Identification of a pepducin acting as S1P3 receptor antagonist

Journal of Peptide Science

Volumn 19, Issue 11, 2013, Pages 717-724

  Severino, Beatrice ^a   Incisivo, Giuseppina Maria ^a   Fiorino, Ferdinando ^a   Bertolino, Antonio ^a   Frecentese, Francesco ^a   Barbato, Francesco ^a   Manganelli, Serena ^b   Maggioni, Giada ^b   Capasso, Domenica ^a   Caliendo, Giuseppe ^a   Santagada, Vincenzo ^a   Sorrentino, Raffaella ^a   Roviezzo, Fiorentina ^a   Perissutti, Elisa ^a  

^a UNIVERSITY OF NAPLES FEDERICO II   (Italy)

^b MARIO NEGRI INSTITUTE FOR PHARMACOLOGICAL RESEARCH   (Italy)

Author keywords

Ala scan; Pepducin; S1P3 antagonist; Sphingosine 1 phosphate (S1P)

Indexed keywords

ALANINE; AMINO ACID; KRX 725; PEPTIDE; RECEPTOR BLOCKING AGENT; SPHINGOSINE 1 PHOSPHATE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; AMINO TERMINAL SEQUENCE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CELL PROLIFERATION; CONFORMATION; DOSE RESPONSE; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN FUNCTION; VASODILATATION;

ALA-SCAN; PEPDUCIN; S1P3 ANTAGONIST; SPHINGOSINE-1-PHOSPHATE (S1P);

AMINO ACID MOTIFS; AMINO ACID SEQUENCE; ANIMALS; AORTA, THORACIC; CELL PROLIFERATION; CELL-PENETRATING PEPTIDES; CELLS, CULTURED; MALE; MICE; MODELS, MOLECULAR; MUSCLE CONTRACTION; PEPTIDE FRAGMENTS; RECEPTORS, LYSOSPHINGOLIPID; VASODILATOR AGENTS;

EID: 84885931857     PISSN: 10752617     EISSN: 10991387     Source Type: Journal    
DOI: 10.1002/psc.2554     Document Type: Article

References (26)

1. Rosen H, Gonzalez-Cabrera PJ, Sanna MG, Brown, S. Sphingosine 1-phosphate receptor signaling. Annu. Rev. Biochem. 2009; 78: 743-768.
2. Ishii I, Fukushima N, Ye X, Chun, J. Lysophospholipid receptors: signaling and biology. Annu. Rev. Biochem. 2004; 73: 321-354
3. Birgbauer E, Chun J. New developments in the biological function of lysophospholipids. Cell. Mol. Life Sci. 2006; 63: 2695-2701.
4. Gardell SE, Dubin AE, Chun J. Emerging medicinal roles for lysophospholipid signaling. Trends Mol. Med. 2006; 12: 65-75.
5. Sugiyama A, Yatomi Y, Ozaki Y, Hashimoto, K. Sphingosine 1-phosphate induces sinus tachycardia and coronary vasoconstriction in the canine heart. Cardiovasc. Res. 2000; 46: 119-125.
6. Ohmori T, Yatomi Y, Osada M, Kazama F, Takafuta T, Ikeda H, Ozaki Y. Sphingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2. Cardiovasc. Res. 2003; 58: 170-177.
7. Karliner JS. Lysophospholipids and the cardiovascular system. Biochim. Biophys. Acta 2002; 1582: 216-221.
8. English D, Brindley DN, Spiegel S, Garcia JGN. Lipid mediators of angiogenesis and the signalling pathways they initiate. Biochim. Biophys. Acta 2002; 1582: 228-239.
9. Garcia JGN, Liu F, Verin AD, Birukova A, Dechert MA, Gerthoffer WT, Bamburg JR, English D. Sphingosine 1-phosphate promotes endothelial cell barrier integrity by Edg-dependent cytoskeletal rearrangement. J. Clin. Invest. 2002, 108: 689-701.
10. Deutschman DH, Carstens JS, Klepper RL, Smith WS, Page MT, Young TR, Gleason LA, Nakajima N, Sabbadini RA. Predicting obstructive coronary artery disease with serum sphingosine-1-phosphate. Am. Heart J. 2003; 146: 62-68.
11. Keul P, Lucke S, von Wnuck LK, Bode C, Gräler M, Heusch G, Levkau B. Sphingosine-1-phosphate receptor 3 promotes recruitment of monocyte/macrophages in inflammation and atherosclerosis. Circ. Res. 2011; 108: 314-323.
12. Hsu A, Zhang W, Lee JF, An J, Ekambaram P, Liu J, Honn KV, Klinge CM, Lee MJ. Sphingosine-1-phosphate receptor-3 signaling up-regulates epidermal growth factor receptor and enhances epidermal growth factor receptor-mediated carcinogenic activities in cultured lung adenocarcinoma cells. Int. J. Oncol. 2012; 40: 1619-1626.
13. 3, sphingosine kinase 1, and extracellular signal-regulated kinase-1/2 is associated with development of tamoxifen resistance in estrogen receptor-positive breast cancer patients. Am. J. Pathol. 2010; 177: 2205-2215.
14. Harris GL, Creason MB, Brulte GB, Herr DR. In vitro and in vivo antagonism of a G protein-coupled receptor (S1P3) with a novel blocking monoclonal antibody. PLoS ONE 2012; 7:e35129.
15. 3 (EDG3). Blood 2003; 102: 2099-2107.
16. O'Callaghan K, Kuliopulos A, Covic L. Turning receptors on and off with intracellular pepducins: new insights into G-protein-coupled receptor drug development. J. Biol. Chem. 2012; 287: 12787-12796.
17. Peeters TL, Macielag MJ, Depoortere I, Konteatis ZD, Florance JR, Lessor RA, Galdes A. D-amino acid and alanine scans of the bioactive portion of porcine motilin. Peptides 1992; 13: 1103-1107.
18. Sahm UG, Olivier GWJ, Branch SK, Moss SH, Pouton CW. Synthesis and biological evaluation of R-MSH analogues substituted with alanine. Peptides 1994; 15: 1297-1302.
19. Tam JP, Liu W, Zhang JW, Galantino M, Bertolero F, Cristiani C, Vaghi F, De Castiglione R. Alanine scan of endothelin: importance of aromatic residues. Peptides 1994; 15: 703-708.
20. Horwell DC, Howson W, Naylor D, Osborne S, Pinnock RD, Ratcliffe GS, Suman-Chauhan N. Alanine scan and N-methyl amide derivatives of Ac-bombesin [7-14]. Int. J. Pept. Protein Res. 1996; 48: 522-531.
21. Atherton E, Sheppard RC. Solid-phase Peptide Synthesis: A Practical Approach. IRL Press: Oxford, UK, 1989.
22. Ohori M, Kinoshita T, Okubo M, Sato K, Yamazaki A, Arakawa H, Nishimura S, Inamura N, Nakajima H, Neya M, Miyake H, Fujii T. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem. Biophys. Res. Commun. 2005; 336: 357-363
23. Dantas AP, Igarashi J, Michel T. Sphingosine 1-phosphate and control of vascular tone. Am. J. Physiol. Heart Circ. Physiol. 2003; 284: H2045-2052.
24. Hofmann KP, Scheerer P, Hildebrand PW, Choe HW, Park JH, Heck M, Ernst OP. A G protein-coupled receptor at work: the rhodopsin model. Trends Biochem. Sci. 2009; 34: 540-552.
25. αq coupling selectivity. J. Biol. Chem. 1997; 272: 23675-23681.
26. Covic L, Misra M, Badar J, Singh C, Kuliopulos A. Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activation. Nat. Med. 2002; 8: 1161-1165.