No.37 文献リスト [GPCR PathHunter Arrestin]-2

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文献リスト [GPCR PathHunter Arrestin]-1

Angiotensin Receptors (アンジオテンシン受容体)

GPCR Target	Reference
AGTR1	Dabul S, Bathgate-Siryk A, Valero TR, Jafferjee M, Sturchler E, McDonald P, Koch WJ, Lymperopoulos A. (2015). Suppression of adrenal βarrestin1-dependent aldosterone production by ARBs: head-to-head comparison. Sci Reports 5:8116.
AGTR1	Li H, Kem DC, Zhang L, Huang B1, Liles C, Benbrook A, Gali H, Veitla V, Scherlag BJ, Cunningham MW, Yu X. (2015). Novel retro-inverso Peptide inhibitor reverses Angiotensin receptor autoantibody-induced hypertension in the rabbit. Hypertension. 65(4):793-9.
AGTR1	Kim KS, Abraham D, Williams B, Violin JD, Mao L and Rockman HA. (2012). Beta-Arrestin-biased AT1R stimulation promotes cell survival during acute cardiac injury. Am J Physiol Heart Circ Physiol 303:H1001-10.
AGTR1	Violin JD, DeWire SM, Yamashita D, Rominger DH, Nguyen L, Schiller K, Whalen EJ, Gowen M and Lark MW. (2010). Selectively engaging beta-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance. J Pharmacol Exp Ther 335(3):572-579.

Apelin Receptors (アペリン受容体)

GPCR Target	Reference
AGTRL1	Siddiquee K, Hampton J, McAnally D, May L and Smith L. (2013). The apelin receptor inhibits the angiotensin II type 1 receptor via allosteric trans-inhibition. Br J Pharmacol 168(5):1104-17.
AGTRL1 (Arrestin & Internalization)	Brame AL, Maguire JJ, Yang P, Dyson A, Torella R, Cheriyan J, Singer M, Glen RC, Wilkinson IB, Davenport AP (2015).Design, characterization, and first-in-human study of the vascular actions of a novel biased apelin receptor agonist. Hypertension. 65(4):834-40.

Calcitonin Receptors (カルシトニン受容体)

GPCR Target	Reference
CALCRL+RAMP1	Hay DL, Harris PWR, Kowalczyk R, Brimble MA, Rathbone DL, Barwell J, Conner AC and Poyner DR. (2014). Structure-activity relationships of the N-terminus of calcitonin gene-related peptide: key roles of alanine-5 and threonine-6 in receptor activation. Br J Pharmacol 171(2):415-26.
CALCRL+RAMP1	Andreassen KV, Hjuler ST, Furness SG, Sexton PM, Christopoulos A, Nosjean O, Karsdal MA, Henriksen K. (2014) Prolonged calcitonin receptor signaling by salmon, but not human calcitonin, reveals ligand bias. Plos One. 9(3):e92042.
CALCRL+RAMP1	Andreassen KV, Feigh M, Hjuler ST, Gydesen S, Henriksen JE, Beck-Nielsen H, Christiansen C, Karsdal MA, Henriksen K. (2014) A novel oral dual amylin and calcitonin receptor agonist (KBP-042) exerts antiobesity and antidiabetic effects in rats. Am J Physiol Endocrinol Metab. 307(1):E24-33.

Cannabinoid Receptors (カンナビノイド受容体)

GPCR Target	Reference
CNR1	Priestley RS, Nickolls SA, Alexander SP, Kendall DA. (2014). A potential role for cannabinoid receptors in the therapeutic action of fenofibrate. FASEB J.
CNR1	Baillie GL, Horswill J, Anavi-Goffer S, Reggio PH, Abood ME, Bolognini D, McAllister S, Strange PG, Stephens GJ, Pertwee RG, et al. (2013). CB1 Receptor Allosteric Modulators Display both Agonist and Signaling Pathway Specificity. Mol Pharmacol 83(2):322-38.
CNR1	van der Lee MM, Blomenruhr M, van der Doelen AA, Wat JW, Smits N, Hanson BJ, van Koppen CJ and Zaman GJ. (2009). Pharmacological characterization of receptor redistribution and beta-arrestin recruitment assays for the cannabinoid receptor 1. J Biomol Screen 14(7):811-23.
CNR1, CNR2	Altomonte S, Baillie GL, Ross RA, Riley J, Zanda M (2014).The pentafluorosulfanyl group in cannabinoid receptor ligands: synthesis and comparison with trifluoromethyl and tert-butyl analogues. RSC Advances 39(4)20164-76.
CNR1, CNR2	Yang R, Fredman G, Krishnamoorthy S, Agrawal N, Irimia D, Piomelli D and Serhan CN. (2011). Decoding functional metabolomics with docosahexaenoyl ethanolamide (DHEA) identifies novel bioactive signals. J Biol Chem 286(36):31532-41.
CNR2	Dossou KS, Devkota KP, Kavanagh PV, Beutler JA, Egan JM and Moaddel R. (2013). Development and preliminary validation of a plate-based CB1/CB2 receptor functional assay. Anal Biochem437(2):138-43.
CNR2	McGuinness D, Malikzay A, Visconti R, Lin K, Bayne M, Monsma F and Lunn CA. (2009). Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter beta-arrestin assay. J Biomol Screen 14(1):49-58.

Chemokine Receptors (ケモカイン受容体)

GPCR Target	Reference
CCR1 (Arrestin & Internalization)	Gilchrist A, Gauntner TD, Fazzini A, Alley KM, Pyen DS, Ahn J, Ha SJ, Willett A, Sansom SE, Yarfi JL, Bachovchin KA, Mazzoni MR, Merritt JR. (2014). Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation andchemotaxis assays. Br J Pharmacol. 171(22):5127-38.
CCR1, CCR5	Rummel PC, Thiele S, Hansen LS, Petersen TP, Sparre-Ulrich AH, Ulven T and Rosenkilde MM. (2013). Extracellular disulfide bridges serve different purposes in two homologous chemokine receptors, CCR1 and CCR5. Mol Pharm 84(3):335-45
CCR4	Santulli-Marotto S, Fisher J, Petley T, Boakye K, Panavas T, Luongo J, Kavalkovich K, Rycyzyn M, Wu B, Gutshall L, Coelho A, Hogaboam CM and Ryan, M. (2013). Surrogate antibodies that specifically bind and neutralize CCL17 but not CCL22. Monoclon Antib Immunodiagn Immunother 32(3):162-71.
CCR4	Santulli-Marotto S, Boakye K, Lacy E, Wu S, Luongo J, Kavalkovich K, Coelh A, Hogaboam CM and Ryan M. (2013). Engagement of two distinct binding domains on CCL17 Is required for signaling through CCR4 and establishment of localized inflammatory conditions in the lung. PLoS ONE 8(12): e81465.
CCR5	Steen A, Thiele S, Guo D, Hansen LS, Frimurer TM and Rosenkilde MM. (2013). Biased and constitutive signaling in the CC-chemokine receptor CCR5 by manipulating the interface between transmembrane helices 6 and 7. J Biol Chem 288(18):12511-21.
CCR5	Steen A, Sparre-Ulrich AH, Thiele S, Guo D, Frimurer TM, Rosenkilde MM. (2013). Gating Function of Isoleucine-116 in TM3 (position III:16/3.40) for the activity state of the CC-chemokine receptor 5 (CCR5). Br J Pharmacol 171(6):1566-79.
CCR5	White GE, McNeill E, Christou I, Channon KM and Greaves DR. (2011). Site-directed mutagenesis of the CC chemokine binding protein 35K-Fc reveals residues essential for activity and mutations that increase the potency of CC chemokine blockade. Mol Pharmacol 80(2):328-36.
CCR7, CCR9, PTHR1	Watts AO, Verkaar F, van der Lee MM, Timmerman CA, Kuijer M, van Offenbeek J, van Lith LH, Smit MJ, Leurs R, Zaman GJ and Vischer HF. (2013). β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR. J Biol Chem 288(10):7169-81.
Chemokines (multiple)	Verkaar F, van Offenbeek J, van der Lee MM, van Lith LH, Watts AO, Rops AL, Aguilar DC, Ziarek JJ, van der Vlag J, Handel TM, Volkman BF, Proudfoot AE, Vischer HF, Zaman GJ, Smit MJ. (2014). Chemokine cooperativity is caused by competitive glycosaminoglycan binding. J Immunol 192(8):3908-14.
Chemokines (multiple)	Garin A, Johnson Z, Hermant A, Beltran F, Ratinaud Y, Michel A, Krohn S, Gaudet M, Carboni S, Ji H, Missotten M, Leger O, Power C and Proudfoot A. (2013). Chemokine receptor antagonist development. Methods Mol Biol 1013:67-92.
Chemokines (multiple)	Rajagopal S, Bassoni DL, Campbell JJ, Gerard NP, Gerard C and Wehrman TS. (2013). Biased agonism as a mechanism for differential signaling by chemokine receptors. J Biol Chem 288(49):35039-48.
CMKLR1	Graham KL, Zhang JV, Lewen S, Burke TM, Dang T, Zoudilova M, Sobel RA, Butcher EC, Zabel BA. (2014). A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease. PLoS One. 9(12):e112925.
CXCR2	Kashima K, Watanabe M, Sato Y, Hata J, Ishii N, Aoki Y. (2014).Inhibition of metastasis of rhabdomyosarcoma by a novel neutralizing antibody to CXC chemokine receptor-4. Cancer Sci 105(10):1343-50.
CXCR2	de Kruijf P, van Heteren J, Lim HD, Conti PG, van der Lee MM, Bosch L, Ho KK, Auld D, Ohlmeyer M, Smit MJ, et al. (2009). Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor. J Pharmacol Exp Ther 329(2):783-90.
CXCR3	Bernat V, Brox R, Heinrich MR, Auberson YP, Tschammer N. (2015) Ligand-Biased and Probe-Dependent Modulation of Chemokine Receptor CXCR3 Signaling by Negative Allosteric Modulators. ChemMedChem. 10(3):566-74.
CXCR3	Bernat V, Admas TH, Brox R, Heinemann FW, Tschammer N. (2014). Boronic Acids as Probes for Investigation of Allosteric Modulation of the Chemokine Receptor CXCR3. ACS Chem Biol. 9(11):2664-77.
CXCR3	Scholten DJ, Canals M, Wijtmans M, de Munnik S, Nguyen P, Verzijl D, de Esch IJ, Vischer HF, Smit MJ and Leurs R. (2012). Pharmacological characterization of a small-molecule agonist for the chemokine receptor CXCR3. Br J Pharmacol 166(3):898-911.
CXCR4	Castaldo C, Benicchi T, Otrocka M, Mori E, Pilli E, Ferruzzi P, Valensin S, Diamanti D, Fecke W, Varrone M, Porcari V. (2014) CXCR4 Antagonists: A Screening Strategy for Identification of Functionally Selective Ligands. J Biomol Screen. 19(6):859-869.
CXCR4, CXCR7	Segers VF, Revin V, Wu W, Qiu H, Yan Z, Lee RT and Sandrasagra A.(2011). Protease-resistant stromal cell-derived factor-1 for the treatment of experimental peripheral artery disease. Circulation 123(12):1306-15.
CXCR7	Zabel BA, Wang Y, Lewen S, Berahovich RD, Penfold ME, Zhang P, Powers J, Summers BC, Miao Z, Zhao B, Jalili A, Janowska-Wieczorek A, Jaen JC and Schall TJ. (2009). Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol183(5):3204-11.
CXCR7 (Internalization)	Liu S, Alomran R, Chernikova SB, Lartey F, Stafford J, Jang T, Merchant M, Zboralski D, Zollner S, Kruschinski A, Klussmann S, Recht L, and Brown MJ. (2014). Blockade of SDF-1 after irradiation inhibits tumor recurrences of autochthonous brain tumors in rats. Neuro-Oncol 16(1): 2-18

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