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Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).
Brooks CA, Barton LS, Behm DJ, Brnardic EJ, Costell MH, Holt DA, Jolivette LJ, Matthews JM, McAtee JJ, McCleland BW, Patterson JR, Pero JE, Rivero RA, Roethke TJ, Sanchez RM, Shenje R, Terrell LR, Lawhorn BG. Brooks CA, et al. Among authors: lawhorn bg. J Med Chem. 2019 Oct 24;62(20):9270-9280. doi: 10.1021/acs.jmedchem.9b01247. Epub 2019 Oct 9. J Med Chem. 2019. PMID: 31532662
Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).
Brnardic EJ, Ye G, Brooks C, Donatelli C, Barton L, McAtee J, Sanchez RM, Shu A, Erhard K, Terrell L, Graczyk-Millbrandt G, He Y, Costell MH, Behm DJ, Roethke T, Stoy P, Holt DA, Lawhorn BG. Brnardic EJ, et al. Among authors: lawhorn bg. J Med Chem. 2018 Nov 8;61(21):9738-9755. doi: 10.1021/acs.jmedchem.8b01317. Epub 2018 Oct 18. J Med Chem. 2018. PMID: 30335378
Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.
Pero JE, Matthews JM, Behm DJ, Brnardic EJ, Brooks C, Budzik BW, Costell MH, Donatelli CA, Eisennagel SH, Erhard K, Fischer MC, Holt DA, Jolivette LJ, Li H, Li P, McAtee JJ, McCleland BW, Pendrak I, Posobiec LM, Rivera KLK, Rivero RA, Roethke TJ, Sender MR, Shu A, Terrell LR, Vaidya K, Xu X, Lawhorn BG. Pero JE, et al. Among authors: lawhorn bg. J Med Chem. 2018 Dec 27;61(24):11209-11220. doi: 10.1021/acs.jmedchem.8b01344. Epub 2018 Dec 12. J Med Chem. 2018. PMID: 30500190
TRPV4 antagonists: a patent review (2015-2020).
Lawhorn BG, Brnardic EJ, Behm DJ. Lawhorn BG, et al. Expert Opin Ther Pat. 2021 Sep;31(9):773-784. doi: 10.1080/13543776.2021.1903432. Epub 2021 Mar 24. Expert Opin Ther Pat. 2021. PMID: 33724130 Review.
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).
Brooks CA, Barton LS, Behm DJ, Eidam HS, Fox RM, Hammond M, Hoang TH, Holt DA, Hilfiker MA, Lawhorn BG, Patterson JR, Stoy P, Roethke TJ, Ye G, Zhao S, Thorneloe KS, Goodman KB, Cheung M. Brooks CA, et al. Among authors: lawhorn bg. ACS Med Chem Lett. 2019 Jul 15;10(8):1228-1233. doi: 10.1021/acsmedchemlett.9b00274. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31413810 Free PMC article.
Recent advances in TRPV4 agonists and antagonists.
Lawhorn BG, Brnardic EJ, Behm DJ. Lawhorn BG, et al. Bioorg Med Chem Lett. 2020 Apr 15;30(8):127022. doi: 10.1016/j.bmcl.2020.127022. Epub 2020 Feb 8. Bioorg Med Chem Lett. 2020. PMID: 32063431 Review.
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Lawhorn BG, Philp J, Zhao Y, Louer C, Hammond M, Cheung M, Fries H, Graves AP, Shewchuk L, Wang L, Cottom JE, Qi H, Zhao H, Totoritis R, Zhang G, Schwartz B, Li H, Sweitzer S, Holt DA, Gatto GJ Jr, Kallander LS. Lawhorn BG, et al. J Med Chem. 2015 Sep 24;58(18):7431-48. doi: 10.1021/acs.jmedchem.5b00931. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26355916
22 results