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Page 1
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: kerekes ad. 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 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: kerekes ad. 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
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Yu T, Zhang Y, Kerekes AD, Tagat JR, Doll RJ, Xiao Y, Esposite S, Hruza A, Belanger DB, Voss M, Rainka MP, Basso A, Liu M, Liang L, Sui N, Prelusky D, Rindgen D, Zhang L. Yu T, et al. Among authors: kerekes ad. Bioorg Med Chem Lett. 2018 May 1;28(8):1397-1403. doi: 10.1016/j.bmcl.2018.02.037. Epub 2018 Feb 23. Bioorg Med Chem Lett. 2018. PMID: 29545102
Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core.
Yu T, Tagat JR, Kerekes AD, Doll RJ, Zhang Y, Xiao Y, Esposite S, Belanger DB, Curran PJ, Mandal AK, Siddiqui MA, Shih NY, Basso AD, Liu M, Gray K, Tevar S, Jones J, Lee S, Liang L, Ponery S, Smith EB, Hruza A, Voigt J, Ramanathan L, Prosise W, Hu M. Yu T, et al. Among authors: kerekes ad. ACS Med Chem Lett. 2010 Jun 7;1(5):214-8. doi: 10.1021/ml100063w. eCollection 2010 Aug 12. ACS Med Chem Lett. 2010. PMID: 24900197 Free PMC article.
Concise syntheses and HCV NS5B polymerase inhibition of (2'R)-3 and (2'S)-2'-ethynyluridine-10 and related nucleosides.
Bennett F, Buevich AV, Huang HC, Girijavallabhan V, Kerekes AD, Huang Y, Malikzay A, Smith E, Ferrari E, Senior M, Osterman R, Wang L, Wang J, Pu H, Truong QT, Tawa P, Bogen SL, Davies IW, Weber AE. Bennett F, et al. Among authors: kerekes ad. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5349-5352. doi: 10.1016/j.bmcl.2017.06.064. Epub 2017 Jun 24. Bioorg Med Chem Lett. 2017. PMID: 29056248
SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors.
Basso AD, Liu M, Gray K, Tevar S, Lee S, Liang L, Ponery A, Smith EB, Monsma FJ Jr, Yu T, Zhang Y, Kerekes AD, Esposite S, Xiao Y, Tagat JR, Hicklin DJ, Kirschmeier P. Basso AD, et al. Among authors: kerekes ad. Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33. doi: 10.1007/s00280-011-1568-1. Epub 2011 Feb 5. Cancer Chemother Pharmacol. 2011. PMID: 21298383
2'-Modified Guanosine Analogs for the Treatment of HCV.
Girijavallabhan V, Arasappan A, Bennett F, Chen K, Dang Q, Huang Y, Kerekes A, Nair L, Pissarnitski D, Verma V, Alvarez C, Chen P, Cole D, Esposite S, Huang Y, Hong Q, Liu Z, Pan W, Pu H, Rossman R, Truong Q, Vibulbhan B, Wang J, Zhao Z, Olsen D, Stamford A, Bogen S, Njoroge FG. Girijavallabhan V, et al. Nucleosides Nucleotides Nucleic Acids. 2016 Jun 2;35(6):277-94. doi: 10.1080/15257770.2016.1154968. Epub 2016 Apr 22. Nucleosides Nucleotides Nucleic Acids. 2016. PMID: 27104963
13 results