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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: lancelot j. 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.
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. Among authors: lancelot j. PLoS Pathog. 2013;9(9):e1003645. doi: 10.1371/journal.ppat.1003645. Epub 2013 Sep 26. PLoS Pathog. 2013. PMID: 24086136 Free PMC article.
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: lancelot j. 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.
Synthesis, Crystallization Studies, and in vitro Characterization of Cinnamic Acid Derivatives as SmHDAC8 Inhibitors for the Treatment of Schistosomiasis.
Bayer T, Chakrabarti A, Lancelot J, Shaik TB, Hausmann K, Melesina J, Schmidtkunz K, Marek M, Erdmann F, Schmidt M, Robaa D, Romier C, Pierce RJ, Jung M, Sippl W. Bayer T, et al. Among authors: lancelot j. ChemMedChem. 2018 Aug 10;13(15):1517-1529. doi: 10.1002/cmdc.201800238. Epub 2018 Jul 4. ChemMedChem. 2018. PMID: 29806110
Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants.
Marek M, Shaik TB, Heimburg T, Chakrabarti A, Lancelot J, Ramos-Morales E, Da Veiga C, Kalinin D, Melesina J, Robaa D, Schmidtkunz K, Suzuki T, Holl R, Ennifar E, Pierce RJ, Jung M, Sippl W, Romier C. Marek M, et al. Among authors: lancelot j. J Med Chem. 2018 Nov 21;61(22):10000-10016. doi: 10.1021/acs.jmedchem.8b01087. Epub 2018 Nov 8. J Med Chem. 2018. PMID: 30347148 Free article.
83 results