber,

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 necessarily needing thiamine transporters (ThTr1 and ThTr2) for cell penetration. The synthesis, SAR, and structure-based rationale for highly potent non-thiazolium TK antagonists are presented.

Non-charged thiamine analogs as inhibitors of enzyme transketolase. Publishing Authors By Initials

AA Thomas,J De Meese,Y Le Huerou,SA Boyd,TT Romoff,SS Gonzales,I Gunawardana,T Kaplan,F Sullivan,K Condroski,JP Lyssikatos,TD Aicher,J Ballard,B Bernat,W DeWolf,M Han,C Lemieux,D Smith,S Weiler,SK Wright,G Vigers,B Brandhuber,AA Thomas,J De Meese,Y Le Huerou,SA Boyd,TT Romoff,SS Gonzales,I Gunawardana,T Kaplan,F Sullivan,K Condroski,JP Lyssikatos,TD Aicher,J Ballard,B Bernat,W Dewolf,M Han,C Lemieux,D Smith,S Weiler,SK Wright,G Vigers,B Brandhuber,

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Non-charged thiamine analogs as inhibitors of enzyme transketolase. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 509-12

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 3

MONTH: 12

YEAR: 2007

Non-charged thiamine analogs as inhibitors of enzyme transketolase. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Non-charged thiamine analogs as inhibitors of enzyme transketolase.

AFFILIATION: Array BioPharma Inc., 3200 Walnut Street, Boulder, CO 80301, USA.

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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