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Page 1
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.
Malosh C, Turlington M, Bridges TM, Rook JM, Noetzel MJ, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martínez-Viturro CM, Piedrafita M, Sánchez-Casado MR, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Malosh C, et al. Among authors: bartolome nebreda jm. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5115-20. doi: 10.1016/j.bmcl.2015.10.009. Epub 2015 Oct 9. Bioorg Med Chem Lett. 2015. PMID: 26475522 Free PMC article.
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).
Turlington M, Malosh C, Jacobs J, Manka JT, Noetzel MJ, Vinson PN, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martín-Martín ML, Tong HM, López S, MacDonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Turlington M, et al. J Med Chem. 2014 Jul 10;57(13):5620-37. doi: 10.1021/jm500259z. Epub 2014 Jun 25. J Med Chem. 2014. PMID: 24914612 Free PMC article.
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.
Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Turlington M, et al. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3641-6. doi: 10.1016/j.bmcl.2014.04.087. Epub 2014 May 2. Bioorg Med Chem Lett. 2014. PMID: 24961642 Free PMC article.
Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents.
Rook JM, Xiang Z, Lv X, Ghoshal A, Dickerson JW, Bridges TM, Johnson KA, Foster DJ, Gregory KJ, Vinson PN, Thompson AD, Byun N, Collier RL, Bubser M, Nedelcovych MT, Gould RW, Stauffer SR, Daniels JS, Niswender CM, Lavreysen H, Mackie C, Conde-Ceide S, Alcazar J, Bartolomé-Nebreda JM, Macdonald GJ, Talpos JC, Steckler T, Jones CK, Lindsley CW, Conn PJ. Rook JM, et al. Among authors: bartolome nebreda jm. Neuron. 2015 May 20;86(4):1029-1040. doi: 10.1016/j.neuron.2015.03.063. Epub 2015 Apr 30. Neuron. 2015. PMID: 25937172 Free PMC article.
Diazaspirononane Nonsaccharide Inhibitors of O-GlcNAcase (OGA) for the Treatment of Neurodegenerative Disorders.
Martínez-Viturro CM, Trabanco AA, Royes J, Fernández E, Tresadern G, Vega JA, Del Cerro A, Delgado F, García Molina A, Tovar F, Shaffer P, Ebneth A, Bretteville A, Mertens L, Somers M, Alonso JM, Bartolomé-Nebreda JM. Martínez-Viturro CM, et al. Among authors: bartolome nebreda jm. J Med Chem. 2020 Nov 25;63(22):14017-14044. doi: 10.1021/acs.jmedchem.0c01479. Epub 2020 Nov 16. J Med Chem. 2020. PMID: 33197187
IP-LC-MSMS Enables Identification of Three Tau O-GlcNAcylation Sites as O-GlcNAcase Inhibition Pharmacodynamic Readout in Transgenic Mice Overexpressing Human Tau.
Bijttebier S, Rodrigues Martins D, Mertens L, Grauwen K, Bruinzeel W, Willems R, Bartolomé-Nebreda JM, Theunis C, Bretteville A, Ebneth A, Dillen L. Bijttebier S, et al. Among authors: bartolome nebreda jm. J Proteome Res. 2023 Apr 7;22(4):1309-1321. doi: 10.1021/acs.jproteome.2c00822. Epub 2023 Mar 8. J Proteome Res. 2023. PMID: 36888912
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.
Conde-Ceide S, Alcázar J, Alonso de Diego SA, López S, Martín-Martín ML, Martínez-Viturro CM, Pena MA, Tong HM, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Lindsley CW, Bartolomé-Nebreda JM. Conde-Ceide S, et al. Among authors: bartolome nebreda jm. Bioorg Med Chem Lett. 2016 Jan 15;26(2):429-434. doi: 10.1016/j.bmcl.2015.11.098. Epub 2015 Nov 28. Bioorg Med Chem Lett. 2016. PMID: 26684851 Free PMC article.
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.
Zhou Y, Malosh C, Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Zhou Y, et al. Among authors: bartolome nebreda jm. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3515-9. doi: 10.1016/j.bmcl.2015.06.096. Epub 2015 Jul 4. Bioorg Med Chem Lett. 2015. PMID: 26183084 Free PMC article.
21 results