Výsledky vyhledávání - "Vincent, Madison"

Potent ketoamide inhibitors of HCV NS3 protease derived from quaternized P1 groups

Autor: Srikanth Venkatraman, Wanli Wu, Melissa Blackman, F. George Njoroge, Vincent Madison, Francisco Velazquez

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:2151-2155

Blood borne hepatitis C infections are the primary cause for liver cirrhosis and hepatocellular carcinoma. HCV NS3 protease, a pivotal enzyme in the replication cycle of HCV virus has been the primary target for development of new drug candidates. Bo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9b3fa4a6e2dc78b50e86aca9729c684
https://doi.org/10.1016/j.bmcl.2010.02.051

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Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors

Autor: Brian M. Beyer, Vincent Madison, Eric M. Parker, Mckittrick Brian A, Daniel F. Wyss, William J. Greenlee, Corey Strickland, T. Nechuta, Johannes H. Voigt, John C. Hunter, Mary M. Senior, Andrew Stamford, Matthew E. Kennedy, Michael Czarniecki, Yu-Sen Wang, Elizabeth M. Smith

Publikováno v: Journal of Medicinal Chemistry. 53:942-950

Fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design were used to identify novel inhibitors for BACE-1. A rapid optimization of an initial NMR hit was achieved by a combination of NMR and a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b051b98c57bda77146034e6e18e44c2d
https://doi.org/10.1021/jm901472u

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Crystal Structures of the Pro-Inflammatory Cytokine Interleukin-23 and Its Complex with a High-Affinity Neutralizing Antibody

Autor: Paul Reichert, Peter Orth, Lata Ramanathan, Hung V. Le, Brian M. Beyer, Vincent Madison, Richard N. Ingram

Publikováno v: Journal of Molecular Biology. 382:942-955

Interleukin (IL)-23 is a pro-inflammatory cytokine playing a key role in the pathogenesis of several autoimmune and inflammatory diseases. We have determined the crystal structures of the heterodimeric p19-p40 IL-23 and its complex with the Fab (anti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d168eb462dd6282229a187738c113151
https://doi.org/10.1016/j.jmb.2008.08.001

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Key steps in the structure-based optimization of the hepatitis C virus NS3/4A protease inhibitor SCH503034

Publikováno v: Journal of Synchrotron Radiation

Crystal structures of protease/inhibitor complexes guided optimization of the buried nonpolar surface area thereby maximizing hydrophobic binding. The resulting potent tripeptide inhibitor is in clinical trials.
The structures of both native and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a19c454d4a047e4eb08a7af266267ad8
http://europepmc.org/articles/PMC2394794

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Discovery of Novel Hydroxamates as Highly Potent Tumor Necrosis Factor-α Converting Enzyme Inhibitors: Part I—Discovery of Two Binding Modes

Autor: Mckittrick Brian A, Richard N. Ingram, Daniel Lundell, Peter Orth, Robert Mazzola, Zhuyan Guo, Xiaoda Niu, Jing Sun, Brian M. Beyer, Vincent Madison, Zhaoning Zhu, Lisa Sinning

Publikováno v: Journal of Medicinal Chemistry. 51:725-736

Through a de novo design approach, hydroxamates derived from trans-cyclopropyl dicarboxylate were examined as potential TNF-alpha converting enzyme (TACE) inhibitors. Two distinctive series of inhibitors (A and B) were identified and shown to have di

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b143cfa67d6971f9a05fe4c6f72e502b
https://doi.org/10.1021/jm070376o

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Structure-guided discovery of cyclin-dependent kinase inhibitors

Autor: David A. Parry, Jose S. Duca, Lata Ramanathan, Alan Hruza, Kamil Paruch, Doll Ronald J, William T. Windsor, Thierry O. Fischmann, Todd Mayhood, Hung V. Le, Wolfgang Seghezzi, Michael P. Dwyer, Vincent Madison, Emma Lees, Timothy J. Guzi

Publikováno v: Biopolymers. 89:372-379

CDK2 inhibitors containing the related bicyclic heterocycles pyrazolopyrimidines and imidazopyrazines were discovered through high-throughput screening. Crystal structures of inhibitors with these bicyclic cores and two more related ones show that al

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db32c7cc5796119bf21e7d5c515893e0
https://doi.org/10.1002/bip.20868

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Discovery of the HCV NS3/4A Protease Inhibitor (1R,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key Steps in Structure-Based Optimization

Publikováno v: Journal of Medicinal Chemistry. 50:2310-2318

The structures of both the native holo-HCV NS3/4A protease domain and the protease domain with a serine 139 to alanine (S139A) mutation were solved to high resolution. Subsequently, structures were...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::12ac27152dd419adc5be903b98a4f491
https://doi.org/10.1021/jm060173k

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Discovery of (1R,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a Selective, Potent, Orally Bioavailable Hepatitis C Virus NS3 Protease Inhibitor: A Potential Therapeutic Agent for the Treatment of Hepatitis C Infection

Autor: Weidong Pan, Prudence Bradley, Kevin X. Chen, Parekh Tejal N, Andrea Hart, Frank Bennett, Danial Prelusky, Srikanth Venkatraman, Robert Chase, Susan Bogdanowich-Knipp, Jianshe Kong, Bancha Vibulbhan, Viyyoor M. Girijavallabhan, Hendrata Siska, Rong Kong, Weiying Yang, Kuo-Chi Cheng, Ashit K. Ganguly, Nancy Butkiewicz, Ashok Arasappan, Yuhua Huang, Andrew Prongay, Bruce A. Malcolm, Xiang Liang, Rong Liu, Xiaoming Cui, Walter A. Korfmacher, Sony Agrawal, Wanli Wu, Zhuyan Guo, Stephane L. Bogen, Pike Russell E, Ronald E. White, Jesse Wong, Yi-Tsung Liu, Jean-Marc Brisson, John Pichardo, Anil K. Saksena, Pavlovsky Anastasia, Bahige M. Baroudy, F. George Njoroge, Vincent Madison, Patrick Pinto, Santhanam Bama, Raymond G. Lovey, Edwin Jao, Lisa Broske, Veljko Popov, Yunsheng Hsieh, Paul Ingravallo, Sumei Ruan, Piwinski John J

Publikováno v: Journal of Medicinal Chemistry. 49:6074-6086

Hepatitis C virus (HCV) infection is the major cause of chronic liver disease, leading to cirrhosis and hepatocellular carcinoma, which affects more than 170 million people worldwide. Currently the only therapeutic regimens are subcutaneous interfero

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8b1025f20fc929de7fcc2e4ce1f01669
https://doi.org/10.1021/jm060325b

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P2–P4 Macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease

Autor: Ashok Arasappan, Andrew Prongay, F. George Njoroge, Vincent Madison, Parekh Tejal N, Viyyoor M. Girijavallabhan, Nancy Butkiewicz, Kevin X. Chen, Srikanth Venkatraman, Haining Gu, John Pichardo

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:3960-3965

Synthesis and HCV NS3 serine protease inhibitory activity of 4-hydroxyproline derived macrocyclic inhibitors and SAR around this macrocyclic core is described in this communication. X-ray structure of inhibitor 38 bound to the protease is discussed.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::182ea8c68029bd73c06fcf909bd17b83
https://doi.org/10.1016/j.bmcl.2006.05.022

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Proline-Based Macrocyclic Inhibitors of the Hepatitis C Virus: Stereoselective Synthesis and Biological Activity

Autor: Kevin X. Chen, John Pichardo, Tze-Ming Chan, Vincent Madison, Andrew Prongay, F. George Njoroge, Bancha Vibulbhan, Alexei V. Buevich

Publikováno v: Angewandte Chemie International Edition. 44:7024-7028

Macrocyclization through a Mitsunobu reaction was used to synthesize a 17-membered macrocycle. The bicyclic acetal core was prepared completely diastereoselectively. The macrocyclic peptidomimetic surrogate of the P2-P3 dipeptide moiety was designed

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aac387567588076a2b9d7c0882d79da4
https://doi.org/10.1002/anie.200501553

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