No.40 文献リスト [GPCR PathHunter Arrestin]-5

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いております。（※ターゲット毎に分類されております。）

文献リスト [GPCR PathHunter Arrestin]-1
文献リスト [GPCR PathHunter Arrestin]-2
文献リスト [GPCR PathHunter Arrestin]-3
文献リスト [GPCR PathHunter Arrestin]-4

Melanin-concentrating Hormone Receptors (メラニン凝集ホルモン受容体)

GPCR Target	Reference
MCHR1	Sakurai T, Ogawa K, Ishihara Y, Kasai S, Nakayama M. (2014). The MCH(1) receptor, an anti-obesity target, is allosterically inhibited by 8-methylquinoline derivatives possessing subnanomolar binding and long residence times. Br J Pharmacol.. 171(5):1287-98.

Melanocortin Receptors (メメラノコルチン受容体)

GPCR Target	Reference
MC1R	Nix MA, Kaelin CB, Ta T, Weis A, Morton GJ, Barsh GS, Millhauser GL. (2013). Molecular and functional analysis of human b-defensin 3 action at melanocortin receptors. Chem Biol 20(6):784-95.
MC1R	Benned-Jensen T, Mokrosinski J, and Rosenkilde MM. (2011). The E92K melanocortin 1 receptor mutant induces cAMP production and arrestin recruitment but not ERK activity indicating biased constitutive signaling. PLoS One 6, e24644.
MC4R	Ghamari-Langroudi M, Digby GJ, Sebag JA, Millhauser GL, Palomino R, Matthews R, Gillyard T, Panaro BL, Tough IR, Cox HM, Denton JS, Cone RD. (2015). G-protein-independent coupling of MC4R to Kir7.1 in hypothalamic neurons. Nature. [Epub ahead of print]

Neurotensin Receptors (ニューロテンシン受容体)

GPCR Target	Reference
NTS1	Hershberger PM, Hedrick MP, Peddibhotla S, Mangravita-Novo A, Gosalia P, Li Y, Gray W, Vicchiarelli M, Smith LH, Chung TD, Thomas JB, Caron MG, Pinkerton AB, Barak LS, Roth GP. (2014) Imidazole-derived agonists for the neurotensin 1 receptor. Bioorg Med Chem Lett. 24(1):262-7.

Opioid Receptors (オピオイド受容体)

GPCR Target	Reference
OPRD1, OPRK1, OPRM1	Hughes FM, Jr., Shaner BE, Brower JO, Woods RJ and Dix TA. (2013). Development of a peptide-derived orally-active kappa-opioid receptor agonist targeting peripheral pain. Open Med Chem J 2013(7):16-22.
OPRK1	Frankowski KJ, Slauson SR, Lovell KM, Phillips AM, Streicher JM, Zhou L, Whipple DA, Schoenen FJ, Prisinzano TE, Bohn LM, Aube J. (2014). Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif. Bioorg Med Chem S0968-0896(14)00881-5.
OPRK1	Schmid CL, Streicher JM, Groer CE, Munro TA, Zhou L and Bohn LM. (2013). Functional selectivity of 6'-guanidinonaltrindole (6'-GNTI) at kappa opioid receptors in striatal neurons. J Biol Chem 288(31):22387-98.
OPRK1	Beguin C, Potuzak J, Xu W, Liu-Chen, LY, Streicher, JM, Groer, CE, Bohn, LM, Carlezon, WA, Jr., and Cohen, B.M. (2012). Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues. Bioorg Med Chem Lett 22(2):1023-6.
OPRK1	Roberts LR, Brady K, Brown A, Davey D, Feng L, Huang H, Liu D, Malet L, McMurray G, Phelan A, Saunders K and Bhat A. (2012). Kappa agonist CovX-Bodies. Bioorg Med Chem Lett 22(12):4173-8.
OPRK1	Hedrick MP, Gosalia P, Frankowski K, Shi S, Prisinzano TE, Schoenen F, Aube J, Su Y, Vasile S, Sergienko E, et al. (2010). Selective KOP receptor antagonists: Probe 1. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information 2010 Feb 28 [updated 2010 Oct 4].
OPRK1, OPRM1	Zhou L, Lovell KM, Frankowski KJ, Slauson SR, Phillips AM, Streicher JM, Stahl EL, Schmid CL, Hodder P, Madoux F, Cameron MD, Prisinzano TE, Aube J and Bohn LM. (2013). Development of functionally selective, small molecule agonists at kappa opioid receptors. J Biol Chem 288(51):36703-16.
OPRM1	Burford NT, Traynor JR and Alt A. (2015). Positive allosteric modulators of the μ-opioid receptor: a novel approach for future pain medications. Br J Pharmacol. 172(2):277-86. (review paper)
OPRM1	Bird MF, Vardanyan RS, Hruby VJ, Calo G, Guerrini R, Salvadori S, Trapella C, McDonald J, Rowbotham DJ, Lambert D (2015). Development and characterisation of novel fentanyl-delta opioid receptor antagonist based bivalent ligands. Br J Anaesth. 114(4):646-56.
OPRM1	Burford NT, Clark MJ, Wehrman TS, Gerritz SW, Banks M, O’Connell J, Traynor JR and Alt A. (2013). Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor. Proc Natl Acad Sci USA 110(26):10830-5.
OPRM1	Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS. (2013). Structure-Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain. J Med Chem 56(20):8019-31.
OPRM1	Nickolls SA, Humphreys S, Clark M and McMurray G. (2013). Co-expression of GRK2 reveals a novel conformational state of the m-opioid receptor. PLoS ONE 8(12): e83691.
OPRM1	Nickolls SA, Waterfield A, Williams RE and Kinloch RA. (2011). Understanding the effect of different assay formats on agonist parameters: a study using the m-opioid receptor. J Biomol Screen16(7):706-16.
OPRM1 (Arrestin & Internalization)	DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW and Violin JD. (2013). A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther 344(3):708-17.
OPRM1 (Internalization)	McPherson J, Rivero G, Baptist M, Llorente J, Al-Sabah S, Krasel C, Dewey WL, Bailey CP, Rosethorne EM, Charlton SJ et al. (2010). m-opioid receptors: correlation of agonist efficacy for signalling with ability to activate internalization. Mol Pharmacol 78(4):756-66.
OPRM1, OPRD1	Burford NT, Wehrman T, Bassoni D, O'Connell J, Banks M, Zhang L, Alt A. (2014). Identification of Selective Agonists and Positive Allosteric Modulators for mu- and δ-Opioid Receptors from a Single High-Throughput Screen. J Biomol Screen. 19(9):1255-65.
OPRM1, OPRD1	Fujita W, Gomes I, Dove LS, Prohaska D, McIntyre G, Devi LA. (2014). Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers. Biochem Pharmacol 92(3):448-56.

Parathyroid Hormone Receptors (副甲状腺ホルモン受容体)

GPCR Target	Reference
PTHR1	Cupp ME, Song B, Kibler P, Raghavender US, Nayak SK, Thomsen W, Galande AK. (2013). Investigating hydrophobic ligand-receptor interactions in parathyroid hormone receptor using peptide probes. J Pept Sci 19(6):337-44.
PTHR1	Bivi N, Lezcano V, Romanello M, Bellido T, Plotkin LI. (2011). Connexin43 interacts with βarrestin: a pre-requisite for osteoblast survival induced by parathyroid hormone. J Cell Biochem112(10):2920-30.
PTHR1 (Internalization)	Cupp ME, Nayak SK, Adem AS and Thomsen WJ. (2013). Parathyroid hormone (PTH) and PTH-related peptide domains contributing to activation of different PTH receptor-mediated signaling pathways. J Pharmacol Exp Ther 345(3):404-18.

Purinergic P2Y Receptors (プリンP2Y受容体)

GPCR Target	Reference
P2YR12	Foster HR, Fuerst E, Lee TH, Cousins DJ and Woszczek G. (2013). Characterisation of P2Y(12) receptor responsiveness to cysteinyl leukotrienes. PLoS One 8:e58305.
P2YR12	Fredman G, Van Dyke TE and Serhan CN. (2010). Resolvin E1 regulates adenosine diphosphate activation of human platelets. Arterioscler Thromb Vasc Biol 30(10):2005-13.

Serotonin Receptors (セロトニン受容体)

GPCR Target	Reference
5HT2A	Schmid CL, Streicher JM, Meltzer HY, Bohn LM. (2014). Clozapine acts as an agonist at serotonin 2A receptors to counter MK-801-induced behaviors through a βarrestin2-independent activation of Akt. Neuropsychopharmacology. 39(8):1902-13.
5HT2A	Blough BE, Landavazo A, Decker AM, Partilla JS, Baumann MH, Rothman RB. (2014). Interaction of psychoactive tryptamines with biogenic amine transporters and serotonin receptor subtypes. Psychopharmacology (Berl). 231(21):4135-44.
5HT2A, 5HT2C	Clarke WP, Chavera TA, Silva M, Sullivan LC, Berg KA. (2013). Signalling profile differences: paliperidone versus risperidone. Br J Pharmacol 170(3):532-45.
5HT2B	Unett DJ, Gatlin J, Anthony TL, Buzard DJ, Chang S, Chen C, Chen X, Dang HTM, Frazer J, Le MK, Sadeque AJM, Xing C and Gaidarov I. (2013). Kinetics of 5-HT2B receptor signaling: profound agonist-dependent effects on signaling onset and duration. J Pharmacol Exp Ther 347(3):645-59.

Somatostatin Receptors (ソマトスタチン受容体)

GPCR Target	Reference
SSTR2	Zhao X, Jones A, Olson KR, Peng K, Wehrman T, Park A, Mallari R, Nebalasca D, Young SW and Xiao SH. (2008). A homogeneous enzyme fragment complementation-based beta-arrestin translocation assay for high-throughput screening of G-protein-coupled receptors. J Biomol Screen 13(8):737-47.

Thyrotropin (Glycoprotein Hormone) Receptorss (サイロトロピン受容体)

GPCR Target	Reference
TSHR	Boutin A, Eliseeva E, Gershengorn MC, Neumann S. (2014). β-Arrestin-1 mediates thyrotropin-enhanced osteoblast differentiation. FASEB J. 28(8):3446-55.

VIP and PACAP Receptors

GPCR Target	Reference
VPAC2	Chu A, Caldwell JS, and Chen YA. (2010). Identification and characterization of a small molecule antagonist of human VPAC(2) receptor. Mol Pharmacol 77(1):95-101.

全文献リストはこちらでもご覧いただけます　→　★