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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: fish pv. 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.
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors.
Atkinson BN, Steadman D, Mahy W, Zhao Y, Sipthorp J, Bayle ED, Svensson F, Papageorgiou G, Jeganathan F, Frew S, Monaghan A, Bictash M, Jones EY, Fish PV. Atkinson BN, et al. Among authors: fish pv. Bioorg Med Chem Lett. 2020 Feb 1;30(3):126751. doi: 10.1016/j.bmcl.2019.126751. Epub 2019 Oct 28. Bioorg Med Chem Lett. 2020. PMID: 31862412 Free PMC article.
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. Among authors: fish pv. 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
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: fish pv. 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
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: fish pv. 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.
Small-molecule inhibitors of carboxylesterase Notum.
Zhao Y, Jolly S, Benvegnu S, Jones EY, Fish PV. Zhao Y, et al. Among authors: fish pv. 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.
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. Among authors: fish pv. 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.
61 results