Evidence for biased agonists and antagonists at the endothelin receptors

Life Sciences

Volumn 159, Issue , 2016, Pages 30-33

  Maguire, Janet J ^a  

^a ADDENBROOKE S HOSPITAL   (United Kingdom)

Author keywords

Biased agonism; Biased antagonism; Bosentan; Endothelin; ETA; ETB; G protein coupled receptors; IRL1620; Pathway selectivity; Arrestin

Indexed keywords

BETA ARRESTIN; BOSENTAN; CELL PENETRATING PEPTIDE; ENDOTHELIN A RECEPTOR; ENDOTHELIN B RECEPTOR; ENDOTHELIN RECEPTOR; ENDOTHELIN RECEPTOR AGONIST; ENDOTHELIN RECEPTOR ANTAGONIST; GUANINE NUCLEOTIDE BINDING PROTEIN; N ACETYLENDOTHELIN 1 [6-21][11,15 ALANINE]; SARAFOTOXIN S6B; SUCCINYLENDOTHELIN 1 [8-21][9 GLUTAMIC ACID 11,15 ALANINE]; PEPTIDE;

ARTICLE; DRUG ANTAGONISM; DRUG BINDING SITE; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; HUMAN; INTRACELLULAR SIGNALING; NONHUMAN; OVARY CANCER; PHASE 2 CLINICAL TRIAL (TOPIC); PROTEIN PROTEIN INTERACTION; PULMONARY HYPERTENSION; AGONISTS; ANIMAL; METABOLISM;

ANIMALS; ENDOTHELIN RECEPTOR ANTAGONISTS; HUMANS; PEPTIDES; RECEPTORS, ENDOTHELIN;

EID: 84959045331     PISSN: 00243205     EISSN: 18790631     Source Type: Journal    
DOI: 10.1016/j.lfs.2016.02.069     Document Type: Article

References (29)

1. [1] Wisler, J.W., Xiao, K., Thomsen, A.R.B., Lefkowitz, R.J., Recent developments in biased agonism. Curr. Opin. Cell Biol. 27 (2014), 18–24.
2. [2] Shukla, A.K., Xiao, K., Lefkowitz, R.J., Emerging paradigms of β-arrestin-dependent seven transmembrane receptor signalling. Trends Biochem. Sci. 36 (2011), 457–469.
3. [3] Soergel, D.G., Subach, R.A., Burnham, N., Lark, M.W., James, I.E., Sadler, B.M., Skobieranda, F., Violin, J.D., Webster, L.R., Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: a randomized, double-blind, placebo-controlled, crossover study in healthy volunteers. Pain 155 (2014), 1829–1835.
4. [4] Thompson, G.L., Lane, J.R., Coudrat, T., Sexton, P.M., Christopoulos, A., Canals, M., Biased agonism of endogenous opioid peptides at the μ-opioid receptor. Mol. Pharmacol. 88 (2015), 335–346.
5. [5] Maguire, J.J., Kuc, R.E., Rous, B.A., Davenport, A.P., Failure of BQ123, a more potent antagonist of sarafotoxin 6b than of endothelin-1, to distinguish between these agonists in binding experiments. Br. J. Pharmacol. 118 (1996), 335–342.
6. [6] De Mey, J.G., Compeer, M.G., Lemkens, P., Meens, M.J., ETA-receptor antagonists or allosteric modulators?. Trends Pharmacol. Sci. 32 (2011), 345–351.
7. [7] Kenakin, T., What is pharmacological ‘affinity’? Relevance to biased agonism and antagonism. Trends Pharmacol. Sci. 35 (2014), 434–441.
8. [8] Compeer, M.G., Janssen, G.M.J., De Mey, J.G.R., Endothelin-1 and endothelin-2 initiate and maintain contractile responses by different mechanisms in rat mesenteric and cerebral arteries. Br. J. Pharmacol. 170 (2013), 1199–1209.
9. A receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br. J. Pharmacol. 115 (1995), 191–197.
10. B receptor signalling via G-protein and β-arrestin pathways. Life Sci. 91 (2012), 544–549.
11. 2-adrenergic receptor ligands: implications for drug taxonomy. Mol. Pharmacol. 85 (2014), 492–509.
12. [12] Leonard, M.G., Gulati, A., Endothelin B receptor agonist, IRL-1620, enhances angiogenesis and neurogenesis following cerebral ischemia in rats. Brain Res. 1528 (2013), 28–41.
13. [13] Rajeshkumar, N.V., Matwyshyn, G., Gulati, A., IRL-1620, a tumor selective vasodilator, augments the uptake and efficacy of chemotherapeutic agents in prostate tumor rats. Prostate 67 (2007), 701–713.
14. [14] Clozel, M., Breu, V., Gray, G.A., Kalina, B., Löffler, B.-M., Burri, K., Cassal, J.-M., Hirth, G., Müller, M., Neidhart, W., Ramuz, H., Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 270 (1994), 228–235.
15. [15] Peter, M.G., Davenport, A.P., Characterization of the endothelin receptor selective agonist, BQ3020 and antagonists BQ123, FR139317, BQ788, 50235, Ro462005 and bosentan in the heart. Br. J. Pharmacol. 117 (1996), 455–462.
16. [16] Maguire, J.J., Kuc, R.E., Davenport, A.P., Defining the affinity and receptor sub-type selectivity of four classes of endothelin antagonists in clinically relevant human cardiovascular tissues. Life Sci. 91 (2012), 681–686.
17. [17] Bacon, C.R., Davenport, A.P., Endothelin receptors in human coronary artery and aorta. Br. J. Pharmacol. 117 (1996), 986–992.
18. 2 receptor-mediated cell signaling and migration in arterial smooth muscle. Am. J. Physiol. Cell Physiol. 302 (2012), C723–C734.
19. [19] Dimond, P., Carlson, K., Bouvier, M., Gerard, C., Xu, L., Covic, L., Agarwal, A., Ernst, O.P., Janz, J.M., Schwartz, T.W., Gardella, T.J., Milligan, G., Kuliopulos, A., Sakmar, T.P., Hunt, S.W., G protein-coupled receptor modulation with pepducins: moving closer to the clinic. Ann. N. Y. Acad. Sci. 1226 (2011), 34–49.
20. [20] Green, D.S., Rupasinghe, C., Warburton, R., Wilson, J.L., Sallum, C.O., Taylor, L., Yatawara, A., Mierke, D., Polgar, P., Hill, N., A cell permeable peptide targeting the intracellular loop 2 of endothelin B receptor reduces pulmonary hypertension in a hypoxic rat model. PLoS ONE, 8, 2013, e81309.
21. [21] Cianfrocca, R., Tocci, P., Semprucci, E., Spinella, F., Di Castro, V., Bagnato, A., Rosanò, L., β-Arrestin 1 is required for endothelin-1-induced NF-κB activation in ovarian cancer cells. Life Sci. 118 (2014), 179–184.
22. [22] Rosanò, L., Cianfrocca, R., Masi, S., Spinella, F., Di Castro, V., Biroccio, A., Salvati, E., Nicotra, M.R., Natali, P.G., Bagnato, A., Beta-arrestin links endothelin A receptor to beta-catenin signaling to induce ovarian cancer cell invasion and metastasis. Proc. Natl. Acad. Sci. U. S. A. 106 (2009), 2806–2811.
23. [23] Rosanò, L., Cianfrocca, R., Tocci, P., Spinella, F., Di Castro, V., Spadaro, F., Salvati, E., Biroccio, A.M., Natali, P.G., Bagnato, A., β-Arrestin-1 is a nuclear transcriptional regulator of endothelin-1-induced β-catenin signalling. Oncogene 32 (2013), 5066–5077.
24. [24] Teoh, J.P., Park, K.M., Wang, Y., Hu, Q., Kimb, S., Wuc, G., Huang, S., Maihle, N., Kima, I.M., Endothelin-1/endothelin A receptor-mediated biased signaling is a new player in modulating human ovarian cancer cell tumorigenesis. Cell. Signal. 26 (2014), 2885–2895.
25. [25] Carr, R. III, Du, Y., Quoyer, J., Panettieri, R.A. Jr., Janz, J.M., Bouvier, M., Kobilka, B.K., Benovic, J.L., Development and characterization of pepducins as Gs-biased allosteric agonists. J. Biol. Chem. 289 (2014), 35668–35684.
26. [26] Ikeda, Y., Kumagai, H., Motozawa, Y., Suzuki, J., Kimuro, I., Biased agonism of the angiotensin II type I receptor. Int. Heart J. 56 (2015), 485–488.
27. [27] Li, J., Philip, J.L., Xu, X., Theccanat, T., Razzaque, M.A., Akhter, S.A., β-Arrestins regulate human cardiac fibroblast transformation and collagen synthesis in adverse ventricular remodelling. J. Mol. Cell. Cardiol. 76 (2014), 73–83.
28. [28] Kohan, D.E., Cleland, J.G., Rubin, L.J., Theodorescu, D., Barton, M., Clinical trials with endothelin receptor antagonists: what went wrong and where can we improve?. Life Sci. 91 (2012), 528–539.
29. [29] Lehmann, L.H., Rostosky, J.S., Buss, S.J., Kreusser, M.M., Krebs, J., Mier, W., Enseleit, F., Spiger, K., Hardt, S.E., Wieland, T., Hauss, M., Lüscher, T.F., Schneider, M.D., Parlato, R., Gröne, H.-J., Haberkorn, U., Yanagisawa, M., Katus, H.A., Backs, J., Essential role of sympathetic endothelin A receptors for adverse cardiac remodeling. Proc. Natl. Acad. Sci. U. S. A. 113 (2014), 13499–13504.