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TBX2 represses CST6 resulting in uncontrolled legumain activity to sustain breast cancer proliferation: a novel cancer-selective target pathway with therapeutic opportunities.
D'Costa ZC, Higgins C, Ong CW, Irwin GW, Boyle D, McArt DG, McCloskey K, Buckley NE, Crawford NT, Thiagarajan L, Murray JT, Kennedy RD, Mulligan KA, Harkin DP, Waugh DJ, Scott CJ, Salto-Tellez M, Williams R, Mullan PB. D'Costa ZC, et al. Among authors: williams r. Oncotarget. 2014 Mar 30;5(6):1609-20. doi: 10.18632/oncotarget.1707. Oncotarget. 2014. PMID: 24742492 Free PMC article.
Identification and SAR exploration of a novel series of Legumain inhibitors.
Eddie SL, Gregson A, Graham E, Burton S, Harrison T, Burden R, Scott CJ, Mullan PB, Williams R. Eddie SL, et al. Among authors: williams r. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1546-1548. doi: 10.1016/j.bmcl.2019.03.019. Epub 2019 Mar 29. Bioorg Med Chem Lett. 2019. PMID: 31005445
USP17 is required for peripheral trafficking of lysosomes.
Lin J, McCann AP, Sereesongsaeng N, Burden JM, Alsa'd AA, Burden RE, Micu I, Williams R, Van Schaeybroeck S, Evergren E, Mullan P, Simpson JC, Scott CJ, Burrows JF. Lin J, et al. Among authors: williams r. EMBO Rep. 2022 Apr 5;23(4):e51932. doi: 10.15252/embr.202051932. Epub 2022 Jan 26. EMBO Rep. 2022. PMID: 35080333 Free PMC article.
Development of a potent and selective cell penetrant Legumain inhibitor.
Ness KA, Eddie SL, Higgins CA, Templeman A, D'Costa Z, Gaddale KK, Bouzzaoui S, Jordan L, Janssen D, Harrison T, Burkamp F, Young A, Burden R, Scott CJ, Mullan PB, Williams R. Ness KA, et al. Among authors: williams r. Bioorg Med Chem Lett. 2015 Dec 1;25(23):5642-5. doi: 10.1016/j.bmcl.2015.10.001. Epub 2015 Oct 9. Bioorg Med Chem Lett. 2015. PMID: 26522952
TBX2 acts as a potent transcriptional silencer of tumour suppressor genes through interaction with the CoREST complex to sustain the proliferation of breast cancers.
McIntyre AJ, Angel CZ, Smith JS, Templeman A, Beattie K, Beattie S, Ormrod A, Devlin E, McGreevy C, Bothwell C, Eddie SL, Buckley NE, Williams R, Mullan PB. McIntyre AJ, et al. Among authors: williams r. Nucleic Acids Res. 2022 Jun 24;50(11):6154-6173. doi: 10.1093/nar/gkac494. Nucleic Acids Res. 2022. PMID: 35687133 Free PMC article.
P3 SAR exploration of biphenyl carbamate based Legumain inhibitors.
Higgins C, Bouazzaoui S, Gaddale K, D'Costa Z, Templeman A, O'Rourke M, Young A, Scott C, Harrison T, Mullan P, Williams R. Higgins C, et al. Among authors: williams r. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2521-4. doi: 10.1016/j.bmcl.2014.04.002. Epub 2014 Apr 12. Bioorg Med Chem Lett. 2014. PMID: 24775305
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