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Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors.
Koltun DO, Zilbershtein TM, Migulin VA, Vasilevich NI, Parkhill EQ, Glushkov AI, McGregor MJ, Brunn SA, Chu N, Hao J, Mollova N, Leung K, Chisholm JW, Zablocki J. Koltun DO, et al. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. doi: 10.1016/j.bmcl.2009.06.017. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19577469
CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.
Elzein E, Ibrahim P, Koltun DO, Rehder K, Shenk KD, Marquart TA, Jiang B, Li X, Natero R, Li Y, Nguyen M, Kerwar S, Chu N, Soohoo D, Hao J, Maydanik VY, Lustig DA, Zeng D, Leung K, Zablocki JA. Elzein E, et al. Among authors: koltun do. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6017-21. doi: 10.1016/j.bmcl.2004.09.077. Bioorg Med Chem Lett. 2004. PMID: 15546720
Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors.
Koltun DO, Vasilevich NI, Parkhill EQ, Glushkov AI, Zilbershtein TM, Mayboroda EI, Boze MA, Cole AG, Henderson I, Zautke NA, Brunn SA, Chu N, Hao J, Mollova N, Leung K, Chisholm JW, Zablocki J. Koltun DO, et al. Bioorg Med Chem Lett. 2009 Jun 1;19(11):3050-3. doi: 10.1016/j.bmcl.2009.04.004. Epub 2009 Apr 8. Bioorg Med Chem Lett. 2009. PMID: 19394219
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Hirakawa R, Smith-Maxwell C, Wu L, Dhalla AK, Rajamani S, Mollova N, Stafford B, Tang J, Belardinelli L, Zablocki JA. Koltun DO, et al. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3207-3211. doi: 10.1016/j.bmcl.2016.03.096. Epub 2016 Mar 26. Bioorg Med Chem Lett. 2016. PMID: 27038498
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. 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
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. 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 Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.
Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC. Zablocki JA, et al. Among authors: koltun do. J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27690427
13 results