Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor
Emily Borretto
1
,
Loretta Lazzarato
1
,
Francesco Spallotta
2
,
Chiara Cencioni
2
,
Yuri D’Alessandra
2
,
Carlo Gaetano
3
,
Roberta Fruttero
1
,
Alberto Gasco
1
2
Publication type: Journal Article
Publication date: 2013-09-06
scimago Q1
wos Q2
SJR: 0.805
CiteScore: 5.8
Impact factor: 4.0
ISSN: 19485875
PubMed ID:
24900596
Organic Chemistry
Drug Discovery
Biochemistry
Abstract
The NO-donor histone deacetylase inhibitor 2, formally obtained by joining Entinostat 1, a moderately selective Class I histone deacetylases (HDACs) inhibitor, to a 4-(methylaminomethyl)furoxan-3-carbonitrile scaffold, is described and its preliminary biological profile discussed. This hybrid regulates Classes I and II HDACs. Nitric oxide (NO) released by the compound activates soluble guanylate cyclase (sGC), causing Class II nuclear shuttling and chromatin modifications, with consequences on gene expression. The hybrid affects a number of micro-RNAs not modulated by its individual components; it promotes myogenic differentiation, inducing the formation of larger myotubes with significantly more nuclei per fiber, in a more efficient manner than the 1:1 mixture of its two components. The hybrid is an example of a new class of NO-donor HDACs now being developed, which should be of interest for treating a number of diseases.
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42
Total citations:
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Citations from 2025:
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(2.38%)
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MLA
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GOST
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Borretto E. et al. Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor // ACS Medicinal Chemistry Letters. 2013. Vol. 4. No. 10. pp. 994-999.
GOST all authors (up to 50)
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Borretto E., Lazzarato L., Spallotta F., Cencioni C., D’Alessandra Y., Gaetano C., Fruttero R., Gasco A. Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor // ACS Medicinal Chemistry Letters. 2013. Vol. 4. No. 10. pp. 994-999.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1021/ml400289e
UR - https://doi.org/10.1021/ml400289e
TI - Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor
T2 - ACS Medicinal Chemistry Letters
AU - Borretto, Emily
AU - Lazzarato, Loretta
AU - Spallotta, Francesco
AU - Cencioni, Chiara
AU - D’Alessandra, Yuri
AU - Gaetano, Carlo
AU - Fruttero, Roberta
AU - Gasco, Alberto
PY - 2013
DA - 2013/09/06
PB - American Chemical Society (ACS)
SP - 994-999
IS - 10
VL - 4
PMID - 24900596
SN - 1948-5875
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2013_Borretto,
author = {Emily Borretto and Loretta Lazzarato and Francesco Spallotta and Chiara Cencioni and Yuri D’Alessandra and Carlo Gaetano and Roberta Fruttero and Alberto Gasco},
title = {Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor},
journal = {ACS Medicinal Chemistry Letters},
year = {2013},
volume = {4},
publisher = {American Chemical Society (ACS)},
month = {sep},
url = {https://doi.org/10.1021/ml400289e},
number = {10},
pages = {994--999},
doi = {10.1021/ml400289e}
}
Cite this
MLA
Copy
Borretto, Emily, et al. “Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.” ACS Medicinal Chemistry Letters, vol. 4, no. 10, Sep. 2013, pp. 994-999. https://doi.org/10.1021/ml400289e.