The second extracellular loop of GPCRs determines subtype-selectivity and controls efficacy as evidenced by loop exchange study at A2 adenosine receptors

Biochemical Pharmacology

Volumn 85, Issue 9, 2013, Pages 1317-1329

  Seibt, Benjamin F ^a   Schiedel, Anke C ^a   Thimm, Dominik ^a   Hinz, Sonja ^a   Sherbiny, Farag F ^a   Müller, Christa E ^a  

^a UNIVERSITY OF BONN   (Germany)

Author keywords

Keywords Mutagenesis G protein coupled receptors Receptor activation Ligand binding site Overlap extension mutagenesis EL2 loop exchange

Indexed keywords

2 [4 (2 CARBOXYETHYL)PHENETHYLAMINO]ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE; ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE A2A RECEPTOR; ADENOSINE A2B RECEPTOR; ADENOSINE RECEPTOR STIMULATING AGENT; ALANINE; ASPARTIC ACID; BAY60 6583; G PROTEIN COUPLED RECEPTOR; GLUTAMIC ACID; SERINE; THREONINE; UNCLASSIFIED DRUG; VALINE;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG EFFICACY; GENE MUTATION; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; SECOND EXTRACELLULAR LOOP;

ADENOSINE A2 RECEPTOR AGONISTS; AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; CYCLIC AMP; HUMANS; MOLECULAR DOCKING SIMULATION; MOLECULAR SEQUENCE DATA; MUTATION; PROTEIN CONFORMATION; RADIOLIGAND ASSAY; RECEPTOR, ADENOSINE A2A; RECEPTOR, ADENOSINE A2B; SEQUENCE HOMOLOGY, AMINO ACID; SIGNAL TRANSDUCTION;

EID: 84875719574     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2013.03.005     Document Type: Article

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