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Identification and characterization of a MAPT-targeting locked nucleic acid antisense oligonucleotide therapeutic for tauopathies.
Easton A, Jensen ML, Wang C, Hagedorn PH, Li Y, Weed M, Meredith JE, Guss V, Jones K, Gill M, Krause C, Brown JM, Hunihan L, Natale J, Fernandes A, Lu Y, Polino J, Bookbinder M, Cadelina G, Benitex Y, Sane R, Morrison J, Drexler D, Mercer SE, Bon C, Pandya NJ, Jagasia R, Ou Yang TH, Distler T, Grüninger F, Meldgaard M, Terrigno M, Macor JE, Albright CF, Loy J, Hoeg AM, Olson RE, Cacace AM. Easton A, et al. Among authors: polino j. Mol Ther Nucleic Acids. 2022 Aug 4;29:625-642. doi: 10.1016/j.omtn.2022.07.027. eCollection 2022 Sep 13. Mol Ther Nucleic Acids. 2022. PMID: 36090761 Free PMC article.
Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder.
Bristow LJ, Gulia J, Weed MR, Srikumar BN, Li YW, Graef JD, Naidu PS, Sanmathi C, Aher J, Bastia T, Paschapur M, Kalidindi N, Kumar KV, Molski T, Pieschl R, Fernandes A, Brown JM, Sivarao DV, Newberry K, Bookbinder M, Polino J, Keavy D, Newton A, Shields E, Simmermacher J, Kempson J, Li J, Zhang H, Mathur A, Kallem RR, Sinha M, Ramarao M, Vikramadithyan RK, Thangathirupathy S, Warrier J, Islam I, Bronson JJ, Olson RE, Macor JE, Albright CF, King D, Thompson LA, Marcin LR, Sinz M. Bristow LJ, et al. Among authors: polino j. J Pharmacol Exp Ther. 2017 Dec;363(3):377-393. doi: 10.1124/jpet.117.242784. Epub 2017 Sep 27. J Pharmacol Exp Ther. 2017. PMID: 28954811
Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.
Wu YJ, Conway CM, Sun LQ, Machet F, Chen J, Chen P, He H, Bourin C, Calandra V, Polino JL, Davis CD, Heman K, Gribkoff VK, Boissard CG, Knox RJ, Thompson MW, Fitzpatrick W, Weaver D, Harden DG, Natale J, Dworetzky SI, Starrett JE Jr. Wu YJ, et al. Among authors: polino jl. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6188-91. doi: 10.1016/j.bmcl.2013.08.092. Epub 2013 Sep 8. Bioorg Med Chem Lett. 2013. PMID: 24070783
Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1 receptors in rats.
Lelas S, Wong H, Li YW, Heman KL, Ward KA, Zeller KL, Sieracki KK, Polino JL, Godonis HE, Ren SX, Yan XX, Arneric SP, Robertson DW, Hartig PR, Grossman S, Trainor GL, Taub RA, Zaczek R, Gilligan PJ, McElroy JF. Lelas S, et al. Among authors: polino jl. J Pharmacol Exp Ther. 2004 Apr;309(1):293-302. doi: 10.1124/jpet.103.058784. Epub 2004 Jan 23. J Pharmacol Exp Ther. 2004. PMID: 14742750