Výsledky vyhledávání - "Josie H. Lee"

Akademický článek

Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V.

Autor: Bryan D Moyer, Justin K Murray, Joseph Ligutti, Kristin Andrews, Philippe Favreau, John B Jordan, Josie H Lee, Dong Liu, Jason Long, Kelvin Sham, Licheng Shi, Reto Stöcklin, Bin Wu, Ruoyuan Yin, Violeta Yu, Anruo Zou, Kaustav Biswas, Les P Miranda

Publikováno v: PLoS ONE, Vol 13, Iss 5, p e0196791 (2018)

Identification of voltage-gated sodium channel NaV1.7 inhibitors for chronic pain therapeutic development is an area of vigorous pursuit. In an effort to identify more potent leads compared to our previously reported GpTx-1 peptide series, electrophy

Externí odkaz: https://doaj.org/article/05d6c798f5064771a7180e9f1fa3d097

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Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 362:146-160

Potent and selective antagonists of the voltage-gated sodium channel NaV1.7 represent a promising avenue for the development of new chronic pain therapies. We generated a small molecule atropisomer quinolone sulfonamide antagonist AMG8379 and a less

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d863f2d2c28cbf4708d06dfd96734ade
https://doi.org/10.1124/jpet.116.239590

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Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V

Autor: John B. Jordan, Justin K. Murray, Kristin L. Andrews, Licheng Shi, Philippe Favreau, Ruoyuan Yin, Violeta Yu, Josie H. Lee, Kelvin K. C. Sham, Bin Wu, Kaustav Biswas, Dong Liu, Anruo Zou, Joseph Ligutti, Jason Long, Les P. Miranda, Bryan D. Moyer, Reto Stöcklin

Publikováno v: PLoS ONE, Vol 13, Iss 5, p e0196791 (2018)
PLoS ONE

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59eb0148307a9c0a0a9fe2b23d52da70
http://europepmc.org/articles/PMC5933747?pdf=render

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Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity

Autor: Beth D. Youngblood, Alessandro Boezio, Stephanie D. Geuns-Meyer, Maosheng Zhang, Angel Guzman-Perez, Laurie B. Schenkel, Yohannes Teffera, Weiya Wang, Philip R. Olivieri, Renee Emkey, Hakan Gunaydin, Josie H. Lee, Holly L. Deak, Violeta Yu, Russell Graceffa, Sonya G. Lehto, Narender R. Gavva

Publikováno v: Journal of medicinal chemistry. 59(6)

There has been significant interest in developing a transient receptor potential A1 (TRPA1) antagonist for the treatment of pain due to a wealth of data implicating its role in pain pathways. Despite this, identification of a potent small molecule to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d84f5df9ce36a611f66ca351b52ba08
https://pubmed.ncbi.nlm.nih.gov/26942860

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Discovery of α-amidosulfones as potent and selective agonists of CB2: Synthesis, SAR, and pharmacokinetic properties

Autor: Ryan White, Erin F. DiMauro, Stephen Hitchcock, Robert T. Fremeau, Ming Y. Huang, Isaac E. Marx, Jason Brooks Human, Liyue Huang, Josie H. Lee, Alan C. Cheng, Vinod F. Patel, Xingwen Li, Matthew W. Martin, Renee Emkey

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:31-35

A series of α-amidosulfones were found to be potent and selective agonists of CB2. The discovery, synthesis, and structure–activity relationships of this series of agonists are reported. In addition, the pharmacokinetic properties of the most prom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e0daa5a47b3ce311b575c1293b5ea28
https://doi.org/10.1016/j.bmcl.2008.11.026

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Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: Synthesis, SAR, and pharmacokinetic properties

Autor: Ryan White, David C. Mcgowan, Xiaotian Zhu, Matthew W. Martin, John Newcomb, John L. Buchanan, Theodore Faust, Faye Hsieh, Xin Huang, Erin F. DiMauro, Susan M. Turci, Christina Boucher, Stephen Schneider, Joseph J. Nunes, Jean Bemis, Josie H. Lee

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:2299-2304

2,3-Diarylfuro[2,3-b]pyridine-4-amines are a novel class of potent and selective inhibitors of Lck. The discovery, synthesis, and structure activity relationships of this series of inhibitors are reported. The most promising compounds were also profi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4cec8aa93efe43539a086c398621a2de
https://doi.org/10.1016/j.bmcl.2007.01.048

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N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR

Autor: Alan C. Cheng, Stephen Schneider, Joseph J. Nunes, Xiaotian Zhu, Paul Gallant, Erin F. DiMauro, Xin Huang, Vinod F. Patel, John Newcomb, Brian L. Hodous, Holly L. Deak, Christina Boucher, Susan M. Turci, Josie H. Lee, Linda F. Epstein

Publikováno v: Bioorganicmedicinal chemistry letters. 18(3)

N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of selective Lck inhibitors. This series of compounds derives its selectivity from a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal structural data, struct

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a79e72e4e6984650f09152ff1fcc2fe7
https://pubmed.ncbi.nlm.nih.gov/18083554

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Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR

Autor: Alan C. Cheng, Ryan White, Stephen Schneider, Joseph J. Nunes, John L. Buchanan, Jean Bemis, Faye Hsieh, William H. Buckner, Susan M. Turci, Matthew W. Martin, Christina Boucher, John Newcomb, Xin Huang, Xiaotian Zhu, Josie H. Lee, Theodore Faust, Erin F. DiMauro, David C. Mcgowan, Teresa L. Marshall

Publikováno v: Bioorganicmedicinal chemistry letters. 17(8)

4-Amino-5,6-biaryl-furo[2,3-d]pyrimidines were identified as potent non-selective inhibitors of Lck. A novel, divergent, and practical synthetic route was developed to access derivatives from bifunctional intermediates. Lead optimization was guided b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8596032c12f0ec265ab314e83b4a1d9
https://pubmed.ncbi.nlm.nih.gov/17280833

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