Molecular determinants of potent P2X2 antagonism identified by functional analysis, mutagenesis, and homology docking

Molecular Pharmacology

Volumn 79, Issue 4, 2011, Pages 649-661

  Wolf, Christian ^a   Rosefort, Christiane ^a   Fallah, Ghada ^a   Kassack, Matthias U ^b   Hamacher, Alexandra ^b   Bodnar, Mandy ^c   Wang, Haihong ^c   Illes, Peter ^c   Kless, Achim ^d   Bahrenberg, Gregor ^d   Schmalzing, Günther ^a   Hausmann, Ralf ^a  

^a UNIVERSITY HOSPITAL RWTH AACHEN   (Germany)

^b HEINRICH HEINE UNIVERSITY   (Germany)

^c UNIVERSITY OF LEIPZIG   (Germany)

^d GRÜNENTHAL GMBH   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

6,6' (CARBONYLBIS(IMINO 3,1 PHENYLENECARBONYLIMINO 3,1 ( 4 METHYLPHENYLENE)CARBONYLIMINO))BIS( 1 METHOXYNAPHTHALENE 3,5 DISULFONIC ACID)TETRASODIUM SALT; 7,7' (CARBONYLBIS(IMINO 3,1 PHENYLENECARBONYLIMINO 3,1 ( 4 METHYLPHENYLENE)CARBONYLIMINO))BIS( 1 METHOXY NAPHTHALENE 3,6 DISULFONIC ACID)TETRASODIUM SALT; 8,8' (CARBONYLBIS(IMINO 3,1 PHENYLENECARBONYLIMINO 3,1 ( 4 METHYLPHENYLENE)CARBONYLIMINO))BIS( 1 METHOXYNAPHTHALENE 3,6 DISULFONIC ACID)TETRASODIUM SALT; ADENOSINE TRIPHOSPHATE; ARGININE; CARBONYL DERIVATIVE; GLUTAMIC ACID; GLYCINE; HYDROXYL GROUP; NAPHTHALENESULFONIC ACID DERIVATIVE; NF 742; NF 769; NF 770; NF 778; PHENYLENECARBONYLIMINO; PURINERGIC P2X2 RECEPTOR; PURINERGIC P2X2 RECEPTOR ANTAGONIST; PURINERGIC P2X4 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; SULFONIC ACID DERIVATIVE; SURAMIN; UNCLASSIFIED DRUG; UREA;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; CHEMICAL STRUCTURE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ANTAGONISM; DRUG INHIBITION; DRUG POTENCY; DRUG STRUCTURE; IC 50; MOLECULAR DOCKING; MUTATIONAL ANALYSIS; NONHUMAN; PRIORITY JOURNAL; PROTEIN PROTEIN INTERACTION; RAT; SEQUENCE HOMOLOGY; SITE DIRECTED MUTAGENESIS; STRUCTURE ACTIVITY RELATION; ZEBRA FISH;

ANIMALS; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; FEMALE; GLUTAMIC ACID; GLYCINE; LIGANDS; MUTAGENESIS, SITE-DIRECTED; PREDICTIVE VALUE OF TESTS; PROTEIN BINDING; PURINERGIC P2 RECEPTOR ANTAGONISTS; RATS; RECEPTORS, PURINERGIC P2X2; SEQUENCE HOMOLOGY, AMINO ACID; SURAMIN;

EID: 79953023121     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.110.068700     Document Type: Article

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