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PLOS ONE, ISSN 1932-6203, 01/2015, Volume 10, Issue 1
In contrast to the corresponding mouse and rat orthologs, the human histamine H-4 receptor (hH(4)R) shows extraordinarily high constitutive activity. In the... 
SITE | ACTIVATION | POTENT | MULTIDISCIPLINARY SCIENCES | 2ND | PROTEIN-COUPLED RECEPTORS | HIGH-AFFINITY STATE | DISULFIDE BOND | H-4-RECEPTOR | DRY MOTIF | AGONIST
Journal Article
FASEB Journal, ISSN 0892-6638, 12/2012, Volume 26, Issue 12, pp. 5092 - 5105
While it is evident that the carboxylterminal region of natural peptide ligands bind to the amino-terminal domain of class B GPCRs, how their biologically... 
Class B GPCRs | Ligand binding | Molecular modeling | LIGAND-BINDING | BASIC RESIDUES | BIOCHEMISTRY & MOLECULAR BIOLOGY | PHOTOAFFINITY CROSS-LINKING | AGONIST BINDING | MUTATIONAL ANALYSIS | CELL BIOLOGY | 2ND TRANSMEMBRANE HELIX | molecular modeling | PEPTIDE RECEPTOR | BIOLOGY | MOLECULAR-BASIS | ligand binding | PROTEIN-COUPLED-RECEPTOR | ANTAGONIST PEPTIDES | class B GPCRs | Disulfides - metabolism | Receptors, Gastrointestinal Hormone - chemistry | Cricetulus | Receptors, G-Protein-Coupled - metabolism | Proline - metabolism | Humans | Cercopithecus aethiops | Tryptophan - chemistry | Receptors, Gastrointestinal Hormone - metabolism | Tryptophan - metabolism | Cysteine - genetics | Proline - genetics | Secretin - genetics | Peptides - metabolism | Disulfides - chemistry | Phenylalanine - chemistry | Cysteine - metabolism | Secretin - chemistry | CHO Cells | Binding, Competitive | Protein Structure, Tertiary | Cricetinae | Phenylalanine - metabolism | Peptides - chemistry | Tryptophan - genetics | Models, Molecular | Cysteine - chemistry | Proline - chemistry | Protein Interaction Mapping - methods | Animals | Phenylalanine - genetics | Receptors, Gastrointestinal Hormone - genetics | Protein Binding | Ligands | Receptors, G-Protein-Coupled - genetics | Mutation | COS Cells | Receptors, G-Protein-Coupled - chemistry | Secretin - metabolism | Index Medicus | Research Communications
Journal Article
BRITISH JOURNAL OF PHARMACOLOGY, ISSN 0007-1188, 08/2007, Volume 151, Issue 8, pp. 1293 - 1304
Background and purpose: Rodent alpha(2A)-adrenoceptors bind the classical alpha(2)-antagonists yohimbine and rauwolscine with lower affinity than the human... 
LIGAND-BINDING | 2ND EXTRACELLULAR LOOP | H-3 RAUWOLSCINE | BETA-ADRENERGIC-RECEPTOR | PROTEIN-COUPLED RECEPTORS | TRANSMEMBRANE DOMAIN | ANTAGONIST BINDING | ALPHA-ADRENERGIC RECEPTORS | PHARMACOLOGY & PHARMACY | DOPAMINE-RECEPTORS | PHARMACOLOGICAL-PROPERTIES
Journal Article
Journal Article
NATURE, ISSN 0028-0836, 07/2008, Volume 454, Issue 7203, pp. 486 - 491
G-protein-coupled receptors have a major role in transmembrane signalling in most eukaryotes and many are important drug targets. Here we report the 2.7... 
AGONIST ACTIVATION | BETA-ADRENERGIC-RECEPTORS | 2ND EXTRACELLULAR LOOP | CRYSTAL-STRUCTURE | AMINO-ACIDS | MULTIDISCIPLINARY SCIENCES | BETA-1-ADRENERGIC RECEPTOR | HIGH-AFFINITY BINDING | MUSCARINIC RECEPTOR | PROVIDE EVIDENCE | BETA-ADRENERGIC RECEPTOR
Journal Article
NATURE CHEMICAL BIOLOGY, ISSN 1552-4450, 11/2011, Volume 7, Issue 11, pp. 769 - 778
G protein-coupled receptors (GPCRs) are intensely studied as drug targets and for their role in signaling. With the determination of the first crystal... 
DESIGN | DATABASE | 2ND EXTRACELLULAR LOOP | BIOCHEMISTRY & MOLECULAR BIOLOGY | DRUG DISCOVERY | BINDING-SITE | ANTAGONISTS | MOLECULAR DOCKING | AGONISTS | PROTEIN-COUPLED-RECEPTOR | D3 RECEPTOR
Journal Article
STRUCTURE, ISSN 0969-2126, 08/2017, Volume 25, Issue 8, pp. 1275 - 1275
The adenosine A(1) and A(2A) receptors belong to the purinergic family of G protein-coupled receptors, and regulate diverse functions of the cardiovascular,... 
RADIOLIGAND | 2ND EXTRACELLULAR LOOP | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | HIGH-AFFINITY ANTAGONIST | FEATURES | CELL BIOLOGY | BIOPHYSICS | LIGANDS | A-ADENOSINE | SPECIES-DIFFERENCES | BINDING | AGONIST
Journal Article
CELL, ISSN 0092-8674, 02/2017, Volume 168, Issue 5, pp. 867 - 867
The adenosine A(1) receptor (A(1)-AR) is a G-proteincoupled receptor that plays a vital role in cardiac, renal, and neuronal processes but remains poorly... 
ACUTE HEART-FAILURE | MOLECULAR-DYNAMICS | PROTEIN-COUPLED RECEPTOR | 2ND EXTRACELLULAR LOOP | BIOCHEMISTRY & MOLECULAR BIOLOGY | DRUG DESIGN | CRYSTAL-STRUCTURES | A(2A) RECEPTOR | ALLOSTERIC MODULATION | FORCE-FIELDS | ADENOSINE-A1-RECEPTOR BINDING | CELL BIOLOGY
Journal Article
Nature Chemical Biology, ISSN 1552-4450, 01/2019, Volume 15, Issue 1, pp. 11 - 17
Misoprostol is a life-saving drug in many developing countries for women at risk of post-partum hemorrhaging owing to its affordability, stability, ease of... 
REFINEMENT | SUBTYPE | PROSTANOID RECEPTORS | LIGAND-BINDING | 2ND EXTRACELLULAR LOOP | BIOCHEMISTRY & MOLECULAR BIOLOGY | RESOLUTION | PROTEINS | AGONIST | FEATURES | PGE
Journal Article
Journal Article
PHARMACOLOGICAL REVIEWS, ISSN 0031-6997, 01/2013, Volume 65, Issue 1, pp. 500 - 543
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 03/2010, Volume 285, Issue 10, pp. 7459 - 7474
Muscarinic acetylcholine receptors contain at least one allosteric site that is topographically distinct from the acetylcholine, orthosteric binding site.... 
CONFORMATIONAL-CHANGES | SUBTYPE SELECTIVITY | 2ND EXTRACELLULAR LOOP | CONSERVED DISULFIDE BOND | AMINO-ACIDS | DIRECTED MUTAGENESIS | N-DESMETHYLCLOZAPINE | BIOCHEMISTRY & MOLECULAR BIOLOGY | TRANSMEMBRANE DOMAIN | FUNCTIONAL SELECTIVITY | SCANNING MUTAGENESIS
Journal Article
JOURNAL OF CLINICAL INVESTIGATION, ISSN 0021-9738, 05/2004, Volume 113, Issue 10, pp. 1419 - 1429
Today, dilated cardiomyopathy (DCM) represents the main cause of severe heart failure and disability in younger adults and thus is a challenge for public... 
ANTIBODIES | IMMUNOADSORPTION | MEDICINE, RESEARCH & EXPERIMENTAL | HYPERTROPHY | CARDIAC AUTOANTIBODIES | RAT | 2ND EXTRACELLULAR LOOP | SUBSEQUENT IMMUNOGLOBULIN SUBSTITUTION | HEART-FAILURE | DISEASE | DYSFUNCTION
Journal Article
Journal Article