Zobrazeno 1 - 10
of 20
pro vyhledávání: '"David J. Matson"'
Autor:
David J Matson, Darryl T Hamamoto, Howard Bregman, Melanie Cooke, Erin F DiMauro, Liyue Huang, Danielle Johnson, Xingwen Li, Jeff McDermott, Carrie Morgan, Ben Wilenkin, Annika B Malmberg, Stefan I McDonough, Donald A Simone
Publikováno v:
PLoS ONE, Vol 10, Iss 9, p e0138140 (2015)
While genetic evidence shows that the Nav1.7 voltage-gated sodium ion channel is a key regulator of pain, it is unclear exactly how Nav1.7 governs neuronal firing and what biophysical, physiological, and distribution properties of a pharmacological N
Externí odkaz:
https://doaj.org/article/0837a210c9304876b8143a23aa472839
Autor:
Jacinthe Gingras, Sarah Smith, David J Matson, Danielle Johnson, Kim Nye, Lauren Couture, Elma Feric, Ruoyuan Yin, Bryan D Moyer, Matthew L Peterson, James B Rottman, Rudolph J Beiler, Annika B Malmberg, Stefan I McDonough
Publikováno v:
PLoS ONE, Vol 9, Iss 9, p e105895 (2014)
Clinical genetic studies have shown that loss of Nav1.7 function leads to the complete loss of acute pain perception. The global deletion is reported lethal in mice, however, and studies of mice with promoter-specific deletions of Nav1.7 have suggest
Externí odkaz:
https://doaj.org/article/49c66d94391141b6b07f7e6d7d29e53b
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:
Shuyan Yi, Sonya G. Lehto, Stefan I. McDonough, Klaus Michelsen, Erin F. DiMauro, Hao Chen, Maosheng Zhang, Stephen Schneider, Shawn Ayube, Jason A. Luther, Matthew H. Plant, Xin Huang, David J. Matson, Jeffrey R. Simard, Howard Bregman, Jacinthe Gingras, Paul L. Shaffer, Yohannes Teffera
Publikováno v:
Nature Structural & Molecular Biology. 24:108-113
Current therapies to treat persistent pain and neuropathic pain are limited by poor efficacy, side effects and risk of addiction. Here, we present a novel class of potent selective, central nervous system (CNS)-penetrant potentiators of glycine recep
Autor:
Daniel S, La, Emily A, Peterson, Christiane, Bode, Alessandro A, Boezio, Howard, Bregman, Margaret Y, Chu-Moyer, James, Coats, Erin F, DiMauro, Thomas A, Dineen, Bingfan, Du, Hua, Gao, Russell, Graceffa, Hakan, Gunaydin, Angel, Guzman-Perez, Robert, Fremeau, Xin, Huang, Christopher, Ilch, Thomas J, Kornecook, Charles, Kreiman, Joseph, Ligutti, Min-Hwa, Jasmine Lin, Jeff S, McDermott, Isaac, Marx, David J, Matson, Stefan I, McDonough, Bryan D, Moyer, Hanh, Nho Nguyen, Kristin, Taborn, Violeta, Yu, Matthew M, Weiss
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(15)
The voltage-gated sodium channel Na
Autor:
E Galbreath, Sonya G. Lehto, N Rampal, C Yang, Beth D. Youngblood, Stephen G. Waxman, Dong Liu, M Lepherd, Jacinthe Gingras, Bryan D. Moyer, David J. Matson, Maosheng Zhang, Matthew Alsaloum, S Allred, Kristin Taborn, R Ferrando, B Grubinska, Sulayman D. Dib-Hajj, Thomas Kornecook, Lubin Chen
Publikováno v:
Molecular Pain. 15:174480691988184
Recapitulating human disease pathophysiology using genetic animal models is a powerful approach to enable mechanistic understanding of genotype–phenotype relationships for drug development. NaV1.7 ...
Autor:
Kevin Gaida, Marissa van der Valk, BaoXi Gao, Lei Cao, David J. Matson, Jean-Christophe Harmange, Todd Juan, Katrina W. Copeland, Stephanie Springer, Markus Hierl, Jeff S. McDermott, Dan Waldon, Hong Deng, Brian K. Albrecht, Wenhong Guo, Kristie Clarkin, Hung Q. Nguyen, Johannes Knop, Sonya G. Lehto, Stefan I. McDonough, Alessandro Boezio, Annika B. Malmberg
Publikováno v:
Pain. 149:33-49
Nicotinic acetylcholine receptors (nAChRs) are longstanding targets for a next generation of pain therapeutics, but the nAChR subtypes that govern analgesia remain unknown. We tested a series of nicotinic agonists, including many molecules used or tr
Autor:
Harry Brielmann, David J. Matson, Bertrand L. Chenard, Mark T. Kershaw, W. Rycroft, Nicola Burnaby-Davies, Marci Crandall, Stéphane De Lombaert, Kevin J. Hodgetts, William J. Martin, Rajagopal Bakthavatchalam, Beth Ann Murphy, Timothy M. Caldwell, G Mason, A. Brian Jones, Xiaozhang Zheng, Helen Perrett, Susan Boyce, James E. Krause, Daniel N. Cortright, Charles A. Blum, Rachael Conley, Scott M. Capitosti
Publikováno v:
Journal of Medicinal Chemistry. 53:3330-3348
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a nonselective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective a
Autor:
Rajagopal Bakthavatchalam, Lawrence K. Fung, Bertrand L. Chenard, David J. Matson, Chu K. Ngo, Marci Crandall, Stéphane De Lombaert, Daniel N. Cortright, Harry Brielmann, Charles A. Blum, Mark T. Kershaw, Jayaraman Chandrasekhar, Marta Day, Xiaozhang Zheng, James E. Krause, Kevin J. Hodgetts
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4573-4577
A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates excellent in vivo potency and efficacy in an acute inflam