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Structural Insights into Notum Covalent Inhibition.
Zhao Y, Svensson F, Steadman D, Frew S, Monaghan A, Bictash M, Moreira T, Chalk R, Lu W, Fish PV, Jones EY. Zhao Y, et al. J Med Chem. 2021 Aug 12;64(15):11354-11363. doi: 10.1021/acs.jmedchem.1c00701. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34292747 Free PMC article.
Small-molecule inhibitors of carboxylesterase Notum.
Zhao Y, Jolly S, Benvegnu S, Jones EY, Fish PV. Zhao Y, et al. Future Med Chem. 2021 Jun;13(11):1001-1015. doi: 10.4155/fmc-2021-0036. Epub 2021 Apr 22. Future Med Chem. 2021. PMID: 33882714 Free PMC article. Review.
Notum deacylates octanoylated ghrelin.
Zhao Y, Schuhmacher LN, Roberts M, Kakugawa S, Bineva-Todd G, Howell S, O'Reilly N, Perret C, Snijders AP, Vincent JP, Jones EY. Zhao Y, et al. Mol Metab. 2021 Jul;49:101201. doi: 10.1016/j.molmet.2021.101201. Epub 2021 Feb 27. Mol Metab. 2021. PMID: 33647468 Free PMC article.
5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit.
Mahy W, Willis NJ, Zhao Y, Woodward HL, Svensson F, Sipthorp J, Vecchia L, Ruza RR, Hillier J, Kjær S, Frew S, Monaghan A, Bictash M, Salinas PC, Whiting P, Vincent JP, Jones EY, Fish PV. Mahy W, et al. J Med Chem. 2020 Nov 12;63(21):12942-12956. doi: 10.1021/acs.jmedchem.0c01391. Epub 2020 Oct 30. J Med Chem. 2020. PMID: 33124429
Screening of a Custom-Designed Acid Fragment Library Identifies 1-Phenylpyrroles and 1-Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity.
Mahy W, Patel M, Steadman D, Woodward HL, Atkinson BN, Svensson F, Willis NJ, Flint A, Papatheodorou D, Zhao Y, Vecchia L, Ruza RR, Hillier J, Frew S, Monaghan A, Costa A, Bictash M, Walter MW, Jones EY, Fish PV. Mahy W, et al. J Med Chem. 2020 Sep 10;63(17):9464-9483. doi: 10.1021/acs.jmedchem.0c00660. Epub 2020 Aug 18. J Med Chem. 2020. PMID: 32787107
15 results