Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 983.36 of the human histamine H4 receptor

British Journal of Pharmacology

Volumn 170, Issue 1, 2013, Pages 89-100

  Nijmeijer, S ^a   Engelhardt, H ^a,b   Schultes, S ^a,b   Van De Stolpe, A C ^a   Lusink, V ^a   De Graaf, C ^a   Wijtmans, M ^a   Haaksma, E E J ^b   De Esch, I J P ^a   Stachurski, K ^b   Vischer, H F ^a   Leurs, R ^a  

^a AMSTERDAM INSTITUTE FOR MOLECULES   (Netherlands)

^b BOEHRINGER INGELHEIM RCV GMBH AND CO KG   (Austria)

Author keywords

covalent binder; GPCR; histamine H4 receptor; pyrimidine

Indexed keywords

2 METHYL 4 (4 METHYLPIPERAZIN 1 YL) 6 PHENYLPYRIMIDINE; 4 (4 METHYLPIPERAZIN 1 YL) 6 PHENYL 2 VINYLPYRIMIDINE; BETA ARRESTIN 2; CYSTEINE; CYSTEINE ETHYL ESTER; GLUTATHIONE; GUANINE NUCLEOTIDE BINDING PROTEIN; HISTAMINE H4 RECEPTOR; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ARTICLE; BINDING AFFINITY; BINDING SITE; CHEMICAL INTERACTION; CONTROLLED STUDY; COVALENT BOND; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN TRANSPORT; RECEPTOR BINDING; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

COVALENT BINDER; GPCR; HISTAMINE H4 RECEPTOR; PYRIMIDINE;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ARRESTINS; DRUG DESIGN; DRUG PARTIAL AGONISM; GTP-BINDING PROTEINS; HEK293 CELLS; HISTAMINE AGONISTS; HUMANS; LIGANDS; PROTEIN CONFORMATION; PYRIMIDINES; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, HISTAMINE; SIGNAL TRANSDUCTION; VINYL COMPOUNDS;

EID: 84881629897     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/bph.12113     Document Type: Article

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