Abstract
As a class, epigenetic enzymes have been identified as clear targets for cancer therapeutics based on their broad hyperactivity in solid and hematological malignancies. The search for effective inhibitors of histone writers and of histone erasers has been a focus of drug discovery efforts both in academic and pharmaceutical laboratories and has led to the identification of some promising leads. This review focuses on the discovery strategies and preclinical evaluation studies of a subset of the more advanced compounds that target histone writers or histone erasers. The specificity and anticancer potential of these small molecules is discussed within the context of their development pipeline.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 2243-2261 |
| Number of pages | 19 |
| Journal | Future Medicinal Chemistry |
| Volume | 7 |
| Issue number | 16 |
| DOIs | |
| State | Published - Oct 1 2015 |
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ASJC Scopus subject areas
- Drug Discovery
- Pharmacology
- Molecular Medicine
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Successful strategies in the discovery of small-molecule epigenetic modulators with anticancer potential. / Bayo, Juan; Dalvi, Maithili P.; Martinez, Elisabeth D.
In: Future Medicinal Chemistry, Vol. 7, No. 16, 01.10.2015, p. 2243-2261.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Successful strategies in the discovery of small-molecule epigenetic modulators with anticancer potential
AU - Bayo, Juan
AU - Dalvi, Maithili P.
AU - Martinez, Elisabeth D.
PY - 2015/10/1
Y1 - 2015/10/1
N2 - As a class, epigenetic enzymes have been identified as clear targets for cancer therapeutics based on their broad hyperactivity in solid and hematological malignancies. The search for effective inhibitors of histone writers and of histone erasers has been a focus of drug discovery efforts both in academic and pharmaceutical laboratories and has led to the identification of some promising leads. This review focuses on the discovery strategies and preclinical evaluation studies of a subset of the more advanced compounds that target histone writers or histone erasers. The specificity and anticancer potential of these small molecules is discussed within the context of their development pipeline.
AB - As a class, epigenetic enzymes have been identified as clear targets for cancer therapeutics based on their broad hyperactivity in solid and hematological malignancies. The search for effective inhibitors of histone writers and of histone erasers has been a focus of drug discovery efforts both in academic and pharmaceutical laboratories and has led to the identification of some promising leads. This review focuses on the discovery strategies and preclinical evaluation studies of a subset of the more advanced compounds that target histone writers or histone erasers. The specificity and anticancer potential of these small molecules is discussed within the context of their development pipeline.
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UR - http://www.scopus.com/inward/citedby.url?scp=84947601296&partnerID=8YFLogxK
U2 - 10.4155/fmc.15.140
DO - 10.4155/fmc.15.140
M3 - Article
C2 - 26510529
AN - SCOPUS:84947601296
VL - 7
SP - 2243
EP - 2261
JO - Future Medicinal Chemistry
JF - Future Medicinal Chemistry
SN - 1756-8919
IS - 16
ER -