Kinetic characterization and inhibition of the rat MAB elastase-2, an angiotensin I-converting serine protease (2002)
- Authors:
- Autor USP: SANTOS, CARLOS FERREIRA DOS - FOB
- Unidade: FOB
- DOI: 10.1139/y02-004
- Subjects: ANGIOTENSINAS; RATOS
- Language: Inglês
- Abstract: An elastase-2 has been recently described as the major angiotensin (Ang) II-forming enzyme of the rat mesenteric arterial bed (MAB) perfusate. Here, we have investigated the interaction of affinity-purified rat MAB elastase-2 with some substrates and inhibitors of both pancreatic elastases-2 and Ang II-forming chymases. The Ang II precursor ['Pro POT. 11'-D-'Ala PROT. 12]-Ang I was converted into Ang II by the rat MAB elastase-2 with a catalytic efficiency of 8.6 'min POT. -1'x 'mü' 'M POT. -1', and the chromogenic substrates N-succinyl-Ala-Ala-Pro-Leu-p-nitroanilide and N-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide were hydrolyzed by the enzyme with catalytic efficiencies of 10.6 'min POT. -1'x 'MÜ' 'M POT. -1' and 7.6 'min POT -1'x 'mü' 'M POT. -1', respectively. The non-cleavable peptide inhibitor CH-5450 inhibited the rat MAB elastase-2 activities toward the substrates Ang I ('IC INT. 50' = 49 'mü' M) and N-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide ('IC INT. 50 = 4.8 'mü' M), whereas N-acetyl-Ala-Ala-Pro-Leu-chloromethylketone, an effective active site-directed inhibitor of pancreatic elastase-2, efficiently blocked the Ang II-generating activity of the rat MAB enzyme ('IC INT. 50 = 4.5 'mü' M). Altogether, the data presented here confirm and extend the enzymological similarities between pancreatic elastase-2 and its rat MAB counterpart. Moreover, the thus far unrealized interaction of elastase-2 with ['Pro POT. 11'-D-'Ala POT. 12']-Ang I and CH-5450, bothregarded as selective for chymases, suggests that evidence for the in vivo formation of Ang II by chymases may have been overestimated in previous investigations of Ang II-forming pathways
- Imprenta:
- Source:
- Título: Canadian Journal of Physiology and Pharmacology
- ISSN: 0008-4166
- Volume/Número/Paginação/Ano: v. 80, n. 3, p. 42-47, Jan. 2002
- Este periódico é de assinatura
- Este artigo NÃO é de acesso aberto
- Cor do Acesso Aberto: closed
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ABNT
SANTOS, Carlos Ferreira dos et al. Kinetic characterization and inhibition of the rat MAB elastase-2, an angiotensin I-converting serine protease. Canadian Journal of Physiology and Pharmacology, v. 80, n. Ja 2002, p. 42-47, 2002Tradução . . Disponível em: https://doi.org/10.1139/y02-004. Acesso em: 19 out. 2024. -
APA
Santos, C. F. dos, Paula, C. A., Salgado, M. C. O., & Oliveira, E. B. (2002). Kinetic characterization and inhibition of the rat MAB elastase-2, an angiotensin I-converting serine protease. Canadian Journal of Physiology and Pharmacology, 80( Ja 2002), 42-47. doi:10.1139/y02-004 -
NLM
Santos CF dos, Paula CA, Salgado MCO, Oliveira EB. Kinetic characterization and inhibition of the rat MAB elastase-2, an angiotensin I-converting serine protease [Internet]. Canadian Journal of Physiology and Pharmacology. 2002 ; 80( Ja 2002): 42-47.[citado 2024 out. 19 ] Available from: https://doi.org/10.1139/y02-004 -
Vancouver
Santos CF dos, Paula CA, Salgado MCO, Oliveira EB. Kinetic characterization and inhibition of the rat MAB elastase-2, an angiotensin I-converting serine protease [Internet]. Canadian Journal of Physiology and Pharmacology. 2002 ; 80( Ja 2002): 42-47.[citado 2024 out. 19 ] Available from: https://doi.org/10.1139/y02-004 - Em meio à pandemia do coronavírus, a FOB-USP completa 58 anos hoje
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Informações sobre o DOI: 10.1139/y02-004 (Fonte: oaDOI API)
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