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Development of a Dihydroquinoline-Pyrazoline GluN2C/2D-Selective Negative Allosteric Modulator of the N-Methyl-d-aspartate Receptor.
D'Erasmo MP, Akins NS, Ma P, Jing Y, Swanger SA, Sharma SK, Bartsch PW, Menaldino DS, Arcoria PJ, Bui TT, Pons-Bennaceur A, Le P, Allen JP, Ullman EZ, Nocilla KA, Zhang J, Perszyk RE, Kim S, Acker TM, Taz A, Burton SL, Coe K, Fritzemeier RG, Burnashev N, Yuan H, Liotta DC, Traynelis SF. D'Erasmo MP, et al. Among authors: menaldino ds. ACS Chem Neurosci. 2023 Sep 6;14(17):3059-3076. doi: 10.1021/acschemneuro.3c00181. Epub 2023 Aug 11. ACS Chem Neurosci. 2023. PMID: 37566734 Free PMC article.
A Novel Negative Allosteric Modulator Selective for GluN2C/2D-Containing NMDA Receptors Inhibits Synaptic Transmission in Hippocampal Interneurons.
Swanger SA, Vance KM, Acker TM, Zimmerman SS, DiRaddo JO, Myers SJ, Bundgaard C, Mosley CA, Summer SL, Menaldino DS, Jensen HS, Liotta DC, Traynelis SF. Swanger SA, et al. Among authors: menaldino ds. ACS Chem Neurosci. 2018 Feb 21;9(2):306-319. doi: 10.1021/acschemneuro.7b00329. Epub 2017 Nov 2. ACS Chem Neurosci. 2018. PMID: 29043770 Free PMC article.
Distinct GluN1 and GluN2 Structural Determinants for Subunit-Selective Positive Allosteric Modulation of N-Methyl-d-aspartate Receptors.
Strong KL, Epplin MP, Ogden KK, Burger PB, Kaiser TM, Wilding TJ, Kusumoto H, Camp CR, Shaulsky G, Bhattacharya S, Perszyk RE, Menaldino DS, McDaniel MJ, Zhang J, Le P, Banke TG, Hansen KB, Huettner JE, Liotta DC, Traynelis SF. Strong KL, et al. Among authors: menaldino ds. ACS Chem Neurosci. 2021 Jan 6;12(1):79-98. doi: 10.1021/acschemneuro.0c00561. Epub 2020 Dec 16. ACS Chem Neurosci. 2021. PMID: 33326224 Free PMC article.
The Structure-Activity Relationship of a Tetrahydroisoquinoline Class of N-Methyl-d-Aspartate Receptor Modulators that Potentiates GluN2B-Containing N-Methyl-d-Aspartate Receptors.
Strong KL, Epplin MP, Bacsa J, Butch CJ, Burger PB, Menaldino DS, Traynelis SF, Liotta DC. Strong KL, et al. Among authors: menaldino ds. J Med Chem. 2017 Jul 13;60(13):5556-5585. doi: 10.1021/acs.jmedchem.7b00239. Epub 2017 Jun 26. J Med Chem. 2017. PMID: 28586221 Free PMC article.
The Bioactive Protein-Ligand Conformation of GluN2C-Selective Positive Allosteric Modulators Bound to the NMDA Receptor.
Kaiser TM, Kell SA, Kusumoto H, Shaulsky G, Bhattacharya S, Epplin MP, Strong KL, Miller EJ, Cox BD, Menaldino DS, Liotta DC, Traynelis SF, Burger PB. Kaiser TM, et al. Among authors: menaldino ds. Mol Pharmacol. 2018 Feb;93(2):141-156. doi: 10.1124/mol.117.110940. Epub 2017 Dec 14. Mol Pharmacol. 2018. PMID: 29242355 Free PMC article.
Biased modulators of NMDA receptors control channel opening and ion selectivity.
Perszyk RE, Swanger SA, Shelley C, Khatri A, Fernandez-Cuervo G, Epplin MP, Zhang J, Le P, Bülow P, Garnier-Amblard E, Gangireddy PKR, Bassell GJ, Yuan H, Menaldino DS, Liotta DC, Liebeskind LS, Traynelis SF. Perszyk RE, et al. Among authors: menaldino ds. Nat Chem Biol. 2020 Feb;16(2):188-196. doi: 10.1038/s41589-019-0449-5. Epub 2020 Jan 20. Nat Chem Biol. 2020. PMID: 31959964 Free PMC article.
Discovery of Dihydropyrrolo[1,2-a]pyrazin-3(4H)-one-Based Second-Generation GluN2C- and GluN2D-Selective Positive Allosteric Modulators (PAMs) of the N-Methyl-d-Aspartate (NMDA) Receptor.
Epplin MP, Mohan A, Harris LD, Zhu Z, Strong KL, Bacsa J, Le P, Menaldino DS, Traynelis SF, Liotta DC. Epplin MP, et al. Among authors: menaldino ds. J Med Chem. 2020 Jul 23;63(14):7569-7600. doi: 10.1021/acs.jmedchem.9b01733. Epub 2020 Jul 6. J Med Chem. 2020. PMID: 32538088 Free PMC article.
25 results