Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Thomas, Kornecook"'
Autor:
John R, Butler, Gwenaella, Rescourio, Benjamin C, Milgram, Robert S, Foti, Thomas, Kornecook, Joseph, Ligutti, Bryan D, Moyer, Kristin, Taborn, Beth D, Youngblood, Violeta, Yu, Roman, Shimanovich, Alessandro, Boezio, Matthew, Weiss
Publikováno v:
Bioorganicmedicinal chemistry letters. 73
Na
Autor:
William J. McCarty, Thomas Kornecook, Jonathan Roberts, Marcus Soto, Helming Tan, Brian A. Sparling, Paul S. Andrews, Hao Chen, Charles G. Knutson, James Meyer, Stephen Schneider, Maosheng Zhang
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 371:476-486
There is an unmet medical need for nonopioid pain therapies in human populations; several pathways are under investigation for possible therapeutic intervention. Tetrahydrobiopterin (BH4) has received attention recently as a mediator of neuropathic p
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
Autor:
Bin Wu, Shanti Amagasu, Jason Long, Justin K. Murray, Kristin L. Andrews, Jennifer Aral, Les P. Miranda, Xuhai Be, Kaustav Biswas, Min-Hwa Jasmine Lin, Dong Liu, Zhulun Wang, Anruo Zou, Bryan D. Moyer, Joseph Ligutti, Xiaoshan Min, Kelvin Sham, Thomas Kornecook, Christopher P Ilch
Publikováno v:
Journal of Medicinal Chemistry. 61:9500-9512
Inhibitors of the voltage-gated sodium channel NaV1.7 are being investigated as pain therapeutics due to compelling human genetics. We previously identified NaV1.7-inhibitory peptides GpTx-1 and JzTx-V from tarantula venom screens. Potency and select
Autor:
Stefan I. McDonough, Min-Hwa Jasmine Lin, Erin F. DiMauro, Violeta Yu, Angel Guzman-Perez, Kristin Taborn, Christiane Bode, Thomas Kornecook, Thomas Dineen, Xin Huang, Robert T. Fremeau, Margaret Chu-Moyer, James R. Coats, Bingfan Du, Jeff S. McDermott, Hakan Gunaydin, Daniel S. La, Hua Gao, Bryan D. Moyer, Russell Graceffa, Alessandro Boezio, Charles Kreiman, Matthew Weiss, Hanh Nho Nguyen, David J. Matson, Joseph Ligutti, Christopher P Ilch, Isaac E. Marx, Emily A. Peterson, Howard Bregman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:3477-3485
The voltage-gated sodium channel NaV1.7 has received much attention from the scientific community due to compelling human genetic data linking gain- and loss-of-function mutations to pain phenotypes. Despite this genetic validation of NaV1.7 as a tar
Autor:
Kristin Taborn, Joseph Ligutti, Josie H. Lee, Thomas Kornecook, Dong Liu, Dawn Zhu, Stephen Altmann, Ruoyuan Yin, Xuhai Be, Robert T. Fremeau, Jinti Wang, John Roberts, David J. Matson, Danielle Johnson, Violeta Yu, Christopher P Ilch, Bryan D. Moyer, Jason A. Luther, Virginia Berry, Matthew Weiss, Danny Ortuno, Michael Jarosh, Sonya G. Lehto
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 362:146-160
Potent and selective antagonists of the voltage-gated sodium channel NaV1.7 represent a promising avenue for the development of new chronic pain therapies. We generated a small molecule atropisomer quinolone sulfonamide antagonist AMG8379 and a less
Autor:
Jessica Able, Benjamin C. Milgram, Loren Berry, Melanie Cooke, Liyue Huang, John Butler, Hongbing Huang, Violeta Yu, Kristin Taborn, John D. Roberts, Steven Altmann, Margaret Y. Chu-Moyer, John Yeoman, Jean Wang, Roman Shimanovich, Russell Graceffa, Matthew Weiss, Thomas Kornecook, Christopher P Ilch, Bryan D. Moyer, Christiane Boezio, Isaac E. Marx, Brian A. Sparling, Emily A. Peterson, Gwen Rescourio, Charles Kreiman, Elma Feric Bojic, Karina R. Vaida, Angel Guzman-Perez, Dawn Zhu, Hua Gao, Laurie B. Schenkel, Michael Jarosh, Hanh Nho Nguyen, Joseph Ligutti, Alessandro Boezio, Hakan Gunaydin, Daniel S. La, Thomas Dineen, Robert T. Fremeau, Robert S. Foti, Min-Hwa Jasmine Lin, Erin F. DiMauro, John Stellwagen
Publikováno v:
Journal of Medicinal Chemistry. 60:5990-6017
Because of its strong genetic validation, NaV1.7 has attracted significant interest as a target for the treatment of pain. We have previously reported on a number of structurally distinct bicyclic heteroarylsulfonamides as NaV1.7 inhibitors that demo
Autor:
Robert T. Fremeau, Isaac E. Marx, Emily A. Peterson, Charles Kreiman, Thomas Dineen, Hua Gao, Alessandro Boezio, Hakan Gunaydin, Min-Hwa Jasmine Lin, Steven Altmann, Elma Feric Bojic, Kristin Taborn, Robert S. Foti, Russell Graceffa, Daniel S. La, Liyue Huang, Matthew Weiss, Paul E. Rose, Angel Guzman-Perez, Beth D. Youngblood, Hongbing Huang, Violeta Yu, Dong Liu, Thomas Kornecook, Bryan D. Moyer, Howard Bregman, Hanh Nho Nguyen, Joseph Ligutti, Margaret Y. Chu-Moyer, Michael Jarosh, Erin F. DiMauro
Publikováno v:
Journal of Medicinal Chemistry. 60:5969-5989
Several reports have recently emerged regarding the identification of heteroarylsulfonamides as NaV1.7 inhibitors that demonstrate high levels of selectivity over other NaV isoforms. The optimization of a series of internal NaV1.7 leads that address
Autor:
Robert S. Foti, Brian A. Sparling, Thomas Kornecook, Erin F. DiMauro, Joseph Ligutti, Angel Guzman-Perez, Shuyan Yi, Howie Bregman, Michael Jarosh, Hua Gao, Hongbing Huang, Violeta Yu, Beth D. Youngblood, Bryan D. Moyer, Jessica Able, Benjamin Charles Milgram, Matthew Weiss
Publikováno v:
MedChemComm. 8:744-754
NaV1.7 is a particularly compelling target for the treatment of pain. Herein, we report the discovery and evaluation of a series of piperazine amides that exhibit state-dependent inhibition of NaV1.7. After demonstrating significant pharmacodynamic a
Autor:
Russell F, Graceffa, Alessandro A, Boezio, Jessica, Able, Steven, Altmann, Loren M, Berry, Christiane, Boezio, John R, Butler, Margaret, Chu-Moyer, Melanie, Cooke, Erin F, DiMauro, Thomas A, Dineen, Elma, Feric Bojic, Robert S, Foti, Robert T, Fremeau, Angel, Guzman-Perez, Hua, Gao, Hakan, Gunaydin, Hongbing, Huang, Liyue, Huang, Christopher, Ilch, Michael, Jarosh, Thomas, Kornecook, Charles R, Kreiman, Daniel S, La, Joseph, Ligutti, Benjamin C, Milgram, Min-Hwa Jasmine, Lin, Isaac E, Marx, Hanh N, Nguyen, Emily A, Peterson, Gwen, Rescourio, John, Roberts, Laurie, Schenkel, Roman, Shimanovich, Brian A, Sparling, John, Stellwagen, Kristin, Taborn, Karina R, Vaida, Jean, Wang, John, Yeoman, Violeta, Yu, Dawn, Zhu, Bryan D, Moyer, Matthew M, Weiss
Publikováno v:
Journal of medicinal chemistry. 60(14)
Because of its strong genetic validation, Na