Search Results - "Kerns, Jeffrey"

Structure of the BTB domain of Keap1 and its interaction with the triterpenoid antagonist CDDO by Cleasby, Anne, Yon, Jeff, Day, Philip J, Richardson, Caroline, Tickle, Ian J, Williams, Pamela A, Callahan, James F, Carr, Robin, Concha, Nestor, Kerns, Jeffrey K, Qi, Hongwei, Sweitzer, Thomas, Ward, Paris, Davies, Thomas G

“…The protein Keap1 is central to the regulation of the Nrf2-mediated cytoprotective response, and is increasingly recognized as an important target for…”
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Keap Calm, and Carry on Covalently by Wilson, Anthony J, Kerns, Jeffrey K, Callahan, James F, Moody, Christopher J

“…The Nrf2–Keap1 system plays a major role in cellular defense against oxidative stress. Upon exposure to electrophiles, the cysteine-rich protein Keap1 is…”
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Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery by Davies, Thomas G, Wixted, William E, Coyle, Joseph E, Griffiths-Jones, Charlotte, Hearn, Keisha, McMenamin, Rachel, Norton, David, Rich, Sharna J, Richardson, Caroline, Saxty, Gordon, Willems, Henriëtte M. G, Woolford, Alison J.-A, Cottom, Joshua E, Kou, Jen-Pyng, Yonchuk, John G, Feldser, Heidi G, Sanchez, Yolanda, Foley, Joseph P, Bolognese, Brian J, Logan, Gregory, Podolin, Patricia L, Yan, Hongxing, Callahan, James F, Heightman, Tom D, Kerns, Jeffrey K

“…KEAP1 is the key regulator of the NRF2-mediated cytoprotective response, and increasingly recognized as a target for diseases involving oxidative stress…”
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Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction by Heightman, Tom D, Callahan, James F, Chiarparin, Elisabetta, Coyle, Joseph E, Griffiths-Jones, Charlotte, Lakdawala, Ami S, McMenamin, Rachel, Mortenson, Paul N, Norton, David, Peakman, Torren M, Rich, Sharna J, Richardson, Caroline, Rumsey, William L, Sanchez, Yolanda, Saxty, Gordon, Willems, Henriëtte M. G, Wolfe, Lawrence, Woolford, Alison J.-A, Wu, Zining, Yan, Hongxing, Kerns, Jeffrey K, Davies, Thomas G

“…The KEAP1–NRF2-mediated cytoprotective response plays a key role in cellular homoeostasis. Insufficient NRF2 signaling during chronic oxidative stress may be…”
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Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein−Protein Interaction by Norton, David, Bonnette, William G, Callahan, James F, Carr, Maria G, Griffiths-Jones, Charlotte M, Heightman, Tom D, Kerns, Jeffrey K, Nie, Hong, Rich, Sharna J, Richardson, Caroline, Rumsey, William, Sanchez, Yolanda, Verdonk, Marcel L, Willems, Henriëtte M. G, Wixted, William E, Woolford, Alison J.-A, Wu, Zining, Davies, Thomas G

“…The NRF2-mediated cytoprotective response is central to cellular homoeostasis, and there is increasing interest in developing small-molecule activators of this…”
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Characterization of the Potent, Selective Nrf2 Activator, 3-(Pyridin-3-Ylsulfonyl)-5-(Trifluoromethyl)-2 H -Chromen-2-One, in Cellular and In Vivo Models of Pulmonary Oxidative Stress by Yonchuk, John G, Foley, Joseph P, Bolognese, Brian J, Logan, Gregory, Wixted, William E, Kou, Jen-Pyng, Chalupowicz, Diana G, Feldser, Heidi G, Sanchez, Yolanda, Nie, Hong, Callahan, James F, Kerns, Jeffrey K, Podolin, Patricia L

“…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…”
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3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent by Kerns, Jeffrey K, Busch-Petersen, Jakob, Fu, Wei, Boehm, Jeffrey C, Nie, Hong, Muratore, Michael, Bullion, Ann, Lin, Guoliang, Li, Huijie, Davis, Roderick, Lin, Xichen, Lakdawala, Ami S, Cousins, Rick, Field, Rita, Payne, Jeremy, Miller, David D, Bamborough, Paul, Christopher, John A, Baldwin, Ian, Osborn, Ruth R, Yonchuk, John, Webb, Edward, Rumsey, William L

“…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…”
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Discovery of 6-Aryl-7-alkoxyisoquinoline Inhibitors of IκB Kinase-β (IKK-β) by Christopher, John A, Bamborough, Paul, Alder, Catherine, Campbell, Amanda, Cutler, Geoffrey J, Down, Kenneth, Hamadi, Ahmed M, Jolly, Adrian M, Kerns, Jeffrey K, Lucas, Fiona S, Mellor, Geoffrey W, Miller, David D, Morse, Mary A, Pancholi, Kiritkant D, Rumsey, William, Solanke, Yemisi E, Williamson, Rick

“…The identification and progression of a potent and selective series of isoquinoline inhibitors of IκB kinase-β (IKK-β) are described. Hit-generation chemistry…”
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The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-α and IKK-β kinases by Christopher, John A., Avitabile, Barbara G., Bamborough, Paul, Champigny, Aurelie C., Cutler, Geoffrey J., Dyos, Susan L., Grace, Ken G., Kerns, Jeffrey K., Kitson, Jeremy D., Mellor, Geoffrey W., Morey, James V., Morse, Mary A., O’Malley, Carolyn F., Patel, Champa B., Probst, Nicholas, Rumsey, William, Smith, Clive A., Wilson, Michael J.

“…A potent and selective series of 2-amino-3,5-diarylbenzamide inhibitors of IKK-α and IKK-β is described. The most potent compounds are 8h, 8r and 8v, with…”
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Spongipyran synthetic studies. Total synthesis of (+)-spongistatin 2 by Smith, Amos B., Lin, Qiyan, Doughty, Victoria A., Zhuang, Linghang, McBriar, Mark D., Kerns, Jeffrey K., Boldi, Armen M., Murase, Noriaki, Moser, William H., Brook, Christopher S., Bennett, Clay S., Nakayama, Kiyoshi, Sobukawa, Masao, Lee Trout, Robert E.

“…Evolution of a convergent synthetic strategy to access (+)-spongistatin 2 ( 2), a potent cytotoxic marine macrolide, is described. Highlights of the synthesis…”
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3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IKK-β by Miller, David D., Bamborough, Paul, Christopher, John A., Baldwin, Ian R., Champigny, Aurelie C., Cutler, Geoffrey J., Kerns, Jeffrey K., Longstaff, Timothy, Mellor, Geoffrey W., Morey, James V., Morse, Mary A., Nie, Hong, Rumsey, William L., Taggart, John J.

“…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…”
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Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent by Kerns, Jeffrey K., Nie, Hong, Bondinell, William, Widdowson, Katherine L., Yamashita, Dennis S., Rahman, Attiq, Podolin, Patricia L., Carpenter, Donald C., Jin, Qi, Riflade, Benoit, Dong, Xiaoyang, Nevins, Neysa, Keller, Paul M., Mitchell, Laura, Tomaszek, Thaddeus

“…A series of azepanone inhibitors of cathepsin S is described. Selectivity over both cathepsin K and cathepsin L was achieved by varying the P2 substituent…”
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The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2 by Smith III, Amos B., Lin, Qiyan, Doughty, Victoria A., Zhuang, Linghang, McBriar, Mark D., Kerns, Jeffrey K., Brook, Christopher S., Murase, Noriaki, Nakayama, Kiyoshi

“…An advanced ABCD fragment (see picture) constructed on the way to the total synthesis of the potent antitumor agent (+)‐spongistatin 2 has also been used in a…”
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3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists by Wang, Yonghui, Busch-Petersen, Jakob, Wang, Feng, Ma, Lanping, Fu, Wei, Kerns, Jeffrey K, Jin, Jian, Palovich, Michael R, Shen, Jing-Kang, Burman, Miriam, Foley, James J, Schmidt, Dulcie B, Hunsberger, Gerald E, Sarau, Henry M, Widdowson, Katherine L

“…A series of 3-arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides were prepared and shown to be novel and selective antagonists of the CXCR2 receptor…”
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Growth Inhibition of Hepatoma Cells Induced by Vitamin K and Its Analogs by Nishikawa, Y, Carr, B I, Wang, M, Kar, S, Finn, F, Dowd, P, Zheng, Z B, Kerns, J, Naganathan, S

“…Congeners of vitamin K are known to inhibit cell growth, although the precise mechanisms of growth inhibition are not well understood. To investigate the…”
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Inhibition of Hepatoma Cell Growth in Vitro by Arylating and Non-arylating K Vitamin Analogs by Nishikawa, Yuji, Wang, Ziqiu, Kerns, Jeffrey, Wilcox, Craig S., Carr, Brian I.

“…We recently found that a thioether analog of K vitamin (Cpd 5) inhibited the activity of protein-tyrosine phosphatases (PTPases) and induced protein-tyrosine…”
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Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo by Boehm, Jeffrey, Davis, Roderick, Murar, Claudia E., Li, Tindy, McCleland, Brent, Dong, Shuping, Yan, Hongxing, Kerns, Jeffrey, Moody, Christopher J., Wilson, Anthony J., Graves, Alan P., Mentzer, Mary, Qi, Hongwei, Yonchuk, John, Kou, Jen-Pyng, Foley, Joseph, Sanchez, Yolanda, Podolin, Patricia L., Bolognese, Brian, Booth-Genthe, Catherine, Galop, Marc, Wolfe, Lawrence, Carr, Robin, Callahan, James F.

“…[Display omitted] The antioxidant natural product sulforaphane (SFN) is an oil with poor aqueous and thermal stability. Recent work with SFN has sought to…”
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A Highly Convergent Synthesis of 2-Phenyl Quinoline as Dual Antagonists for NK2 and NK3 Receptors by Yan, Hongxing, Kerns, Jeffrey K., Jin, Qi, Zhu, Chongjie, Barnette, Mary S., Callahan, James F., Hay, Douglas W. P., Jolivette, Larry J., Luttmann, Mark A., Sarau, Henry M., Ward, Keith W., Widdowson, Katherine L., Wan, Zehong

“…A novel and highly convergent synthesis leading to 2-phenyl-quinolines has been developed. As demonstrated in the preparation of…”
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The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2 Financial support was provided by the National Institutes of Health (National Cancer Institute) through Grant CA-70329, a NIH Postdoctoral Fellowship to C.S.B., a Japan Society for Promotion of Science Fellowship to N.M., and a Royal Society Fulbright Fellowship to V.A.D. We also thank the Daiichi Pharmaceutical Co., Ltd, and the by Smith III, Amos B., Lin, Qiyan, Doughty, Victoria A., Zhuang, Linghang, McBriar, Mark D., Kerns, Jeffrey K., Brook, Christopher S., Murase, Noriaki, Nakayama, Kiyoshi

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Self-Efficacy Perceptions of Novice and Career Teachers in Instructional Strategies, Student Engagement, and Classroom Management by Kerns, Jeffrey S

“…The purpose of this study is to contribute to the body of literature that identifies where in the career cycle that teachers need the most support and they…”
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