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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: hrupka b. 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
JNJ-40255293, a novel adenosine A2A/A1 antagonist with efficacy in preclinical models of Parkinson's disease.
Atack JR, Shook BC, Rassnick S, Jackson PF, Rhodes K, Drinkenburg WH, Ahnaou A, Te Riele P, Langlois X, Hrupka B, De Haes P, Hendrickx H, Aerts N, Hens K, Wellens A, Vermeire J, Megens AA. Atack JR, et al. Among authors: hrupka b. ACS Chem Neurosci. 2014 Oct 15;5(10):1005-19. doi: 10.1021/cn5001606. Epub 2014 Sep 24. ACS Chem Neurosci. 2014. PMID: 25203719
The Alzheimer's disease-linked protease BACE2 cleaves VEGFR3 and modulates its signaling.
Schmidt A, Hrupka B, van Bebber F, Sunil Kumar S, Feng X, Tschirner SK, Aßfalg M, Müller SA, Hilger LS, Hofmann LI, Pigoni M, Jocher G, Voytyuk I, Self EL, Ito M, Hyakkoku K, Yoshimura A, Horiguchi N, Feederle R, De Strooper B, Schulte-Merker S, Lammert E, Moechars D, Schmid B, Lichtenthaler SF. Schmidt A, et al. Among authors: hrupka b. J Clin Invest. 2024 Jun 18;134(16):e170550. doi: 10.1172/JCI170550. J Clin Invest. 2024. PMID: 38888964 Free PMC article.
N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.
Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK. Gregory KJ, et al. Among authors: hrupka bj. J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21. J Pharmacol Exp Ther. 2013. PMID: 23965381 Free PMC article.
32 results