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Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.
Huang Y, Strobel ED, Ho CY, Reynolds CH, Conway KA, Piesvaux JA, Brenneman DE, Yohrling GJ, Moore Arnold H, Rosenthal D, Alexander RS, Tounge BA, Mercken M, Vandermeeren M, Parker MH, Reitz AB, Baxter EW. Huang Y, et al. Among authors: mercken m. Bioorg Med Chem Lett. 2010 May 15;20(10):3158-60. doi: 10.1016/j.bmcl.2010.03.097. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20399652
2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead.
Baxter EW, Conway KA, Kennis L, Bischoff F, Mercken MH, Winter HL, Reynolds CH, Tounge BA, Luo C, Scott MK, Huang Y, Braeken M, Pieters SM, Berthelot DJ, Masure S, Bruinzeel WD, Jordan AD, Parker MH, Boyd RE, Qu J, Alexander RS, Brenneman DE, Reitz AB. Baxter EW, et al. Among authors: mercken mh. J Med Chem. 2007 Sep 6;50(18):4261-4. doi: 10.1021/jm0705408. Epub 2007 Aug 8. J Med Chem. 2007. PMID: 17685503
Passive immunotherapy with a novel antibody against 3pE-modified Aβ demonstrates potential for enhanced efficacy and favorable safety in combination with BACE inhibitor treatment in plaque-depositing mice.
Janssens J, Hermans B, Vandermeeren M, Barale-Thomas E, Borgers M, Willems R, Meulders G, Wintmolders C, Van den Bulck D, Bottelbergs A, Ver Donck L, Larsen P, Moechars D, Edwards W, Mercken M, Van Broeck B. Janssens J, et al. Among authors: mercken m. Neurobiol Dis. 2021 Jul;154:105365. doi: 10.1016/j.nbd.2021.105365. Epub 2021 Apr 10. Neurobiol Dis. 2021. PMID: 33848635 Free article.
Discovery and Functional Characterization of hPT3, a Humanized Anti-Phospho Tau Selective Monoclonal Antibody.
Van Kolen K, Malia TJ, Theunis C, Nanjunda R, Teplyakov A, Ernst R, Wu SJ, Luo J, Borgers M, Vandermeeren M, Bottelbergs A, Wintmolders C, Lacy E, Maurin H, Larsen P, Willems R, Van De Casteele T, Triana-Baltzer G, Slemmon R, Galpern W, Trojanowski JQ, Sun H, Mercken MH. Van Kolen K, et al. Among authors: mercken mh. J Alzheimers Dis. 2020;77(4):1397-1416. doi: 10.3233/JAD-200544. J Alzheimers Dis. 2020. PMID: 32894244
110 results