Výsledky vyhledávání - "Nicholas John Silvester Huby"

Characterization of a Novel Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor with a Unique Mechanism of Action for Cancer Therapy

Autor: Yang Wen, Yang He, Nader Fotouhi, Sherif Daouti, Packman Kathryn E, Norman Kong, Wen-hui Li, Kenneth Kolinsky, David C. Heimbrook, Anthony Specian, Frank John Podlaski, Qing Xiang, Nicholas John Silvester Huby, Huisheng Wang, Brian Higgins, Huifeng Niu

Publikováno v: Cancer Research. 69:1924-1932

The mitogen-activated protein kinase (MAPK) signal transduction pathway plays a central role in regulating tumor cell growth, survival, differentiation, and angiogenesis. The key components of the Ras/Raf/MEK/ERK signal module are frequently altered

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88d97f0577a8efa56ee33c335664b715
https://doi.org/10.1158/0008-5472.can-08-2627

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N-Cycloalkanoyl-l-Phenylalanine Derivatives as VCAM/VLA-4 Antagonists

Autor: Louis M. Renzetti, Li Chen, Karen Rowan, Allen Sheffron, Tai-Nan Huang, Jian Ping Lou, Jefferson Wright Tilley, Kenneth G. Hull, Virginia Schwinge, Gerry Kaplan, Achyutharao Sidduri, Robert M. Campbell, Robert William Guthrie, Nicholas John Silvester Huby

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:2475-2478

A systematic structure-activity relationship investigation of the lead compound 1 resulted the identification of several N-[(substituted alkyl)cycloalkanoyl]-4-[((2,6-dichlorophenyl)carbonyl)amino]-L-phenylalanine derivatives as potent VCAM/VLA-4 ant

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53da7a5e27aecfcea2db394b82b8d572
https://doi.org/10.1016/s0960-894x(02)00386-4

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Peptidomimetic compounds that inhibit antigen presentation by autoimmune disease-associated class II major histocompatibility molecules

Autor: Gary L. Olson, Damir Vidovic, Ramakanth Sarabu, J. Hammer, Francesco Sinigaglia, Zoltan A. Nagy, Michael Steinmetz, Nicholas John Silvester Huby, Jeanmarie Guenot, Charles Belunis, Kouichi Ito, Robert K. Campbell, Paul Gillespie, David Robert Bolin, Steven Joseph Berthel, Vincent S. Madison, Fiorenza Falcioni

Publikováno v: Nature Biotechnology. 17:562-567

We have identified a heptapeptide with high affinity to rheumatoid arthritis-associated class II major histocompatibility (MHC) molecules. Using a model of its interaction with the class II binding site, a variety of mimetic substitutions were introd

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70409305cc5fff290c510e7758273981
https://doi.org/10.1038/9865

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Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models

Autor: Huifeng Niu, Brian Higgins, Kenneth Kolinsky, Huisheng Wang, Jia Kui Li, Sherif Daouti, Harpreet K. Sandhu, Petra Goelzer, David C. Heimbrook, Mei Liu, Packman Kathryn E, Aruna Railkar, Nader Fotouhi, John Anthony Moliterni, Nicholas John Silvester Huby, Christine Rizzo

Publikováno v: Molecular cancer therapeutics. 9(1)

Targeting the Ras/Raf/mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK) pathway represents a promising anticancer strategy. Recently, we have reported a novel class of potent and selective non–ATP-competitive

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a10022a43f230d2596f5b4e8f29b8ef
https://pubmed.ncbi.nlm.nih.gov/20053779

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C-8 Modifications of 3-alkyl-1,8-dibenzylxanthines as inhibitors of human cytosolic phosphoenolpyruvate carboxykinase

Autor: Sherrie L. Pietranico, Ping Wang, Nicholas John Silvester Huby, Mary-Lou Gubler, Louise H. Foley, Weiya Yun, John Vermeulen, Stanley Wertheimer, Gwendolyn Ramsey, Pete William Dunten, Katherine Toth

Publikováno v: Bioorganicmedicinal chemistry letters. 17(14)

New modifications on the C-8 4-aminobenzyl unit of the previously reported 3-alkyl-1,8-dibenzylxanthine inhibitors of cPEPCK are presented. The most active compound reported here is the 5-chloro-1,3-dimethyl-1H-pyrazole-4-sulfonic acid amide derivati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f839692387a725882496d7a69df64713
https://pubmed.ncbi.nlm.nih.gov/17532214

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Peptide and peptide mimetic inhibitors of antigen presentation by HLA-DR class II MHC molecules. Design, structure-activity relationships, and X-ray crystal structures

Publikováno v: Journal of medicinal chemistry. 43(11)

Molecular features of ligand binding to MHC class II HLA-DR molecules have been elucidated through a combination of peptide structure-activity studies and structure-based drug design, resulting in analogues with nanomolar affinity in binding assays.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62a02373e6636582778d59d10e031420
https://pubmed.ncbi.nlm.nih.gov/10841792

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Abstract A247: Preclinical antitumor activity of the MEK inhibitor RO5068760 in human tumor xenograft models

Autor: Sherif Daouti, Higgins Brian, Christine Rizzo, Huisheng Wang, Packman Kathryn E, Nicholas John Silvester Huby, Huifeng Niu, Kenneth Kolinsky

Publikováno v: Molecular Cancer Therapeutics. 8:A247-A247

RO5068760 is a representative member of a new class of potent, highly selective, non-adenosine triphosphate (ATP) competitive MEK inhibitors. In tumor cells, RO5068760 selectively blocked MAPK pathway signaling by inhibiting the phosphorylation of bo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::10396dd8cb444c69daf82b4204ca5103
https://doi.org/10.1158/1535-7163.targ-09-a247

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