List of works - Sergio Valente

"Shock and kill" effects of class I-selective histone deacetylase inhibitors in combination with the glutathione synthesis inhibitor buthionine sulfoximine in cell line models for HIV-1 quiescence

scientific article

1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells

scientific article published on 08 July 2014

1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells

scientific article published on 21 December 2015

3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity

scientific article published on February 2004

3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies

scientific article published on March 2004

3-D QSAR Studies on Histone Deacetylase Inhibitors. A GOLPE/GRID Approach on Different Series of Compounds

scientific article published on 01 May 2006

A nitric oxide-dependent cross-talk between class I and III histone deacetylases accelerates skin repair

scientific article published on 5 March 2013

A novel coumarin-quinone derivative SV37 inhibits CDC25 phosphatases, impairs proliferation, and induces cell death.

scientific article published on 24 October 2013

Altered mitochondrial function in cells carrying a premutation or unmethylated full mutation of the FMR1 gene

scientific article published on 09 January 2020

Altered modulation of lamin A/C-HDAC2 interaction and p21 expression during oxidative stress response in HGPS

scientific article published on 15 August 2018

Amino acid starvation induces reactivation of silenced transgenes and latent HIV-1 provirus via down-regulation of histone deacetylase 4 (HDAC4)

scientific article

Antimalarial and antileishmanial activities of aroyl-pyrrolyl-hydroxyamides, a new class of histone deacetylase inhibitors

scientific article published on April 2004

Application of 3 μm particle-based amylose-derived chiral stationary phases for the enantioseparation of potential histone deacetylase inhibitors

scientific article published on 24 September 2011

Application of Small Epigenetic Modulators in Pediatric Medulloblastoma

scientific article published on 03 December 2018

Aroyl-pyrrolyl hydroxyamides: influence of pyrrole C4-phenylacetyl substitution on histone deacetylase inhibition

scientific article published on February 2006

Biochemical, structural, and biological evaluation of tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and LSD2

scientific article

Chronic stress and antidepressant induced changes in Hdac5 and Sirt2 affect synaptic plasticity.

scientific article

Class II HDAC inhibition hampers hepatic stellate cell activation by induction of microRNA-29

scientific article

Context-selective death of acute myeloid leukemia cells triggered by the novel hybrid retinoid-HDAC inhibitor MC2392.

scientific article published on 24 February 2014

Correction to 'Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells'

scientific article published on 01 September 2018

Coumarin polysulfides inhibit cell growth and induce apoptosis in HCT116 colon cancer cells.

scientific article published on 30 December 2011

Determinants of epigenetic resistance to HDAC inhibitors in dystrophic fibro-adipogenic progenitors

scientific article published on 04 April 2022

Detrimental effect of class-selective histone deacetylase inhibitors during tissue regeneration following hindlimb ischemia

scientific article published on 07 July 2013

Developing novel non-hydroxamate histone deacetylase inhibitors: the chelidamic warhead

Development of alkyl glycerone phosphate synthase inhibitors: Structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells

scientific article published on 28 November 2018

Discovery of Inhibitors for the Ether Lipid-Generating Enzyme AGPS as Anti-Cancer Agents

scientific article published on 31 August 2015

Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent

scientific article published on 24 December 2015

Discovery of the First Human Arylsulfatase A Reversible Inhibitor Impairing Mouse Oocyte Fertilization

scientific article published on 02 April 2020

Dissecting the role of novel EZH2 inhibitors in primary glioblastoma cell cultures: effects on proliferation, epithelial-mesenchymal transition, migration, and on the pro-inflammatory phenotype

scientific article published on 02 December 2019

EZH2 inhibitors: a patent review (2014-2016).

scientific article published on 10 April 2017

Editorial: Molecular Mechanisms and New Therapeutic Targets in Epithelial to Mesenchymal Transition (EMT) and Fibrosis

scientific article published on 01 January 2019

Effect of Class II HDAC inhibition on glutamate transporter expression and survival in SOD1-ALS mice

scientific article published on 18 July 2017

Emerging approaches for histone deacetylase inhibitor drug discovery

scientific article published on 20 April 2015

Epi-drugs in combination with immunotherapy: a new avenue to improve anticancer efficacy

scientific article published on 30 May 2017

Evaluation of histone deacetylases as drug targets in Huntington's disease models. Study of HDACs in brain tissues from R6/2 and CAG140 knock-in HD mouse models and human patients and in a neuronal HD cell model

scientific article

Evaluation of ∆2-pioglitazone, an analogue of pioglitazone, on colon cancer cell survival: Evidence of drug treatment association with autophagy and activation of the Nrf2/Keap1 pathway.

scientific article published on 29 April 2014

HDAC-class II specific inhibition involves HDAC proteasome-dependent degradation mediated by RANBP2.

scientific article

HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation

scientific article published on 16 July 2010

Histone Deacetylases Contribute to Excitotoxicity-Triggered Degeneration of Retinal Ganglion Cells In Vivo

scientific article published on 03 June 2019

Histone deacetylase inhibitors and neurodegenerative disorders: holding the promise

scientific article published on January 2009

Histone deacetylase inhibitors restore IL-10 expression in lipopolysaccharide-induced cell inflammation and reduce IL-1β and IL-6 production in breast silicone implant in C57BL/6J wild-type murine model.

scientific article published on 20 January 2016

Histone deacetylases as an epigenetic pillar for the development of hybrid inhibitors in cancer

scientific article published on 12 April 2019

Histone deacetylation in epigenetics: an attractive target for anticancer therapy

scientific article

Histone post-translational modifications by HPLC-ESI-MS after HT29 cell treatment with histone deacetylase inhibitors

scientific article published in December 2009

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

scientific article

Identification of Two New Synthetic Histone Deacetylase Inhibitors That Modulate Globin Gene Expression in Erythroid Cells from Healthy Donors and Patients with Thalassemia

article

Identification of a novel quinoline-based DNA demethylating compound highly potent in cancer cells

scientific article published on 06 May 2019

Identification of novel quinazoline derivatives as potent antiplasmodial agents

scientific article published on 17 October 2018

Inhibition of class I histone deacetylases unveils a mitochondrial signature and enhances oxidative metabolism in skeletal muscle and adipose tissue

scientific article published on 15 October 2012

Interplay among nucleosomal DNA, histone tails, and corepressor CoREST underlies LSD1-mediated H3 demethylation

scientific article

LSD1 inhibitors: a patent review (2010-2015).

scientific article published on 28 March 2016

MC1568 inhibits HDAC6/8 activity and influenza A virus replication in lung epithelial cells: role of Hsp90 acetylation

scientific article published on 14 October 2016

New insights on the mechanism of quinoline-based DNA Methyltransferase inhibitors.

scientific article published on 18 December 2014

New pyrrole-based histone deacetylase inhibitors: binding mode, enzyme- and cell-based investigations

scientific article published on 12 September 2008

Nitric oxide determines mesodermic differentiation of mouse embryonic stem cells by activating class IIa histone deacetylases: potential therapeutic implications in a mouse model of hindlimb ischemia

scientific article

Nitric oxide modulates chromatin folding in human endothelial cells via protein phosphatase 2A activation and class II histone deacetylases nuclear shuttling

scientific article published on 01 November 2007

Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity

scientific article published on 13 June 2011

Novel benzofuran–chromone and –coumarin derivatives: synthesis and biological activity in K562 human leukemia cells

article published in 2013

Novel cinnamyl hydroxyamides and 2-aminoanilides as histone deacetylase inhibitors: apoptotic induction and cytodifferentiation activity

scientific article published on 4 March 2011

Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells

scientific article published on 30 April 2015

Novel inhibitors of human histone deacetylases: design, synthesis and bioactivity of 3-alkenoylcoumarines

scientific article published on 28 June 2014

Novel pyrrole-containing histone deacetylase inhibitors endowed with cytodifferentiation activity

scientific article published on 4 April 2007

Novel reversible monoamine oxidase A inhibitors: highly potent and selective 3-(1H-pyrrol-3-yl)-2-oxazolidinones

scientific article published on 7 November 2011

Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities

scientific article published on 22 March 2008

Nucleocytoplasmic export of HDAC5 and SIRT2 downregulation: two epigenetic mechanisms by which antidepressants enhance synaptic plasticity markers

scientific article published on 08 August 2018

Oxidative stress and epigenetic regulation in ageing and age-related diseases

scientific article

PRMT1 arginine methyltransferase accumulates in cytoplasmic bodies that respond to selective inhibition and DNA damage

scientific article

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

scientific article

Pharmacological inhibition of EZH2 as a promising differentiation therapy in embryonal RMS

scientific article

Properly Substituted Cyclic Bis-(2-bromobenzylidene) Compounds Behaved as Dual p300/CARM1 Inhibitors and Induced Apoptosis in Cancer Cells

scientific article published on 08 July 2020

Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.

scientific article

Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts

article

Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

Pyrrole-based hydroxamates and 2-aminoanilides: histone deacetylase inhibition and cellular activities

scientific article

Reversible acetylation regulates vascular endothelial growth factor receptor-2 activity

scientific article

Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes ⬇️

scientific article

Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells

scientific article published on 15 January 2014

Sirtuin modulators control reactive gliosis in an in vitro model of Alzheimer's disease

scientific article published on 13 May 2014

Sirtuin modulators: an updated patent review (2012 - 2014).

scientific article

Six Years (2012-2018) of Researches on Catalytic EZH2 Inhibitors: The Boom of the 2-Pyridone Compounds

scientific article published on 19 October 2018

Small-molecule inhibitors of histone deacetylase for the treatment of cancer and non-cancer diseases: a patent review (2011 - 2013).

scientific article published on 08 January 2014

Specific activity of class II histone deacetylases in human breast cancer cells

scientific article

Structure-Activity Relationships on Cinnamoyl Derivatives as Inhibitors of p300 Histone Acetyltransferase.

scientific article published on 27 March 2017

Study of 1,4-dihydropyridine structural scaffold: discovery of novel sirtuin activators and inhibitors

scientific article

Synthesis and biological evaluation of 2-, 3-, and 4-acylaminocinnamyl-N-hydroxyamides as novel synthetic HDAC inhibitors

scientific article published on 01 May 2005

Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases.

scientific article

Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors

scientific article published on July 2007

Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A

scientific article

TNF/p38α/polycomb signaling to Pax7 locus in satellite cells links inflammation to the epigenetic control of muscle regeneration.

scientific article

Targeting Lysine Deacetylases (KDACs) in Parasites

scientific article

Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors

scientific article published on 4 January 2018

Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoic acid-induced differentiation

scientific article published on 08 April 2020

The Polycomb group (PcG) protein EZH2 supports the survival of PAX3-FOXO1 alveolar rhabdomyosarcoma by repressing FBXO32 (Atrogin1/MAFbx).

scientific article published on 11 November 2013

The Protein Arginine Methyltransferases 1 and 5 affect Myc properties in glioblastoma stem cells

scientific article published on 04 November 2019

epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors.

scientific article

tert-Butylcarbamate-containing histone deacetylase inhibitors: apoptosis induction, cytodifferentiation, and antiproliferative activities in cancer cells

scientific article published on 25 March 2013

List of works by Sergio Valente

"Shock and kill" effects of class I-selective histone deacetylase inhibitors in combination with the glutathione synthesis inhibitor buthionine sulfoximine in cell line models for HIV-1 quiescence

1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells

1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells

3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity

3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies

3-D QSAR Studies on Histone Deacetylase Inhibitors. A GOLPE/GRID Approach on Different Series of Compounds

A nitric oxide-dependent cross-talk between class I and III histone deacetylases accelerates skin repair

A novel coumarin-quinone derivative SV37 inhibits CDC25 phosphatases, impairs proliferation, and induces cell death.

Altered mitochondrial function in cells carrying a premutation or unmethylated full mutation of the FMR1 gene

Altered modulation of lamin A/C-HDAC2 interaction and p21 expression during oxidative stress response in HGPS

Amino acid starvation induces reactivation of silenced transgenes and latent HIV-1 provirus via down-regulation of histone deacetylase 4 (HDAC4)

Antimalarial and antileishmanial activities of aroyl-pyrrolyl-hydroxyamides, a new class of histone deacetylase inhibitors

Application of 3 μm particle-based amylose-derived chiral stationary phases for the enantioseparation of potential histone deacetylase inhibitors

Application of Small Epigenetic Modulators in Pediatric Medulloblastoma

Aroyl-pyrrolyl hydroxyamides: influence of pyrrole C4-phenylacetyl substitution on histone deacetylase inhibition

Biochemical, structural, and biological evaluation of tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and LSD2

Chronic stress and antidepressant induced changes in Hdac5 and Sirt2 affect synaptic plasticity.

Class II HDAC inhibition hampers hepatic stellate cell activation by induction of microRNA-29

Context-selective death of acute myeloid leukemia cells triggered by the novel hybrid retinoid-HDAC inhibitor MC2392.

Correction to 'Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells'

Coumarin polysulfides inhibit cell growth and induce apoptosis in HCT116 colon cancer cells.

Determinants of epigenetic resistance to HDAC inhibitors in dystrophic fibro-adipogenic progenitors

Detrimental effect of class-selective histone deacetylase inhibitors during tissue regeneration following hindlimb ischemia

Developing novel non-hydroxamate histone deacetylase inhibitors: the chelidamic warhead

Development of alkyl glycerone phosphate synthase inhibitors: Structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells

Discovery of Inhibitors for the Ether Lipid-Generating Enzyme AGPS as Anti-Cancer Agents

Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent

Discovery of the First Human Arylsulfatase A Reversible Inhibitor Impairing Mouse Oocyte Fertilization

Dissecting the role of novel EZH2 inhibitors in primary glioblastoma cell cultures: effects on proliferation, epithelial-mesenchymal transition, migration, and on the pro-inflammatory phenotype

EZH2 inhibitors: a patent review (2014-2016).

Editorial: Molecular Mechanisms and New Therapeutic Targets in Epithelial to Mesenchymal Transition (EMT) and Fibrosis

Effect of Class II HDAC inhibition on glutamate transporter expression and survival in SOD1-ALS mice

Emerging approaches for histone deacetylase inhibitor drug discovery

Epi-drugs in combination with immunotherapy: a new avenue to improve anticancer efficacy

Evaluation of histone deacetylases as drug targets in Huntington's disease models. Study of HDACs in brain tissues from R6/2 and CAG140 knock-in HD mouse models and human patients and in a neuronal HD cell model

Evaluation of ∆2-pioglitazone, an analogue of pioglitazone, on colon cancer cell survival: Evidence of drug treatment association with autophagy and activation of the Nrf2/Keap1 pathway.

HDAC-class II specific inhibition involves HDAC proteasome-dependent degradation mediated by RANBP2.

HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation

Histone Deacetylases Contribute to Excitotoxicity-Triggered Degeneration of Retinal Ganglion Cells In Vivo

Histone deacetylase inhibitors and neurodegenerative disorders: holding the promise

Histone deacetylase inhibitors restore IL-10 expression in lipopolysaccharide-induced cell inflammation and reduce IL-1β and IL-6 production in breast silicone implant in C57BL/6J wild-type murine model.

Histone deacetylases as an epigenetic pillar for the development of hybrid inhibitors in cancer

Histone deacetylation in epigenetics: an attractive target for anticancer therapy

Histone post-translational modifications by HPLC-ESI-MS after HT29 cell treatment with histone deacetylase inhibitors

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

Identification of Two New Synthetic Histone Deacetylase Inhibitors That Modulate Globin Gene Expression in Erythroid Cells from Healthy Donors and Patients with Thalassemia

Identification of a novel quinoline-based DNA demethylating compound highly potent in cancer cells

Identification of novel quinazoline derivatives as potent antiplasmodial agents

Inhibition of class I histone deacetylases unveils a mitochondrial signature and enhances oxidative metabolism in skeletal muscle and adipose tissue

Interplay among nucleosomal DNA, histone tails, and corepressor CoREST underlies LSD1-mediated H3 demethylation

LSD1 inhibitors: a patent review (2010-2015).

MC1568 inhibits HDAC6/8 activity and influenza A virus replication in lung epithelial cells: role of Hsp90 acetylation

New insights on the mechanism of quinoline-based DNA Methyltransferase inhibitors.

New pyrrole-based histone deacetylase inhibitors: binding mode, enzyme- and cell-based investigations

Nitric oxide determines mesodermic differentiation of mouse embryonic stem cells by activating class IIa histone deacetylases: potential therapeutic implications in a mouse model of hindlimb ischemia

Nitric oxide modulates chromatin folding in human endothelial cells via protein phosphatase 2A activation and class II histone deacetylases nuclear shuttling

Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity

Novel benzofuran–chromone and –coumarin derivatives: synthesis and biological activity in K562 human leukemia cells

Novel cinnamyl hydroxyamides and 2-aminoanilides as histone deacetylase inhibitors: apoptotic induction and cytodifferentiation activity

Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells

Novel inhibitors of human histone deacetylases: design, synthesis and bioactivity of 3-alkenoylcoumarines

Novel pyrrole-containing histone deacetylase inhibitors endowed with cytodifferentiation activity

Novel reversible monoamine oxidase A inhibitors: highly potent and selective 3-(1H-pyrrol-3-yl)-2-oxazolidinones

Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities

Nucleocytoplasmic export of HDAC5 and SIRT2 downregulation: two epigenetic mechanisms by which antidepressants enhance synaptic plasticity markers

Oxidative stress and epigenetic regulation in ageing and age-related diseases

PRMT1 arginine methyltransferase accumulates in cytoplasmic bodies that respond to selective inhibition and DNA damage

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

Pharmacological inhibition of EZH2 as a promising differentiation therapy in embryonal RMS

Properly Substituted Cyclic Bis-(2-bromobenzylidene) Compounds Behaved as Dual p300/CARM1 Inhibitors and Induced Apoptosis in Cancer Cells

Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.

Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts

Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

Pyrrole-based hydroxamates and 2-aminoanilides: histone deacetylase inhibition and cellular activities

Reversible acetylation regulates vascular endothelial growth factor receptor-2 activity

Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes ⬇️

Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells

Sirtuin modulators control reactive gliosis in an in vitro model of Alzheimer's disease

Sirtuin modulators: an updated patent review (2012 - 2014).