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Selective inhibitors of the PSEN1-gamma-secretase complex.
Serneels L, Narlawar R, Perez-Benito L, Municoy M, Guallar V, T'Syen D, Dewilde M, Bischoff F, Fraiponts E, Tresadern G, Roevens PWM, Gijsen HJM, De Strooper B. Serneels L, et al. Among authors: gijsen hjm. J Biol Chem. 2023 Jun;299(6):104794. doi: 10.1016/j.jbc.2023.104794. Epub 2023 May 9. J Biol Chem. 2023. PMID: 37164155 Free PMC article.
5-Sulfonyl-benzimidazoles as selective CB2 agonists.
Verbist BM, De Cleyn MA, Surkyn M, Fraiponts E, Aerssens J, Nijsen MJ, Gijsen HJ. Verbist BM, et al. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2574-9. doi: 10.1016/j.bmcl.2008.03.048. Epub 2008 Mar 20. Bioorg Med Chem Lett. 2008. PMID: 18394887
The mechanism of γ-Secretase dysfunction in familial Alzheimer disease.
Chávez-Gutiérrez L, Bammens L, Benilova I, Vandersteen A, Benurwar M, Borgers M, Lismont S, Zhou L, Van Cleynenbreugel S, Esselmann H, Wiltfang J, Serneels L, Karran E, Gijsen H, Schymkowitz J, Rousseau F, Broersen K, De Strooper B. Chávez-Gutiérrez L, et al. EMBO J. 2012 May 16;31(10):2261-74. doi: 10.1038/emboj.2012.79. Epub 2012 Apr 13. EMBO J. 2012. PMID: 22505025 Free PMC article.
Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators.
Oehlrich D, Rombouts FJ, Berthelot D, Bischoff FP, De Cleyn MA, Jaroskova L, Macdonald G, Mercken M, Surkyn M, Trabanco AA, Tresadern G, Van Brandt S, Velter AI, Wu T, Gijsen HJ. Oehlrich D, et al. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4794-800. doi: 10.1016/j.bmcl.2013.06.100. Epub 2013 Jul 11. Bioorg Med Chem Lett. 2013. PMID: 23890837
Anilinotriazoles as potent gamma secretase modulators.
Velter AI, Bischoff FP, Berthelot D, De Cleyn M, Oehlrich D, Jaroskova L, Macdonald G, Minne G, Pieters S, Rombouts F, Van Brandt S, Van Roosbroeck Y, Surkyn M, Trabanco AA, Tresadern G, Wu T, Borghys H, Mercken M, Masungi C, Gijsen H. Velter AI, et al. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5805-5813. doi: 10.1016/j.bmcl.2014.10.024. Epub 2014 Oct 18. Bioorg Med Chem Lett. 2014. PMID: 25454273
1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.
Rombouts FJ, Tresadern G, Delgado O, Martínez-Lamenca C, Van Gool M, García-Molina A, Alonso de Diego SA, Oehlrich D, Prokopcova H, Alonso JM, Austin N, Borghys H, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Alexander R, Macdonald G, Moechars D, Gijsen H, Trabanco AA. Rombouts FJ, et al. J Med Chem. 2015 Oct 22;58(20):8216-35. doi: 10.1021/acs.jmedchem.5b01101. Epub 2015 Oct 10. J Med Chem. 2015. PMID: 26378740
Qualitative changes in human γ-secretase underlie familial Alzheimer's disease.
Szaruga M, Veugelen S, Benurwar M, Lismont S, Sepulveda-Falla D, Lleo A, Ryan NS, Lashley T, Fox NC, Murayama S, Gijsen H, De Strooper B, Chávez-Gutiérrez L. Szaruga M, et al. J Exp Med. 2015 Nov 16;212(12):2003-13. doi: 10.1084/jem.20150892. Epub 2015 Oct 19. J Exp Med. 2015. PMID: 26481686 Free PMC article.
40 results