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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.
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. 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
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. J Clin Invest. 2024 Jun 18;134(16):e170550. doi: 10.1172/JCI170550. J Clin Invest. 2024. PMID: 38888964 Free PMC article.
26 results