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Page 1
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.
Roecker AJ, Layton ME, Pero JE, Kelly MJ 3rd, Greshock TJ, Kraus RL, Li Y, Klein R, Clements M, Daley C, Jovanovska A, Ballard JE, Wang D, Zhao F, Brunskill APJ, Peng X, Wang X, Sun H, Houghton AK, Burgey CS. Roecker AJ, et al. Among authors: jovanovska a. ACS Med Chem Lett. 2021 Jun 1;12(6):1038-1049. doi: 10.1021/acsmedchemlett.1c00218. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141090 Free PMC article.
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice.
Roecker AJ, Egbertson M, Jones KLG, Gomez R, Kraus RL, Li Y, Koser AJ, Urban MO, Klein R, Clements M, Panigel J, Daley C, Wang J, Finger EN, Majercak J, Santarelli V, Gregan I, Cato M, Filzen T, Jovanovska A, Wang YH, Wang D, Joyce LA, Sherer EC, Peng X, Wang X, Sun H, Coleman PJ, Houghton AK, Layton ME. Roecker AJ, et al. Among authors: jovanovska a. Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093. doi: 10.1016/j.bmcl.2017.03.085. Epub 2017 Mar 30. Bioorg Med Chem Lett. 2017. PMID: 28389149
Benzoxazolinone aryl sulfonamides as potent, selective Nav1.7 inhibitors with in vivo efficacy in a preclinical pain model.
Pero JE, Rossi MA, Lehman HDGF, Kelly MJ 3rd, Mulhearn JJ, Wolkenberg SE, Cato MJ, Clements MK, Daley CJ, Filzen T, Finger EN, Gregan Y, Henze DA, Jovanovska A, Klein R, Kraus RL, Li Y, Liang A, Majercak JM, Panigel J, Urban MO, Wang J, Wang YH, Houghton AK, Layton ME. Pero JE, et al. Among authors: jovanovska a. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2683-2688. doi: 10.1016/j.bmcl.2017.04.040. Epub 2017 Apr 22. Bioorg Med Chem Lett. 2017. PMID: 28465103
Trazodone inhibits T-type calcium channels.
Kraus RL, Li Y, Jovanovska A, Renger JJ. Kraus RL, et al. Among authors: jovanovska a. Neuropharmacology. 2007 Aug;53(2):308-17. doi: 10.1016/j.neuropharm.2007.05.011. Epub 2007 May 26. Neuropharmacology. 2007. PMID: 17610910
Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3).
Kuduk SD, Di Marco CN, Chang RK, Dipardo RM, Cook SP, Cato MJ, Jovanovska A, Urban MO, Leitl M, Spencer RH, Kane SA, Bilodeau MT, Hartman GD, Bock MG. Kuduk SD, et al. Among authors: jovanovska a. Bioorg Med Chem Lett. 2009 May 1;19(9):2514-8. doi: 10.1016/j.bmcl.2009.03.029. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19339181
Identification of potent inhibitors of the sortilin-progranulin interaction.
Stachel SJ, Ginnetti AT, Johnson SA, Cramer P, Wang Y, Bukhtiyarova M, Krosky D, Stump C, Hurzy DM, Schlegel KA, Cooke AJ, Allen S, O'Donnell G, Ziebell M, Parthasarathy G, Getty KL, Ho T, Ou Y, Jovanovska A, Carroll SS, Pausch M, Lumb K, Mosser SD, Voleti B, Klein DJ, Soisson SM, Zerbinatti C, Coleman PJ. Stachel SJ, et al. Among authors: jovanovska a. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127403. doi: 10.1016/j.bmcl.2020.127403. Epub 2020 Jul 15. Bioorg Med Chem Lett. 2020. PMID: 32738972
High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.
Wolkenberg SE, Zhao Z, Mulhearn JJ, Harrison ST, Sanders JM, Cato MJ, Jovanovska A, Panigel J, Cook SP, Henze DA, Kane SA, Hartman GD, Barrow JC. Wolkenberg SE, et al. Among authors: jovanovska a. Bioorg Med Chem Lett. 2011 May 1;21(9):2646-9. doi: 10.1016/j.bmcl.2010.12.115. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21257308
Amidine derived inhibitors of acid-sensing ion channel-3 (ASIC3).
Kuduk SD, Chang RK, Wai JM, Di Marco CN, Cofre V, DiPardo RM, Cook SP, Cato MJ, Jovanovska A, Urban MO, Leitl M, Spencer RH, Kane SA, Hartman GD, Bilodeau MT. Kuduk SD, et al. Among authors: jovanovska a. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4059-63. doi: 10.1016/j.bmcl.2009.06.021. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19553111
Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3).
Kuduk SD, Chang RK, Di Marco CN, Dipardo RM, Cook SP, Cato MJ, Jovanovska A, Urban MO, Leitl M, Spencer RH, Kane SA, Hartman GD, Bilodeau MT. Kuduk SD, et al. Among authors: jovanovska a. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4255-8. doi: 10.1016/j.bmcl.2011.05.064. Epub 2011 May 27. Bioorg Med Chem Lett. 2011. PMID: 21669528
Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567.
Kuduk SD, Di Marco CN, Bodmer-Narkevitch V, Cook SP, Cato MJ, Jovanovska A, Urban MO, Leitl M, Sain N, Liang A, Spencer RH, Kane SA, Hartman GD, Bilodeau MT. Kuduk SD, et al. Among authors: jovanovska a. ACS Chem Neurosci. 2010 Jan 20;1(1):19-24. doi: 10.1021/cn9000186. Epub 2009 Oct 6. ACS Chem Neurosci. 2010. PMID: 22778804 Free PMC article.
46 results