Výsledky vyhledávání - "Michael Paul Capparelli"

3,5-Diarylazoles as novel and selective inhibitors of protein kinase D

Autor: Istvan J. Enyedy, Wanlin Yan, Vinayak Hosagrahara, Timothy A. McKinsey, Erik Meredith, Nicolas Soldermann, Keith A. Koch, Nikos Pagratis, Qingming Zhu, Robin Burgis, Olga Rozhitskaya, Michael Paul Capparelli, Richard B. Vega, Ji-Hu Zhang, Chang Rao, Lauren G. Monovich, Kimberley Beattie, Gabriel G. Gamber

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:1447-1451

The synthesis and preliminary studies of the SAR of novel 3,5-diarylazole inhibitors of Protein Kinase D (PKD) are reported. Notably, optimized compounds in this class have been found to be active in cellular assays of phosphorylation-dependant HDAC5

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::415a80ddabae37926dced21c7706873a
https://doi.org/10.1016/j.bmcl.2011.01.014

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Discovery of CGS 27023A, a Non-Peptidic, Potent, and Orally Active Stromelysin Inhibitor That Blocks Cartilage Degradation in Rabbits

Autor: Ronald L. Goldberg, V. Blancuzzi, Michael R. Justice, Lijuan Zhu, Michael Paul Capparelli, Salvatore Spirito, L R Fryer, Brian J Carroll, J. R. Doughty, Erol K. Bayburt, Elizabeth O'Byrne, Robert Goldstein, Vishwas Ganu, Doug Wilson, Macpherson Lawrence J, David Thomas Parker, Richard Melton, Shou-Ih Hu

Publikováno v: Journal of Medicinal Chemistry. 40:2525-2532

Structure-activity relationships of a lead hydroxamic acid inhibitor of recombinant human stromelysin were systematically defined by taking advantage of a concise synthesis that allowed diverse functionality to be explored at each position in a templ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3dc0e55fbdb3e0fba95712bb4532024
https://doi.org/10.1021/jm960871c

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Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors

Autor: Erik Meredith, Michael Paul Capparelli, Gary Michael Ksander, Chang Rao, Robin Burgis, Julien Papillon, Lauren G. Monovich, Dean F. Rigel, Alok K. Singh, Arco Y. Jeng, Chii-Whei Hu, Karl Miranda, Daniel LaSala, Qian Liu, Fumin Fu, Michael E. Beil, Qi-Ying Hu, Patrick J. Morris

Publikováno v: ACS medicinal chemistry letters. 4(12)

Aldosterone is a key signaling component of the renin-angiotensin-aldosterone system and as such has been shown to contribute to cardiovascular pathology such as hypertension and heart failure. Aldosterone synthase (CYP11B2) is responsible for the fi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24dde8962d19a1a500167875ed7ff669
https://pubmed.ncbi.nlm.nih.gov/24900631

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Design and synthesis of an orally active macrocyclic neutral endopeptidase 24.11 inhibitor

Autor: Jane Peppard, Angelo J. Trapani, Frank H Clarke, Macpherson Lawrence J, Erol K. Bayburt, Yumi Sakane, Michael Paul Capparelli, Carol Berry, R. D. Ghai, Regine Bohacek

Publikováno v: Journal of Medicinal Chemistry. 36:3821-3828

A potent macrocyclic inhibitor of neutral endopeptidase (NEP) 24.11 was designed using a computer model of the active site of thermolysin. This 10-membered ring lactam represents a general mimic for any hydrophobic dipeptide in which the two amino ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc0f9db2efac991e69e995a8e5bca888
https://doi.org/10.1021/jm00076a009

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Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design

Publikováno v: Journal of medicinal chemistry. 44(26)

Cathepsin B is a member of the papain superfamily of cysteine proteases and has been implicated in the pathology of numerous diseases, including arthritis and cancer. As part of an effort to identify potent, reversible inhibitors of this protease, we

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66cd9702d74ca2af2d4b39b2c718d403
https://pubmed.ncbi.nlm.nih.gov/11741472

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A novel kinase inhibitor establishes a predominant role for protein kinase D as a cardiac class IIa histone deacetylase kinase

Autor: Keith A. Koch, Timothy A. McKinsey, Dillon Phan, Chang Rao, David B. Hood, Lauren G. Monovich, Joseph A. Chapo, Richard B. Vega, Karl Miranda, Douglas D. Lemon, Erik Meredith, Michael Paul Capparelli

Publikováno v: FEBS Letters. (3):631-637

Class IIa histone deacetylases (HDACs) repress genes involved in pathological cardiac hypertrophy. The anti-hypertrophic action of class IIa HDACs is overcome by signals that promote their phosphorylation-dependent nuclear export. Several kinases hav

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e884ca5573742348b10af16923e7d0e

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