C
Charles W. Bruseo
Researcher at Novartis
Publications - 13
Citations - 800
Charles W. Bruseo is an academic researcher from Novartis. The author has contributed to research in topics: Endothelin converting enzyme 1 & Atrial natriuretic peptide. The author has an hindex of 9, co-authored 13 publications receiving 773 citations.
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Journal ArticleDOI
Small-molecule antagonists of the oncogenic Tcf/β-catenin protein complex
Maina Lepourcelet,Ying-Nan P. Chen,Huisheng Wang,Phillip Crews,Frank Petersen,Charles W. Bruseo,Alexander W. Wood,Ramesh A. Shivdasani,Ramesh A. Shivdasani +8 more
TL;DR: These compounds meet predicted criteria for disrupting Tcf/beta-catenin complexes and define a general standard to establish mechanism-based activity of small molecule inhibitors of this pathogenic protein-protein interaction.
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Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500.
Joseph L. Balwierczak,Charles W. Bruseo,D. Delgrande,Arco Y. Jeng,Paula Savage,Suraj S. Shetty +5 more
TL;DR: IRL 2500 is a potent and selective ETB receptor antagonist that can be used to delineate ET responses mediated by the ETB receptors.
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CGS 35601 and its orally active prodrug CGS 37808 as triple inhibitors of endothelin-converting enzyme-1, neutral endopeptidase 24.11, and angiotensin-converting enzyme.
Angelo J. Trapani,Michael E. Beil,Charles W. Bruseo,Paula Savage,Fariborz Firooznia,Arco Y. Jeng +5 more
TL;DR: By suppressing the biosyntheses of endothelin-1 and angiotensin II, two potent vasoconstrictors, while simultaneously potentiating the circulating levels of ANP, a vasorelaxant and diuretic, CGS 35601 and CGS 37808 may represent novel agents for the treatment of cardiovascular and renal diseases.
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CGS 34226, a thiol-based dual inhibitor of endothelin converting enzyme-1 and neutral endopeptidase 24.11.
Y. Arco Jeng,Paula Savage,Michael E. Beil,Charles W. Bruseo,Hoyer Denton W,Cynthia A. Fink,Angelo J. Trapani +6 more
TL;DR: Results show that CGS 34226 is a potent dual inhibitor of ECE-1 and NEP in vitro and in vivo and that the compound may represent a novel agent for the treatment of cardiovascular and renal dysfunction.
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Pharmacological properties of CGS 35066, a potent and selective endothelin-converting enzyme inhibitor, in conscious rats.
TL;DR: It is demonstrated that CGS 35066 is the most potent and selective ECE inhibitor identified to date.