No.39 文献リスト [GPCR PathHunter Arrestin]-4

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

Endothelin Receptors (エンドセリン受容体)

GPCR Target	Reference
EDNRA, EDNRB	Maguire JJ, Kuc RE, Pell VR, Green A, Brown M, Kumar S, Wehrman T, Quinn E and Davenport AP. (2012). Comparison of human ET(A) and ET(B) receptor signalling via G-protein and beta-arrestin pathways. Life Sci 91(13-14):544-9.

Follicle Stimulating Hormone Receptors (Glycoprotein Hormone Receptors) 
(卵胞刺激ホルモン受容体・糖蛋白ホルモン受容体)

GPCR Target	Reference
FSHR	Jiang X, Fischer D, Chen X, McKenna SD, Liu H, Sriraman V, Yu HN, Goutopoulos A, Arkinstall S, He X. (2014). AEvidence for Follicle-stimulating Hormone Receptor as a Functional Trimer. J Biol Chem. 289(20):14273-82.

Formylpeptide Receptors (ホルミルペプチド受容体)

GPCR Target	Reference
FPR1	Forsman H, Onnheim K, Andreasson E and Dahlgren C. (2011). What formyl peptide receptors, if any, are triggered by compound 43 and lipoxin A4? Scand J Immunol 74(3):227-34.
FPR1, FPR2	Cilibrizzi A, Schepetkin IA, Bartolucci G, Crocetti L, Dal Piaz V, Giovannoni MP, Graziano A, Kirpotina LN, Quinn MT and Vergelli C. (2012). Synthesis, enantioresolution, and activity profile of chiral 6-methyl-2,4-disubstituted pyridazin-3(2H)-ones as potent N-formyl peptide receptor agonists. Bioorg Med Chem 20(12):3781-92.
FPR2/ALX	Dalli J, Consalvo AP, Ray V, Di Filippo C, D'Amico M, Mehta N and Perretti M. (2013). Proresolving and tissue-protective actions of annexin A1-based cleavage-resistant peptides are mediated by formyl peptide receptor 2/lipoxin A4 receptor. J Immunol 190(12):6478-87.

Ghrelin Receptors (グレリン受容体)

GPCR Target

Reference

GHSR

Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando D, Gao H, Hepworth D, Jackson VM, Khot V, Kong J, Kosa RE, Lapham K, Loria PM, Londregan AT, McClure KF, Orr ST, Patel J, Rose C, Saenz J, Stock IA, Storer G, VanVolkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y. (2014). Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett. 5(5):474-9.

Glucagon Receptors (グルカゴン受容体)

GPCR Target	Reference
GLP1R	Al-Sabah S, Al-Fulaij M, Shaaban G, Ahmed HA, Mann RJ, Donnelly D, Bunemann M, Krasel C. (2014). The GIP receptor displays higher basal activity than the GLP-1 receptor but does not recruit GRK2 or arrestin3 effectively. PLoS ONE 9(9):e106890.
GLP1R	Heard KR, Wu W, Li Y, Zhao P, Woznica I, Lai JH, Beinborn M, Sanford DG, Dimare MT, Chiluwal AK, Peters DE, Whicher D, Sudmeier JL, Bachovchin WW. (2013). A General Method for Making Peptide Therapeutics Resistant to Serine Protease Degradation: Application to Dipeptidyl Peptidase IV Substrates. J Med Chem 56(21):8339-51.
GLP1R (Arrestin & Internalization)	Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW. (2014). Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). J Med Chem. 57(23):10192-7.

Histamine Receptors (ヒスタミン受容体)

GPCR Target	Reference
HRH4	Nijmeijer S, Vischer HF, Sirci F, Schultes S, Engelhardt H, de Graaf C, Rosethorne EM, Charlton SJ and Leurs R. (2013). Detailed analysis of biased histamine H4 receptor signalling by JNJ 7777120 analogues. Br J Pharmacol 170(1):78-88.
HRH4	Rosethorne EM and Charlton SJ. (2011). Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits beta-arrestin without activating G proteins. Mol Pharmacol 79(4):749-57.

Lysophospholipid Receptors (リゾリン脂質受容体)

GPCR Target	Reference
S1P1 (EDG1)	Gatfield J, Monnier L, Studer R, Bolli MH, Steiner B, Nayler O (2014). Sphingosine-1-phosphate (S1P) displays sustained S1P1 receptor agonism and signaling through S1P lyase-dependent receptor recycling. Cell Signal. 26(7):1576-88.
S1P1 (EDG1)	Purschke WG, Hoehlig K, Buchner K, Zboralski D, Schwoebel F, Vater A, Klussmann S (2014). Identification and characterization of a mirror-image oligonucleotide that binds and neutralizes sphingosine 1-phosphate, a central mediator of angiogenesis. Biochem J 462(1):153-62.
S1P1 (EDG1)	Lundstrom K. (2013). Present and future approaches to screening of G-protein-coupled receptors. Future Med Chem 5(5): 523-38.
S1P1 (EDG1)	Xu H, McElvain M, Fiorino M, Henkle B, Sherman L, Xu Y, Tominey E, Kelley K, Adlam M, Burli R, Siu J, Wong M and Cee VJ. (2013). Predictability of peripheral lymphocyte reduction of novel S1P1 sgonists by in vitro GPCR signaling, J Biomol Screen 18(9):997-1007.
S1P1 (EDG1)	Taylor S, Gray JR, Willis R, Deeks N, Haynes A, Campbell C, Gaskin P, Leavens K, Demont E, Dowell S, Cryan J, Morse M, Patel A, Garden H and Witherington J.(2012). The utility of pharmacokinetic-pharmacodynamic modeling in the discovery and optimization of selective S1P(1) agonists. Xenobiotica 42(7):671-86.
S1P1 (EDG1)	Sanders MP, Roumen L, van der Horst E, Lane JR, Vischer HF, van Offenbeek J, de Vries H, Verhoeven S, Chow KY, Verkaar F, Beukers MW, McGuire R, Leurs R, Ijzerman AP, de Vlieg J, de Esch IJ, Zaman GJ, Klomp JP, Bender A and de Graaf C. (2012). A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design. J Med Chem55(11):5311-25.
S1P1 (EDG1)	van Der Lee MM, Bras M, van Koppen CJ and Zaman GJ.(2008). beta-Arrestin recruitment assay for the identification of agonists of the sphingosine 1-phosphate receptor EDG1. J Biomol Screen 13(10):986-98.
S1P1 (EDG1) (Arrestin & Internalization)	Sykes DA, Riddy DM, Stamp C, Bradley ME, McGuiness N, Sattikar A, Guerini D, Rodrigues I, Glaenzel A, Dowling MR, Mullershausen F, Charlton SJ. (2014). Investigating the molecular mechanisms through which FTY720-P causes persistent S1P1 receptor internalization. Br J Pharmacol. 171(21):4797-807.
S1P3 (EDG3)	Riddy D, Stamp C, Sykes D, Charlton S and Dowling M. (2012). Reassessment of the pharmacology of sphingosine-1-phosphate S1P(3) receptor ligands using the DiscoveRx PathHunter and Ca(2+) release functional assays. Br J Pharmacol 167(4):868-80.

全文献リストはこちらでもご覧いただけます　→　★