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Page 1
Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement.
Barton LS, Callahan JF, Cantizani J, Concha NO, Cotillo Torrejon I, Goodwin NC, Joshi-Pangu A, Kiesow TJ, McAtee JJ, Mellinger M, Nixon CJ, Padrón-Barthe L, Patterson JR, Pearson ND, Pouliot JJ, Rendina AR, Buitrago Santanilla A, Schneck JL, Sanz O, Thalji RK, Ward P, Williams SP, King BW. Barton LS, et al. Bioorg Med Chem. 2024 Feb 15;100:117618. doi: 10.1016/j.bmc.2024.117618. Epub 2024 Jan 29. Bioorg Med Chem. 2024. PMID: 38309201
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Tian X, Suarez D, Thomson D, Li W, King EA, LaFrance L, Boehm J, Barton L, Di Marco C, Martyr C, Thalji R, Medina J, Knight S, Heerding D, Gao E, Nartey E, Cecconie T, Nixon C, Zhang G, Berrodin TJ, Phelps C, Patel A, Bai X, Lind K, Prabhu N, Messer J, Zhu Z, Shewchuk L, Reid R, Graves AP, McHugh C, Mangatt B. Tian X, et al. J Med Chem. 2022 Nov 10;65(21):14391-14408. doi: 10.1021/acs.jmedchem.2c00670. Epub 2022 Oct 27. J Med Chem. 2022. PMID: 36302181
Improving the developability profile of pyrrolidine progesterone receptor partial agonists.
Kallander LS, Washburn DG, Hoang TH, Frazee JS, Stoy P, Johnson L, Lu Q, Hammond M, Barton LS, Patterson JR, Azzarano LM, Nagilla R, Madauss KP, Williams SP, Stewart EL, Duraiswami C, Grygielko ET, Xu X, Laping NJ, Bray JD, Thompson SK. Kallander LS, et al. Among authors: barton ls. Bioorg Med Chem Lett. 2010 Jan 1;20(1):371-4. doi: 10.1016/j.bmcl.2009.10.092. Epub 2009 Oct 25. Bioorg Med Chem Lett. 2010. PMID: 19926282
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.
Washburn DG, Holt DA, Dodson J, McAtee JJ, Terrell LR, Barton L, Manns S, Waszkiewicz A, Pritchard C, Gillie DJ, Morrow DM, Davenport EA, Lozinskaya IM, Guss J, Basilla JB, Negron LK, Klein M, Willette RN, Fries RE, Jensen TC, Xu X, Schnackenberg CG, Marino JP Jr. Washburn DG, et al. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4979-84. doi: 10.1016/j.bmcl.2013.06.047. Epub 2013 Jun 26. Bioorg Med Chem Lett. 2013. PMID: 23886683
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: barton ls. 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 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: barton ls. 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.
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. 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
Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.
Samanen JM, Ali FE, Barton LS, Bondinell WE, Burgess JL, Callahan JF, Calvo RR, Chen W, Chen L, Erhard K, Feuerstein G, Heys R, Hwang SM, Jakas DR, Keenan RM, Ku TW, Kwon C, Lee CP, Miller WH, Newlander KA, Nichols A, Parker M, Peishoff CE, Rhodes G, Ross S, Shu A, Simpson R, Takata D, Yellin TO, Uzsinskas I, Venslavsky JW, Yuan CK, Huffman WF. Samanen JM, et al. Among authors: barton ls. J Med Chem. 1996 Dec 6;39(25):4867-70. doi: 10.1021/jm960558a. J Med Chem. 1996. PMID: 8960544 No abstract available.