메뉴 건너뛰기




Volumn 9, Issue 2, 2009, Pages 75-78

Does targeting the lipophilic milieu provide advantages for an endothelin antagonist?

Author keywords

[No Author keywords available]

Indexed keywords

ACT 132577; BOSENTAN; CYCLO(DEXTRO GLUTAMYLALANYL DEXTRO VALYLLEUCYL DEXTRO TRYPTOPHYL); ENDOTHELIN 1; ENDOTHELIN 2; ENDOTHELIN 3; ENDOTHELIN A RECEPTOR; ENDOTHELIN A RECEPTOR ANTAGONIST; ENDOTHELIN B RECEPTOR; ENDOTHELIN RECEPTOR ANTAGONIST; MACITENTAN; SITAXSENTAN; UNCLASSIFIED DRUG;

EID: 65949120920     PISSN: 15340384     EISSN: 15432548     Source Type: Journal    
DOI: 10.1124/mi.9.2.6     Document Type: Review
Times cited : (4)

References (33)
  • 1
    • 0027452151 scopus 로고
    • Purification and characterization of a phosphoramidon-sensitive endothelin-converting enzyme in porcine aortic endothelium
    • Ohnaka, K., Takayanagi, R., Nishikawa, M., Haji, M., and Nawata, H. Purification and characterization of a phosphoramidon-sensitive endothe- lin-converting enzyme in porcine aortic endothelium. J. Biol. Chem. 268, 26759-26766 (1993).
    • (1993) J. Biol. Chem. , vol.268 , pp. 26759-26766
    • Ohnaka, K.1    Takayanagi, R.2    Nishikawa, M.3    Haji, M.4    Nawata, H.5
  • 2
    • 0028181105 scopus 로고
    • Characterization of two endothelin converting enzymes and their preference for big endothelin-1 and -2 as substrates
    • Chiou W.J., Shiosaki, K., Tasker, A.S., and Wu-Wong, J.R. Characterization of two endothelin converting enzymes and their preference for big endothelin-1 and -2 as substrates. Life Sci. 54, 1613-1619 (1994).
    • (1994) Life Sci. , vol.54 , pp. 1613-1619
    • Chiou, W.J.1    Shiosaki, K.2    Tasker, A.S.3    Wu-Wong, J.R.4
  • 3
    • 0027992642 scopus 로고
    • ECE-1: A membrane-bound metalloprotease that catalyzes the proteolytic activation of big endothelin-1
    • Xu, D., Emoto, N., Giaid, A., Slaughter, C., Kaw, S., deWit, D., and Yanagisawa, M. ECE-1: A membrane-bound metalloprotease that catalyzes the proteolytic activation of big endothelin-1. Cell 78, 473-485 (1994).
    • (1994) Cell , vol.78 , pp. 473-485
    • Xu, D.1    Emoto, N.2    Giaid, A.3    Slaughter, C.4    Kaw, S.5    De Wit, D.6    Yanagisawa, M.7
  • 5
    • 0025605930 scopus 로고
    • Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor
    • Sakurai, T., Yanagisawa, M., Takuwa, Y., Miyazaki, H., Kimura, S., Goto, K., and Masaki, T. Cloning of a cDNA encoding a non-isopeptide-selec- tive subtype of the endothelin receptor. Nature 348, 732-735 (1990).
    • (1990) Nature , vol.348 , pp. 732-735
    • Sakurai, T.1    Yanagisawa, M.2    Takuwa, Y.3    Miyazaki, H.4    Kimura, S.5    Goto, K.6    Masaki, T.7
  • 6
    • 0027499701 scopus 로고
    • The human endothelin-B receptor gene structural organization and chromosomal assignment
    • Arai, H., Nakao, K., Takaya, K., Hosoda, K., Ogawa, Y., Nakanishi, S., and Imura, H. The human endothelin-B receptor gene. Structural organization and chromosomal assignment. J. Biol. Chem. 268, 3463-3470 (1993).
    • (1993) J. Biol. Chem. , vol.268 , pp. 3463-3470
    • Arai, H.1    Nakao, K.2    Takaya, K.3    Hosoda, K.4    Ogawa, Y.5    Nakanishi, S.6    Imura, H.7
  • 7
    • 33847031260 scopus 로고    scopus 로고
    • Contrasting actions of endothelin ETA and ETB receptors in cardiovascular disease
    • A fairly recent and thorough review of endothelin receptor specific actions in physiology and disease focusing on receptor specific actions
    • Schneider, M.P., Boesen, E.I., and Pollock, D.M. Contrasting actions of endothelin ETA and ETB receptors in cardiovascular disease. Annu. Rev. Pharmacol. Toxicol. 47, 731-759 (2007). A fairly recent and thorough review of endothelin receptor specific actions in physiology and disease focusing on receptor specific actions.
    • (2007) Annu. Rev. Pharmacol. Toxicol. , vol.47 , pp. 731-759
    • Schneider, M.P.1    Boesen, E.I.2    Pollock, D.M.3
  • 8
    • 0025815672 scopus 로고
    • Endothelin-1 induces hypertrophy with enhanced expression of muscle-specific genes in cultured neonatal rat cardiomyocytes
    • Ito, H., Hirata, Y., Hiroe, M., Tsujino, M., Adachi, S., Takamoto, T., Nitta, M., Taniguchi, K., and Marumo, F. Endothelin-1 induces hypertrophy with enhanced expression of muscle-specific genes in cultured neonatal rat cardiomyocytes. Circ. Res. 69, 209-215 (1991).
    • (1991) Circ. Res. , vol.69 , pp. 209-215
    • Ito, H.1    Hirata, Y.2    Hiroe, M.3    Tsujino, M.4    Adachi, S.5    Takamoto, T.6    Nitta, M.7    Taniguchi, K.8    Marumo, F.9
  • 9
    • 0025836185 scopus 로고
    • Endothelin an endothelial-dependent vasoconstrictor in scleroderma enhanced production and profibrotic action
    • Kahaleh, M.B. Endothelin, an endothelial-dependent vasoconstrictor in scleroderma. Enhanced production and profibrotic action. Arthritis Rheum. 34, 978-983 (1991).
    • (1991) Arthritis Rheum. , vol.34 , pp. 978-983
    • Kahaleh, M.B.1
  • 10
    • 0000445909 scopus 로고    scopus 로고
    • Endothelin-1 regulation of intercellular adhesion molecule-1 expression in normal and sclerodermal fibroblasts
    • Xu, S.W., Denton, C.P., Dashwood, M.R., Abraham, D.J., and Black, C.M. Endothelin-1 regulation of intercellular adhesion molecule-1 expression in normal and sclerodermal fibroblasts. J. Cardiovasc. Pharmacol. 31 (Suppl 1), S545-S547 (1998).
    • (1998) J. Cardiovasc. Pharmacol. , vol.31 , Issue.1 SUPPL.
    • Xu, S.W.1    Denton, C.P.2    Dashwood, M.R.3    Abraham, D.J.4    Black, C.M.5
  • 11
    • 0029022496 scopus 로고
    • Acute pro-inflammatory actions of endothelin-1 in the guinea-pig lung: Involvement of ETA and ETB receptors
    • Filep, J.G., Fournier, A. and Foldes-Filep, E. Acute pro-inflammatory actions of endothelin-1 in the guinea-pig lung: Involvement of ETA and ETB receptors. Br. J. Pharmacol. 115, 227-236 (1995).
    • (1995) Br. J. Pharmacol. , vol.115 , pp. 227-236
    • Filep, J.G.1    Fournier, A.2    Foldes-Filep, E.3
  • 12
    • 0028788150 scopus 로고
    • Neurohormonal activation in patients with right ventricular failure from pulmonary hypertension: Relation to hemodynamic variables and endothelin levels
    • Nootens, M., Kaufmann, E., Rector, T., Toher, C., Judd, D., Francis, G.S., and Rich, S. Neurohormonal activation in patients with right ventricular failure from pulmonary hypertension: Relation to hemodynamic variables and endothelin levels. J. Am. Coll. Cardiol. 26, 1581-1585 (1995).
    • (1995) J. Am. Coll. Cardiol. , vol.26 , pp. 1581-1585
    • Nootens, M.1    Kaufmann, E.2    Rector, T.3    Toher, C.4    Judd, D.5    Francis, G.S.6    Rich, S.7
  • 13
    • 0035171979 scopus 로고    scopus 로고
    • Big endothelin-1 and endothelin-1 plasma levels are correlated with the severity of primary pulmonary hypertension
    • Rubens, C., Ewert, R., Halank, M., Wensel, R., Orzechowski, H.D., Schultheiss, H.P., and Hoeffken, G. Big endothelin-1 and endothelin-1 plasma levels are correlated with the severity of primary pulmonary hypertension. Chest 120, 1562-1569 (2001).
    • (2001) Chest , vol.120 , pp. 1562-1569
    • Rubens, C.1    Ewert, R.2    Halank, M.3    Wensel, R.4    Orzechowski, H.D.5    Schultheiss, H.P.6    Hoeffken, G.7
  • 14
    • 49749102732 scopus 로고    scopus 로고
    • Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: Does selectivity matter?
    • Opitz, C.F., Ewert, R., Kirch, W., and Pittrow, D. Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: Does selectivity matter? Eur. Heart J. 29, 1936-1948 (2008).
    • (2008) Eur. Heart J. , vol.29 , pp. 1936-1948
    • Opitz, C.F.1    Ewert, R.2    Kirch, W.3    Pittrow, D.4
  • 15
    • 0025195718 scopus 로고
    • D-Arg1 D-Phe5 D-Trp7 9 Leu11 substance P a neuropeptide antagonist blocks binding Ca2+-mobilizing and mitogenic effects of endothelin and vasoactive intestinal contractor in mouse 3T3 cells
    • Fabregat, I. and Rozengurt, E. [D-Arg1,D-Phe5,D-Trp7,9,Leu11] substance P, a neuropeptide antagonist, blocks binding, Ca2+-mobilizing, and mitogenic effects of endothelin and vasoactive intestinal contractor in mouse 3T3 cells. J. Cell Physiol. 145, 88-94 (1990).
    • (1990) J. Cell Physiol. , vol.145 , pp. 88-94
    • Fabregat, I.1    Rozengurt, E.2
  • 16
    • 0026593030 scopus 로고
    • Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor
    • Study describing the discovery and origins of the first widely used endothelin receptor antagonists
    • Ihara, M., Noguchi, K., Saeki, T. et al. Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor. Life Sci. 50, 247-255 (1992). Study describing the discovery and origins of the first widely used endothelin receptor antagonists.
    • (1992) Life Sci. , vol.50 , pp. 247-255
    • Ihara, M.1    Noguchi, K.2    Saeki, T.3
  • 17
    • 0035986906 scopus 로고    scopus 로고
    • Bosentan: A dual endothelin receptor antagonist
    • A review of the discovery and utility of bosentan, the first endothelin antagonist approved for use in humans
    • Rubin, L.J. and Roux, S. Bosentan: A dual endothelin receptor antagonist. Expert Opin. Investig. Drugs 11, 991-1002 (2002). A review of the discovery and utility of bosentan, the first endothelin antagonist approved for use in humans.
    • (2002) Expert Opin. Investig. Drugs , vol.11 , pp. 991-1002
    • Rubin, L.J.1    Roux, S.2
  • 18
  • 19
    • 62749192201 scopus 로고    scopus 로고
    • A meta-analysis of randomized controlled trials in pulmonary arterial hypertension
    • A recent review that places endothelin antagonists in context with other clinical trials in the treatment of pulmonary hypertension
    • Galie, N., Manes, A., Negro, L., Palazzini, M., Bacchi-Reggiani, M.L., and Branzi, A. A meta-analysis of randomized controlled trials in pulmonary arterial hypertension. Eur. Heart J. 30, 394-403 (2009). A recent review that places endothelin antagonists in context with other clinical trials in the treatment of pulmonary hypertension.
    • (2009) Eur. Heart J. , vol.30 , pp. 394-403
    • Galie, N.1    Manes, A.2    Negro, L.3    Palazzini, M.4    Bacchi-Reggiani, M.L.5    Branzi, A.6
  • 20
    • 0028292620 scopus 로고
    • Pharmacological characterization of bosentan a new potent orally active nonpeptide endothelin receptor antagonist
    • Pharmacology of the first orally active, commerially available endothelin receptor antagonist
    • Clozel, M., Breu, V., Gray, G.A. et al. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 270, 228-235 (1994). Pharmacology of the first orally active, commerially available endothelin receptor antagonist.
    • (1994) J. Pharmacol. Exp. Ther. , vol.270 , pp. 228-235
    • Clozel, M.1    Breu, V.2    Gray, G.A.3
  • 21
    • 0027299798 scopus 로고
    • Endothelin receptor subtype B mediates synthesis of nitric oxide by cultured bovine endothelial cells
    • Hirata, Y., Emori, T., Eguchi, S., Kanno, K., Imai, T., Ohta, K., and Marumo, F. Endothelin receptor subtype B mediates synthesis of nitric oxide by cultured bovine endothelial cells. J. Clin. Invest. 91, 1367-1373 (1993).
    • (1993) J. Clin. Invest. , vol.91 , pp. 1367-1373
    • Hirata, Y.1    Emori, T.2    Eguchi, S.3    Kanno, K.4    Imai, T.5    Ohta, K.6    Marumo, F.7
  • 22
    • 0141730234 scopus 로고    scopus 로고
    • Emergence of smooth muscle cell endothelin B-mediated vasoconstriction in lambs with experimental congenital heart disease and increased pulmonary blood flow
    • Black, S.M., Mata-Greenwood, E., Dettman, R.W. et al. Emergence of smooth muscle cell endothelin B-mediated vasoconstriction in lambs with experimental congenital heart disease and increased pulmonary blood flow. Circulation 108, 1646-1654 (2003).
    • (2003) Circulation , vol.108 , pp. 1646-1654
    • Black, S.M.1    Mata-Greenwood, E.2    Dettman, R.W.3
  • 23
    • 33744922911 scopus 로고    scopus 로고
    • Profile of past and current clinical trials involving endothelin receptor antagonists: The novel "-sentan" class of drug
    • A comprehensive review of clinical trials involving endothelin receptor antagnists and includes excellent summaries of receptor selectivity, pharmacokinetics, common adverse effects, success or failure to achieve therapeutic benefit in the targeted diseases and outcomes of selective preclinical studies in animals Report of the first endothelin receptor antagonist designed to target lipophilic environments
    • Battistini, B., Berthiaume, N., Kelland, N.F., Webb, D.J., and Kohan, D.E. Battistini, B., Berthiaume, N., Kelland, N.F., Webb, D.J., and Kohan, D.E. Profile of past and current clinical trials involving endothelin receptor antagonists: The novel "-sentan" class of drug. Exp. Biol. Med. (Maywood) 231, 653-695 (2006). A comprehensive review of clinical trials involving endothelin receptor antagnists and includes excellent summaries of receptor selectivity, pharmacokinetics, common adverse effects, success or failure to achieve therapeutic benefit in the targeted diseases and outcomes of selective preclinical studies in animals.
    • (2006) Exp. Biol. Med. (Maywood) , vol.231 , pp. 653-695
    • Battistini, B.1    Berthiaume, N.2    Kelland, N.F.3    Webb, D.J.4    Kohan, D.E.5
  • 24
    • 57349133022 scopus 로고    scopus 로고
    • Pharmacology of macitentan an orally active tissue-targeting dual endothelin receptor antagonist
    • Report of the first endothelin receptor antagonist designed to target lipophilic environments
    • Iglarz, M., Binkert, C., Morrison, K., Fischli W., et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 327, 736-745 (2008). Report of the first endothelin receptor antagonist designed to target lipophilic environments.
    • (2008) J. Pharmacol. Exp. Ther. , vol.327 , pp. 736-745
    • Iglarz, M.1    Binkert, C.2    Morrison, K.3    Fischli, W.4
  • 25
    • 0032977585 scopus 로고    scopus 로고
    • Central effects of endothelin and its antagonists on sympathetic and cardiovascular regulation in SHR-SP
    • Nakamura, K., Sasaki, S., Moriguchi, J., Morimoto, S., et al. Central effects of endothelin and its antagonists on sympathetic and cardiovascular regulation in SHR-SP. J. Cardiovasc. Pharmacol. 33, 876-882 (1999).
    • (1999) J. Cardiovasc. Pharmacol. , vol.33 , pp. 876-882
    • Nakamura, K.1    Sasaki, S.2    Moriguchi, J.3    Morimoto, S.4
  • 26
    • 17444382354 scopus 로고    scopus 로고
    • Effect of endothelin antagonist (TAK-044) on cerebral ischemic volume oxidative stress markers and neurobehavioral parameters in the middle cerebral artery occlusion model of stroke in rats
    • Gupta, Y.K., Briyal, S., Sharma, U., Jagannathan, N.R., and Gulati, A. Effect of endothelin antagonist (TAK-044) on cerebral ischemic volume, oxidative stress markers and neurobehavioral parameters in the middle cerebral artery occlusion model of stroke in rats. Life Sci. 77, 15-27 (2005).
    • (2005) Life Sci. , vol.77 , pp. 15-27
    • Gupta, Y.K.1    Briyal, S.2    Sharma, U.3    Jagannathan, N.R.4    Gulati, A.5
  • 27
  • 28
    • 0032881899 scopus 로고    scopus 로고
    • Endothelin-1 is elevated in the cerebrospinal fluid of HIV- infected patients with encephalopathy
    • Rolinski, B., Heigermoser, A., Lederer, E., Bogner, J.R., Loch, O., and Goebel, F.D. Endothelin-1 is elevated in the cerebrospinal fluid of HIV- infected patients with encephalopathy. Infection 27, 244-247 (1999).
    • (1999) Infection , vol.27 , pp. 244-247
    • Rolinski, B.1    Heigermoser, A.2    Lederer, E.3    Bogner, J.R.4    Loch, O.5    Goebel, F.D.6
  • 29
    • 0034803324 scopus 로고    scopus 로고
    • Evidence for endothelin involvement in the response to high salt
    • Pollock, D.M. and Pollock, J.S. Evidence for endothelin involvement in the response to high salt. Am. J. Physiol. Renal Physiol. 281, F144-F150 (2001).
    • (2001) Am. J. Physiol. Renal Physiol. , vol.281
    • Pollock, D.M.1    Pollock, J.S.2
  • 30
    • 33845423984 scopus 로고    scopus 로고
    • Collecting duct-specific knockout of the endothelin B receptor causes hypertension and sodium retention
    • Convincing evidence that ETB receptors within the kidney play a critical role in preventing salt-dependent hypertension
    • Ge, Y., Bagnall, A., Stricklett, P. K., Strait, K., Webb, D.J., Kotelevtsev, Y., and Kohan D.E. Collecting duct-specific knockout of the endothelin B receptor causes hypertension and sodium retention. Am. J. Physiol. Renal Physiol. 291, F1274-F1280 (2006). Convincing evidence that ETB receptors within the kidney play a critical role in preventing salt-dependent hypertension.
    • (2006) Am. J. Physiol. Renal Physiol. , vol.291
    • Ge, Y.1    Bagnall, A.2    Stricklett, P.K.3    Strait, K.4    Webb, D.J.5    Kotelevtsev, Y.6    Kohan, D.E.7
  • 31
    • 3242767660 scopus 로고    scopus 로고
    • Roles of endothelin ETA and ETB receptors in the pathogenesis of monocro- taline-induced pulmonary hypertension
    • Nishida, M., Eshiro, K., Okada, Y., Takaoka, M., and Matsumura, Y. Roles of endothelin ETA and ETB receptors in the pathogenesis of monocro- taline-induced pulmonary hypertension. J. Cardiovasc. Pharmacol. 44, 187-191 (2004).
    • (2004) J. Cardiovasc. Pharmacol. , vol.44 , pp. 187-191
    • Nishida, M.1    Eshiro, K.2    Okada, Y.3    Takaoka, M.4    Matsumura, Y.5
  • 32
    • 0035895324 scopus 로고    scopus 로고
    • Effectiveness of a nonselective ETA/B and a selective ETA antagonist in rats with monocrota- line-induced pulmonary hypertension
    • Jasmin, J.F., Lucas, M., Cernacek, P. and Dupuis, J. Effectiveness of a nonselective ETA/B and a selective ETA antagonist in rats with monocrota- line-induced pulmonary hypertension. Circulation 103, 314-318 (2001).
    • (2001) Circulation , vol.103 , pp. 314-318
    • Jasmin, J.F.1    Lucas, M.2    Cernacek, P.3    Dupuis, J.4
  • 33
    • 33645469407 scopus 로고    scopus 로고
    • Diabetic endothelin B receptor-deficient rats develop severe hypertension and progressive renal failure
    • Pfab, T., Thone-Reineke, C., Theilig, F. et al. Diabetic endothelin B receptor-deficient rats develop severe hypertension and progressive renal failure. J. Am. Soc. Nephrol. 17, 1082-1089 (2006).
    • (2006) J. Am. Soc. Nephrol. , vol.17 , pp. 1082-1089
    • Pfab, T.1    Thone-Reineke, C.2    Theilig, F.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.