Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Michael Jarosh"'
Autor:
Owen B. McManus, Vivian Hecht, Violeta Yu, Chris M Hempel, Graham T. Dempsey, Ryan J. Babcock, Michael Jarosh, Joseph G. McGivern, Hongkang Zhang, Kevin Dong, Bryan D. Moyer, Christopher A. Werley
Publikováno v:
SLAS Discovery. 25:434-446
The voltage-gated sodium channel Nav1.7 is a genetically validated target for pain; pharmacological blockers are promising as a new class of nonaddictive therapeutics. The search for Nav1.7 subtype selective inhibitors requires a reliable, scalable,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b158bb79b66d537a5d39c6d8bdd18fe7
https://doi.org/10.1177/2472555220914532
https://doi.org/10.1177/2472555220914532
Autor:
Hongkang, Zhang, Bryan D, Moyer, Violeta, Yu, Joseph G, McGivern, Michael, Jarosh, Christopher A, Werley, Vivian C, Hecht, Ryan J, Babcock, Kevin, Dong, Graham T, Dempsey, Owen B, McManus, Chris M, Hempel
Publikováno v:
SLAS discovery : advancing life sciences RD. 25(5)
The voltage-gated sodium channel Nav1.7 is a genetically validated target for pain; pharmacological blockers are promising as a new class of nonaddictive therapeutics. The search for Nav1.7 subtype selective inhibitors requires a reliable, scalable,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::0fd21ab9bf663c041689f61b02b49514
https://pubmed.ncbi.nlm.nih.gov/32292096
https://pubmed.ncbi.nlm.nih.gov/32292096
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d863f2d2c28cbf4708d06dfd96734ade
https://doi.org/10.1124/jpet.116.239590
https://doi.org/10.1124/jpet.116.239590
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bb6062704d531ce83c1a6122ecc44600
https://doi.org/10.1021/acs.jmedchem.6b01850
https://doi.org/10.1021/acs.jmedchem.6b01850
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3616b7030b42538cb45a4828f9c4821e
https://doi.org/10.1021/acs.jmedchem.6b01851
https://doi.org/10.1021/acs.jmedchem.6b01851
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::af0547c7c59fef471565d7454331d0af
https://doi.org/10.1039/c6md00578k
https://doi.org/10.1039/c6md00578k
Autor:
Laurie B, Schenkel, Erin F, DiMauro, Hanh N, Nguyen, Nagasree, Chakka, Bingfan, Du, Robert S, Foti, Angel, Guzman-Perez, Michael, Jarosh, Daniel S, La, Joseph, Ligutti, Benjamin C, Milgram, Bryan D, Moyer, Emily A, Peterson, John, Roberts, Violeta L, Yu, Matthew M, Weiss
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(16)
The Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::feccab44327957064eb9a4c9ed77e708
https://pubmed.ncbi.nlm.nih.gov/28684121
https://pubmed.ncbi.nlm.nih.gov/28684121
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b8ea84d65ab7dd59414c7bfc36426140
https://pubmed.ncbi.nlm.nih.gov/28324649
https://pubmed.ncbi.nlm.nih.gov/28324649
Autor:
Matthew M, Weiss, Thomas A, Dineen, Isaac E, Marx, Steven, Altmann, Alessandro, Boezio, Howard, Bregman, Margaret, Chu-Moyer, Erin F, DiMauro, Elma, Feric Bojic, Robert S, Foti, Hua, Gao, Russell, Graceffa, Hakan, Gunaydin, Angel, Guzman-Perez, Hongbing, Huang, Liyue, Huang, Michael, Jarosh, Thomas, Kornecook, Charles R, Kreiman, Joseph, Ligutti, Daniel S, La, Min-Hwa Jasmine, Lin, Dong, Liu, Bryan D, Moyer, Hanh N, Nguyen, Emily A, Peterson, Paul E, Rose, Kristin, Taborn, Beth D, Youngblood, Violeta, Yu, Robert T, Fremeau
Publikováno v:
Journal of medicinal chemistry. 60(14)
Several reports have recently emerged regarding the identification of heteroarylsulfonamides as Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::7836a4ad57471118cec766361a3f5db3
https://pubmed.ncbi.nlm.nih.gov/28287723
https://pubmed.ncbi.nlm.nih.gov/28287723
Autor:
Robert T. Fremeau, Joseph Ligutti, Paul E. Rose, Dong Liu, Elma Feric Bojic, Yan Wang, Hongbing Huang, Violeta Yu, Thomas Kornecook, Angel Guzman-Perez, Laurie B. Schenkel, Hakan Gunaydin, Stephen Altmann, Jean Wang, Kristin Taborn, Matthew Weiss, Margaret Y. Chu-Moyer, Michael Jarosh, Howard Bregman, Hua Gao, Robert S. Foti, Bryan D. Moyer, Brian E. Hall, Loren Berry, Nagasree Chakka, Josie Lee, Daniel Ortuno, Erin F. DiMauro
Publikováno v:
Journal of medicinal chemistry. 59(17)
The majority of potent and selective hNaV1.7 inhibitors possess common pharmacophoric features that include a heteroaryl sulfonamide headgroup and a lipophilic aromatic tail group. Recently, reports of similar aromatic tail groups in combination with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae84d39f884bb9eb14c6496cd67e32ce
https://pubmed.ncbi.nlm.nih.gov/27441383
https://pubmed.ncbi.nlm.nih.gov/27441383