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Page 1
CryoEM structures of the human CLC-2 voltage gated chloride channel reveal a ball and chain gating mechanism.
Xu M, Neelands T, Powers AS, Liu Y, Miller SD, Pintilie G, Bois JD, Dror RO, Chiu W, Maduke M. Xu M, et al. Among authors: neelands t. bioRxiv [Preprint]. 2023 Nov 29:2023.08.13.553136. doi: 10.1101/2023.08.13.553136. bioRxiv. 2023. Update in: Elife. 2024 Feb 12;12:RP90648. doi: 10.7554/eLife.90648 PMID: 37645939 Free PMC article. Updated. Preprint.
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Nav1.7/ Nav1.8 blockers for the treatment of pain.
Patel MV, Peltier HM, Matulenko MA, Koenig JR, C Scanio MJ, Gum RJ, El-Kouhen OF, Fricano MM, Lundgaard GL, Neelands T, Zhang XF, Zhan C, Pai M, Ghoreishi-Haack N, Hudzik T, Gintant G, Martin R, McGaraughty S, Xu J, Bow D, Kalvass JC, Kym PR, DeGoey DA, Kort ME. Patel MV, et al. Among authors: neelands t. Bioorg Med Chem. 2022 Jun 1;63:116743. doi: 10.1016/j.bmc.2022.116743. Epub 2022 Apr 11. Bioorg Med Chem. 2022. PMID: 35436748
Biological Characterization of F508delCFTR Protein Processing by the CFTR Corrector ABBV-2222/GLPG2222.
Singh AK, Fan Y, Balut C, Alani S, Manelli AM, Swensen AM, Jia Y, Neelands TR, Vortherms TA, Liu B, Searle XB, Wang X, Gao W, Hwang TC, Ren HY, Cyr D, Kym PR, Conrath K, Tse C. Singh AK, et al. Among authors: neelands tr. J Pharmacol Exp Ther. 2020 Jan;372(1):107-118. doi: 10.1124/jpet.119.261800. Epub 2019 Nov 15. J Pharmacol Exp Ther. 2020. PMID: 31732698 Free PMC article.
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.
Gomtsyan A, Schmidt RG, Bayburt EK, Gfesser GA, Voight EA, Daanen JF, Schmidt DL, Cowart MD, Liu H, Altenbach RJ, Kort ME, Clapham B, Cox PB, Shrestha A, Henry R, Whittern DN, Reilly RM, Puttfarcken PS, Brederson JD, Song P, Li B, Huang SM, McDonald HA, Neelands TR, McGaraughty SP, Gauvin DM, Joshi SK, Banfor PN, Segreti JA, Shebley M, Faltynek CR, Dart MJ, Kym PR. Gomtsyan A, et al. Among authors: neelands tr. J Med Chem. 2016 May 26;59(10):4926-47. doi: 10.1021/acs.jmedchem.6b00287. Epub 2016 May 2. J Med Chem. 2016. PMID: 27077528
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
Frost JM, DeGoey DA, Shi L, Gum RJ, Fricano MM, Lundgaard GL, El-Kouhen OF, Hsieh GC, Neelands T, Matulenko MA, Daanen JF, Pai M, Ghoreishi-Haack N, Zhan C, Zhang XF, Kort ME. Frost JM, et al. Among authors: neelands t. J Med Chem. 2016 Apr 14;59(7):3373-91. doi: 10.1021/acs.jmedchem.6b00063. Epub 2016 Apr 5. J Med Chem. 2016. PMID: 27015369
Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.
Voight EA, Gomtsyan AR, Daanen JF, Perner RJ, Schmidt RG, Bayburt EK, DiDomenico S, McDonald HA, Puttfarcken PS, Chen J, Neelands TR, Bianchi BR, Han P, Reilly RM, Franklin PH, Segreti JA, Nelson RA, Su Z, King AJ, Polakowski JS, Baker SJ, Gauvin DM, Lewis LR, Mikusa JP, Joshi SK, Faltynek CR, Kym PR, Kort ME. Voight EA, et al. Among authors: neelands tr. J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21. J Med Chem. 2014. PMID: 25100568
Mechanistic insights into the analgesic efficacy of A-1264087, a novel neuronal Ca(2+) channel blocker that reduces nociception in rat preclinical pain models.
Zhu CZ, Vortherms TA, Zhang M, Xu J, Swensen AM, Niforatos W, Neelands T, Milicic I, Lewis LG, Zhong C, Gauvin D, Mikusa J, Zhan C, Pai M, Roderwald V, Chu KL, Cole EE, Bespalov A, Searle XB, McGaraughty S, Bitner RS, Jarvis MF, Bannon AW, Joshi SK, Scott VE, Lee CH. Zhu CZ, et al. Among authors: neelands t. J Pain. 2014 Apr;15(4):387.e1-14. doi: 10.1016/j.jpain.2013.12.002. Epub 2013 Dec 25. J Pain. 2014. PMID: 24374196 Free article.
Pharmacology of modality-specific transient receptor potential vanilloid-1 antagonists that do not alter body temperature.
Reilly RM, McDonald HA, Puttfarcken PS, Joshi SK, Lewis L, Pai M, Franklin PH, Segreti JA, Neelands TR, Han P, Chen J, Mantyh PW, Ghilardi JR, Turner TM, Voight EA, Daanen JF, Schmidt RG, Gomtsyan A, Kort ME, Faltynek CR, Kym PR. Reilly RM, et al. Among authors: neelands tr. J Pharmacol Exp Ther. 2012 Aug;342(2):416-28. doi: 10.1124/jpet.111.190314. Epub 2012 May 8. J Pharmacol Exp Ther. 2012. PMID: 22570364
45 results