Výsledky vyhledávání - "Theresa J. Roethke"

Perspective on high-throughput bioanalysis to support in vitro assays in early drug discovery

Autor: Brandon G Santiago, Stephen H Eisennagel, Gregory E Peckham, Amanda M Liebhardt, Chad L Alburn, Theresa J Roethke, Michael A Reilly, Jens R Sydor, Molly Z Karlinsey

Publikováno v: Bioanalysis. 15:177-191

As the desire for a shortened design/make/test/learn cycle increases in early drug discovery, the pressure to rapidly deliver drug metabolism pharmacokinetic data continues to rise. From a bioanalytical standpoint, in vitro assays are challenging bec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1e8e751797d6b6f729953d29d28319b9
https://doi.org/10.4155/bio-2022-0207

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Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4)

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

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Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4)

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

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Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions

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

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Identification of a Human Whole Blood-Based Endothelial Cell Impedance Assay for Assessing Clinical Transient Receptor Potential Vanilloid 4 Target Engagement Ex Vivo

Autor: Kevin S. Thorneloe, Theresa J. Roethke, Krista B. Goodman, Jaclyn R. Patterson, Dennis L. Sprecher, Navin Goyal, Melissa H. Costell, David J. Behm, Christian H. James, Patrick Stoy, Xiaoping Xu

Publikováno v: The Journal of pharmacology and experimental therapeutics. 376(3)

Transient receptor potential vanilloid 4 (TRPV4) channels expressed on pulmonary endothelial cells are activated by elevated pulmonary vascular pressure, resulting in endothelial shape change, pulmonary barrier disruption, and edema. As such, TRPV4 b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50663aab15250e2bcb3f8a1a370e399c
https://pubmed.ncbi.nlm.nih.gov/33376150

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Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1

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

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Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4

Autor: Theresa J. Roethke, Weike Bao, Dennis A. Holt, David J. Behm, Eidam Hilary Schenck, Dennis Lee, Robert N. Willette, Kevin S. Thorneloe, Guosen Ye, Krista B. Goodman, Fox Ryan Michael, Mui Cheung, Carl Brooks, Sarah E. Dowdell, Xiaoping Xu, Michael Jonathan Bury

Publikováno v: ACS Medicinal Chemistry Letters. 8:549-554

Transient Receptor Potential Vanilloid 4 (TRPV4) is a member of the Transient Receptor Potential (TRP) superfamily of cation channels. TRPV4 is expressed in the vascular endothelium in the lung and regulates the integrity of the alveolar septal barri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::946ddf5ee0cef902be67bf984b1c2a8c
https://doi.org/10.1021/acsmedchemlett.7b00094

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Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4)

Autor: Arthur Shu, Carla A. Donatelli, Sanchez Robert, Melissa H. Costell, Carl Brooks, Yanan He, Jeff J. McAtee, David J. Behm, Guosen Ye, Dennis A. Holt, Theresa J. Roethke, Brian G. Lawhorn, Grazyna Graczyk-Millbrandt, Lamont Roscoe Terrell, Edward J. Brnardic, Patrick Stoy, Linda S. Barton, Karl F. Erhard

Publikováno v: Journal of medicinal chemistry. 61(21)

A novel series of pyrrolidine sulfonamide transient receptor potential vanilloid-4 (TRPV4) antagonists was developed by modification of a previously reported TRPV4 inhibitor (1). Several core-structure modifications were identified that improved TRPV

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::188dc34bb0a3617511cb674a19186ee6
https://pubmed.ncbi.nlm.nih.gov/30335378

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