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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: vecchia l. 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.
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: vecchia l. 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: vecchia l. 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: vecchia l. 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
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: vecchia l. 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.
Experimental phasing opportunities for macromolecular crystallography at very long wavelengths.
El Omari K, Duman R, Mykhaylyk V, Orr CM, Latimer-Smith M, Winter G, Grama V, Qu F, Bountra K, Kwong HS, Romano M, Reis RI, Vogeley L, Vecchia L, Owen CD, Wittmann S, Renner M, Senda M, Matsugaki N, Kawano Y, Bowden TA, Moraes I, Grimes JM, Mancini EJ, Walsh MA, Guzzo CR, Owens RJ, Jones EY, Brown DG, Stuart DI, Beis K, Wagner A. El Omari K, et al. Among authors: vecchia l. Commun Chem. 2023 Oct 12;6(1):219. doi: 10.1038/s42004-023-01014-0. Commun Chem. 2023. PMID: 37828292 Free PMC article.
220 results