Crystal structure of the peroxisome proliferator-activated receptor γ (PPARγ) ligand binding domain complexed with a novel partial agonist: A new region of the hydrophobic pocket could be exploited for drug design

Journal of Medicinal Chemistry

Volumn 51, Issue 24, 2008, Pages 7768-7776

  Montanari, Roberta ^a   Saccoccia, Fulvio ^a   Scotti, Elena ^b   Crestani, Maurizio ^b   Godio, Cristina ^b   Gilardi, Federica ^b   Loiodice, Fulvio ^c   Fracchiolla, Giuseppe ^c   Laghezza, Antonio ^c   Tortorella, Paolo ^c   Lavecchia, Antonio ^d   Novellino, Ettore ^d   Mazza, Fernando ^a,e   Aschi, Massimiliano ^e   Pochetti, Giorgio ^a  

^a CNR   (Italy)

^b UNIVERSITY OF MILAN   (Italy)

^c UNIVERSITY OF BARI   (Italy)

^d UNIVERSITY OF NAPLES FEDERICO II   (Italy)

^e UNIVERSITY OF L'AQUILA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 (4 PHENYLPHENOXY) 3 PHENYLPROPANOIC ACID; CLOFIBRIC ACID DERIVATIVE; METHYL 2 (4 PHENYLPHENOXY) 3 PHENYLPROPANOATE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; UNCLASSIFIED DRUG;

ALPHA HELIX; ARTICLE; COMPLEX FORMATION; CONFORMATIONAL TRANSITION; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; ENANTIOMER; GLUCOSE METABOLISM; HUMAN; HUMAN CELL; HYDROPHOBICITY; LIGAND BINDING; LIPID METABOLISM; MOLECULAR MODEL; NONHUMAN; PROTEIN CONFORMATION; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN STABILITY; STRUCTURE ANALYSIS; X RAY CRYSTALLOGRAPHY;

ANIMALS; CHEMISTRY, PHARMACEUTICAL; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; HYPOGLYCEMIC AGENTS; LIGANDS; MICE; MODELS, CHEMICAL; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PPAR ALPHA; PPAR GAMMA; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY;

EID: 58149101957     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm800733h     Document Type: Article

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