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A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models.
Zhou Y, Castonguay P, Sidhom EH, Clark AR, Dvela-Levitt M, Kim S, Sieber J, Wieder N, Jung JY, Andreeva S, Reichardt J, Dubois F, Hoffmann SC, Basgen JM, Montesinos MS, Weins A, Johnson AC, Lander ES, Garrett MR, Hopkins CR, Greka A. Zhou Y, et al. Among authors: hopkins cr. Science. 2017 Dec 8;358(6368):1332-1336. doi: 10.1126/science.aal4178. Science. 2017. PMID: 29217578 Free PMC article.
Inhibition of the TRPC5 ion channel protects the kidney filter.
Schaldecker T, Kim S, Tarabanis C, Tian D, Hakroush S, Castonguay P, Ahn W, Wallentin H, Heid H, Hopkins CR, Lindsley CW, Riccio A, Buvall L, Weins A, Greka A. Schaldecker T, et al. Among authors: hopkins cr. J Clin Invest. 2013 Dec;123(12):5298-309. doi: 10.1172/JCI71165. Epub 2013 Nov 15. J Clin Invest. 2013. PMID: 24231357 Free PMC article.
Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903.
Sharma SH, Pablo JL, Montesinos MS, Greka A, Hopkins CR. Sharma SH, et al. Among authors: hopkins cr. Bioorg Med Chem Lett. 2019 Jan 15;29(2):155-159. doi: 10.1016/j.bmcl.2018.12.007. Epub 2018 Dec 4. Bioorg Med Chem Lett. 2019. PMID: 30538066 Free PMC article.
Further Exploration of the Benzimidazole Scaffold as TRPC5 Inhibitors: Identification of 1-Alkyl-2-(pyrrolidin-1-yl)-1H-benzo[d]imidazoles as Potent and Selective Inhibitors.
Sharma S, L Pablo J, Tolentino KT, Gallegos W, Hinman J, Beninato M, Asche M, Greka A, Hopkins CR. Sharma S, et al. Among authors: hopkins cr. ChemMedChem. 2022 Jul 19;17(14):e202200151. doi: 10.1002/cmdc.202200151. Epub 2022 May 24. ChemMedChem. 2022. PMID: 35557491 Free PMC article.
Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.
Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA; NIH Molecular Libraries Project Team. Schreiber SL, et al. Among authors: hopkins cr. Cell. 2015 Jun 4;161(6):1252-65. doi: 10.1016/j.cell.2015.05.023. Cell. 2015. PMID: 26046436 Free PMC article. Review.
Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992.
Kharade SV, Kurata H, Bender AM, Blobaum AL, Figueroa EE, Duran A, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, Denton JS. Kharade SV, et al. Among authors: hopkins cr. Mol Pharmacol. 2018 Aug;94(2):926-937. doi: 10.1124/mol.118.112359. Epub 2018 Jun 12. Mol Pharmacol. 2018. PMID: 29895592 Free PMC article.
244 results