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41. Rau RE et al (2016) DOT1L as a therapeutic target for the treatment of DNMT3A-mutant
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42. Wong M, Polly P, Liu T (2015) The histone methyltransferase DOT1L: regulatory functions
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43. Wang L et al (2016) JQ1, a small molecule inhibitor of BRD4, suppresses cell growth and
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44. Daigle SR et al (2011) Selective killing of mixed lineage leukemia cells by a potent
small-molecule DOT1L inhibitor. Cancer Cell 20(1):53–65
45. Herold JM et al (2011) Small-molecule ligands of methyl-lysine binding proteins. J Med
Chem 54(7):2504–2511
46. Loharch S, et al (2015) EpiDBase: a manually curated database for small molecule
modulators of epigenetic landscape. Database (Oxford), 2015
47. Huggins DJ, Venkitaraman AR, Spring DR (2011) Rational methods for the selection of
diverse screening compounds. ACS Chem Biol 6(3):208–217
48. Walters WP, Namchuk M (2003) Designing screens: how to make your hits a hit. Nat Rev
Drug Discov 2(4):259–266
49. Brenk R et al (2008) Lessons learnt from assembling screening libraries for drug discovery
for neglected diseases. ChemMedChem 3(3):435–444
50. Bemis GW, Murcko MA (1996) The properties of known drugs. 1. Molecular frameworks.
J Med Chem 39(15):2887–2893
51. McMillan M, Kahn M (2005) Investigating Wnt signaling: a chemogenomic safari. Drug
Discov Today 10(21):1467–1474
52. Nilakantan R, Bauman N, Haraki KS (1997) Database diversity assessment: new ideas,
concepts, and tools. J Comput Aided Mol Des 11(5):447–452
53. Lee ML, Schneider G (2001) Scaffold architecture and pharmacophoric properties of natural
products and trade drugs: application in the design of natural product-based combinatorial
libraries. J Comb Chem 3(3):284–289
54. Lewell XQ et al (2003) Drug rings database with web interface. A tool for identifying
alternative chemical rings in lead discovery programs. J Med Chem 46(15):3257–3274
55. Kho R et al (2005) Ring systems in mutagenicity databases. J Med Chem 48(21):6671–6678
266
S. Loharch et al.
Res 18(13):3509–3515
32. Iyer SP, Foss FF (2015) Romidepsin for the treatment of peripheral T-cell lymphoma.
Oncologist 20(9):1084–1091
33. Iwamoto FM et al (2011) A phase I/II trial of the histone deacetylase inhibitor romidepsin for
adults with recurrent malignant glioma: North American Brain Tumor Consortium Study
03-03. Neuro Oncol 13(5):509–516
34. Rashidi A, Cashen AF (2015) Belinostat for the treatment of relapsed or refractory peripheral
T-cell lymphoma. Future Oncol 11(11):1659–1664
35. McCabe MT et al (2012) EZH2 inhibition as a therapeutic strategy for lymphoma with
EZH2-activating mutations. Nature 492(7427):108–112
36. Chen YT et al (2016) The novel EZH2 inhibitor, GSK126, suppresses cell migration and
angiogenesis via down-regulating VEGF-A. Cancer Chemother Pharmacol 77(4):757–765
37. Zeng D, Liu M, Pan J (2017) Blocking EZH2 methylation transferase activity by GSK126
decreases stem cell-like myeloma cells. Oncotarget 8(2):3396–3411
38. Bowers EM et al (2010) Virtual ligand screening of the p300/CBP histone acetyltransferase:
identification of a selective small molecule inhibitor. Chem Biol 17(5):471–482
39. Oike T et al (2014) C646, a selective small molecule inhibitor of histone acetyltransferase
p300, radiosensitizes lung cancer cells by enhancing mitotic catastrophe. Radiother Oncol
111(2):222–227
40. Zhao D et al (2015) C646, a novel p300/CREB-binding protein-specific inhibitor of histone
acetyltransferase, attenuates influenza A virus infection. Antimicrob Agents Chemother
60(3):1902–1906
41. Rau RE et al (2016) DOT1L as a therapeutic target for the treatment of DNMT3A-mutant
acute myeloid leukemia. Blood 128(7):971–981
42. Wong M, Polly P, Liu T (2015) The histone methyltransferase DOT1L: regulatory functions
and a cancer therapy target. Am J Cancer Res 5(9):2823–2837
43. Wang L et al (2016) JQ1, a small molecule inhibitor of BRD4, suppresses cell growth and
invasion in oral squamous cell carcinoma. Oncol Rep 36(4):1989–1996
44. Daigle SR et al (2011) Selective killing of mixed lineage leukemia cells by a potent
small-molecule DOT1L inhibitor. Cancer Cell 20(1):53–65
45. Herold JM et al (2011) Small-molecule ligands of methyl-lysine binding proteins. J Med
Chem 54(7):2504–2511
46. Loharch S, et al (2015) EpiDBase: a manually curated database for small molecule
modulators of epigenetic landscape. Database (Oxford), 2015
47. Huggins DJ, Venkitaraman AR, Spring DR (2011) Rational methods for the selection of
diverse screening compounds. ACS Chem Biol 6(3):208–217
48. Walters WP, Namchuk M (2003) Designing screens: how to make your hits a hit. Nat Rev
Drug Discov 2(4):259–266
49. Brenk R et al (2008) Lessons learnt from assembling screening libraries for drug discovery
for neglected diseases. ChemMedChem 3(3):435–444
50. Bemis GW, Murcko MA (1996) The properties of known drugs. 1. Molecular frameworks.
J Med Chem 39(15):2887–2893
51. McMillan M, Kahn M (2005) Investigating Wnt signaling: a chemogenomic safari. Drug
Discov Today 10(21):1467–1474
52. Nilakantan R, Bauman N, Haraki KS (1997) Database diversity assessment: new ideas,
concepts, and tools. J Comput Aided Mol Des 11(5):447–452
53. Lee ML, Schneider G (2001) Scaffold architecture and pharmacophoric properties of natural
products and trade drugs: application in the design of natural product-based combinatorial
libraries. J Comb Chem 3(3):284–289
54. Lewell XQ et al (2003) Drug rings database with web interface. A tool for identifying
alternative chemical rings in lead discovery programs. J Med Chem 46(15):3257–3274
55. Kho R et al (2005) Ring systems in mutagenicity databases. J Med Chem 48(21):6671–6678
266
S. Loharch et al.