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Page 1
Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain.
Wu YJ, Guernon J, Shi J, Ditta J, Robbins KJ, Rajamani R, Easton A, Newton A, Bourin C, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: dzierba c. J Med Chem. 2017 Mar 23;60(6):2513-2525. doi: 10.1021/acs.jmedchem.6b01918. Epub 2017 Mar 10. J Med Chem. 2017. PMID: 28234467
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.
Dzierba CD, Takvorian AG, Rafalski M, Kasireddy-Polam P, Wong H, Molski TF, Zhang G, Li YW, Lelas S, Peng Y, McElroy JF, Zaczek RC, Taub RA, Combs AP, Gilligan PJ, Trainor GL. Dzierba CD, et al. J Med Chem. 2004 Nov 4;47(23):5783-90. doi: 10.1021/jm049737f. J Med Chem. 2004. PMID: 15509177
Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.
Dzierba CD, Tebben AJ, Wilde RG, Takvorian AG, Rafalski M, Kasireddy-Polam P, Klaczkiewicz JD, Pechulis AD, Davis AL, Sweet MP, Woo AM, Yang Z, Ebeltoft SM, Molski TF, Zhang G, Zaczek RC, Trainor GL, Combs AP, Gilligan PJ. Dzierba CD, et al. J Med Chem. 2007 May 3;50(9):2269-72. doi: 10.1021/jm0611410. Epub 2007 Apr 3. J Med Chem. 2007. PMID: 17402721
Small molecule receptor protein tyrosine phosphatase γ (RPTPγ) ligands that inhibit phosphatase activity via perturbation of the tryptophan-proline-aspartate (WPD) loop.
Sheriff S, Beno BR, Zhai W, Kostich WA, McDonnell PA, Kish K, Goldfarb V, Gao M, Kiefer SE, Yanchunas J, Huang Y, Shi S, Zhu S, Dzierba C, Bronson J, Macor JE, Appiah KK, Westphal RS, O'Connell J, Gerritz SW. Sheriff S, et al. Among authors: dzierba c. J Med Chem. 2011 Oct 13;54(19):6548-62. doi: 10.1021/jm2003766. Epub 2011 Sep 20. J Med Chem. 2011. PMID: 21882820
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
Dzierba CD, Bi Y, Dasgupta B, Hartz RA, Ahuja V, Cianchetta G, Kumi G, Dong L, Aleem S, Fink C, Garcia Y, Green M, Han J, Kwon S, Qiao Y, Wang J, Zhang Y, Liu Y, Zipp G, Liang Z, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Grace J, Wilson A, Nouraldeen A, Westphal R, Kimball D, Carson K, Bronson JJ, Macor JE. Dzierba CD, et al. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1448-52. doi: 10.1016/j.bmcl.2015.01.036. Epub 2015 Jan 28. Bioorg Med Chem Lett. 2015. PMID: 25690789
The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.
Bi Y, Dzierba CD, Fink C, Garcia Y, Green M, Han J, Kwon S, Kumi G, Liang Z, Liu Y, Qiao Y, Zhang Y, Zipp G, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Westphal RS, Kimball D, Bronson JJ, Macor JE. Bi Y, et al. Among authors: dzierba cd. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1443-7. doi: 10.1016/j.bmcl.2015.02.038. Epub 2015 Feb 21. Bioorg Med Chem Lett. 2015. PMID: 25754495
Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.
Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF. Kostich W, et al. Among authors: dzierba c. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13. J Pharmacol Exp Ther. 2016. PMID: 27411717 Free PMC article.
[3H]BMT-046091 a potent and selective radioligand to determine AAK1 distribution and target engagement.
Louis JV, Lu Y, Pieschl R, Tian Y, Hong Y, Dandapani K, Naidu S, Vikramadithyan RK, Dzierba C, Sarvasiddhi SK, Nara SJ, Bronson J, Macor JE, Albright C, Kostich W, Li YW. Louis JV, et al. Among authors: dzierba c. Neuropharmacology. 2017 May 15;118:167-174. doi: 10.1016/j.neuropharm.2017.03.015. Epub 2017 Mar 15. Neuropharmacology. 2017. PMID: 28315351
Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.
Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: dzierba c. Bioorg Med Chem. 2017 Oct 15;25(20):5490-5505. doi: 10.1016/j.bmc.2017.08.012. Epub 2017 Aug 9. Bioorg Med Chem. 2017. PMID: 28818462
Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.
Wu YJ, Guernon J, McClure A, Venables B, Rajamani R, Robbins KJ, Knox RJ, Matchett M, Pieschl RL, Herrington J, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: dzierba c. Bioorg Med Chem Lett. 2018 Mar 1;28(5):958-962. doi: 10.1016/j.bmcl.2018.01.035. Epub 2018 Feb 1. Bioorg Med Chem Lett. 2018. PMID: 29439904
26 results