Zobrazeno 1 - 10
of 46
pro vyhledávání: '"Andrea K. Houghton"'
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:
Fuqiang Zhao, Xiangjun Meng, Sherry Lu, Lynn A. Hyde, Matthew E. Kennedy, Andrea K. Houghton, Jeffrey L. Evelhoch, Catherine D.G. Hines
Publikováno v:
NeuroImage, Vol 213, Iss , Pp 116725- (2020)
Functional magnetic resonance imaging (fMRI) is a valuable tool for studying neural activations in the central nervous system of animals due to its wide spatial coverage and non-invasive nature. However, the advantages of fMRI have not been fully rea
Externí odkaz:
https://doaj.org/article/23615477c4224772ac051ceaf925b948
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
Autor:
Bao Jen Shyong, David G. McLaren, Maria Webb, Joel Mane, Stephen F. Previs, Haihong Zhou, David E. Kelley, Carlos G. Rodriguez, Kevin P. Bateman, Yichen Wang, Daniel P. Downes, Natalie A. Daurio, George H. Addona, Andrea K. Houghton, Ying Chen, Peter Zafian, Ester Carballo-Jane, Rena Zhang
Publikováno v:
American Journal of Physiology-Endocrinology and Metabolism. 316:E1105-E1117
The regulation of nutrient homeostasis, i.e., the ability to transition between fasted and fed states, is fundamental in maintaining health. Since food is typically consumed over limited (anabolic) periods, dietary components must be processed and st
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
Autor:
Anthony J, Roecker, Mark E, Layton, Joseph E, Pero, Michael J, Kelly, Thomas J, Greshock, Richard L, Kraus, Yuxing, Li, Rebecca, Klein, Michelle, Clements, Christopher, Daley, Aneta, Jovanovska, Jeanine E, Ballard, Deping, Wang, Fuqiang, Zhao, Andrew P J, Brunskill, Xuanjia, Peng, Xiu, Wang, Haiyan, Sun, Andrea K, Houghton, Christopher S, Burgey
Publikováno v:
ACS Med Chem Lett
[Image: see text] The voltage-gated sodium channel Na(v)1.7 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 adv
Autor:
Joshua D. Vardigan, Christopher R. Gibson, Darrell A. Henze, Andrea K. Houghton, Marie A. Holahan, Fuqiang Zhao, Parul S. Pall, Richard L. Kraus, Yuxing Li, Jeanine E. Ballard, Christopher S. Burgey
Publikováno v:
Pharmaceutical Research
Purpose This work describes a staged approach to the application of pharmacokinetic-pharmacodynamic (PK-PD) modeling in the voltage-gated sodium ion channel (NaV1.7) inhibitor drug discovery effort to address strategic questions regarding in vitro to
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
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