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2014 6
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Page 1
Structural Analysis and Development of Notum Fragment Screening Hits.
Zhao Y, Mahy W, Willis NJ, Woodward HL, Steadman D, Bayle ED, Atkinson BN, Sipthorp J, Vecchia L, Ruza RR, Harlos K, Jeganathan F, Constantinou S, Costa A, Kjær S, Bictash M, Salinas PC, Whiting P, Vincent JP, Fish PV, Jones EY. Zhao Y, et al. ACS Chem Neurosci. 2022 Jul 6;13(13):2060-2077. doi: 10.1021/acschemneuro.2c00325. Epub 2022 Jun 22. ACS Chem Neurosci. 2022. PMID: 35731924 Free PMC article.
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.
Willis NJ, Mahy W, Sipthorp J, Zhao Y, Woodward HL, Atkinson BN, Bayle ED, Svensson F, Frew S, Jeganathan F, Monaghan A, Benvegnù S, Jolly S, Vecchia L, Ruza RR, Kjær S, Howell S, Snijders AP, Bictash M, Salinas PC, Vincent JP, Jones EY, Whiting P, Fish PV. Willis NJ, et al. J Med Chem. 2022 May 26;65(10):7212-7230. doi: 10.1021/acs.jmedchem.2c00162. Epub 2022 May 10. J Med Chem. 2022. PMID: 35536179 Free PMC article.
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.
NOTUM from Apc-mutant cells biases clonal competition to initiate cancer.
Flanagan DJ, Pentinmikko N, Luopajärvi K, Willis NJ, Gilroy K, Raven AP, Mcgarry L, Englund JI, Webb AT, Scharaw S, Nasreddin N, Hodder MC, Ridgway RA, Minnee E, Sphyris N, Gilchrist E, Najumudeen AK, Romagnolo B, Perret C, Williams AC, Clevers H, Nummela P, Lähde M, Alitalo K, Hietakangas V, Hedley A, Clark W, Nixon C, Kirschner K, Jones EY, Ristimäki A, Leedham SJ, Fish PV, Vincent JP, Katajisto P, Sansom OJ. Flanagan DJ, et al. Nature. 2021 Jun;594(7863):430-435. doi: 10.1038/s41586-021-03525-z. Epub 2021 Jun 2. Nature. 2021. PMID: 34079124 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
47 results