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Page 1
Phosphoramidon inhibits the integral membrane protein zinc metalloprotease ZMPSTE24.
Goblirsch BR, Arachea BT, Councell DJ, Wiener MC. Goblirsch BR, et al. Acta Crystallogr D Struct Biol. 2018 Aug 1;74(Pt 8):739-747. doi: 10.1107/S2059798318003431. Epub 2018 Jul 24. Acta Crystallogr D Struct Biol. 2018. PMID: 30082509 Free PMC article.
As part of an effort to understand the structural and functional relationships between ZMPSTE24 and soluble zinc metalloproteases, the inhibition of ZMPSTE24 by phosphoramidon [N-(alpha-rhamnopyranosyl-oxyhydroxyphosphinyl)-Leu-Trp], a transition-state analog and competiti …
As part of an effort to understand the structural and functional relationships between ZMPSTE24 and soluble zinc metalloproteases, the inhib …
Structures of soluble rabbit neprilysin complexed with phosphoramidon or thiorphan.
Labiuk SL, Sygusch J, Grochulski P. Labiuk SL, et al. Acta Crystallogr F Struct Biol Commun. 2019 Jun 1;75(Pt 6):405-411. doi: 10.1107/S2053230X19006046. Epub 2019 May 10. Acta Crystallogr F Struct Biol Commun. 2019. PMID: 31204686 Free PMC article.
The structure of the soluble extracellular domain (residues 55-750) of rabbit neprilysin was solved both in its native form at 2.1 A resolution, and bound to the inhibitors phosphoramidon and thiorphan at 2.8 and 3.0 A resolution, respectively. Consistent with the extracel …
The structure of the soluble extracellular domain (residues 55-750) of rabbit neprilysin was solved both in its native form at 2.1 A resolut …
Phosphoramidon inhibition of the in vivo conversion of big endothelin-1 to endothelin-1 in the human forearm.
Plumpton C, Haynes WG, Webb DJ, Davenport AP. Plumpton C, et al. Br J Pharmacol. 1995 Sep;116(2):1821-8. doi: 10.1111/j.1476-5381.1995.tb16669.x. Br J Pharmacol. 1995. PMID: 8528566 Free PMC article.
The levels of IR big ET-1 and CTF were unchanged. Co-infusion of phosphoramidon (30 nmol min-1) with ET-1 had no significant effect on the plasma IR levels of ET, big ET-1, CTF, or blood flow. 3. ...However, IR CTF was still detected, suggesting that either some conversion …
The levels of IR big ET-1 and CTF were unchanged. Co-infusion of phosphoramidon (30 nmol min-1) with ET-1 had no significant effect o …
Phosphoramidon-sensitive endothelin-converting enzyme in vascular endothelial cells converts big endothelin-1 and big endothelin-3 to their mature form.
Matsumura Y, Tsukahara Y, Kuninobu K, Takaoka M, Morimoto S. Matsumura Y, et al. FEBS Lett. 1992 Jun 29;305(2):86-90. doi: 10.1016/0014-5793(92)80870-m. FEBS Lett. 1992. PMID: 1618346 Free article.
Both responses were markedly suppressed by phosphoramidon. By the gel filtration of 0.5% CHAPS-solubilized fraction of membrane pellets of ECs, the molecular mass of the proteinase which converts big ET-1 and big ET-3 to their mature form was estimated to be 300-350 kDa. …
Both responses were markedly suppressed by phosphoramidon. By the gel filtration of 0.5% CHAPS-solubilized fraction of membrane pelle …
Phosphoramidon potentiates the bronchoconstriction induced by inhaled bombesin in guinea pigs.
Lagente V, Boichot E, Mencia-Huerta JM, Braquet P. Lagente V, et al. Life Sci. 1993;53(5):PL75-80. doi: 10.1016/0024-3205(93)90652-j. Life Sci. 1993. PMID: 7687732
The effect of the neutral endopeptidase inhibitor, phosphoramidon, on the bronchoconstriction induced by aerosolized bombesin in the guinea pig was investigated. ...Pretreatment of the guinea-pigs with phosphoramidon (0.1 mM), administered by aerosol for 15 min, 15 …
The effect of the neutral endopeptidase inhibitor, phosphoramidon, on the bronchoconstriction induced by aerosolized bombesin in the …
Phosphoramidon, an endothelin-converting enzyme inhibitor, attenuates lipopolysaccharide-induced acute lung injury.
Bhavsar TM, Cerreta JM, Liu M, Reznik SE, Cantor JO. Bhavsar TM, et al. Exp Lung Res. 2008 Mar;34(3):141-54. doi: 10.1080/01902140701884430. Exp Lung Res. 2008. PMID: 18307123 Free article.
Phosphoramidon blocks the formation of endothelin-1 (ET-1), a proinflammatory mediator implicated in the pathogenesis of a variety of lung diseases. To determine whether phosphoramidon can ameliorate pulmonary inflammation, our laboratory undertook a series of exper …
Phosphoramidon blocks the formation of endothelin-1 (ET-1), a proinflammatory mediator implicated in the pathogenesis of a variety of …
Antagonism of phosphoramidon-induced antinociception in mice by mu- but not kappa-opioid receptor blockers.
Pruhs RJ, Peña RT, Quock RM. Pruhs RJ, et al. Life Sci. 2007 Apr 17;80(19):1816-20. doi: 10.1016/j.lfs.2007.02.019. Epub 2007 Feb 22. Life Sci. 2007. PMID: 17379253
Naltrexone significantly attenuated phosphoramidon-induced antinociception at an i.c.v. dose that also blocked both sufentanil and U-50,488H. ...A low dose (10 microg) of nor-BNI had no effect on either phosphoramidon or sufentanil but did reduce U-50,488H antinocic …
Naltrexone significantly attenuated phosphoramidon-induced antinociception at an i.c.v. dose that also blocked both sufentanil and U- …
Phosphoramidon attenuates big endothelin-1-induced vasoconstriction in canine stomach.
Wood JG, Yan ZY, Davis JM, Cheung LY. Wood JG, et al. Am J Physiol. 1994 Feb;266(2 Pt 1):G311-7. doi: 10.1152/ajpgi.1994.266.2.G311. Am J Physiol. 1994. PMID: 8141304
In other experiments, using 15-min peptide infusions, we found that pretreatment with phosphoramidon, an inhibitor of endothelin-converting enzyme, markedly reduced response to big endothelin-1 but not to endothelin-1. ...In addition, it appears that big endothelin-1 is de …
In other experiments, using 15-min peptide infusions, we found that pretreatment with phosphoramidon, an inhibitor of endothelin-conv …
Phosphoramidon, a metalloproteinase inhibitor, suppresses the secretion of endothelin-1 from cultured endothelial cells by inhibiting a big endothelin-1 converting enzyme.
Ikegawa R, Matsumura Y, Tsukahara Y, Takaoka M, Morimoto S. Ikegawa R, et al. Biochem Biophys Res Commun. 1990 Sep 14;171(2):669-75. doi: 10.1016/0006-291x(90)91198-2. Biochem Biophys Res Commun. 1990. PMID: 2206130
Time-dependent secretion of immunoreactive-endothelin (IR-ET) from cultured porcine aortic endothelial cells was markedly suppressed by phosphoramidon is due to proteinase inhibitor. Analysis of the culture supernatant with or without phosphoramidon by reverse-phase …
Time-dependent secretion of immunoreactive-endothelin (IR-ET) from cultured porcine aortic endothelial cells was markedly suppressed by p …
In vivo characterization of a phosphoramidon-sensitive endothelin-converting enzyme in the rat.
Pollock DM, Divish BJ, Milicic I, Novosad EI, Burres NS, Opgenorth TJ. Pollock DM, et al. Eur J Pharmacol. 1993 Feb 16;231(3):459-64. doi: 10.1016/0014-2999(93)90124-z. Eur J Pharmacol. 1993. PMID: 8449237
The EC50 for phosphoramidon was determined to be in the range of 1 to 3 mg/kg. The pressor response to big ET-1 60 min after phosphoramidon injection was attenuated by roughly 60% indicating a long inhibitory half-life. Very high doses of big ET-1 (> 20 mg/kg) we …
The EC50 for phosphoramidon was determined to be in the range of 1 to 3 mg/kg. The pressor response to big ET-1 60 min after phosp …
1,479 results