Packham G - Search Results

1

Protein recognition by short peptide reversible inhibitors of the chromatin-modifying LSD1/CoREST lysine demethylase.

Tortorici M, Borrello MT, Tardugno M, Chiarelli LR, Pilotto S, Ciossani G, Vellore NA, Bailey SG, Cowan J, O'Connell M, Crabb SJ, Packham G, Mai A, Baron R, Ganesan A, Mattevi A. Tortorici M, et al. Among authors: packham g. ACS Chem Biol. 2013 Aug 16;8(8):1677-82. doi: 10.1021/cb4001926. Epub 2013 Jun 11. ACS Chem Biol. 2013. PMID: 23721412

2

Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors.

Benelkebir H, Hodgkinson C, Duriez PJ, Hayden AL, Bulleid RA, Crabb SJ, Packham G, Ganesan A. Benelkebir H, et al. Among authors: packham g. Bioorg Med Chem. 2011 Jun 15;19(12):3709-16. doi: 10.1016/j.bmc.2011.02.017. Epub 2011 Feb 13. Bioorg Med Chem. 2011. PMID: 21382717

3

Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A).

Borrello MT, Schinor B, Bartels K, Benelkebir H, Pereira S, Al-Jamal WT, Douglas L, Duriez PJ, Packham G, Haufe G, Ganesan A. Borrello MT, et al. Among authors: packham g. Bioorg Med Chem Lett. 2017 May 15;27(10):2099-2101. doi: 10.1016/j.bmcl.2017.03.081. Epub 2017 Mar 29. Bioorg Med Chem Lett. 2017. PMID: 28390942 Free article.

4

Synthesis of Carboxamide-Containing Tranylcypromine Analogues as LSD1 (KDM1A) Inhibitors Targeting Acute Myeloid Leukemia.

Teresa Borrello M, Benelkebir H, Lee A, Hin Tam C, Shafat M, Rushworth SA, Bowles KM, Douglas L, Duriez PJ, Bailey S, Crabb SJ, Packham G, Ganesan A. Teresa Borrello M, et al. Among authors: packham g. ChemMedChem. 2021 Apr 20;16(8):1316-1324. doi: 10.1002/cmdc.202000754. Epub 2021 Feb 3. ChemMedChem. 2021. PMID: 33533576

5

Will histone deacetylase inhibitors require combination with other agents to fulfil their therapeutic potential?

Nolan L, Johnson PW, Ganesan A, Packham G, Crabb SJ. Nolan L, et al. Among authors: packham g. Br J Cancer. 2008 Sep 2;99(5):689-94. doi: 10.1038/sj.bjc.6604557. Epub 2008 Aug 19. Br J Cancer. 2008. PMID: 18728657 Free PMC article. Review.

6

S-adenosylhomocysteine hydrolase inhibition by 3-deazaneplanocin A analogues induces anti-cancer effects in breast cancer cell lines and synergy with both histone deacetylase and HER2 inhibition.

Hayden A, Johnson PW, Packham G, Crabb SJ. Hayden A, et al. Among authors: packham g. Breast Cancer Res Treat. 2011 May;127(1):109-19. doi: 10.1007/s10549-010-0982-0. Epub 2010 Jun 17. Breast Cancer Res Treat. 2011. PMID: 20556507

7

Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.

Benelkebir H, Marie S, Hayden AL, Lyle J, Loadman PM, Crabb SJ, Packham G, Ganesan A. Benelkebir H, et al. Among authors: packham g. Bioorg Med Chem. 2011 Jun 15;19(12):3650-8. doi: 10.1016/j.bmc.2011.02.024. Epub 2011 Feb 17. Bioorg Med Chem. 2011. PMID: 21420302

8

Vacuolar ATPase as a potential therapeutic target and mediator of treatment resistance in cancer.

Whitton B, Okamoto H, Packham G, Crabb SJ. Whitton B, et al. Among authors: packham g. Cancer Med. 2018 Aug;7(8):3800-3811. doi: 10.1002/cam4.1594. Epub 2018 Jun 21. Cancer Med. 2018. PMID: 29926527 Free PMC article. Review.

9

Thioflavin S (NSC71948) interferes with Bcl-2-associated athanogene (BAG-1)-mediated protein-protein interactions.

Sharp A, Crabb SJ, Johnson PW, Hague A, Cutress R, Townsend PA, Ganesan A, Packham G. Sharp A, et al. Among authors: packham g. J Pharmacol Exp Ther. 2009 Nov;331(2):680-9. doi: 10.1124/jpet.109.153601. Epub 2009 Aug 18. J Pharmacol Exp Ther. 2009. PMID: 19690191 Free PMC article.

10

LSD1 inhibition attenuates androgen receptor V7 splice variant activation in castration resistant prostate cancer models.

Regufe da Mota S, Bailey S, Strivens RA, Hayden AL, Douglas LR, Duriez PJ, Borrello MT, Benelkebir H, Ganesan A, Packham G, Crabb SJ. Regufe da Mota S, et al. Among authors: packham g. Cancer Cell Int. 2018 May 9;18:71. doi: 10.1186/s12935-018-0568-1. eCollection 2018. Cancer Cell Int. 2018. PMID: 29760584 Free PMC article.

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