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Structural basis for the inhibition of histone deacetylase 8 (HDAC8), a key epigenetic player in the blood fluke Schistosoma mansoni.
Marek M, Kannan S, Hauser AT, Moraes Mourão M, Caby S, Cura V, Stolfa DA, Schmidtkunz K, Lancelot J, Andrade L, Renaud JP, Oliveira G, Sippl W, Jung M, Cavarelli J, Pierce RJ, Romier C. Marek M, et al. PLoS Pathog. 2013;9(9):e1003645. doi: 10.1371/journal.ppat.1003645. Epub 2013 Sep 26. PLoS Pathog. 2013. PMID: 24086136 Free PMC article.
Molecular basis for the antiparasitic activity of a mercaptoacetamide derivative that inhibits histone deacetylase 8 (HDAC8) from the human pathogen schistosoma mansoni.
Stolfa DA, Marek M, Lancelot J, Hauser AT, Walter A, Leproult E, Melesina J, Rumpf T, Wurtz JM, Cavarelli J, Sippl W, Pierce RJ, Romier C, Jung M. Stolfa DA, et al. Among authors: marek m. J Mol Biol. 2014 Oct 9;426(20):3442-53. doi: 10.1016/j.jmb.2014.03.007. Epub 2014 Mar 20. J Mol Biol. 2014. PMID: 24657767 Free article.
Hydroxamates of para-aminobenzoic acid as selective inhibitors of HDAC8.
Kulandaivelu U, Chilakamari LM, Jadav SS, Rao TR, Jayaveera KN, Shireesha B, Hauser AT, Senger J, Marek M, Romier C, Jung M, Jayaprakash V. Kulandaivelu U, et al. Among authors: marek m. Bioorg Chem. 2014 Dec;57:116-120. doi: 10.1016/j.bioorg.2014.08.005. Epub 2014 Sep 3. Bioorg Chem. 2014. PMID: 25462986
Schistosome sirtuins as drug targets.
Lancelot J, Cabezas-Cruz A, Caby S, Marek M, Schultz J, Romier C, Sippl W, Jung M, Pierce RJ. Lancelot J, et al. Among authors: marek m. Future Med Chem. 2015;7(6):765-82. doi: 10.4155/fmc.15.24. Future Med Chem. 2015. PMID: 25996069 Free article. Review.
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis.
Heimburg T, Chakrabarti A, Lancelot J, Marek M, Melesina J, Hauser AT, Shaik TB, Duclaud S, Robaa D, Erdmann F, Schmidt M, Romier C, Pierce RJ, Jung M, Sippl W. Heimburg T, et al. Among authors: marek m. J Med Chem. 2016 Mar 24;59(6):2423-35. doi: 10.1021/acs.jmedchem.5b01478. Epub 2016 Mar 14. J Med Chem. 2016. PMID: 26937828 Free article.
257 results