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Page 1
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Milbank JB, Knauer CS, Augelli-Szafran CE, Sakkab-Tan AT, Lin KK, Yamagata K, Hoffman JK, Zhuang N, Thomas J, Galatsis P, Wendt JA, Mickelson JW, Schwarz RD, Kinsora JJ, Lotarski SM, Stakich K, Gillespie KK, Lam WW, Mutlib AE. Milbank JB, et al. Among authors: galatsis p. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. doi: 10.1016/j.bmcl.2007.06.030. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17590335
Carboxylate bioisosteres of pregabalin.
Schwarz JB, Colbry NL, Zhu Z, Nichelson B, Barta NS, Lin K, Hudack RA, Gibbons SE, Galatsis P, DeOrazio RJ, Manning DD, Vartanian MG, Kinsora JJ, Lotarski SM, Li Z, Dickerson MR, El-Kattan A, Thorpe AJ, Donevan SD, Taylor CP, Wustrow DJ. Schwarz JB, et al. Among authors: galatsis p. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3559-63. doi: 10.1016/j.bmcl.2006.03.083. Epub 2006 Apr 18. Bioorg Med Chem Lett. 2006. PMID: 16621528
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL. Zhang L, et al. Among authors: galatsis p. J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24392688
Inhibition of interleukin-1beta converting enzyme (ICE or caspase 1) by aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones.
Galatsis P, Caprathe B, Downing D, Gilmore J, Harter W, Hays S, Kostlan C, Linn K, Lunney E, Para K, Thomas A, Warmus J, Allen H, Brady K, Talanian R, Walker N. Galatsis P, et al. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5089-94. doi: 10.1016/j.bmcl.2010.07.031. Epub 2010 Jul 11. Bioorg Med Chem Lett. 2010. PMID: 20674352
Ligand-protein interactions of selective casein kinase 1δ inhibitors.
Mente S, Arnold E, Butler T, Chakrapani S, Chandrasekaran R, Cherry K, DiRico K, Doran A, Fisher K, Galatsis P, Green M, Hayward M, Humphrey J, Knafels J, Li J, Liu S, Marconi M, McDonald S, Ohren J, Paradis V, Sneed B, Walton K, Wager T. Mente S, et al. Among authors: galatsis p. J Med Chem. 2013 Sep 12;56(17):6819-28. doi: 10.1021/jm4006324. Epub 2013 Aug 28. J Med Chem. 2013. PMID: 23919824
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