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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: steadman d. 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
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: steadman d. 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.
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: steadman d. 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.
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: steadman d. 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.
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: steadman d. 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.
New approaches for the treatment of Alzheimer's disease.
Fish PV, Steadman D, Bayle ED, Whiting P. Fish PV, et al. Among authors: steadman d. Bioorg Med Chem Lett. 2019 Jan 15;29(2):125-133. doi: 10.1016/j.bmcl.2018.11.034. Epub 2018 Nov 19. Bioorg Med Chem Lett. 2019. PMID: 30501965 Review.
Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells.
Powell J, Mota F, Steadman D, Soudy C, Miyauchi JT, Crosby S, Jarvis A, Reisinger T, Winfield N, Evans G, Finniear A, Yelland T, Chou YT, Chan AWE, O'Leary A, Cheng L, Liu D, Fotinou C, Milagre C, Martin JF, Jia H, Frankel P, Djordjevic S, Tsirka SE, Zachary IC, Selwood DL. Powell J, et al. Among authors: steadman d. J Med Chem. 2018 May 10;61(9):4135-4154. doi: 10.1021/acs.jmedchem.8b00210. Epub 2018 Apr 24. J Med Chem. 2018. PMID: 29648813 Free PMC article.
98 results