A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties

FASEB Journal

Volumn 21, Issue 9, 2007, Pages 2124-2134

  Maillet, Emeline L ^a,c   Pellegrini, Nadia ^a   Valant, Celine ^a   Bucher, Bernard ^a,b   Hibert, Marcel ^a   Bourguignon, Jean Jacques ^a   Galzi, Jean Luc ^a  

^a UNIVERSITÉ DE STRASBOURG   (France)

^b Laboratoire de Pharmacochimie   (France)

^c MOUNT SINAI SCHOOL OF MEDICINE   (United States)

Author keywords

Allosterism; Drug discovery; GPCR; Neurokinin; Signal transduction

Indexed keywords

CALCIUM; CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; LPI 805; NEUROKININ 2 RECEPTOR; NEUROKININ A; TACHYKININ; UNCLASSIFIED DRUG;

ALLOSTERISM; ARTICLE; CONFORMATION; DISSOCIATION; DRUG INHIBITION; EMBRYO; HUMAN; HUMAN CELL; KINETICS; KNOWLEDGE; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; RAT;

ALLOSTERIC REGULATION; AMINOACETONITRILE; ANIMALS; CALCIUM; CALCIUM SIGNALING; CELL LINE; CYCLIC AMP; CYCLIC AMP-DEPENDENT PROTEIN KINASES; FLUORESCENCE RESONANCE ENERGY TRANSFER; FLUORESCENT DYES; GENES, REPORTER; HUMANS; KIDNEY; KINETICS; NAPHTHALENES; NEUROKININ A; PROTEIN BINDING; PROTEIN CONFORMATION; RATS; RECEPTORS, NEUROKININ-2; RECOMBINANT FUSION PROTEINS; SECOND MESSENGER SYSTEMS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 34347395367     PISSN: 08926638     EISSN: None     Source Type: Journal    
DOI: 10.1096/fj.06-7683com     Document Type: Article

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