Molecular requirements for inhibition of the chemokine receptor CCR8 - Probe-dependent allosteric interactions

British Journal of Pharmacology

Volumn 167, Issue 6, 2012, Pages 1206-1217

  Rummel, P C ^a   Arfelt, K N ^a   Baumann, L ^b   Jenkins, T J ^c   Thiele, S ^a   Luttichau H R ^a   Johnsen, A ^d   Pease, J ^e   Ghosh, S ^c,f   Kolbeck, R ^c,g   Rosenkilde, M M ^a,h  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b UNIVERSITY OF LEIPZIG   (Germany)

^c MILLENNIUM PHARMACEUTICALS INC   (United States)

^d Rigshospitalet   (Denmark)

^e NATIONAL HEART AND LUNG INSTITUTE   (United Kingdom)

^f Pharmaceuticals Inc   (United States)

^g MEDIMMUNE   (United States)

^h BIOGEN   (United States)

Author keywords

allosteric interaction; chemokine receptor; receptor conformation; small molecule antagonist

Indexed keywords

2 METHYL N [4 [N (1 PYRIMIDINE 2 YL)PIPERIDINE 4 YL]NAPHTHALENE 1 YL]BENZAMIDE; 2 METHYL N [4 [N [1 (4 METHYLPIPERAZINE 1 CARBONYL)PIPERIDINE 4 YL]SULFAMOYL]NAPHTHALENE 1 YL] 2 METHYLBENZAMIDE; CCL1 CHEMOKINE; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR8; CHEMOKINE RECEPTOR CCR8 ANTAGONIST; ETHYL 4 (5 BENZAMIDONAPHTHALENE 1 SULFONAMINO)PIPERIDINE 1 CARBOXYLATE; ETHYL 4 [4 (2 METHYLBENZAMIDE)NAPHTHALENE 1 SULFONYLAMINO]PIPERIDINE 1 CARBOXYLATE; ETHYL 4 [5 (THIOPENE 2 CARBOXAMIDO)NAPHTHALENE 1 SULFONYLAMINO]PIPERIDINE 1 CARBOXYLATE; INHIBITORY GUANINE NUCLEOTIDE BINDING PROTEIN; MC 148; N [4 [N [(2 AMINOPROPANOYL) 3 METHYLPIPERIDINE 4 YL]SULFAMOYL]NAPHTHALENE 1 YL] 2 METHYLBENZAMIDE; N [5 [N (1 BUTYRYL 3 METHYLPIPERIDINE 4 YL)SULFAMOYL]NAPHTHALENE 1 YL] 2 METHYLBENZAMIDE; N [5 [N [(2 AMINOPROPANOYL) 3 METHYLPIPERIDINE 4 YL]SULFAMOYL]NAPHTHALENE 1 YL] 2 METHYLBENZAMIDE; RADIOLIGAND; UNCLASSIFIED DRUG;

ALLOSTERISM; ARTICLE; BINDING AFFINITY; BINDING COMPETITION; CELL STRAIN COS7; CHEMOTAXIS; DRUG POTENCY; DRUG STRUCTURE; GENETIC TRANSFECTION; HUMAN; INHIBITION KINETICS; MOLECULAR INTERACTION; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION;

ANIMALS; BINDING SITES; BINDING, COMPETITIVE; CERCOPITHECUS AETHIOPS; CHEMOKINE CCL1; CHEMOKINES, CC; COS CELLS; LIGANDS; NAPHTHALENES; RECEPTORS, CCR8; VIRAL PROTEINS;

EID: 84867792512     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.02076.x     Document Type: Article

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