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Page 1
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: willis nj. 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: willis nj. 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: willis nj. 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: willis nj. 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. 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 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: willis nj. 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.
22 results