Recent advances in TRPV4 agonists and antagonists
Lawhorn, Brian G., Brnardic, Edward J., Behm, David J.
Published in Bioorganic & medicinal chemistry letters (15.04.2020)
Published in Bioorganic & medicinal chemistry letters (15.04.2020)
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Journal Article
TRPV4 antagonists: a patent review (2015-2020)
Lawhorn, Brian G, Brnardic, Edward J, Behm, David J
Published in Expert opinion on therapeutic patents (02.09.2021)
Published in Expert opinion on therapeutic patents (02.09.2021)
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Journal Article
Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions
Patterson, Jaclyn R, Terrell, Lamont R, Donatelli, Carla A, Holt, Dennis A, Jolivette, Larry J, Rivero, Ralph A, Roethke, Theresa J, Shu, Arthur, Stoy, Patrick, Ye, Guosen, Youngman, Mark, Lawhorn, Brian G
Published in Journal of medicinal chemistry (10.12.2020)
Published in Journal of medicinal chemistry (10.12.2020)
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Journal Article
4,6-Diaminopyrimidines as Highly Preferred Troponin I‑Interacting Kinase (TNNI3K) Inhibitors
Philp, Joanne, Lawhorn, Brian G, Graves, Alan P, Shewchuk, Lisa, Rivera, Katrina L, Jolivette, Larry J, Holt, Dennis A, Gatto, Gregory J, Kallander, Lara S
Published in Journal of medicinal chemistry (12.04.2018)
Published in Journal of medicinal chemistry (12.04.2018)
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Journal Article
Substituent Effects on Drug–Receptor H‑bond Interactions: Correlations Useful for the Design of Kinase Inhibitors
Lawhorn, Brian G, Philp, Joanne, Graves, Alan P, Holt, Dennis A, Gatto, Gregory J, Kallander, Lara S
Published in Journal of medicinal chemistry (08.12.2016)
Published in Journal of medicinal chemistry (08.12.2016)
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Journal Article
Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid‑4 (TRPV4)
Brnardic, Edward J, Ye, Guosen, Brooks, Carl, Donatelli, Carla, Barton, Linda, McAtee, Jeff, Sanchez, Robert M, Shu, Arthur, Erhard, Karl, Terrell, Lamont, Graczyk-Millbrandt, Grazyna, He, Yanan, Costell, Melissa H, Behm, David J, Roethke, Theresa, Stoy, Patrick, Holt, Dennis A, Lawhorn, Brian G
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
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Journal Article
Inhibition of the cardiomyocyte-specific kinase TNNI3K limits oxidative stress, injury, and adverse remodeling in the ischemic heart
Vagnozzi, Ronald J, Gatto, Jr, Gregory J, Kallander, Lara S, Hoffman, Nicholas E, Mallilankaraman, Karthik, Ballard, Victoria L T, Lawhorn, Brian G, Stoy, Patrick, Philp, Joanne, Graves, Alan P, Naito, Yoshiro, Lepore, John J, Gao, Erhe, Madesh, Muniswamy, Force, Thomas
Published in Science translational medicine (16.10.2013)
Published in Science translational medicine (16.10.2013)
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Journal Article
Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid‑4 (TRPV4)
Brooks, Carl A, Barton, Linda S, Behm, David J, Brnardic, Edward J, Costell, Melissa H, Holt, Dennis A, Jolivette, Larry J, Matthews, Jay M, McAtee, John J, McCleland, Brent W, Patterson, Jaclyn R, Pero, Joseph E, Rivero, Ralph A, Roethke, Theresa J, Sanchez, Robert M, Shenje, Raynold, Terrell, Lamont R, Lawhorn, Brian G
Published in Journal of medicinal chemistry (24.10.2019)
Published in Journal of medicinal chemistry (24.10.2019)
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Journal Article
Identification of Purines and 7‑Deazapurines as Potent and Selective Type I Inhibitors of Troponin I‑Interacting Kinase (TNNI3K)
Lawhorn, Brian G, Philp, Joanne, Zhao, Yongdong, Louer, Christopher, Hammond, Marlys, Cheung, Mui, Fries, Harvey, Graves, Alan P, Shewchuk, Lisa, Wang, Liping, Cottom, Joshua E, Qi, Hongwei, Zhao, Huizhen, Totoritis, Rachel, Zhang, Guofeng, Schwartz, Benjamin, Li, Hu, Sweitzer, Sharon, Holt, Dennis A, Gatto, Gregory J, Kallander, Lara S
Published in Journal of medicinal chemistry (24.09.2015)
Published in Journal of medicinal chemistry (24.09.2015)
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Journal Article
Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid‑4 with in Vivo Activity in a Pulmonary Edema Model
Pero, Joseph E, Matthews, Jay M, Behm, David J, Brnardic, Edward J, Brooks, Carl, Budzik, Brian W, Costell, Melissa H, Donatelli, Carla A, Eisennagel, Stephen H, Erhard, Karl, Fischer, Michael C, Holt, Dennis A, Jolivette, Larry J, Li, Huijie, Li, Peng, McAtee, John J, McCleland, Brent W, Pendrak, Israil, Posobiec, Lorraine M, Rivera, Katrina L.K, Rivero, Ralph A, Roethke, Theresa J, Sender, Matthew R, Shu, Arthur, Terrell, Lamont R, Vaidya, Kalindi, Xu, Xiaoping, Lawhorn, Brian G
Published in Journal of medicinal chemistry (27.12.2018)
Published in Journal of medicinal chemistry (27.12.2018)
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Journal Article
Identification, Synthesis, and Characterization of a Major Circulating Human Metabolite of TRPV4 Antagonist GSK2798745
Pero, Joseph E, McAtee, John J, Behm, David J, Briand, Jacques, Graczyk-Millbrandt, Grazyna, Erhard, Karl, Roberts, Andrew D, Rivero, Ralph A, Holt, Dennis A, Lawhorn, Brian G
Published in ACS medicinal chemistry letters (09.09.2021)
Published in ACS medicinal chemistry letters (09.09.2021)
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Journal Article
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4)
Brooks, Carl A, Barton, Linda S, Behm, David J, Eidam, Hilary S, Fox, Ryan M, Hammond, Marlys, Hoang, Tram H, Holt, Dennis A, Hilfiker, Mark A, Lawhorn, Brian G, Patterson, Jaclyn R, Stoy, Patrick, Roethke, Theresa J, Ye, Guosen, Zhao, Steve, Thorneloe, Kevin S, Goodman, Krista B, Cheung, Mui
Published in ACS medicinal chemistry letters (08.08.2019)
Published in ACS medicinal chemistry letters (08.08.2019)
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Journal Article
Top Down Characterization of Larger Proteins (45 kDa) by Electron Capture Dissociation Mass Spectrometry
Ge, Ying, Lawhorn, Brian G, ElNaggar, Mariam, Strauss, Erick, Park, Joo-Heon, Begley, Tadhg P, McLafferty, Fred W
Published in Journal of the American Chemical Society (30.01.2002)
Published in Journal of the American Chemical Society (30.01.2002)
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Journal Article
Structure-Activity Relationship Studies of Fostriecin, Cytostatin, and Key Analogs, with PP1, PP2A, PP5, and (β12âβ13)-Chimeras (PP1/PP2A and PP5/PP2A), Provide Further Insight into the Inhibitory Actions of Fostriecin Family Inhibitors
Swingle, Mark R, Amable, Lauren, Lawhorn, Brian G, Buck, Suzanne B, Burke, Christopher P, Ratti, Pukar, Fischer, Kimberly L, Boger, Dale L, Honkanen, Richard E
Published in The Journal of pharmacology and experimental therapeutics (01.10.2009)
Published in The Journal of pharmacology and experimental therapeutics (01.10.2009)
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Journal Article
Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1
Kallander, Lara S., Washburn, David, Hilfiker, Mark A., Eidam, Hilary Schenck, Lawhorn, Brian G., Prendergast, Joanne, Fox, Ryan, Dowdell, Sarah, Manns, Sharada, Hoang, Tram, Zhao, Steve, Ye, Guosen, Hammond, Marlys, Holt, Dennis A., Roethke, Theresa, Hong, Xuan, Reid, Robert A., Gampe, Robert, Zhang, Hong, Diaz, Elsie, Rendina, Alan R., Quinn, Amy M., Willette, Bob
Published in ACS medicinal chemistry letters (12.07.2018)
Published in ACS medicinal chemistry letters (12.07.2018)
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Journal Article
Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition
Lawhorn, Brian G., Tran, Tritin, Hong, Victor S., Morgan, Lisa A., Le, BaoChau T., Harpel, Mark R., Jolivette, Larry, Diaz, Elsie, Schwartz, Benjamin, Gross, Jeffrey W., Tomaszek, Thaddeus, Semus, Simon, Concha, Nestor, Smallwood, Angela, Holt, Dennis A., Kallander, Lara S.
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
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Journal Article
Total Synthesis and Evaluation of Cytostatin, Its C10−C11 Diastereomers, and Additional Key Analogues: Impact on PP2A Inhibition
Lawhorn, Brian G, Boga, Sobhana B, Wolkenberg, Scott E, Colby, David A, Gauss, Carla-Maria, Swingle, Mark R, Amable, Lauren, Honkanen, Richard E, Boger, Dale L
Published in Journal of the American Chemical Society (27.12.2006)
Published in Journal of the American Chemical Society (27.12.2006)
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Journal Article