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Page 1
Activation of the Amino Acid Response Pathway Blunts the Effects of Cardiac Stress.
Qin P, Arabacilar P, Bernard RE, Bao W, Olzinski AR, Guo Y, Lal H, Eisennagel SH, Platchek MC, Xie W, Del Rosario J, Nayal M, Lu Q, Roethke T, Schnackenberg CG, Wright F, Quaile MP, Halsey WS, Hughes AM, Sathe GM, Livi GP, Kirkpatrick RB, Qu XA, Rajpal DK, Faelth Savitski M, Bantscheff M, Joberty G, Bergamini G, Force TL, Gatto GJ Jr, Hu E, Willette RN. Qin P, et al. Among authors: roethke t. J Am Heart Assoc. 2017 May 9;6(5):e004453. doi: 10.1161/JAHA.116.004453. J Am Heart Assoc. 2017. PMID: 28487390 Free PMC article.
An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
Thorneloe KS, Cheung M, Bao W, Alsaid H, Lenhard S, Jian MY, Costell M, Maniscalco-Hauk K, Krawiec JA, Olzinski A, Gordon E, Lozinskaya I, Elefante L, Qin P, Matasic DS, James C, Tunstead J, Donovan B, Kallal L, Waszkiewicz A, Vaidya K, Davenport EA, Larkin J, Burgert M, Casillas LN, Marquis RW, Ye G, Eidam HS, Goodman KB, Toomey JR, Roethke TJ, Jucker BM, Schnackenberg CG, Townsley MI, Lepore JJ, Willette RN. Thorneloe KS, et al. Sci Transl Med. 2012 Nov 7;4(159):159ra148. doi: 10.1126/scitranslmed.3004276. Sci Transl Med. 2012. PMID: 23136043
Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase.
Thalji RK, McAtee JJ, Belyanskaya S, Brandt M, Brown GD, Costell MH, Ding Y, Dodson JW, Eisennagel SH, Fries RE, Gross JW, Harpel MR, Holt DA, Israel DI, Jolivette LJ, Krosky D, Li H, Lu Q, Mandichak T, Roethke T, Schnackenberg CG, Schwartz B, Shewchuk LM, Xie W, Behm DJ, Douglas SA, Shaw AL, Marino JP Jr. Thalji RK, et al. Among authors: roethke t. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3584-8. doi: 10.1016/j.bmcl.2013.04.019. Epub 2013 Apr 16. Bioorg Med Chem Lett. 2013. PMID: 23664879
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Cheung M, Bao W, Behm DJ, Brooks CA, Bury MJ, Dowdell SE, Eidam HS, Fox RM, Goodman KB, Holt DA, Lee D, Roethke TJ, Willette RN, Xu X, Ye G, Thorneloe KS. Cheung M, et al. Among authors: roethke tj. ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. doi: 10.1021/acsmedchemlett.7b00094. eCollection 2017 May 11. ACS Med Chem Lett. 2017. PMID: 28523109 Free PMC 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 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: roethke tj. 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
Development of potent and selective small-molecule human Urotensin-II antagonists.
McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ. McAtee JJ, et al. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10. Bioorg Med Chem Lett. 2008. PMID: 18502123
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ. McAtee JJ, et al. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. doi: 10.1016/j.bmcl.2008.05.058. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18524591
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: roethke tj. 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: roethke t. 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
25 results