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Discovery of the Oxadiazine FRM-024: A Potent CNS-Penetrant Gamma Secretase Modulator.
Bursavich MG, Harrison BA, Acharya R, Costa DE, Freeman EA, Hrdlicka LA, Jin H, Kapadnis S, Moffit JS, Murphy D, Nolan SJ, Patzke H, Tang C, Van Voorhies HE, Wen M, Koenig G, Blain JF, Burnett DA. Bursavich MG, et al. Among authors: koenig g. J Med Chem. 2021 Oct 14;64(19):14426-14447. doi: 10.1021/acs.jmedchem.1c00904. Epub 2021 Sep 22. J Med Chem. 2021. PMID: 34550687
Characterization of FRM-36143 as a new γ-secretase modulator for the potential treatment of familial Alzheimer's disease.
Blain JF, Bursavich MG, Freeman EA, Hrdlicka LA, Hodgdon HE, Chen T, Costa DE, Harrison BA, Kapadnis S, Murphy DA, Nolan S, Tu Z, Tang C, Burnett DA, Patzke H, Koenig G. Blain JF, et al. Among authors: koenig g. Alzheimers Res Ther. 2016 Aug 30;8(1):34. doi: 10.1186/s13195-016-0199-5. Alzheimers Res Ther. 2016. PMID: 27572246 Free PMC article.
Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease.
Bursavich MG, Harrison BA, Acharya R, Costa DE, Freeman EA, Hodgdon HE, Hrdlicka LA, Jin H, Kapadnis S, Moffit JS, Murphy DA, Nolan S, Patzke H, Tang C, Wen M, Koenig G, Blain JF, Burnett DA. Bursavich MG, et al. Among authors: koenig g. J Med Chem. 2017 Mar 23;60(6):2383-2400. doi: 10.1021/acs.jmedchem.6b01620. Epub 2017 Mar 10. J Med Chem. 2017. PMID: 28230986
Modulation of γ-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice.
Rogers K, Felsenstein KM, Hrdlicka L, Tu Z, Albayya F, Lee W, Hopp S, Miller MJ, Spaulding D, Yang Z, Hodgdon H, Nolan S, Wen M, Costa D, Blain JF, Freeman E, De Strooper B, Vulsteke V, Scrocchi L, Zetterberg H, Portelius E, Hutter-Paier B, Havas D, Ahlijanian M, Flood D, Leventhal L, Shapiro G, Patzke H, Chesworth R, Koenig G. Rogers K, et al. Among authors: koenig g. Mol Neurodegener. 2012 Dec 18;7:61. doi: 10.1186/1750-1326-7-61. Mol Neurodegener. 2012. PMID: 23249765 Free PMC article.
Discovery of quinuclidine modulators of cellular progranulin.
Lanter JC, Chen AY, Williamson T, Koenig G, Blain JF, Burnett DA. Lanter JC, et al. Among authors: koenig g. Bioorg Med Chem Lett. 2021 Sep 1;47:128209. doi: 10.1016/j.bmcl.2021.128209. Epub 2021 Jun 18. Bioorg Med Chem Lett. 2021. PMID: 34153473
BACE1 Inhibitor MK-8931 Alters Formation but Not Stability of Dendritic Spines.
Blume T, Filser S, Jaworska A, Blain JF, Koenig G, Moschke K, Lichtenthaler SF, Herms J. Blume T, et al. Among authors: koenig g. Front Aging Neurosci. 2018 Jul 26;10:229. doi: 10.3389/fnagi.2018.00229. eCollection 2018. Front Aging Neurosci. 2018. PMID: 30093858 Free PMC article.
α7-nAChR agonist enhances neural plasticity in the hippocampus via a GABAergic circuit.
Townsend M, Whyment A, Walczak JS, Jeggo R, van den Top M, Flood DG, Leventhal L, Patzke H, Koenig G. Townsend M, et al. Among authors: koenig g. J Neurophysiol. 2016 Dec 1;116(6):2663-2675. doi: 10.1152/jn.00243.2016. Epub 2016 Sep 21. J Neurophysiol. 2016. PMID: 27655963 Free PMC article.
Here we report that an alpha(7)-nAChR agonist (FRM-17848) enhances long-term potentiation (LTP) in rat septo-hippocampal slices far below the cellular EC(50) but at a concentration that coincides with multiple functional outcome measures as we reported in Stoiljkovic M, Leventhal …
Here we report that an alpha(7)-nAChR agonist (FRM-17848) enhances long-term potentiation (LTP) in rat septo-hippocampal slices far below th …
Effect of the Histone Deacetylase Inhibitor FRM-0334 on Progranulin Levels in Patients With Progranulin Gene Haploinsufficiency: A Randomized Clinical Trial.
Ljubenkov PA, Edwards L, Iaccarino L, La Joie R, Rojas JC, Koestler M, Harris B, Boeve BF, Borroni B, van Swieten JC, Grossman M, Pasquier F, Frisoni GB, Mummery CJ, Vandenberghe R, Le Ber I, Hannequin D, McGinnis SM, Auriacombe S, Onofrj M, Goodman IJ, Riordan HJ, Wisniewski G, Hesterman J, Marek K, Haynes BA, Patzke H, Koenig G, Hilt D, Moebius H, Boxer AL. Ljubenkov PA, et al. Among authors: koenig g. JAMA Netw Open. 2021 Sep 1;4(9):e2125584. doi: 10.1001/jamanetworkopen.2021.25584. JAMA Netw Open. 2021. PMID: 34559230 Free PMC article. Clinical Trial.
165 results