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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: vos a. 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.
Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor.
Spurny R, Debaveye S, Farinha A, Veys K, Vos AM, Gossas T, Atack J, Bertrand S, Bertrand D, Danielson UH, Tresadern G, Ulens C. Spurny R, et al. Among authors: vos am. Proc Natl Acad Sci U S A. 2015 May 12;112(19):E2543-52. doi: 10.1073/pnas.1418289112. Epub 2015 Apr 27. Proc Natl Acad Sci U S A. 2015. PMID: 25918415 Free PMC article.
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: vos a. 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
Fragment Binding to β-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches.
Rombouts FJR, Alexander R, Cleiren E, De Groot A, Carpentier M, Dijkmans J, Fierens K, Masure S, Moechars D, Palomino-Schätzlein M, Pineda-Lucena A, Trabanco AA, Van Glabbeek D, Vos A, Tresadern G. Rombouts FJR, et al. Among authors: vos a. ACS Omega. 2017 Feb 28;2(2):685-697. doi: 10.1021/acsomega.6b00482. Epub 2017 Feb 24. ACS Omega. 2017. PMID: 28626832 Free PMC article.
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Rombouts FJR, Kusakabe KI, Alexander R, Austin N, Borghys H, De Cleyn M, Dhuyvetter D, Gijsen HJM, Hrupka B, Jacobs T, Jerhaoui S, Lammens L, Leclercq L, Tsubone K, Ueno T, Morimoto K, Einaru S, Sumiyoshi H, Van den Bergh A, Vos A, Surkyn M, Teisman A, Moechars D. Rombouts FJR, et al. Among authors: vos a. J Med Chem. 2021 Oct 14;64(19):14175-14191. doi: 10.1021/acs.jmedchem.1c00935. Epub 2021 Sep 23. J Med Chem. 2021. PMID: 34553934
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.
Peschiulli A, Oehlrich D, Van Gool M, Austin N, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Tresadern G, Rombouts FJR, Macdonald GJ, Moechars D, Trabanco AA, Gijsen HJM. Peschiulli A, et al. Among authors: vos a. ACS Med Chem Lett. 2021 Dec 1;13(1):76-83. doi: 10.1021/acsmedchemlett.1c00445. eCollection 2022 Jan 13. ACS Med Chem Lett. 2021. PMID: 35059126 Free PMC article.
Discovery of an Oral, Beyond-Rule-of-Five Mcl-1 Protein-Protein Interaction Modulator with the Potential of Treating Hematological Malignancies.
Romanov-Michailidis F, Hsiao CC, Urner LM, Jerhaoui S, Surkyn M, Miller B, Vos A, Dominguez Blanco M, Bueters R, Vinken P, Bekkers M, Walker D, Pietrak B, Eyckmans W, Dores-Sousa JL, Joo Koo S, Lento W, Bauser M, Philippar U, Rombouts FJR. Romanov-Michailidis F, et al. Among authors: vos a. J Med Chem. 2023 May 11;66(9):6122-6148. doi: 10.1021/acs.jmedchem.2c01953. Epub 2023 Apr 28. J Med Chem. 2023. PMID: 37114951
1,118 results