Order this structure laser-etched in crystal Release date: 2007-10-30 Citations: 111 Downloads: 52528 Total score: 1807
Molecular functions: (select from list to view only structures with selected function) Activation of adenylate cyclase activityActivation of adenylate cyclase activity by G-protein signaling pathwaActivation of transmembrane receptor protein tyrosine kinase activityAdenylate cyclase bindingAdrenoceptor activityApical plasma membraneAxonBeta2-adrenergic receptor activityBone resorptionBrown fat cell differentiationCaveolaCell surface receptor linked signal transductionDendriteDesensitization of G-protein coupled receptor protein signaling pathwaDiet induced thermogenesisDrug bindingEndosomeEndosome to lysosome transportG-protein coupled receptor activityG-protein coupled receptor protein signaling pathwayG-protein signaling, coupled to cAMP nucleotide second messengerHeat generationIntegral to membraneIntegral to plasma membraneIntracellular partLysosomeMembraneMembrane fractionNegative regulation of calcium ion transport via voltage-gated calciumNegative regulation of inflammatory responseNegative regulation of multicellular organism growthNegative regulation of ossificationNegative regulation of smooth muscle contractionNorepinephrine bindingNucleusPlasma membranePositive regulation of apoptosisPositive regulation of bone mineralizationPositive regulation of cell proliferationPositive regulation of heart contractionPositive regulation of MAPKKK cascadePositive regulation of skeletal muscle growthPositive regulation of transcription from RNA polymerase II promoterPositive regulation of vasodilationPotassium channel regulator activityProtein bindingProtein complex bindingProtein homodimerization activityReceptor activityReceptor complexReceptor-mediated endocytosisRegulation of sensory perception of painRegulation of sodium ion transportRegulation of systemic arterial blood pressure by norepinephrine-epineResponse to coldSarcolemmaSignal transducer activitySignal transductionVasodilation by norepinephrine-epinephrine involved in regulation of s Scientists: (select from list to view only structures from selected author) CHEREZOV, V.CHOI, H.J.HANSON, M.A.KOBILKA, B.K.KOBILKA, T.S.KUHN, P.RASMUSSEN, S.G.F.ROSENBAUM, D.M.STEVENS, R.C.THIAN, F.S.WEIS, W.I.				Other databases: View entry in RCSB
High-Resolution Crystal Structure of an Engineered Human {beta}2-Adrenergic G Protein Coup G protein-coupled receptors comprise the largest family of eukaryotic signal transduction proteins that communicate across the membrane. We report the crystal structure of a human beta2-adrenergic receptor-T4 lysozyme fusion protein bound to the partial inverse agonist carazolol at 2.4 A resolution. The structure provides a high-resolution view of a human G protein-coupled receptor bound to a diffusible ligand. Ligand-binding site accessibility is enabled by the second extracellular loop which is held out of the binding cavity by a pair of closely spaced disulfide bridges and a short helical segment within the loop. Cholesterol, a necessary component for crystallization, mediates an intriguing parallel association of receptor molecules in the crystal lattice. Although the location of carazolol in the beta2-adrenergic receptor is very similar to that of retinal in rhodopsin, structural differences in the ligand binding site and other regions highlight the challenges in using rhodopsin as a template model for this large receptor family. [Pubmed record]