No.36 文献リスト [GPCR PathHunter Arrestin]-1

DiscoveRxのPathHunter アレスチンアッセイは、高い信頼性を誇るGPCR機能アッセイでございます。現在150報以上に及ぶ文献が報告されており、世界中の研究者の皆様にご活用いただいています。5回に分けて本ブログに掲載させていただきたいと思います。（※ターゲット毎に分類されております。）

Multiple GPCRs (複数GPCR)

GPCR Target	Reference
Multiple	Stahl EL, Zhou L, Ehlert FJ, Bohn LM. (2015). A Novel Method for Analyzing Extremely Biased Agonism at G Protein-Coupled Receptors. Mol Pharmacol.
Multiple	Tena-Campos M, Ramon E, Rivera D, Borroto-Escuela DO, Romero-Fernandez W, Fuxe K, Garriga P. (2014). G-protein-coupled receptors oligomerization: emerging signaling units and new opportunities for drug design. Curr Protein Pept Sci. 15(7):648-58
Multiple	Verkaar F, van Rosmalen JW, Blomenröhr M, van Koppen CJ, Blankesteijn WM, Smits JF and Zaman GJ.(2008). G protein-independent cell-based assays for drug discovery on seven-transmembrane receptors. Biotechnol Annu Rev 14:253-74.
Multiple (ProLink Vector, Parental)	Yin H, Chu A, Li W, Wang B, Shelton F, Otero F, Nguyen DG, Caldwell JS and Chen YA. (2009). Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay. J Biol Chem 284(18):12328-38.
S1P1, GCGR, CHRM5, HRH2, OPRD1, ADRB2	Bassoni DL, Raab WJ, Achacoso PL, Loh CY and Wehrman TS. (2012). Measurements of beta-arrestin recruitment to activated seven transmembrane receptors using enzyme complementation. Methods Mol Biol 897:181-203.

Acetylcholine Receptors　(アセチルコリン受容体)

GPCR Target	Reference
CHRM1	Digby GJ, Noetzel MJ, Bubser M, Utley TJ, Walker AG, Byun NE, Lebois EP, Xiang Z, Sheffler DJ, Cho HP, et al. (2012). Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. J Neurosci 32(25):8532-44.
CHRM1	Watt ML, Schober DA, Hitchcock S, Liu B, Chesterfield AK, McKinzie D and Felder CC. (2011). Pharmacological characterization of LY593093, an M1 muscarinic acetylcholine receptor-selective partial orthosteric agonist. J Pharmacol Exp Ther 338(2):622-632.
CHRM1	Ma L, Seager MA, Wittmann M, Jacobson M, Bickel D, Burno M, Jones K, Graufelds VK, Xu G, Pearson M et al. (2009). Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. Proc Natl Acad Sci USA 106(37):15950-5.
CHRM3	Li H, Yu X, Liles C, Khan M, Vanderlinde-Wood M, Galloway A, Zillner C, Benbrook A, Reim S, Collier D, Hill MA, Raj SR, Okamoto LE, Cunningham MW, Aston CE, Kem DC. (2014). Autoimmune basis for postural tachycardia syndrome. J Am Heart Assoc. 26;3(1):e000755.
CHRM3	Li H, Kem DC, Reim S, Khan M, Vanderlinde-Wood M, Zillner C, Collier D, Liles C, Hill MA, Cunningham MW, Aston CE and Yu X. (2012). Agonistic autoantibodies as vasodilators in orthostatic hypotension: a new mechanism. Hypertension 59(2):402-8.
CHRM3	Poulin B, Butcher A, McWilliams P, Bourgognon JM, Pawlak R, Kong KC, Bottrill A, Mistry S, Wess J, Rosethorne EM, Charlton SJ and Tobin AB. (2010). The M3-muscarinic receptor regulates learning and memory in a receptor phosphorylation/arrestin-dependent manner. Proc Natl Acad Sci U S A 107(20):9440-5.
CHRM3	Kong KC, Butcher AJ, McWilliams P, Jones D, Wess J, Hamdan FF, Werry T, Rosethorne EM, Charlton SJ, Munson SE, Cragg HA, Smart AD and Tobin AB. (2010). M3-muscarinic receptor promotes insulin release via receptor phosphorylation/arrestin-dependent activation of protein kinase D1. Proc Natl Acad Sci USA 107(49):21181-6.

Adenosine Receptors　(アデノシン受容体)

GPCR Target	Reference
ADORA2B	Gao ZG, Balasubramanian R, Kiselev E, Wei Q, Jacobson KA. (2014). Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor. Biochem Pharmacol. 90(3):297-306.
ADORA3	Verzijl D and Ijzerman AP. (2011). Functional selectivity of adenosine receptor ligands. Purinergic Signal 7(2):171-92.
ADORA3	Gao ZG, Verzijl D, Zweemer A, Ye K, Goblyos A, Ijzerman AP and Jacobson KA. (2011). Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers. Biochem Pharmacol 82(6):658-68.
ADORA3	Gao ZG and Jacobson KA. (2008). Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways. Pharmacol Res 57(4):303-11.
ADRA2C	Kurko D, Kapui Z, Nagy J, Lendvai B, Kolok S. (2014). Analysis of functional selectivity through G protein-dependent and -independent signaling pathways at the adrenergic α2C receptor. Brain Res Bull. 107: 89-10.

Adrenoreceptors　(アドレナリン受容体)

GPCR Target	Reference
ADRB1	Hutchings CJ, Cseke G, Osborne G, Woolard J, Zhukov A, Koglin M, Jazayeri A, Pandya-Pathak J, Langmead CJ, Hill SJ, Weir M, Marshall FH. (2014). Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment. mAbs. 6(1):246-61.
ADRB2	Rosethorne EM, Bradley ME, Kent TC, Charlton SJ. (2015). Functional desensitization of the β2 adrenoceptor is not dependent on agonist efficacy. Pharmacol Res Perspect. 3(1):e00101.
ADRB2	Kopra K, Kainulainen M, Mikkonen P, Rozwandowicz-Jansen A, Hänninen P and Härmä H. (2013). Multiparametric homogeneous method for identification of ligand binding to G protein-coupled receptors: receptor-ligand binding and β-arrestin assay. Analytical Chemistry 85(4):2276-228.
ADRB2	Weiss DR, Ahn S, Sassano MF, Kleist A, Zhu X, Strachan R, Roth BL, Lefkowitz RJ and Shoichet BK. (2013). Conformation guides molecular efficacy in docking screens of activated β-2 adrenergic G-protein coupled receptor. ACS Chem Biol 8(5):1018-26.

Anaphylotoxin Chemotactic Receptors (Complement Peptide Family)　（アナフィラトキシン)

GPCR Target	Reference
C5L2	Van Lith LH, Oosterom J, Van Elsas A and Zaman GJ. (2009). C5a-stimulated recruitment of β-Arrestin2 to the nonsignaling 7-transmembrane decoy receptor C5L2. J Biomol Screen14(9):1067-75.

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