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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: myers r. 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
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: myers r. 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
Tuft cell-derived acetylcholine regulates epithelial fluid secretion.
Billipp TE, Fung C, Webeck LM, Sargent DB, Gologorsky MB, McDaniel MM, Kasal DN, McGinty JW, Barrow KA, Rich LM, Barilli A, Sabat M, Debley JS, Myers R, Howitt MR, von Moltke J. Billipp TE, et al. Among authors: myers r. bioRxiv [Preprint]. 2023 Mar 22:2023.03.17.533208. doi: 10.1101/2023.03.17.533208. bioRxiv. 2023. Update in: Immunity. 2024 Jun 11;57(6):1243-1259.e8. doi: 10.1016/j.immuni.2024.03.023. PMID: 36993541 Free PMC article. Updated. Preprint.
Tuft cell-derived acetylcholine promotes epithelial chloride secretion and intestinal helminth clearance.
Billipp TE, Fung C, Webeck LM, Sargent DB, Gologorsky MB, Chen Z, McDaniel MM, Kasal DN, McGinty JW, Barrow KA, Rich LM, Barilli A, Sabat M, Debley JS, Wu C, Myers R, Howitt MR, von Moltke J. Billipp TE, et al. Among authors: myers r. Immunity. 2024 Jun 11;57(6):1243-1259.e8. doi: 10.1016/j.immuni.2024.03.023. Epub 2024 May 13. Immunity. 2024. PMID: 38744291
3,729 results