Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Joseph E. Pero"'
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:
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:
John J. McAtee, Jacques Briand, David J. Behm, Karl F. Erhard, Andrew D. Roberts, Ralph A. Rivero, Brian G. Lawhorn, Joseph E. Pero, Grazyna Graczyk-Millbrandt, Dennis A. Holt
Publikováno v:
ACS Med Chem Lett
[Image: see text] GSK2798745, an antagonist of the transient receptor potential vanilloid 4 (TRPV4) ion channel, was recently investigated in clinical trials for the treatment of cardiac and respiratory diseases. Human plasma and urine samples collec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b6d51b5ede72ceaac42c737d6c5900d
https://europepmc.org/articles/PMC8436415/
https://europepmc.org/articles/PMC8436415/
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:
Joseph E. Pero, Dennis A. Holt, Carl Brooks, Matthews Jay M, Melissa H. Costell, Raynold Shenje, John J. McAtee, David J. Behm, Ralph A. Rivero, Larry J. Jolivette, Sanchez Robert, Brent W. Mccleland, Lamont Roscoe Terrell, Jaclyn R. Patterson, Edward J. Brnardic, Theresa J. Roethke, Brian G. Lawhorn, Linda S. Barton
Publikováno v:
Journal of Medicinal Chemistry. 62:9270-9280
GSK3527497, a preclinical candidate for the inhibition of TRPV4, was identified starting from the previously reported pyrrolidine sulfonamide TRPV4 inhibitors 1 and 2. Optimization of projected human dose was accomplished by specifically focusing on
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:
Brian G. Lawhorn, Brian Budzik, Karl F. Erhard, Huijie Li, Carla A. Donatelli, Kalindi Vaidya, Melissa H. Costell, Joseph E. Pero, John J. McAtee, Carl Brooks, Lorraine M. Posobiec, Larry J. Jolivette, Dennis A. Holt, Theresa J. Roethke, Stephen H. Eisennagel, Michael C. Fischer, Matthews Jay M, Arthur Shu, Brent W. Mccleland, Lamont Roscoe Terrell, Sender Matthew Robert, Katrina Rivera, David J. Behm, Israil Pendrak, Ralph A. Rivero, Xiaoping Xu, Edward J. Brnardic, Peng Li
Publikováno v:
Journal of medicinal chemistry. 61(24)
Pulmonary edema is a common ailment of heart failure patients and has remained an unmet medical need due to dose-limiting side effects associated with current treatments. Preclinical studies in rodents have suggested that inhibition of transient rece
Autor:
Kirsten V. Smith, Joseph E. Pero, Ralph A. Rivero, Donald O. Somers, Vipulkumar Kantibhai Patel, Agnes C. L. Martin, Rachel McMenamin, Sridhar Aravapalli, Finn P. Holding, Eric S. Manas, Lionel Trottet, Alison Jo-Anne Woolford, Neipp Christopher E, Lydia Y. W. Lee, Ranganadh Velagaleti, Sharna J. Rich, Ren Xie, Peng Li, Glyn Williams, Andrew M. Dodson, Brent W. Mccleland, Lee William Page, Joseph P. Marino, Pascal Grondin, Florent Potvain, Joseph E. Coyle, Christopher William Murray, Philip J. Day, Valerio Berdini
Publikováno v:
Journal of Medicinal Chemistry. 59:5356-5367
Elevated levels of human lipoprotein-associated phospholipase A2 (Lp-PLA2) are associated with cardiovascular disease and dementia. A fragment screen was conducted against Lp-PLA2 in order to identify novel inhibitors. Multiple fragment hits were obs
Autor:
Edward C. Sherer, Hannah D. G. F. Lehman, Kerry L. Fillgrove, Robert M. Garbaccio, Jason M. Uslaner, Brian C. Magliaro, Marlene A. Jacobson, Cuyue Tang, Yuhsin Kuo, Rossi Michael A, Michael J. Kelly, Joseph E. Pero, Julie A. O'Brien, Leo A. Joyce, Mark E. Layton, Sarah L. Huszar
Publikováno v:
ACS Medicinal Chemistry Letters. 7:312-317
Investigation of a novel amino-aza-benzimidazolone structural class of positive allosteric modulators (PAMs) of metabotropic glutamate receptor 2 (mGluR2) identified [2.2.2]-bicyclic amine 12 as an intriguing lead structure due to its promising physi
Autor:
Joseph E, Pero, Michael A, Rossi, Hannah D G F, Lehman, Michael J, Kelly, James J, Mulhearn, Scott E, Wolkenberg, Matthew J, Cato, Michelle K, Clements, Christopher J, Daley, Tracey, Filzen, Eleftheria N, Finger, Yun, Gregan, Darrell A, Henze, Aneta, Jovanovska, Rebecca, Klein, Richard L, Kraus, Yuxing, Li, Annie, Liang, John M, Majercak, Jacqueline, Panigel, Mark O, Urban, Jixin, Wang, Ying-Hong, Wang, Andrea K, Houghton, Mark E, Layton
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(12)
Studies on human genetics have suggested that inhibitors of the Na