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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. Among authors: moechars d. 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
Discovery of N-(Pyridin-4-yl)-1,5-naphthyridin-2-amines as Potential Tau Pathology PET Tracers for Alzheimer's Disease.
Rombouts FJ, Andrés JI, Ariza M, Alonso JM, Austin N, Bottelbergs A, Chen L, Chupakhin V, Cleiren E, Fierens K, Fontana A, Langlois X, Leenaerts JE, Mariën J, Martínez Lamenca C, Salter R, Schmidt ME, Te Riele P, Wintmolders C, Trabanco AA, Zhang W, Macdonald G, Moechars D. Rombouts FJ, et al. Among authors: moechars d. J Med Chem. 2017 Feb 23;60(4):1272-1291. doi: 10.1021/acs.jmedchem.6b01173. Epub 2017 Feb 10. J Med Chem. 2017. PMID: 28106992
Evaluation of a Series of β-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads.
Oehlrich D, Peschiulli A, Tresadern G, Van Gool M, Vega JA, De Lucas AI, Alonso de Diego SA, Prokopcova H, Austin N, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Rombouts FJR, Macdonald G, Moechars D, Gijsen HJM, Trabanco AA. Oehlrich D, et al. Among authors: moechars d. ACS Med Chem Lett. 2019 Jul 2;10(8):1159-1165. doi: 10.1021/acsmedchemlett.9b00181. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31413800 Free PMC article.
Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors.
Tresadern G, Delgado F, Delgado O, Gijsen H, Macdonald GJ, Moechars D, Rombouts F, Alexander R, Spurlino J, Van Gool M, Vega JA, Trabanco AA. Tresadern G, et al. Among authors: moechars d. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7255-60. doi: 10.1016/j.bmcl.2011.10.050. Epub 2011 Oct 20. Bioorg Med Chem Lett. 2011. PMID: 22071305
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: moechars d. Neurobiol Dis. 2021 Jul;154:105365. doi: 10.1016/j.nbd.2021.105365. Epub 2021 Apr 10. Neurobiol Dis. 2021. PMID: 33848635 Free article.
BACE1 Dynamics Upon Inhibition with a BACE Inhibitor and Correlation to Downstream Alzheimer's Disease Markers in Elderly Healthy Participants.
Timmers M, Barão S, Van Broeck B, Tesseur I, Slemmon J, De Waepenaert K, Bogert J, Shaw LM, Engelborghs S, Moechars D, Mercken M, Van Nueten L, Tritsmans L, de Strooper B, Streffer JR. Timmers M, et al. Among authors: moechars d. J Alzheimers Dis. 2017;56(4):1437-1449. doi: 10.3233/JAD-160829. J Alzheimers Dis. 2017. PMID: 28157093 Free PMC article. Clinical Trial.
Phenotypic and biochemical analyses of BACE1- and BACE2-deficient mice.
Dominguez D, Tournoy J, Hartmann D, Huth T, Cryns K, Deforce S, Serneels L, Camacho IE, Marjaux E, Craessaerts K, Roebroek AJ, Schwake M, D'Hooge R, Bach P, Kalinke U, Moechars D, Alzheimer C, Reiss K, Saftig P, De Strooper B. Dominguez D, et al. Among authors: d hooge r, moechars d. J Biol Chem. 2005 Sep 2;280(35):30797-806. doi: 10.1074/jbc.M505249200. Epub 2005 Jun 29. J Biol Chem. 2005. PMID: 15987683 Free article.
121 results