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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. Among authors: vincent jp. 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.
Notum deacylates Wnt proteins to suppress signalling activity.
Kakugawa S, Langton PF, Zebisch M, Howell S, Chang TH, Liu Y, Feizi T, Bineva G, O'Reilly N, Snijders AP, Jones EY, Vincent JP. Kakugawa S, et al. Among authors: vincent jp. Nature. 2015 Mar 12;519(7542):187-192. doi: 10.1038/nature14259. Epub 2015 Feb 25. Nature. 2015. PMID: 25731175 Free PMC article.
Glypicans shield the Wnt lipid moiety to enable signalling at a distance.
McGough IJ, Vecchia L, Bishop B, Malinauskas T, Beckett K, Joshi D, O'Reilly N, Siebold C, Jones EY, Vincent JP. McGough IJ, et al. Among authors: vincent jp. Nature. 2020 Sep;585(7823):85-90. doi: 10.1038/s41586-020-2498-z. Epub 2020 Jul 22. Nature. 2020. PMID: 32699409 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. Among authors: vincent jp. 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
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. Among authors: vincent jp. 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.
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling.
Bayle ED, Svensson F, Atkinson BN, Steadman D, Willis NJ, Woodward HL, Whiting P, Vincent JP, Fish PV. Bayle ED, et al. Among authors: vincent jp. J Med Chem. 2021 Apr 22;64(8):4289-4311. doi: 10.1021/acs.jmedchem.0c01974. Epub 2021 Mar 30. J Med Chem. 2021. PMID: 33783220 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. Among authors: vincent jp. 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.
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. Among authors: vincent jp. 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.
356 results