Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Thomas Nixey"'
Autor:
Alan C. Cheng, Elizabeth M. Doherty, Sheree Johnstone, Erin F. DiMauro, Jennifer Dao, Abhinav Luthra, Jay Ye, Jie Tang, Thomas Nixey, Xiaoshan Min, Philip Tagari, Les P. Miranda, Zhulun Wang
Publikováno v:
Scientific Reports, Vol 8, Iss 1, Pp 1-9 (2018)
Abstract Small molecules and antibodies each have advantages and limitations as therapeutics. Here, we present for the first time to our knowledge, the structure-guided design of “chemibodies” as small molecule-antibody hybrids that offer dual re
Externí odkaz:
https://doaj.org/article/03c054e59aee48aa9fd15ab0e960b901
Autor:
Brad Herberich, Thomas Nixey, Lin Yin, Tayo Ikotun, Kelvin K. C. Sham, Jason Long, Hongyan Li, Charles Glaus, Xuhai Be, Les P. Miranda, Yuan Cheng, Marcus Soto, James R. Falsey, Bryan D. Moyer, Robert S. Foti, Christopher M. Tegley, Chawita Netirojjanakul, Linh Tran, Kip P. Conner, Jennifer Aral, Liyue Huang, Kaustav Biswas, Justin K. Murray, Bin Wu, Loren Berry, Dean Hickman, Dan A. Rock
Publikováno v:
Drug Metabolism and Disposition. 47:1111-1121
The identification of nonopioid alternatives to treat chronic pain has received a great deal of interest in recent years. Recently, the engineering of a series of Nav1.7 inhibitory peptide-antibody conjugates has been reported, and herein, the precli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9aafa704103c2cd45fe6f198cffc5d5f
https://doi.org/10.1124/dmd.119.087742
https://doi.org/10.1124/dmd.119.087742
Autor:
Bryan D. Moyer, Brad Herberich, Kaustav Biswas, Kenneth W. Walker, Beth D. Youngblood, Jennifer Aral, Tayo Ikotun, Min-Hwa Jasmine Lin, Linh Tran, Thomas Kornecook, Hongyan Li, Thomas Nixey, Joseph Ligutti, Shanti Amagasu, Li Yin, Xuhai Be, Kristin L. Andrews, Christopher M. Tegley, Charles Glaus, Marcus Soto, Les P. Miranda, James R. Falsey, Jason Long, Yuan Cheng, Robert S. Foti, Hossein Salimi-Moosavi, Kelvin Sham, Christopher P Ilch, Bin Wu, Justin K. Murray, Margaret Karow, Chawita Netirojjanakul, Liz Doherty
Publikováno v:
ACS Chemical Biology. 14:806-818
Drug discovery research on new pain targets with human genetic validation, including the voltage-gated sodium channel NaV1.7, is being pursued to address the unmet medical need with respect to chronic pain and the rising opioid epidemic. As part of e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::68d1aa4016111a37796e962e98dcd944
https://doi.org/10.1021/acschembio.9b00183
https://doi.org/10.1021/acschembio.9b00183
Autor:
Kristin L. Andrews, J. Russell Lipford, Christine Sastri, Victor J. Cee, Jeff Winston, Andrew Tasker, Liping H. Pettus, Ryan Wurz, Christopher Mohr, Matthew R. Lee, Brian A. Lanman, Bin Wu, Nadia Guerrero, Thomas Nixey, Anthony B. Reed, Hui-Ling Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:775-780
PIM kinases are a family of Ser/Thr kinases that are implicated in tumorigenesis. The discovery of a new class of PIM inhibitors, 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines, is discussed with optimized compounds showing excellent potency against all
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4102f5f33a7997eb18aa2e1429e22aa2
https://doi.org/10.1016/j.bmcl.2014.12.091
https://doi.org/10.1016/j.bmcl.2014.12.091
Autor:
Jennifer Dao, Erin F. DiMauro, Elizabeth M. Doherty, Jie Tang, Philip Tagari, Alan C. Cheng, Jing Ye, Les P. Miranda, Xiaoshan Min, Thomas Nixey, Zhulun Wang, Abhinav Luthra, Sheree Johnstone
Publikováno v:
Acta Crystallographica Section A Foundations and Advances. 75:a220-a220
Small molecules and antibodies each have advantages and limitations as therapeutics. Here, we present for the first time to our knowledge, the structure-guided design of "chemibodies" as small molecule-antibody hybrids that offer dual recognition of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ac612407bf2375fd9f4c06016e1adc3e
https://doi.org/10.1107/s0108767319097836
https://doi.org/10.1107/s0108767319097836
Autor:
Qingyian Liu, Kaustav Biswas, Frank Koegler, Tiffany L. Correll, Toni Williamson, Jodi Bradley, Jennifer R. Allen, Leeanne Zalameda, Darren L. Reid, Michael D. Bartberger, Joe Zhu, Stephen J. Wood, Randy Hungate, Yichin Liu, Frank Chavez, Robert M. Rzasa, Jianhua Zhang, John D. McCarter, Thomas Nixey, Paul H. Wen, Li Zhu, Shannon Rumfelt, Yi Luo, Safura Babu-Khan, Stephen Hitchcock, Ning Chen, Mqhele Ncube, Wenyuan Qian, Frenel Fils Demorin, Dean Hickman, Christopher M. Tegley, Jian J. Chen, Albert Amegadzie, Charles W. Dean, Chester Chenguang Yuan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6447-6454
γ-Secretase modulators (GSMs) are potentially disease-modifying treatments for Alzheimer's disease. They selectively lower pathogenic Aβ42 levels by shifting the enzyme cleavage sites without inhibiting γ-secretase activity, possibly avoiding know
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f9717b5fcc1d773beec78fba83ce7ef
https://doi.org/10.1016/j.bmcl.2013.09.041
https://doi.org/10.1016/j.bmcl.2013.09.041
Autor:
Dah-Ren Hwang, Geraldine Hill Della Puppa, Jamie Wong, Essa Hu, Thomas Nixey, Silke Miller, Hang Chen, Jessica Able, Dianna Lester-Zeiner, James J. S. Treanor, Robert Cho, Santosh Talreja, Roxanne Kunz, Jianxia Shi, Ji Ma, David C. Immke, Jennifer R. Allen, Christopher Biorn, Amy Porter, Klaus Michelsen, Shannon Rumfelt, Stephen Hitchcock
Publikováno v:
Journal of Medicinal Chemistry. 55:4776-4787
A radiolabeled tracer for imaging therapeutic targets in the brain is a valuable tool for lead optimization in CNS drug discovery and for dose selection in clinical development. We report the rapid identification of a novel phosphodiesterase 10A (PDE
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::626c862c5f50bd2845e3c603ba24a357
https://doi.org/10.1021/jm3002372
https://doi.org/10.1021/jm3002372
Autor:
John B. Jordan, Leszek Poppe, Wenge Zhong, Paul D. Schnier, Yax Sun, Thomas Nixey, Xiaoyang Xia, Alan C. Cheng, Klaus Michelsen, Heather Eastwood
Publikováno v:
Journal of Medicinal Chemistry. 55:678-687
Fragment based drug discovery (FBDD) is a widely used tool for discovering novel therapeutics. NMR is a powerful means for implementing FBDD, and several approaches have been proposed utilizing 1H–15N heteronuclear single quantum coherence (HSQC) a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b98f781e1fcced275383796a08c9c143
https://doi.org/10.1021/jm201441k
https://doi.org/10.1021/jm201441k
Autor:
Timothy Powers, Stephen J. Wood, Ted Judd, Vivian S. W. Li, James Brown, E. Allen Sickmier, Klaus Michelsen, David J. St. Jean, Yi Luo, Dean Hickman, Yuan Cheng, Kui Chen, Stephen Hitchcock, Steven W. Louie, Patricia Lopez, Brad Jordan, Thomas Nixey, Robert T. Fremeau, Michael D. Bartberger, Paul H. Wen, Robert C. Wahl, Claire Rattan
Publikováno v:
Journal of Medicinal Chemistry. 54:5836-5857
Using fragment-based screening of a focused fragment library, 2-aminoquinoline 1 was identified as an initial hit for BACE1. Further SAR development was supported by X-ray structures of BACE1 cocrystallized with various ligands and molecular modeling
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd6f6e1fa9855cbd5de616743bac67e1
https://doi.org/10.1021/jm200544q
https://doi.org/10.1021/jm200544q
Autor:
Linda F. Epstein, Josette Carnahan, Manory Fernando, Douglas A. Whittington, Jeffrey Petkus, Joseph L. Kim, Matthew R. Lee, Adrian L. Smith, Nick A. Paras, Qi Huang, Pedro J. Beltran, Elizabeth M. Doherty, Thomas Nixey, Quynh Le, Mark J. Rose, Frenel Fils Demorin, Kristen Hess, Carol Babij
Publikováno v:
Journal of Medicinal Chemistry. 52:6189-6192
The discovery and optimization of a novel series of aminoisoquinolines as potent, selective, and efficacious inhibitors of the mutant B-Raf pathway is presented. The N-linked pyridylpyrimidine benzamide 2 was identified as a potent, modestly selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0ed3cac42b07e4ebb0ebcf1afc3e1c1
https://doi.org/10.1021/jm901081g
https://doi.org/10.1021/jm901081g