Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Jeffrey K Kerns"'
Autor:
Anne Cleasby, Jeff Yon, Philip J Day, Caroline Richardson, Ian J Tickle, Pamela A Williams, James F Callahan, Robin Carr, Nestor Concha, Jeffrey K Kerns, Hongwei Qi, Thomas Sweitzer, Paris Ward, Thomas G Davies
Publikováno v:
PLoS ONE, Vol 9, Iss 6, p e98896 (2014)
The protein Keap1 is central to the regulation of the Nrf2-mediated cytoprotective response, and is increasingly recognized as an important target for therapeutic intervention in a range of diseases involving excessive oxidative stress and inflammati
Externí odkaz:
https://doaj.org/article/e0c4767540824921bd96b680725f39ab
Autor:
Caroline Richardson, Zining Wu, Henriëtte M. G. Willems, William E. Wixted, Alison Jo-Anne Woolford, Charlotte Mary Griffiths-Jones, Yolanda Sanchez, David Norton, Jeffrey K. Kerns, T.G. Davies, William G. Bonnette, Sharna J. Rich, James F. Callahan, Hong Nie, Lawrence Wolfe, Maria Grazia Carr, Marcel L. Verdonk, William L. Rumsey, Tom D. Heightman
Publikováno v:
Journal of Medicinal Chemistry. 64:15949-15972
The NRF2-mediated cytoprotective response is central to cellular homoeostasis, and there is increasing interest in developing small-molecule activators of this pathway as therapeutics for diseases involving chronic oxidative stress. The protein KEAP1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba196f8cf42319174247f8aba6d5c760
https://doi.org/10.1021/acs.jmedchem.1c01351
https://doi.org/10.1021/acs.jmedchem.1c01351
Autor:
Shuping Dong, Yolanda Sanchez, Tindy Li, Claudia E. Murar, Anthony J. Wilson, Brent W. Mccleland, Hongwei Qi, Patricia L. Podolin, Marc Galop, Christopher J. Moody, Hongxing Yan, John Yonchuk, Roderick S. Davis, Alan P. Graves, Catherine Booth-Genthe, Joseph P. Foley, Jen-Pyng Kou, Jeffrey K. Kerns, Brian Bolognese, James F. Callahan, Mary Mentzer, Lawrence Wolfe, Jeffrey C. Boehm, Robin Carr
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:579-588
The antioxidant natural product sulforaphane (SFN) is an oil with poor aqueous and thermal stability. Recent work with SFN has sought to optimize methods of formulation for oral and topical administration. Herein we report the design of new analogs o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b415f7b6666ea7f677038e87013d3b1
https://doi.org/10.1016/j.bmc.2018.12.026
https://doi.org/10.1016/j.bmc.2018.12.026
Autor:
Xichen Lin, Michael E. Muratore, Huijie Li, Ami S. Lakdawala, Jakob Busch-Petersen, Ruth R. Osborn, David D. Miller, Jeffrey K. Kerns, Rick P. C. Cousins, Ian Robert Baldwin, Paul Bamborough, John Yonchuk, Ann M. Bullion, Lin Guoliang, Jeffrey C. Boehm, Wei Fu, John A. Christopher, Edward F. Webb, Roderick S. Davis, William L. Rumsey, Rita Field, Jeremy John Payne, Hong Nie
Publikováno v:
ACS Medicinal Chemistry Letters. 9:1164-1169
[Image: see text] IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization of a series of 3,5-disubstituted-indole-7-carboxamides for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::782cb7b7a63c400db0be5e5461917822
https://doi.org/10.1021/acsmedchemlett.8b00291
https://doi.org/10.1021/acsmedchemlett.8b00291
Autor:
Jen-Pyng Kou, James F. Callahan, John Yonchuk, Joseph P. Foley, Hong Nie, Heidi G. Feldser, Yolanda Sanchez, William E. Wixted, Jeffrey K. Kerns, Diana G Chalupowicz, Gregory A. Logan, Patricia L. Podolin, Brian Bolognese
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 363:114-125
Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is a key regulator of oxidative stress and cellular repair and can be activated through inhibition of its cytoplasmic repressor, Kelch-like ECH-associated protein 1 (Keap1). Several small molecule di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::204466407cf0cd7f7f72972a187970e8
https://doi.org/10.1124/jpet.117.241794
https://doi.org/10.1124/jpet.117.241794
Autor:
John G, Yonchuk, Joseph P, Foley, Brian J, Bolognese, Gregory, Logan, William E, Wixted, Jen-Pyng, Kou, Diana G, Chalupowicz, Heidi G, Feldser, Yolanda, Sanchez, Hong, Nie, James F, Callahan, Jeffrey K, Kerns, Patricia L, Podolin
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 363(1)
Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is a key regulator of oxidative stress and cellular repair and can be activated through inhibition of its cytoplasmic repressor, Kelch-like ECH-associated protein 1 (Keap1). Several small molecule di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::e6721d8982b84be2d15c27c3ee504816
https://pubmed.ncbi.nlm.nih.gov/28790194
https://pubmed.ncbi.nlm.nih.gov/28790194
Publikováno v:
Journal of Medicinal Chemistry. 56:7463-7476
The Nrf2-Keap1 system plays a major role in cellular defense against oxidative stress. Upon exposure to electrophiles, the cysteine-rich protein Keap1 is covalently modified, and it is this modification of Keap1 that allows the accumulation and subse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64687bda702db0bca0ece052f0f6d632
https://doi.org/10.1021/jm400224q
https://doi.org/10.1021/jm400224q
Autor:
Geoffrey J. Cutler, Paul Bamborough, James V. Morey, Geoffrey W. Mellor, Timothy Longstaff, William L. Rumsey, Ian Robert Baldwin, Mary A. Morse, Aurelie C. Champigny, Hong Nie, Taggart John J, Jeffrey K. Kerns, David D. Miller, John A. Christopher
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2255-2258
The discovery and hit-to-lead exploration of a novel series of selective IKK-β kinase inhibitors is described. The initial lead fragment 3 was identified by pharmacophore-directed virtual screening. Homology model-driven SAR exploration of the templ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::861c72b4a56658b231c78ceba6900666
https://doi.org/10.1016/j.bmcl.2011.02.107
https://doi.org/10.1016/j.bmcl.2011.02.107
Autor:
William L. Rumsey, John Liddle, Rick Williamson, John A. Christopher, Jeffrey K. Kerns, Mary A. Morse, David D. Miller, Paul Bamborough, James F. Callahan
Publikováno v:
Current Topics in Medicinal Chemistry. 9:623-639
The IkappaB kinases (IKKs) are essential components of the signaling pathway by which the NF-kappaB p50/RelA transcription factor is activated in response to pro-inflammatory stimuli such as lipopolysaccharide (LPS) and tumor necrosis factor (TNFalph
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::55faf4273952745939190b8a9cfbb3dd
https://doi.org/10.2174/156802609789007336
https://doi.org/10.2174/156802609789007336
Autor:
David D. Miller, Jeffrey K. Kerns, Catherine M. Alder, Adrian M. Jolly, William L. Rumsey, Geoffrey J. Cutler, Paul Bamborough, Fiona S. Lucas, Kiritkant D. Pancholi, Amanda J. Campbell, Yemisi E. Solanke, Mary A. Morse, Kenneth David Down, Rick Williamson, John A. Christopher, Geoffrey W. Mellor, Ahmed Moktar Hamadi
Publikováno v:
Journal of Medicinal Chemistry. 52:3098-3102
The identification and progression of a potent and selective series of isoquinoline inhibitors of IκB kinase-β (IKK-β) are described. Hit-generation chemistry based on IKK-β active-site knowledge yielded a weakly potent but tractable chemotype th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0d06565def93adfcccc60c5ab8e21eba
https://doi.org/10.1021/jm9000117
https://doi.org/10.1021/jm9000117