Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2 non-competitive allosteric inhibitor

British Journal of Pharmacology

Volumn 165, Issue 2, 2012, Pages 436-454

  Bertini, R ^a,i   Barcelos, L S ^b   Beccari, A R ^a   Cavalieri, B ^a,c   Moriconi, A ^a   Bizzarri, C ^a   Di Benedetto, P ^a   Di Giacinto, C ^a   Gloaguen, I ^a   Galliera, E ^d   Corsi, M M ^d,e   Russo, R C ^b   Andrade, S P ^b   Cesta, M C ^a   Nano, G ^a   Aramini, A ^a   Cutrin, J C ^c,f,g   Locati, M ^d,h   Allegretti, M ^a   Teixeira, M M ^b  

^a Chemistry Section   (Italy)

^b FEDERAL UNIVERSITY OF MINAS GERAIS   (Brazil)

^c UNIVERSITY OF TURIN   (Italy)

^d UNIVERSITY OF MILAN   (Italy)

^e IRCCS POLICLINICO SAN DONATO   (Italy)

^f UNIVERSIDAD DE BUENOS AIRES   (Argentina)

^g Facultad de Ciencias Naturales e Instituto M Lillo   (Argentina)

^h HUMANITAS CLINICAL AND RESEARCH CENTER   (Italy)

ⁱ ALTA Srlu   (Italy)

Author keywords

binding mode; chemokine receptors; CXCR1 CXCR2; experimental angiogenesis; ischaemia reperfusion injury; leucocyte recruitment; non competitive allosteric inhibitor

Indexed keywords

(4 TRIFLUOROMETHANESULFONYLOXYPHENYL)PROPIONYLMETHANESULFONAMIDE; ASPARTIC ACID; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CXCR1; CHEMOKINE RECEPTOR CXCR1 INHIBITOR; CHEMOKINE RECEPTOR CXCR2; CHEMOKINE RECEPTOR CXCR2 INHIBITOR; DF 2156A; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); INTERLEUKIN 8; RADIOLIGAND; SULFUR 35; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ALLOSTERISM; AMINO ACID SEQUENCE; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CELL INFILTRATION; CELL MIGRATION; CELL PROLIFERATION; CHEMICAL BOND; CHEMOTAXIS; CHRONIC INFLAMMATION; CONTROLLED STUDY; CYTOKINE PRODUCTION; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; HUMAN; HUMAN CELL; IN VITRO STUDY; INFLAMMATION; LEUKOCYTE; LIVER CELL DAMAGE; LIVER ISCHEMIA; MACROPHAGE; MALE; MONOCYTE; MOUSE; NEOVASCULARIZATION (PATHOLOGY); NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR BINDING; REPERFUSION INJURY; SIGNAL TRANSDUCTION;

ANIMALS; ANTI-INFLAMMATORY AGENTS; CELL MEMBRANE; CELL PROLIFERATION; CHEMOTAXIS, LEUKOCYTE; DISEASE MODELS, ANIMAL; HUMAN UMBILICAL VEIN ENDOTHELIAL CELLS; HUMANS; INTERLEUKIN-8; LEUKOCYTES; LIVER; MALE; MICE; MICE, INBRED C57BL; MODELS, MOLECULAR; MUTAGENESIS, SITE-DIRECTED; NEOVASCULARIZATION, PATHOLOGIC; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, INTERLEUKIN-8A; RECEPTORS, INTERLEUKIN-8B; REPERFUSION INJURY; SKIN; SULFONAMIDES;

EID: 83755220076     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2011.01566.x     Document Type: Article

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