Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Brian G. Lawhorn"'
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:
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5651a745bf69cfd3239b6d132d9cebae
https://doi.org/10.1021/acs.jmedchem.9b01247
https://doi.org/10.1021/acs.jmedchem.9b01247
Autor:
Eidam Hilary Schenck, Theresa J. Roethke, Linda S. Barton, Fox Ryan Michael, Steve Zhao, Kevin S. Thorneloe, David J. Behm, Guosen Ye, Patrick Stoy, Mui Cheung, Tram H. Hoang, Dennis A. Holt, Krista B. Goodman, Brian G. Lawhorn, Marlys Hammond, Mark A. Hilfiker, Carl Brooks, Jaclyn R. Patterson
Publikováno v:
ACS Med Chem Lett
[Image: see text] GSK2798745, a clinical candidate, was identified as an inhibitor of the transient receptor potential vanilloid 4 (TRPV4) ion channel for the treatment of pulmonary edema associated with congestive heart failure. We discuss the lead
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a9fa0019b6d3c13ef62367e4364c46c
https://doi.org/10.1021/acsmedchemlett.9b00274
https://doi.org/10.1021/acsmedchemlett.9b00274
Publikováno v:
Expert opinion on therapeutic patents. 31(9)
Introduction: Transient receptor potential vanilloid 4 (TRPV4) is an ion channel that is widely expressed and is activated by numerous chemical, osmotic and mechanical stimuli. By modulating Ca2+ e...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2df174d61b286a551dea195f73405e07
https://pubmed.ncbi.nlm.nih.gov/33724130
https://pubmed.ncbi.nlm.nih.gov/33724130
Publikováno v:
The Journal of organic chemistry. 86(4)
A two-step metal-halogen exchange and diastereoselective copper-mediated Michael addition onto a complex α,β-unsaturated system has been developed and applied toward the synthesis of bisaryl Nrf2 activators. Optimization of metal-halogen exchange u
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de9144e1fb3bcc9bf8439af538a6c141
https://pubmed.ncbi.nlm.nih.gov/33555189
https://pubmed.ncbi.nlm.nih.gov/33555189
Autor:
Guosen Ye, Arthur Shu, Dennis A. Holt, Patrick Stoy, Carla A. Donatelli, Larry J. Jolivette, Ralph A. Rivero, Mark Youngman, Lamont Roscoe Terrell, Jaclyn R. Patterson, Brian G. Lawhorn, Theresa J. Roethke
Publikováno v:
Journal of medicinal chemistry. 63(23)
Investigation of TRPV4 as a potential target for the treatment of pulmonary edema associated with heart failure generated a novel series of acyclic amine inhibitors displaying exceptional potency and PK properties. The series arose through a scaffold
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef0c927080fe1de87583cbdaf88c1101
https://pubmed.ncbi.nlm.nih.gov/33201708
https://pubmed.ncbi.nlm.nih.gov/33201708
Autor:
Theresa J. Roethke, Guosen Ye, Hong Zhang, Robert T. Gampe, Robert A. Reid, Brian G. Lawhorn, Tram H. Hoang, Dennis A. Holt, Bob Willette, Marlys Hammond, David G. Washburn, Sharada Manns, Mark A. Hilfiker, Steve Zhao, Fox Ryan Michael, Joanne Prendergast, Eidam Hilary Schenck, Amy M. Quinn, Lara S. Kallander, Sarah E. Dowdell, Alan R. Rendina, Elsie Diaz, Xuan Hong
Publikováno v:
ACS Medicinal Chemistry Letters. 9:736-740
[Image: see text] Bone Morphogenetic Protein 1 (BMP1) inhibition is a potential method for treating fibrosis because BMP1, a member of the zinc metalloprotease family, is required to convert pro-collagen to collagen. A novel class of reverse hydroxam
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d24636bada9e4802bb362a0091a96d4
https://doi.org/10.1021/acsmedchemlett.8b00173
https://doi.org/10.1021/acsmedchemlett.8b00173
Autor:
Alan P. Graves, Brian G. Lawhorn, Lara S. Kallander, Gatto Gregory J, Lisa M. Shewchuk, Dennis A. Holt, Katrina Rivera, Larry J. Jolivette, Joanne Philp
Publikováno v:
Journal of Medicinal Chemistry. 61:3076-3088
Structure-guided progression of a purine-derived series of TNNI3K inhibitors directed design efforts that produced a novel series of 4,6-diaminopyrimidine inhibitors, an emerging kinase binding motif. Herein, we report a detailed understanding of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e81adfdc0fbcb68cbcc4de9922daca1
https://doi.org/10.1021/acs.jmedchem.8b00125
https://doi.org/10.1021/acs.jmedchem.8b00125
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d27228c9d20cf9c45f7b03f4e78e172
https://pubmed.ncbi.nlm.nih.gov/30500190
https://pubmed.ncbi.nlm.nih.gov/30500190
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127022
TRPV4 is a ubiquitously expressed, non-selective cation channel activated by a range of stimuli including hypotonicity, temperature, pH, stretch and endogenous ligands. Agents that modulate TRPV4 are sought as potential therapeutics for the treatment
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7ee5b0303d98c41c4fc6e01b27e2bb2
https://doi.org/10.1016/j.bmcl.2020.127022
https://doi.org/10.1016/j.bmcl.2020.127022