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Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Arg-guanidine of RGDX mimetics and the platelet GP IIb-IIIa receptor.
Zablocki JA, Miyano M, Garland RB, Pireh D, Schretzman L, Rao SN, Lindmark RJ, Panzer-Knodle SG, Nicholson NS, Taite BB, et al. Zablocki JA, et al. J Med Chem. 1993 Jun 25;36(13):1811-9. doi: 10.1021/jm00065a003. J Med Chem. 1993. PMID: 8515420
A novel series of orally active antiplatelet agents.
Zablocki JA, Tjoeng FS, Bovy PR, Miyano M, Garland RB, Williams K, Schretzman L, Zupec ME, Rico JG, Lindmark RJ, et al. Zablocki JA, et al. Bioorg Med Chem. 1995 May;3(5):539-51. doi: 10.1016/0968-0896(95)00045-i. Bioorg Med Chem. 1995. PMID: 7648203
SC-54684A: an orally active inhibitor of platelet aggregation.
Nicholson NS, Panzer-Knodle SG, Salyers AK, Taite BB, Szalony JA, Haas NF, King LW, Zablocki JA, Keller BT, Broschat K, et al. Nicholson NS, et al. Among authors: zablocki ja. Circulation. 1995 Jan 15;91(2):403-10. doi: 10.1161/01.cir.91.2.403. Circulation. 1995. PMID: 7805244
Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII).
Koltun DO, Parkhill EQ, Kalla R, Perry TD, Elzein E, Li X, Simonovich SP, Ziebenhaus C, Hansen TR, Marchand B, Hung WK, Lagpacan L, Hung M, Aoyama RG, Murray BP, Perry JK, Somoza JR, Villaseñor AG, Pagratis N, Zablocki JA. Koltun DO, et al. Among authors: zablocki ja. Bioorg Med Chem Lett. 2018 Feb 1;28(3):541-546. doi: 10.1016/j.bmcl.2017.10.040. Epub 2017 Oct 20. Bioorg Med Chem Lett. 2018. PMID: 29254643
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Notte GT, Kalla R, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Smith-Maxwell C, Dhalla AK, Rajamani S, Stafford B, Tang J, Mollova N, Belardinelli L, Zablocki JA. Koltun DO, et al. Among authors: zablocki ja. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3202-3206. doi: 10.1016/j.bmcl.2016.03.101. Epub 2016 Mar 30. Bioorg Med Chem Lett. 2016. PMID: 27080178
Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency.
Farand J, Mai N, Chandrasekhar J, Newby ZE, Van Veldhuizen J, Loyer-Drew J, Venkataramani C, Guerrero J, Kwok A, Li N, Zherebina Y, Wilbert S, Zablocki J, Phillips G, Watkins WJ, Mourey R, Notte GT. Farand J, et al. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5926-5930. doi: 10.1016/j.bmcl.2016.10.092. Epub 2016 Nov 2. Bioorg Med Chem Lett. 2016. PMID: 27876318
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