Zobrazeno 1 - 10
of 28
pro vyhledávání: '"John L. Buchanan"'
Development of Novel Dual Binders as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors
Autor:
Zihao Hua, Bryan Egge, Erin L. Mullady, Hakan Gunaydin, John L. Buchanan, Steve Schneider, Xin Huang, Yohannes Teffera, Renee Emkey, Howard Bregman, Randy Serafino, Mary K. Stanton, Erin F. DiMauro, Jingzhou Liu, Virginia Berry, Douglas Saffran, Angel Guzman-Perez, Jennifer Dovey, Liyue Huang, Craig A. Strathdee, Susan M. Turci, Yan Gu, Paul S. Andrews, John Newcomb, Cindy Wilson, Ankita Mishra, Lisa Acquaviva, Nagasree Chakka
Publikováno v:
Journal of Medicinal Chemistry. 56:10003-10015
Tankyrases (TNKS1 and TNKS2) are proteins in the poly ADP-ribose polymerase (PARP) family. They have been shown to directly bind to axin proteins, which negatively regulate the Wnt pathway by promoting β-catenin degradation. Inhibition of tankyrases
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eba595497eee0272affa9da310eb1804
https://doi.org/10.1021/jm401317z
https://doi.org/10.1021/jm401317z
Autor:
Ryan White, James Brown, Jean-Christophe Harmange, Xiaoyang Xia, Josie Han Lee, Yuan Cheng, Robert T. Fremeau, Beth J. Hoffman, Susan A. Tomlinson, Matthew W. Martin, Liyue Huang, Erin F. DiMauro, Stephen Hitchcock, Hung Q. Nguyen, John L. Buchanan, Vinod F. Patel, Ming Huang, William H. Buckner, Brian K. Albrecht, Fen-Fen Lin, Renee Emkey
Publikováno v:
Journal of Medicinal Chemistry. 51:5019-5034
The CB2 receptor is an attractive therapeutic target for analgesic and anti-inflammatory agents. Herein we describe the discovery of a novel class of oxadiazole derivatives from which potent and selective CB2 agonist leads were developed. Initial hit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0c877b87d7688ce77fe355980c89db7
https://doi.org/10.1021/jm800463f
https://doi.org/10.1021/jm800463f
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
https://doi.org/10.1016/j.bmcl.2007.01.048
Autor:
Joseph L. Kim, Xiaotian Zhu, William H. Buckner, Josie H. Lee, Vinod F. Patel, Lilly Chai, Antonio J. Oliveira-dos-Santos, Ryan White, Holly L. Deak, Brian L. Hodous, Joseph J. Nunes, John L. Buchanan, Paul E. Rose, Huilin Zhao, Andrew A. Welcher, Stephanie D. Geuns-Meyer, Linda F. Epstein, David Powers, Yan Gu, Stephen Schneider, Kurt Morgenstern, Anu Gore, Victor J. Cee, Yanyan Tudor, Ted Faust, Susan A. Tomlinson, Xin Huang, Erin F. DiMauro, Jean Bemis, Susan M. Turci, John Newcomb, David C. Mcgowan, Faye Hsieh, Brad Henkle, Deanna Mohn, Christina Boucher, Li Zhu, Matthew W. Martin, Paul Gallant, Craig E. Masse, Daniela Metz
Publikováno v:
Journal of Medicinal Chemistry. 49:5671-5686
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling media
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbddeb8cdb894dbfd55fa63c5040ddcf
https://doi.org/10.1021/jm0605482
https://doi.org/10.1021/jm0605482
Autor:
Kara A. Loiacono, Ian A. MacNeil, Berkley A. Lynch, Taylor Merry, Chi B. Vu, Ukti Mani, Vaibhav Varkhedkar, John L. Buchanan, Dennis A. Holt, Selvaluxmi G. Pradeepan, Hilary R. Plake, Michael Yang, Evelyn G. Corpuz, Choi Lai Tiong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2359-2364
The structure-activity relationships (SAR) of a novel class of Src SH2 inhibitors are described. Variation at the pY+1 and pY+3 side chain positions using 2,4- and 2,5-substituted thiazoles and 1,2,4-oxadiazoles as scaffolds resulted in inhibitors th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e24c3271625ce90015f47df8c67738d
https://doi.org/10.1016/s0960-894x(99)00389-3
https://doi.org/10.1016/s0960-894x(99)00389-3
Publikováno v:
Tetrahedron Letters. 40:3985-3988
The synthesis of optically active 2,4,5-substituted 1,3-thiazoles (peptide thiazoles) is described. Both the chirality and the set of side chain functionality in this fully-substituted scaffold are derived from a combination of two amino acids and on
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::24f01d5dd246d518830149546721ba38
https://doi.org/10.1016/s0040-4039(99)00659-0
https://doi.org/10.1016/s0040-4039(99)00659-0
Publikováno v:
Tetrahedron Letters. 36:7023-7026
Differential functionalization of the nearly symmetrical bis(dihydropyran) 3 is described, leading to the C(20)→C(36) halichondrin B precursor 1. Double hydroboration, regioselective mono-protection of the resulting diol and two-directional chain e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e0f4fc9f3e9c48b1d8ecae1a7cea8d5a
https://doi.org/10.1016/0040-4039(95)01454-p
https://doi.org/10.1016/0040-4039(95)01454-p
Autor:
Elma Feric, Joseph Ligutti, Anruo Zou, Bingfan Du, Stefan I. McDonough, Dong Liu, Nagasree Chakka, Hanh Nho Nguyen, Erin F. DiMauro, John L. Buchanan, Howie Bregman, Jeff S. McDermott
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(5)
Herein we describe the discovery, optimization, and structure-activity relationships of novel potent pyrrolopyrimidine Na(v)1.7 antagonists. Hit-to-lead SAR studies of the pyrrolopyrimidine core, head, and tail groups of the molecule led to the ident
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28110604868f42d1d07fef20d2052367
https://pubmed.ncbi.nlm.nih.gov/22318156
https://pubmed.ncbi.nlm.nih.gov/22318156
Autor:
Elma Feric, Dong Liu, Joseph Ligutti, Liyue Huang, Hanh Nho Nguyen, Anruo Zou, John L. Buchanan, Jeff S. McDermott, Ben Wilenkin, Howie Bregman, David J. Matson, Bingfan Du, Annika B. Malmberg, Xingwen Li, Vinod F. Patel, Stefan I. McDonough, Erin F. DiMauro
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(2)
Clinical genetic data have shown that the product of the SCN9A gene, voltage-gated sodium ion channel Nav1.7, is a key control point for pain perception and a possible target for a next generation of analgesics. Sodium channels, however, historically
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::471c64db91100bebeeedfbb41dafcef4
https://pubmed.ncbi.nlm.nih.gov/22209205
https://pubmed.ncbi.nlm.nih.gov/22209205
Autor:
Brett Janosky, April Chen, Elma Feric, John L. Buchanan, Xingwen Li, Peter Miu, Joseph Ligutti, Liyue Huang, Jeff S. McDermott, Markus Hierl, David C. Immke, David J. Matson, Stefan I. McDonough, Annika B. Malmberg, Dong Liu, Anruo Zou, Erin F. DiMauro, Bingfan Du, Xiao Mei Zheng, Hanh Nho Nguyen, Loren Berry, Vinod F. Patel, Daniel Waldon, Ben Wilenkin, Howard Bregman, Danielle Johnson
Publikováno v:
Journal of medicinal chemistry. 54(13)
Clinical human genetic studies have recently identified the tetrodotoxin (TTX) sensitive neuronal voltage gated sodium channel Nav1.7 (SCN9A) as a critical mediator of pain sensitization. Herein, we report structure-activity relationships for a novel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0554d821ede56752ff72b8f427a167f
https://pubmed.ncbi.nlm.nih.gov/21634377
https://pubmed.ncbi.nlm.nih.gov/21634377