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Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor.
Johns DG, Campeau LC, Banka P, Bautmans A, Bueters T, Bianchi E, Branca D, Bulger PG, Crevecoeur I, Ding FX, Garbaccio RM, Guetschow ED, Guo Y, Ha SN, Johnston JM, Josien H, Kauh EA, Koeplinger KA, Kuethe JT, Lai E, Lanning CL, Lee AYH, Li L, Nair AG, O'Neill EA, Stoch SA, Thaisrivongs DA, Tucker TJ, Vachal P, van Dyck K, Vanhoutte FP, Volckaert B, Wolford DG, Xu A, Zhao T, Zhou D, Zhou S, Zhu X, Zokian HJ, Walji AM, Wood HB. Johns DG, et al. Circulation. 2023 Jul 11;148(2):144-158. doi: 10.1161/CIRCULATIONAHA.122.063372. Epub 2023 May 1. Circulation. 2023. PMID: 37125593 Free PMC article.
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Tucker TJ, Embrey MW, Alleyne C, Amin RP, Bass A, Bhatt B, Bianchi E, Branca D, Bueters T, Buist N, Ha SN, Hafey M, He H, Higgins J, Johns DG, Kerekes AD, Koeplinger KA, Kuethe JT, Li N, Murphy B, Orth P, Salowe S, Shahripour A, Tracy R, Wang W, Wu C, Xiong Y, Zokian HJ, Wood HB, Walji A. Tucker TJ, et al. Among authors: johns dg. J Med Chem. 2021 Nov 25;64(22):16770-16800. doi: 10.1021/acs.jmedchem.1c01599. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704436
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.
Alleyne C, Amin RP, Bhatt B, Bianchi E, Blain JC, Boyer N, Branca D, Embrey MW, Ha SN, Jette K, Johns DG, Kerekes AD, Koeplinger KA, LaPlaca D, Li N, Murphy B, Orth P, Ricardo A, Salowe S, Seyb K, Shahripour A, Stringer JR, Sun Y, Tracy R, Wu C, Xiong Y, Youm H, Zokian HJ, Tucker TJ. Alleyne C, et al. Among authors: johns dg. J Med Chem. 2020 Nov 25;63(22):13796-13824. doi: 10.1021/acs.jmedchem.0c01084. Epub 2020 Nov 10. J Med Chem. 2020. PMID: 33170686
A gene expression signature that classifies human atherosclerotic plaque by relative inflammation status.
Puig O, Yuan J, Stepaniants S, Zieba R, Zycband E, Morris M, Coulter S, Yu X, Menke J, Woods J, Chen F, Ramey DR, He X, O'Neill EA, Hailman E, Johns DG, Hubbard BK, Yee Lum P, Wright SD, Desouza MM, Plump A, Reiser V. Puig O, et al. Among authors: johns dg. Circ Cardiovasc Genet. 2011 Dec;4(6):595-604. doi: 10.1161/CIRCGENETICS.111.960773. Epub 2011 Oct 18. Circ Cardiovasc Genet. 2011. PMID: 22010137
Effects of anacetrapib on plasma lipids, apolipoproteins and PCSK9 in healthy, lean rhesus macaques.
Roddy TP, McLaren DG, Chen Y, Xie D, Dunn K, Kulick A, Szeto D, Forrest G, Albanese K, Donnelly M, Gai C, Gewain A, Lederman H, Jensen KK, Ai X, Vachal P, Akinsanya KO, Cleary MA, Previs SF, Dansky HM, Johns DG. Roddy TP, et al. Among authors: johns dg. Eur J Pharmacol. 2014 Oct 5;740:410-6. doi: 10.1016/j.ejphar.2014.04.015. Epub 2014 Apr 21. Eur J Pharmacol. 2014. PMID: 24769414
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Vachal P, Duffy JL, Campeau LC, Amin RP, Mitra K, Murphy BA, Shao PP, Sinclair PJ, Ye F, Katipally R, Lu Z, Ondeyka D, Chen YH, Zhao K, Sun W, Tyagarajan S, Bao J, Wang SP, Cote J, Lipardi C, Metzger D, Leung D, Hartmann G, Wollenberg GK, Liu J, Tan L, Xu Y, Chen Q, Liu G, Blaustein RO, Johns DG. Vachal P, et al. Among authors: johns dg. J Med Chem. 2021 Sep 23;64(18):13215-13258. doi: 10.1021/acs.jmedchem.1c00959. Epub 2021 Aug 10. J Med Chem. 2021. PMID: 34375108
Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach.
Wilson JE, Kurukulasuriya R, Reibarkh M, Reiter M, Zwicker A, Zhao K, Zhang F, Anand R, Colandrea VJ, Cumiskey AM, Crespo A, Duffy RA, Murphy BA, Mitra K, Johns DG, Duffy JL, Vachal P. Wilson JE, et al. Among authors: johns dg. ACS Med Chem Lett. 2016 Jan 4;7(3):261-5. doi: 10.1021/acsmedchemlett.5b00404. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985312 Free PMC article.
Reconstituted HDL elicits marked changes in plasma lipids following single-dose injection in C57Bl/6 mice.
Chen Z, O'Neill EA, Meurer RD, Gagen K, Luell S, Wang SP, Ichetovkin M, Frantz-Wattley B, Eveland S, Strack AM, Fisher TS, Johns DG, Sparrow CP, Wright SD, Hubbard BK, Carballo-Jane E. Chen Z, et al. Among authors: johns dg. J Cardiovasc Pharmacol Ther. 2012 Sep;17(3):315-23. doi: 10.1177/1074248411426144. Epub 2011 Nov 8. J Cardiovasc Pharmacol Ther. 2012. PMID: 22067613
An anti-PCSK9 antibody reduces LDL-cholesterol on top of a statin and suppresses hepatocyte SREBP-regulated genes.
Zhang L, McCabe T, Condra JH, Ni YG, Peterson LB, Wang W, Strack AM, Wang F, Pandit S, Hammond H, Wood D, Lewis D, Rosa R, Mendoza V, Cumiskey AM, Johns DG, Hansen BC, Shen X, Geoghagen N, Jensen K, Zhu L, Wietecha K, Wisniewski D, Huang L, Zhao JZ, Ernst R, Hampton R, Haytko P, Ansbro F, Chilewski S, Chin J, Mitnaul LJ, Pellacani A, Sparrow CP, An Z, Strohl W, Hubbard B, Plump AS, Blom D, Sitlani A. Zhang L, et al. Among authors: johns dg. Int J Biol Sci. 2012;8(3):310-27. doi: 10.7150/ijbs.3524. Epub 2012 Feb 9. Int J Biol Sci. 2012. PMID: 22355267 Free PMC article.
246 results