Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Rebecca M, Klein"'
Autor:
Rebecca M. Klein, Mark E. Layton, Hillary Regan, Christopher P. Regan, Yuxing Li, Tracey Filzen, Matt Cato, Michelle K. Clements, Jixin Wang, Raul Sanoja, Thomas J. Greshock, Anthony J. Roecker, Joseph E. Pero, Ron Kim, Christopher Burgey, Christopher T. John, Ying-Hong Wang, Neetesh Bhandari, Arie Struyk, Richard L. Kraus, Darrell A. Henze, Andrea K. Houghton
Publikováno v:
Channels, Vol 16, Iss 1, Pp 230-243 (2022)
As part of a drug discovery effort to identify potent inhibitors of NaV1.7 for the treatment of pain, we observed that inhibitors produced unexpected cardiovascular and respiratory effects in vivo. Specifically, inhibitors administered to rodents pro
Externí odkaz:
https://doaj.org/article/55057518620746559c951066d12dfcf1
Autor:
Jeanine E. Ballard, Parul S. Pall, Joshua Vardigan, Fuqiang Zhao, Marie A. Holahan, Xiaoping Zhou, Nina Jochnowitz, Richard L. Kraus, Rebecca M. Klein, Darrell A. Henze, Andrea K. Houghton, Christopher S. Burgey, Christopher Gibson, Arie Struyk
Publikováno v:
Frontiers in Pharmacology, Vol 12 (2021)
MK-2075 is a small-molecule selective inhibitor of the NaV1.7 channel investigated for the treatment of postoperative pain. A translational strategy was developed for MK-2075 to quantitatively interrelate drug exposure, target modulation, and the des
Externí odkaz:
https://doaj.org/article/b6acf3025c844a49ac376ac7097521ef
Autor:
Christopher Daley, Yuxing Li, Haiyan Sun, Xiu Wang, Fuqiang Zhao, Michelle K. Clements, Rebecca M. Klein, Aneta Jovanovska, Andrew Brunskill, Joseph E. Pero, Xuanjia Peng, Thomas J. Greshock, Christopher S. Burgey, Mark E. Layton, Jeanine E. Ballard, Deping Wang, Richard L. Kraus, Andrea K. Houghton, Anthony J. Roecker, Michael J. Kelly
Publikováno v:
ACS Medicinal Chemistry Letters. 12:1038-1049
The voltage-gated sodium channel Nav1.7 continues to be a high-profile target for the treatment of various pain afflictions due to its strong human genetic validation. While isoform selective molecules have been discovered and advanced into the clini
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5074c01bd9b85bda35e405231de481ea
https://doi.org/10.1021/acsmedchemlett.1c00218
https://doi.org/10.1021/acsmedchemlett.1c00218
Publikováno v:
Pain
Next generation transcriptomics in combination with imaging-based approaches have emerged as powerful tools for the characterization of dorsal root ganglion (DRG) neuronal subpopulations. The mouse DRG has been well-characterized by many independentl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1645a3120ca52f38a53fe7772d07e4e2
https://doi.org/10.1097/j.pain.0000000000001973
https://doi.org/10.1097/j.pain.0000000000001973
Autor:
Richard L. Kraus, Ronald M. Kim, Jeanine E. Ballard, Thomas J. Greshock, Andrea K. Houghton, Michelle K. Clements, Marie A. Holahan, Andrew Danziger, Christopher S. Burgey, Yuxing Li, Mark E. Layton, Jordi Serra, Parul S. Pall, Rebecca M. Klein, Joshua D. Vardigan, Dan Zhou, Fuqiang Zhao, Christopher Daley, Darrell A. Henze
Publikováno v:
Science Translational Medicine. 13
Humans with loss-of-function mutations in the Nav1.7 channel gene (SCN9A) show profound insensitivity to pain, whereas those with gain-of-function mutations can have inherited pain syndromes. Therefore, inhibition of the Nav1.7 channel with a small m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2568b727c558da3b3a2a03b719a658df
https://doi.org/10.1126/scitranslmed.aay1050
https://doi.org/10.1126/scitranslmed.aay1050
Autor:
Andrea K. Houghton, Aneta Jovanovska, Tracey Filzen, Ying-Hong Wang, Jacqueline Panigel, Annie Liang, Michelle K. Clements, Rebecca M. Klein, Richard L. Kraus, John Majercak, Eleftheria N. Finger, Jixin Wang, Matthew J. Cato, Hannah D. G. F. Lehman, Christopher Daley, Yun Gregan, James Mulhearn, Yuxing Li, Michael A. Rossi, Darrell A. Henze, Mark O. Urban, Michael J. Kelly, Scott E. Wolkenberg, Mark E. Layton, Joseph E. Pero
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2683-2688
Studies on human genetics have suggested that inhibitors of the Nav1.7 voltage-gated sodium channel hold considerable promise as therapies for the treatment of chronic pain syndromes. Herein, we report novel, peripherally-restricted benzoxazolinone a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2fa8cc863252cd7ed266d6ff8eb35f8f
https://doi.org/10.1016/j.bmcl.2017.04.040
https://doi.org/10.1016/j.bmcl.2017.04.040
Autor:
Mark E. Layton, Eleftheria N. Finger, Edward C. Sherer, Amy Jo Koser, Aneta Jovanovska, Robert Gomez, Xiu Wang, Deping Wang, Xuanjia Peng, John Majercak, Melissa Egbertson, Paul J. Coleman, Rebecca M. Klein, Kristen L.G. Jones, Richard L. Kraus, Jixin Wang, Tracey Filzen, Mark O. Urban, Yuxing Li, Anthony J. Roecker, Matthew J. Cato, Ying-Hong Wang, Michelle K. Clements, Jacqueline Panigel, Leo A. Joyce, Vincent P. Santarelli, Irene Gregan, Christopher Daley, Haiyan Sun, Andrea K. Houghton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2087-2093
The voltage-gated sodium channel Nav1.7 is a genetically validated target for the treatment of pain with gain-of-function mutations in man eliciting a variety of painful disorders and loss-of-function mutations affording insensitivity to pain. Unfort
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6460ec06d229cf43b30709ab80de83e3
https://doi.org/10.1016/j.bmcl.2017.03.085
https://doi.org/10.1016/j.bmcl.2017.03.085
Autor:
Richard L, Kraus, Fuqiang, Zhao, Parul S, Pall, Dan, Zhou, Joshua D, Vardigan, Andrew, Danziger, Yuxing, Li, Christopher, Daley, Jeanine E, Ballard, Michelle K, Clements, Rebecca M, Klein, Marie A, Holahan, Thomas J, Greshock, Ronald M, Kim, Mark E, Layton, Christopher S, Burgey, Jordi, Serra, Darrell A, Henze, Andrea K, Houghton
Publikováno v:
Science translational medicine. 13(594)
Humans with loss-of-function mutations in the Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::f9833016998efa2956e0258637677db9
https://pubmed.ncbi.nlm.nih.gov/34011626
https://pubmed.ncbi.nlm.nih.gov/34011626
Autor:
Carmen A. Ufret-Vincenty, Marcus D. Collins, Mario G. Rosasco, Gilbert Q. Martinez, Rebecca M. Klein, Sharona E. Gordon
Publikováno v:
The Journal of General Physiology
Phosphoinositides bind to a selective site in the proximal C-terminal region to regulate TRPV1.
Although PI(4,5)P2 is believed to play an essential role in regulating the activity of numerous ion channels and transporters, the mechanisms by whic
Although PI(4,5)P2 is believed to play an essential role in regulating the activity of numerous ion channels and transporters, the mechanisms by whic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c609fa4ce54bfb0ae85d205e50388a9
http://europepmc.org/articles/PMC4411251
http://europepmc.org/articles/PMC4411251
Publikováno v:
Journal of Biological Chemistry. 283:26208-26216
Once thought of as simply an oily barrier that maintains cellular integrity, lipids are now known to play an active role in a large variety of cellular processes. Phosphoinositides are of particular interest because of their remarkable ability to aff
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::794b119e4c42cd9da92201cf6472eb64
https://doi.org/10.1074/jbc.m801912200
https://doi.org/10.1074/jbc.m801912200