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Page 1
From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents.
Barilli A, Aldegheri L, Bianchi F, Brault L, Brodbeck D, Castelletti L, Feriani A, Lingard I, Myers R, Nola S, Piccoli L, Pompilio D, Raveglia LF, Salvagno C, Tassini S, Virginio C, Sabat M. Barilli A, et al. Among authors: aldegheri l. J Med Chem. 2021 May 13;64(9):5931-5955. doi: 10.1021/acs.jmedchem.1c00065. Epub 2021 Apr 23. J Med Chem. 2021. PMID: 33890770
Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators.
Ward SE, Harries M, Aldegheri L, Austin NE, Ballantine S, Ballini E, Bradley DM, Bax BD, Clarke BP, Harris AJ, Harrison SA, Melarange RA, Mookherjee C, Mosley J, Dal Negro G, Oliosi B, Smith KJ, Thewlis KM, Woollard PM, Yusaf SP. Ward SE, et al. Among authors: aldegheri l. J Med Chem. 2011 Jan 13;54(1):78-94. doi: 10.1021/jm100679e. Epub 2010 Dec 3. J Med Chem. 2011. PMID: 21128618
Characterization of three diaminopyrimidines as potent and selective antagonists of P2X3 and P2X2/3 receptors with in vivo efficacy in a pain model.
Ballini E, Virginio C, Medhurst SJ, Summerfield SG, Aldegheri L, Buson A, Carignani C, Chen YH, Giacometti A, Lago I, Powell AJ, Jarolimek W. Ballini E, et al. Among authors: aldegheri l. Br J Pharmacol. 2011 Jul;163(6):1315-25. doi: 10.1111/j.1476-5381.2011.01322.x. Br J Pharmacol. 2011. PMID: 21410458 Free PMC article.
The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent.
Sabat M, Raveglia LF, Aldegheri L, Barilli A, Bianchi F, Brault L, Brodbeck D, Feriani A, Lingard I, Miura J, Myers R, Piccoli L, Tassini S, Tyhonas J, Ton-Nu T, Wang H, Virginio C. Sabat M, et al. Among authors: aldegheri l. Bioorg Med Chem. 2022 Dec 15;76:117084. doi: 10.1016/j.bmc.2022.117084. Epub 2022 Nov 6. Bioorg Med Chem. 2022. PMID: 36402081
Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.
Ward SE, Harries M, Aldegheri L, Andreotti D, Ballantine S, Bax BD, Harris AJ, Harker AJ, Lund J, Melarange R, Mingardi A, Mookherjee C, Mosley J, Neve M, Oliosi B, Profeta R, Smith KJ, Smith PW, Spada S, Thewlis KM, Yusaf SP. Ward SE, et al. Among authors: aldegheri l. J Med Chem. 2010 Aug 12;53(15):5801-12. doi: 10.1021/jm1005429. J Med Chem. 2010. PMID: 20614889 Clinical Trial.
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