Zobrazeno 1 - 10
of 108
pro vyhledávání: '"Mark H. Norman"'
Autor:
Hui-Ling Wang, Kristin L. Andrews, Shon K. Booker, Jude Canon, Victor J. Cee, Frank Chavez, Yuping Chen, Heather Eastwood, Nadia Guerrero, Brad Herberich, Dean Hickman, Brian A. Lanman, Jimmy Laszlo, Matthew R. Lee, J. Russell Lipford, Bethany Mattson, Christopher Mohr, Yen Nguyen, Mark H. Norman, Liping H. Pettus, David Powers, Anthony B. Reed, Karen Rex, Christine Sastri, Nuria Tamayo, Paul Wang, Jeffrey T. Winston, Bin Wu, Qiong Wu, Tian Wu, Ryan P. Wurz, Yang Xu, Yihong Zhou, Andrew S. Tasker
Publikováno v:
Journal of Medicinal Chemistry. 62:1523-1540
Pim kinases are a family of constitutively active serine/threonine kinases that are partially redundant and regulate multiple pathways important for cell growth and survival. In human disease, high expression of the three Pim isoforms has been implic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3743f2a152bf3d38a985da1601967443
https://doi.org/10.1021/acs.jmedchem.8b01733
https://doi.org/10.1021/acs.jmedchem.8b01733
Autor:
Heather Eastwood, Andrew Tasker, Yuping Chen, David Powers, Nadia Guerrero, Christopher Mohr, Anthony B. Reed, Jimmy Laszlo, Paul Wang, Yihong Zhou, Ryan Wurz, Mark H. Norman, Karen Rex, Jeffrey T. Winston, Liping H. Pettus, Dean Hickman, Yang Xu, Brian A. Lanman, Tian Wu, Yen Nguyen, Kristin L. Andrews, J. Russell Lipford, Frank Chavez, Hui-Ling Wang, Christine Sastri, Matthew R. Lee, Bethany Mattson, Nuria A. Tamayo, Victor J. Cee, Jie Chen, Bradley J. Herberich, Bin Wu, Shon Booker
Publikováno v:
Journal of Medicinal Chemistry. 59:6407-6430
The high expression of proviral insertion site of Moloney murine leukemia virus kinases (Pim-1, -2, and -3) in cancers, particularly the hematopoietic malignancies, is believed to play a role in promoting cell survival and proliferation while suppres
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f85b2099ac31a14dc5abf0c6c20c999
https://doi.org/10.1021/acs.jmedchem.6b00610
https://doi.org/10.1021/acs.jmedchem.6b00610
Autor:
Zihao Hua, Michele Potashman, Carol Babij, Manory Fernando, Nobuko Nishimura, Josette Carnahan, Joseph L. Kim, Linda F. Epstein, Matthew R. Lee, Kevin Yang, Richard T. Lewis, Douglas A. Whittington, Longbin Liu, Karina R. Vaida, Howard Bregman, Shuyan Yi, Mark H. Norman, Matthew W. Martin
Publikováno v:
Bioorganic & Medicinal Chemistry. 24:2215-2234
One of the challenges for targeting B-Raf(V600E) with small molecule inhibitors had been achieving adequate selectivity over the wild-type protein B-Raf(WT), as inhibition of the latter has been associated with hyperplasia in normal tissues. Recent s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::827984e880dbf904a5d196e7229c4921
https://doi.org/10.1016/j.bmc.2016.03.055
https://doi.org/10.1016/j.bmc.2016.03.055
Autor:
Michael D. Bartberger, Michael Croghan, Carolyn Moyer, David Lloyd, Rod Cupples, Seifu Tadesse, Nobuko Nishimura, Ke Kong, Gwyneth Van, Christopher H. Fotsch, Randall W. Hungate, David J. St. Jean, Kevin Yang, Kate Ashton, Mark H. Norman, Samer Chmait, Longbin Liu, Lewis D. Pennington, Fang-Tsao Hong, Matthew P. Bourbeau, Clarence Hale, Jiandong Zhang, Aaron C. Siegmund, Jie Chen, Christopher M. Tegley, Steven R. Jordan, Kristin L. Andrews, Klaus Michelsen, Guomin Yao, Glenn Sivits, Andreas Reichelt, Joan Helmering
Publikováno v:
Journal of Medicinal Chemistry. 58:9663-9679
The HTS-based discovery and structure-guided optimization of a novel series of GKRP-selective GK-GKRP disrupters are revealed. Diarylmethanesulfonamide hit 6 (hGK-hGKRP IC50 = 1.2 μM) was optimized to lead compound 32 (AMG-0696; hGK-hGKRP IC50 = 0.0
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c946578bf834df571e0f47d51f90f41
https://doi.org/10.1021/acs.jmedchem.5b01367
https://doi.org/10.1021/acs.jmedchem.5b01367
Autor:
Kevin Yang, Rod Cupples, Gwyneth Van, Nobuko Nishimura, Longbin Liu, David J. St. Jean, Clarence Hale, Glenn Sivits, Jie Chen, Nuria A. Tamayo, Steven R. Jordan, Fang-Tsao Hong, Mark H. Norman, Michael D. Bartberger, Yunxin Bo, Christopher H. Fotsch, Samer Chmait, Seifu Tadesse, David Lloyd
Publikováno v:
Journal of Medicinal Chemistry. 58:4462-4482
The glucokinase-glucokinase regulatory protein (GK-GKRP) complex plays an important role in controlling glucose homeostasis in the liver. We have recently disclosed a series of arylpiperazines as in vitro and in vivo disruptors of the GK-GKRP complex
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0067ff276fb22038ac064d47a32d35c8
https://doi.org/10.1021/jm5018175
https://doi.org/10.1021/jm5018175
Autor:
David Powers, Katja Labitzke, Mark J. Rose, Kristin L. Andrews, Richard Kendall, Kenneth R. Dellamaggiore, Shon Booker, Peter Jaeckel, Silvia Materna-Reichelt, Mark H. Norman, Young-Ah Chung, Holger Beckmann, Paul L. Shaffer, Pedro J. Beltran, Hao Chen, Alexander M. Long, Petia Mitchell, Adrian L. Smith, Jennifer Dao, J. Russell Lipford, Noel D'angelo, Steven F. Bellon, Michelle Wu
Publikováno v:
Journal of Medicinal Chemistry. 58:1426-1441
The structure-based design and optimization of a novel series of selective PERK inhibitors are described resulting in the identification of 44 as a potent, highly selective, and orally active tool compound suitable for PERK pathway biology exploratio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::906c5b60a94b9bc681eaaf3c8dfd6af5
https://doi.org/10.1021/jm5017494
https://doi.org/10.1021/jm5017494
Autor:
Fang-Tsao Hong, Jian Jiang, Brian A. Lanman, Victor J. Cee, Liping H. Pettus, Paul E. Hughes, Nancy Zhang, Douglas A. Whittington, Tisha San Miguel, Anthony B. Reed, Ling Wang, Erin L. Mullady, Kristin L. Andrews, John D. McCarter, Andrew Tasker, Leeanne Zalameda, Mark H. Norman, Tian Wu, Ryan Wurz, Raju Subramanian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:5630-5634
Replacement of the piperazine sulfonamide portion of the PI3Kα inhibitor AMG 511 (1) with a range of aliphatic alcohols led to the identification of a truncated gem-dimethylbenzylic alcohol analog, 2-(5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-((5-fl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ac5698d5fbf21b4947041fb8e3a9326
https://doi.org/10.1016/j.bmcl.2014.10.085
https://doi.org/10.1016/j.bmcl.2014.10.085
Publikováno v:
Tetrahedron Letters. 55:4501-4504
Upon utilization of some common methods described in the literature for the synthesis of chiral, 2-substituted 2,5-diketopiperazines, extensive racemization was observed. Further investigation showed that heating in the presence of a mild base racemi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::751e8669ef15ee81e3900e63fcaadd75
https://doi.org/10.1016/j.tetlet.2014.06.058
https://doi.org/10.1016/j.tetlet.2014.06.058
Autor:
Yunxin Bo, Tisha San Miguel, Nobuko Nishimura, Jian Jiang, Douglas A. Whittington, Paul E. Hughes, Sean Caenepeel, Mark H. Norman, John D. McCarter, Erin L. Mullady, Daniel J. Freeman, Kevin Yang, Ryan Wurz, Longbin Liu, Raju Subramanian, Kristin L. Andrews, Ling Wang, Liping H. Pettus, Nancy Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5714-5720
Phosphoinositide 3-kinase (PI3K) is an important target in oncology due to the deregulation of the PI3K/Akt signaling pathway in a wide variety of tumors. A series of 4-amino-6-methyl-1,3,5-triazine sulfonamides were synthesized and evaluated as inhi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62866028e9510797810acdca23680ada
https://doi.org/10.1016/j.bmcl.2012.06.078
https://doi.org/10.1016/j.bmcl.2012.06.078
Autor:
Bradley J. Herberich, Tian Wu, Paul E. Hughes, Claire L. M. Jackson, Nobuko Nishimura, Nancy Zhang, Ryan Wurz, Douglas A. Whittington, Shon Booker, Sean Caenepeel, Tisha San Miguel, Jian Jiang, Anthony B. Reed, Adrian L. Smith, Seifu Tadesse, Brian A. Lanman, Andrew Tasker, Erin L. Mullady, John D. McCarter, Fang-Tsao Hong, Liping H. Pettus, Divesh Aidasani, Victor J. Cee, Ling Wang, Bin Wu, Mark H. Norman, Daniel J. Freeman, Kevin Yang, Longbin Liu, Leeanne Zalameda, Yunxin Y. Bo, Xiaochun Zhu, Kristin L. Andrews, Markian Stec, Nuria A. Tamayo, Raju Subramanian, Noel D'angelo
Publikováno v:
Journal of Medicinal Chemistry. 55:7796-7816
The phosphoinositide 3-kinase family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger which plays a critical role in important cellular functions such as metabolis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7379e5002efb24d810fb0e1f33a3641
https://doi.org/10.1021/jm300846z
https://doi.org/10.1021/jm300846z