scholarly journals Pharmacological Characterization of a Novel Sulfonylureid-Pyrazole Derivative, SM-19712, a Potent Nonpeptidic Inhibitor of Endothelin Converting Enzyme

2000 ◽  
Vol 84 (1) ◽  
pp. 7-15 ◽  
Author(s):  
Kayo Umekawa ◽  
Hirohiko Hasegawa ◽  
Yasushi Tsutsumi ◽  
Kimihiko Sato ◽  
Yasuo Matsumura ◽  
...  
Keyword(s):  
Converting Enzyme ◽  
Pyrazole Derivative ◽  
Pharmacological Characterization ◽  
Endothelin Converting Enzyme

Characterization of PgPepO, a bacterial homologue of endothelin-converting enzyme-1

2002 ◽  
Vol 103 (s2002) ◽  
pp. 90S-93S ◽  
Author(s):  
Julie A. CARSON ◽  
Toshihiro ANSAI ◽  
Shuji AWANO ◽  
Weixian YU ◽  
Tadamichi TAKEHARA ◽  
...  
Keyword(s):  
Viral Infections ◽  
Structural Information ◽  
Specific Inhibitor ◽  
Periodontal Pathogen ◽  
Striking Similarity ◽  
Converting Enzyme ◽  
Urotensin Ii ◽  
Periodontal Pathogens ◽  
Endothelin Converting Enzyme

PgPepO is a homologue of endothelin-converting enzyme-1 (ECE-1), with which it shares 31% identity. PgPepO was isolated from the periodontal pathogen Porphyromonas gingivalis. Recent studies have suggested a link between periodontal and cardiovascular disease, and several groups have suggested that bacterial and viral infections may contribute to the latter. P. gingivalis possesses the ability to invade, and multiply within, aortic endothelial cells and has been localized to atherosclerotic plaques. PgPepO was expressed and purified to homogeneity and we have begun detailed functional analysis, in terms of substrate preference and inhibitor specificity, in order to provide active-site comparisons with other members of the neprilysin (NEP)/ECE family. PgPepO possesses similar substrate specificity to ECE-1 and has been shown to cleave big endothelin-1 (big ET-1), big ET-2 and big ET-3, converting the substrates into their respective mature endothelin peptides. Substance P, angiotensin I, angiotensin II and neurotensin are all cleaved at multiple sites by PgPepO and the kinetics of these reactions have been compared. The potent vasoconstrictor urotensin II is not hydrolysed by PgPepO. Cleavage of bradykinin by PgPepO occurs at the Pro7-Phe8 bond and is inhibited by the NEP and ECE-1 inhibitor phosphoramidon in a pH-dependent fashion (IC50 = 10µM at pH 7.0) but not by thiorphan, an NEP-specific inhibitor. PgPepO activity is completely inhibited by EDTA. Characterization of this enzyme is important in elucidating possible links between periodontal pathogens and cardiovascular disorders such as atherosclerosis, and provides an opportunity to gain structural information on a bacterial protein with striking similarity to human ECE-1.

Characterization of CGS 31447, a Potent and Nonpeptidic Endothelin-Converting Enzyme Inhibitor

1998 ◽  
Vol 31 ◽  
pp. S68-S70 ◽  
Author(s):  
Suraj S. Shetty ◽  
Paula Savage ◽  
Dominick DelGrande ◽  
Stéphane De Lombaert ◽  
Arco Y. Jeng
Keyword(s):  
Enzyme Inhibitor ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitor ◽  
Endothelin Converting Enzyme

Cloning and functional characterization of the bovine endothelin-converting enzyme-1a promoter

1999 ◽  
Vol 1446 (3) ◽  
pp. 352-358 ◽  
Author(s):  
Hans-Dieter Orzechowski ◽  
Claus-Michael Richter ◽  
Heiko Funke-Kaiser ◽  
Julia Lemmer ◽  
Steffen Theis ◽  
...  
Keyword(s):  
Functional Characterization ◽  
Converting Enzyme ◽  
Endothelin Converting Enzyme

Human endothelin converting enzyme-2 (ECE2): characterization of mRNA species and chromosomal localization

2001 ◽  
Vol 1522 (1) ◽  
pp. 46-52 ◽  
Author(s):  
Maria-Nieves Lorenzo ◽  
Rajal Y. Khan ◽  
Yang Wang ◽  
Sharon C. Tai ◽  
Gary C. Chan ◽  
...  
Keyword(s):  
Chromosomal Localization ◽  
Converting Enzyme ◽  
Mrna Species ◽  
Endothelin Converting Enzyme

New Short Peptide Substrates of Endothelin-Converting Enzyme and Characterization of the Enzyme

2000 ◽  
Vol 36 (Supplement 1) ◽  
pp. S28-S29 ◽  
Author(s):  
Myriam Létourneau ◽  
Philippe Roby ◽  
Fanny Tremblay ◽  
Julie Carette ◽  
Alain Fournier
Keyword(s):  
Converting Enzyme ◽  
Peptide Substrates ◽  
Short Peptide ◽  
Endothelin Converting Enzyme

Localization and Biochemical Characterization of Endothelin-Converting Enzyme

1995 ◽  
Vol 26 ◽  
pp. S37-39
Author(s):  
K. Barnes ◽  
L. J. Murphy ◽  
M. Takahashi ◽  
K. Tanzawa ◽  
A. J. Turner
Keyword(s):  
Biochemical Characterization ◽  
Converting Enzyme ◽  
Endothelin Converting Enzyme

Characterization of the Endothelin-Converting Enzyme in Guinea Pig Upper Bronchus

1995 ◽  
Vol 26 ◽  
pp. S81-83
Author(s):  
Nathalie Lebel ◽  
Pédro DʼOrleans-Juste ◽  
Alain Fournier ◽  
Pierre Sirois
Keyword(s):  
Guinea Pig ◽  
Converting Enzyme ◽  
Endothelin Converting Enzyme

Localization and Biochemical Characterization of Endothelin-Converting Enzyme

1995 ◽  
Vol 26 ◽  
pp. S37-39 ◽  
Author(s):  
K. Barnes ◽  
L. J. Murphy ◽  
M. Takahashi ◽  
K. Tanzawa ◽  
A. J. Turner
Keyword(s):  
Biochemical Characterization ◽  
Converting Enzyme ◽  
Endothelin Converting Enzyme
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