Identification of allosteric PIF-pocket ligands for PDK1 using NMR-based fragment screening and 1H- 15N TROSY experiments

Chemical Biology and Drug Design

Volumn 73, Issue 2, 2009, Pages 179-188

  Stockman, Brian J ^g   Kothe, Michael ^a,g   Kohls, Darcy ^b,g   Weibley, Laura ^c,g   Connolly, Brendan J ^g   Sheils, Alissa L ^g   Cao, Qing ^g   Cheng, Alan C ^d,g   Yang, Lily ^e,g   Kamath, Ajith V ^f,g   Ding, Yuan Hua ^g   Charlton, Maura E ^g  

^a GENZYME CORPORATION   (United States)

^b Novartis AG   (Switzerland)

^c ALNYLAM PHARMACEUTICALS   (United States)

^d AMGEN INC   (United States)

^e ELI LILLY AND COMPANY   (United States)

^f JUBILANT BIOSYS LTD   (India)

^g PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Allosteric; Cancer; Diabetes; Fragment screening; NMR; PDK1

Indexed keywords

ADENOSINE TRIPHOSPHATE; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1;

ALLOSTERISM; AMINO TERMINAL SEQUENCE; ANIMAL CELL; ARTICLE; BINDING SITE; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; ENZYME ACTIVE SITE; ENZYME PHOSPHORYLATION; FLUORINE NUCLEAR MAGNETIC RESONANCE; HUMAN; ISOTOPE LABELING; LIGAND BINDING; NITROGEN NUCLEAR MAGNETIC RESONANCE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; PRIORITY JOURNAL; PROTON NUCLEAR MAGNETIC RESONANCE; SIGNAL TRANSDUCTION; SPECTROSCOPY; TRANSVERSE RELAXATION OPTIMIZED SPECTROSCOPY;

ALLOSTERIC SITE; CATALYTIC DOMAIN; COMPUTER SIMULATION; HUMANS; HYDROGEN; LIGANDS; MAGNETIC RESONANCE SPECTROSCOPY; NITROGEN; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; PROTEIN-SERINE-THREONINE KINASES;

EID: 58849093668     PISSN: 17470277     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1747-0285.2008.00768.x     Document Type: Article

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