Fragment-based screening by X-ray crystallography, MS and isothermal titration calorimetry to identify PNMT (phenylethanolamine N-methyltransferase) inhibitors

Biochemical Journal

Volumn 431, Issue 1, 2010, Pages 51-61

  Drinkwater, Nyssa ^a   Vu, Hoan ^b   Lovell, Kimberly M ^c   Criscione, Kevin R ^c   Collins, Brett M ^a   Prisinzano, Thomas E ^c   Poulsen, Sally Ann ^b   Mcleish, Michael J ^d   Grunewald, Gary L ^c   Martin, Jennifer L ^a  

^a UNIVERSITY OF QUEENSLAND   (Australia)

^b GRIFFITH UNIVERSITY   (Australia)

^c UNIVERSITY OF KANSAS   (United States)

^d INDIANA UNIVERSITY   (United States)

Author keywords

Benzimidazole; Catecholamine; Drug discovery; Enzyme inhibition; Fragment based screening; Phenylethanolamine n methyltransferase (pnmt)

Indexed keywords

BINDING ENERGY; BINDING SITES; BIOCHEMISTRY; CALORIMETRY; ENZYMES; INDICATORS (CHEMICAL); MINERALOGY; TITRATION; X RAY CRYSTALLOGRAPHY;

BENZIMIDAZOLES; CATECHOLAMINE; DRUG DISCOVERY; FRAGMENT-BASED SCREENING; METHYLTRANSFERASES;

ENZYME INHIBITION;

BENZIMIDAZOLE; NORADRENALIN; PHENYLETHANOLAMINE N METHYLTRANSFERASE INHIBITOR; PURINE; QUINOLINE; BENZIMIDAZOLE DERIVATIVE; ENZYME INHIBITOR; LIGAND; PHENYLETHANOLAMINE N METHYLTRANSFERASE;

ARTICLE; ATOM; BINDING AFFINITY; BINDING SITE; ENZYME ANALYSIS; ENZYME SYNTHESIS; ISOTHERMAL TITRATION CALORIMETRY; MASS SPECTROMETRY; PILOT STUDY; PRIORITY JOURNAL; PROTEIN INTERACTION; SCREENING TEST; X RAY CRYSTALLOGRAPHY; ANTAGONISTS AND INHIBITORS; CALORIMETRY; CHEMICAL STRUCTURE; CHEMISTRY; KINETICS; METABOLISM;

BENZIMIDAZOLES; BINDING SITES; CALORIMETRY; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; KINETICS; LIGANDS; MASS SPECTROMETRY; MODELS, MOLECULAR; PHENYLETHANOLAMINE N-METHYLTRANSFERASE;

EID: 77956645261     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20100651     Document Type: Article

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