Zobrazeno 1 - 10 of 24 pro vyhledávání: '"Lauren G Monovich"'
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Design of Thioether Cyclic Peptide Scaffolds with Passive Permeability and Oral Exposure
Autor: Christian M. Gampe, Jingzhou Li, Patel Tajesh Jayprakash, Jakal Amin, Charles Babu, Lihua Yang, Eugene Liu, Andrei Golosov, Katsumasa Nakajima, David Nettleton, Patrick C. Reid, Lauren G. Monovich, Flyer Alec
Publikováno v: Journal of Medicinal Chemistry. 64:2622-2633
Advances in the design of permeable peptides and in the synthesis of large arrays of macrocyclic peptides with diverse amino acids have evolved on parallel but independent tracks. Less precedent combines their respective attributes, thereby limiting
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2dd9795db77b2153f204b31c1dd80d9
https://doi.org/10.1021/acs.jmedchem.0c01505
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5
Evolution of Novartis' Small Molecule Screening Deck Design
Autor: John Joslin, Jerome Giovannoni, John I. Manchester, Eugen Lounkine, Douglas S. Auld, Nikolas Fechner, Philipp Krastel, Caroline Engeloch, Jutta Blank, Manuel Schwarze, Ansgar Schuffenhauer, Nikolaus Stiefl, Johanna M. Jansen, Nadine Schneider, Lauren G. Monovich, Simona Cotesta, Michael Shultz, Samuel Hintermann, Daniel K. Baeschlin, Christoph Gaul, Anna Paola Pelliccioli
Publikováno v: Journal of medicinal chemistry. 63(23)
This article summarizes the evolution of the screening deck at the Novartis Institutes for BioMedical Research (NIBR). Historically, the screening deck was an assembly of all available compounds. In 2015, we designed a first deck to facilitate access
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fe7d489f3ff53766acb91c3cacff935
https://pubmed.ncbi.nlm.nih.gov/33140646
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8
Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models
Autor: Dean F. Rigel, Hidetomo Imase, Kayo Yasoshima, Darcy Kohls, Toshio Kawanami, Yukiko I. Yagi, Jun Yuan, Monish Jain, Hyi-Man Park, Upendra A. Argikar, David Yowe, Paul Taslimi, Xiaoling Xie, Yuki Iwaki, Neeraja Idamakanti, Taeyong Yoon, Ken Yamada, Vidya Kunjathoor, Keith DiPetrillo, Lingfei Xu, Mitsunori Kato, Meicheng Zhu, Julian Levell, Zachary Robinson, Lauren G. Monovich
Publikováno v: Journal of Medicinal Chemistry. 60:7099-7107
The observed structure-activity relationship of three distinct ATP noncompetitive With-No-Lysine (WNK) kinase inhibitor series, together with a crystal structure of a previously disclosed allosteric inhibitor bound to WNK1, led to an overlay hypothes
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3d52943277800bc7194904670e9e1d7
https://doi.org/10.1021/acs.jmedchem.7b00708
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9
2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes
Autor: Anette Von Matt, Wilhelm Stark, Christoph Gaul, Juergen Wagner, Eric Vangrevelinghe, Lauren G. Monovich, Gabriele Rummel, Nicolas Soldermann, Walter Schuler, André Strauss, Sandra W. Cowan-Jacob, Maurice Van Eis, Jean-Pierre Evenou, Philipp Floersheim
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:7367-7372
The present study describes a novel series of ATP-competitive PKC inhibitors based on the 2,6-naphthyridine template. Example compounds potently inhibit the novel Protein Kinase C (PKC) isotypes δ, ε, η, θ (in particular PKCε/η, and display a 1
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a049780df31bdb8fa0ca7b096755c8fe
https://doi.org/10.1016/j.bmcl.2011.10.025
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10
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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