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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: jones ey. 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.
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: jones ey. 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.
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: jones ey. 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
288 results