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List of works by Antonello Mai

"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

2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies

scientific article

3-(1H-Pyrrol-1-yl)-2-oxazolidinones as reversible, highly potent, and selective inhibitors of monoamine oxidase type A.

scientific article published in March 2002

3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-alkylamides as a new class of synthetic histone deacetylase inhibitors. 1. Design, synthesis, biological evaluation, and binding mode studies performed through three different docking procedures

scientific article published on February 2003

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-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors

scientific article published in June 2001

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

scientific article published on 01 May 2006

5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives

scientific article

5-Alkyl-2-alkylamino-6-(2,6-difluorophenylalkyl)-3,4-dihydropyrimidin-4(3H)-ones, a new series of potent, broad-spectrum non-nucleoside reverse transcriptase inhibitors belonging to the DABO family.

scientific article published on March 2005

5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile

scientific article published on 17 July 2008

6-[1-(2,6-difluorophenyl)ethyl]pyrimidinones antagonize cell proliferation and induce cell differentiation by inhibiting (a nontelomeric) endogenous reverse transcriptase

scientific article published on November 2005

6-alkylthio-4-[1-(2,6-difluorophenyl)alkyl]-1H-[1,3,5]triazin-2-ones (ADATs): novel regulators of cell differentiation and proliferation

scientific article published on October 2006

A Quinoline-Based DNA Methyltransferase Inhibitor as a Possible Adjuvant in Osteosarcoma Therapy

scientific article published on 29 June 2018

A closer look into NADPH oxidase inhibitors: Validation and insight into their mechanism of action

scientific article published on 15 February 2020

A new nitrobenzoxadiazole-based GSTP1-1 inhibitor with a previously unheard of mechanism of action and high stability

scientific article published on December 2017

A new water soluble MAPK activator exerts antitumor activity in melanoma cells resistant to the BRAF inhibitor vemurafenib

scientific article

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 Gcn5p inhibitor represses cell growth, gene transcription and histone acetylation in budding yeast

scientific article published on 01 September 2005

A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.

scientific article

A novel orally active water-soluble inhibitor of human glutathione transferase exerts a potent and selective antitumor activity against human melanoma xenografts

scientific article published on February 2015

A photoreactive small-molecule probe for 2-oxoglutarate oxygenases

scientific article

Acute and chronic neurobehavioral effects of the designer drug and bath salt constituent 3,4-methylenedioxypyrovalerone in the rat

scientific article published on 15 January 2019

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

Amphetamine and the Smart Drug 3,4-Methylenedioxypyrovalerone (MDPV) Induce Generalization of Fear Memory in Rats

scientific article published on 29 November 2019

An Analog of BIX-01294 Selectively Inhibits a Family of Histone H3 Lysine 9 Jumonji Demethylases

scientific article

Analytical and semipreparative high performance liquid chromatography separation of stereoisomers of novel 3,4-dihydropyrimidin-4(3H)-one derivatives on the immobilised amylose-based Chiralpak IA chiral stationary phase

scientific article published on 01 July 2006

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

BLUEPRINT to decode the epigenetic signature written in blood.

scientific article

Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells

scientific article published on 7 September 2012

Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation

scientific article published in April 2002

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

scientific article

Biological effects of MC2050, a quinazoline-based PARP-1 inhibitor, in human neuroblastoma and EBV-positive Burkitt's lymphoma cells

scientific article published on 01 March 2011

CDK9 as a Valuable Target in Cancer: From Natural Compounds Inhibitors to Current Treatment in Pediatric Soft Tissue Sarcomas

scientific article published on 13 August 2020

Carprofen analogues as sirtuin inhibitors: enzyme and cellular studies

scientific article published on November 2012

Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues

scientific article published in February 2010

Chemogenomic profiling of the cellular effects associated with histone H3 acetylation impairment by a quinoline-derived compound

scientific article published on 21 August 2010

Chiral HPLC separation and absolute configuration of novel S-DABO derivatives

scientific article

Chiral resolution and molecular modeling investigation of rac-2-cyclopentylthio-6-[1-(2,6-difluorophenyl)ethyl]-3,4-dihydro-5-methylpyrimidin-4(3H)-one (MC-1047), a potent anti-HIV-1 reverse transcriptase agent of the DABO class

scientific article

Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides

scientific article published in May 2005

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

scientific article

Class II-selective histone deacetylase inhibitors. Part 2: Alignment-independent GRIND 3-D QSAR, homology and docking studies

scientific article published on 27 May 2007

Combined HAT/EZH2 modulation leads to cancer-selective cell death.

scientific article published on 22 May 2018

Combining 3-D quantitative structure-activity relationship with ligand based and structure based alignment procedures for in silico screening of new hepatitis C virus NS5B polymerase inhibitors

scientific article published in April 2010

Comparison of the effects of synthetic and plant-derived mTOR regulators on healthy human ovarian cells

scientific article published on 05 April 2019

Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C

scientific article published on February 2004

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

Correction: Sirtinol Treatment Reduces Inflammation in Human Dermal Microvascular Endothelial Cells.

scientific article published on 31 October 2011

Corrigendum: Selective targeting of HDAC1/2 elicits anticancer effects through Gli1 acetylation in preclinical models of SHH Medulloblastoma

scientific article published on 21 April 2017

Crystal structures of the mitochondrial deacylase Sirtuin 4 reveal isoform-specific acyl recognition and regulation features

scientific article published on 15 November 2017

Cytoplasmic HDAC4 regulates the membrane repair mechanism in Duchenne muscular dystrophy

scientific article published on 15 February 2022

DNA Methyltransferases Inhibitors from Natural Sources

scientific article published on 25 August 2015

Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells

scientific article published on 19 March 2020

Design, synthesis and biological evaluation of carboxy analogues of arginine methyltransferase inhibitor 1 (AMI-1).

scientific article published in March 2010

Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors

scientific article

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

Detrimental effects of the 'bath salt' methylenedioxypyrovalerone on social play behavior in male rats

scientific article published on 07 June 2020

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

Development of 1,2,4-Oxadiazoles as Potent and Selective Inhibitors of the Human Deacetylase Sirtuin 2: Structure-Activity Relationship, X-ray Crystal Structure, and Anticancer Activity

scientific article published on 27 February 2017

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

Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level

scientific article published on 25 March 2011

Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series

scientific article published on May 1997

Diphenylene iodonium is a non-covalent MAO inhibitor: a biochemical and structural analysis

scientific article published on 27 May 2020

Discovery of (Aryloxopropenyl)pyrrolyl Hydroxyamides as Selective Inhibitors of Class IIa Histone Deacetylase Homologue HD1-A ⬇️

scientific article published on 01 November 2003

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 salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells

scientific article published on 12 December 2012

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

scientific article published on 02 April 2020

Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans

scientific article published on 12 December 2006

Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors

scientific article published on April 2011

Disruptor of telomeric silencing 1-like (DOT1L): disclosing a new class of non-nucleoside inhibitors by means of ligand-based and structure-based approaches

scientific article published on 15 January 2018

Dissecting histone deacetylase role in pulmonary arterial smooth muscle cell proliferation and migration

scientific article published on 22 July 2014

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

Downregulation of miR-326 and its host gene β-arrestin1 induces pro survival activity of E2F1 and promotes medulloblastoma growth

scientific article published on 13 September 2020

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

scientific article published on 10 April 2017

EZH2, HIF-1, and Their Inhibitors: An Overview on Pediatric Cancers

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

scientific article published on 18 July 2017

Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones

scientific article published on 20 December 2018

Effects of Class II-Selective Histone Deacetylase Inhibitor on Neuromuscular Function and Disease Progression in SOD1-ALS Mice

scientific article published on 26 March 2018

Emerging Therapeutic Potential of SIRT6 Modulators

scientific article published in 2021

Emerging approaches for histone deacetylase inhibitor drug discovery

scientific article published on 20 April 2015

Enzymatic and Biological Characterization of Novel Sirtuin Modulators against Cancer

scientific article published on 12 November 2019

Enzyme kinetics and inhibition of histone acetyltransferase KAT8.

scientific article published on 22 October 2015

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

scientific article published on 30 May 2017

Epi-drugs to fight cancer: from chemistry to cancer treatment, the road ahead

scientific article published on 22 August 2008

Epigenetic Metalloenzymes

scientific article published on 01 January 2019

Epigenetic modulation of PGC-1α activity by GCN5 inhibitors: WO2010007085 ⬇️

scientific article published on July 15, 2011

Epigenetic polypharmacology: A new frontier for epi-drug discovery

article published in 2019

Erratum: Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect

scholarly article published in Oncogene

Essential Oil Extraction, Chemical Analysis and Anti-Candida Activity of Calamintha nepeta (L.) Savi subsp. glandulosa (Req.) Ball-New Approaches.

scientific article published on 26 January 2017

Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies.

scientific article

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

Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates

scientific article

Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes

scientific article

From PARP1 to TNKS2 Inhibition: A Structure-Based Approach

scientific article published on 03 February 2020

Gold drug auranofin restricts the viral reservoir in the monkey AIDS model and induces containment of viral load following ART suspension

scientific article published in July 2011

H19-Dependent Transcriptional Regulation of β3 and β4 Integrins Upon Estrogen and Hypoxia Favors Metastatic Potential in Prostate Cancer

scientific article published on 17 August 2019

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

scientific article

HDAC1 inhibition by MS-275 in mesothelial cells limits cellular invasion and promotes MMT reversal.

scientific article

HDAC2 blockade by nitric oxide and histone deacetylase inhibitors reveals a common target in Duchenne muscular dystrophy treatment

scholarly article

HDAC4-regulated STAT1 activation mediates platinum resistance in ovarian cancer.

scientific article

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

scientific article published on 16 July 2010

Highlights of the Keystone Symposium: sirtuins in metabolism, aging and disease

scientific article published on 18 May 2012

Histone Deacetylase Inhibitors: Structure-Based Modeling and Isoform-Selectivity Prediction ⬇️

scientific article published on July 19, 2012

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

scientific article published on 03 June 2019

Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells

scientific article published on 08 February 2016

Histone acetyltransferase inhibitors and preclinical studies

scientific article published on June 2009

Histone deacetylase inhibition modulates deoxyribonucleotide pools and enhances the antitumor effects of the ribonucleotide reductase inhibitor 3'-C-methyladenosine in leukaemia cells.

scientific article published on 11 February 2011

Histone deacetylase inhibitors and hemoglobin F induction in beta-thalassemia

scientific article published on 29 May 2008

Histone deacetylase inhibitors and neurodegenerative disorders: holding the promise

scientific article published on January 2009

Histone deacetylase inhibitors exert anti-tumor effects on human adherent and stem-like glioma cells

scientific article published on 17 January 2019

Histone deacetylase inhibitors induce thyroid cancer-specific apoptosis through proteasome-dependent inhibition of TRAIL degradation.

scientific article published on 5 October 2009

Histone deacetylase inhibitors may reduce pathogenicity and virulence in Candida albicans

scientific article

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 deacetylase inhibitors: keeping momentum for neuromuscular and cardiovascular diseases treatment

scientific article published on 19 March 2010

Histone deacetylase-3 activation promotes tumor necrosis factor-alpha (TNF-alpha) expression in cardiomyocytes during lipopolysaccharide stimulation

scientific article

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 modifications, stem cells and prostate cancer

scientific article published on January 2014

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

scientific article published in December 2009

Histone-deacetylase 8 drives the immune response and the growth of glioma

scientific article published on 26 July 2021

Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases

scientific article published on 30 December 2008

Identification of Inhibitors to Trypanosoma cruzi Sirtuins Based on Compounds Developed to Human Enzymes ⬇️

scientific article published on 22 May 2020

Identification of NuRSERY, a new functional HDAC complex composed by HDAC5, GATA1, EKLF and pERK present in human erythroid cells

scientific article published on March 2014

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 long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases.

scientific article published on 11 April 2008

Identification of novel quinazoline derivatives as potent antiplasmodial agents

scientific article published on 17 October 2018

Identification of small-molecule enhancers of arginine methylation catalyzed by coactivator-associated arginine methyltransferase 1.

scientific article

Identification of small-molecule inhibitors of the XendoU endoribonucleases family

scientific article

Identification of specific and semi-specific SIRT inhibitors through computer-aided studies ⬇️

scientific article published on September 1, 2011

Identification of structural features of 2-alkylidene-1,3-dicarbonyl derivatives that induce inhibition and/or activation of histone acetyltransferases KAT3B/p300 and KAT2B/PCAF.

scientific article

Identification of tri- and tetracyclic pyrimidinediones as sirtuin inhibitors

scientific article published on May 2010

Inhibition of Histone Deacetylase Class I but not Class II Is Critical for the Sensitization of Leukemic Cells to Tumor Necrosis Factor–Related Apoptosis-Inducing Ligand–Induced Apoptosis

article by Satoshi Inoue et al published 1 July 2006 in Cancer Research

Inhibition of Histone Demethylases LSD1 and UTX Regulates ERα Signaling in Breast Cancer

scientific article published on 16 December 2019

Inhibition of class I HDACs imprints adipogenesis toward oxidative and brown-like phenotype

scientific article published on 02 January 2020

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

Inside Cover: Identification of Structural Features of 2-Alkylidene-1,3-Dicarbonyl Derivatives that Induce Inhibition and/or Activation of Histone Acetyltransferases KAT3B/p300 and KAT2B/PCAF (ChemMedChem 1/2015)

scientific article published on 23 December 2014

Intergenerational inheritance of high fat diet-induced cardiac lipotoxicity in Drosophila

scientific article published in Nature Communications

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

scientific article

Investigation on QSAR and binding mode of a new class of human rhinovirus-14 inhibitors by CoMFA and docking experiments

scientific article published on 01 October 1996

IκB kinase ε targets interferon regulatory factor 1 in activated T lymphocytes.

scientific article published on 06 January 2014

KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumor aggressiveness and target of KAT inhibitor CPTH2.

scientific article published on 4 April 2018

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

scientific article published on 28 March 2016

Lysine Acetyltransferase Inhibitors From Natural Sources

scientific article published on 12 August 2020

Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives

scientific article published on 27 February 2017

Lysine acetylation regulates Bruton's tyrosine kinase in B cell activation

scientific article published on 30 November 2009

Lysine acetyltransferase inhibitors: structure-activity relationships and potential therapeutic implications.

scientific article published on 20 April 2018

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

Mass spectrometry enables the discovery of inhibitors of an LPS transport assembly disruption of protein-protein interactions

scholarly article

Metabolite profiling of ascidian Styela plicata using LC-MS with multivariate statistical analysis and their antitumor activity

scientific article published on December 2017

Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors

scientific article published on 22 July 2011

Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).

scientific article published on 14 January 2011

Multi-omics profiling reveals a distinctive epigenome signature for high-risk acute promyelocytic leukemia.

scientific article

N-[4-(1,1'-biphenyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines as non-oxazolidinone analogues of antimycobacterial U-100480.

scientific article published on June 1998

New 6-nitroquinolones: synthesis and antimicrobial activities

scientific article published on June 2004

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

Nitroquinolones with broad-spectrum antimycobacterial activity in vitro

scientific article

Non-cancer uses of histone deacetylase inhibitors: effects on infectious diseases and beta-hemoglobinopathies

scientific article published on January 2009

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 Pyridine-Based Hydroxamates and 2'-Aminoanilides as Histone Deacetylase Inhibitors: Biochemical Profile and Anticancer Activity

scientific article published on 21 November 2020

Novel Quinoline Compounds Active in Cancer Cells through Coupled DNA Methyltransferase Inhibition and Degradation

scientific article published on 14 February 2020

Novel Targeting of DNA Methyltransferase Activity Inhibits Ewing Sarcoma Cell Proliferation and Enhances Tumor Cell Sensitivity to DNA Damaging Drugs by Activating the DNA Damage Response

scientific article published on 01 January 2022

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 coumarin- and quinolinone-based polycycles as cell division cycle 25-A and -C phosphatases inhibitors induce proliferation arrest and apoptosis in cancer cells.

scientific article published on 10 April 2017

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

Nε-lysine acetylation determines dissociation from GAP junctions and lateralization of connexin 43 in normal and dystrophic heart

scientific article

Ontogenic-Specific Increasesin HDAC1 Activity and Transcription Factor Association During the Maturation of Human Adult Erythroblasts in Vitro.

scientific article published in 2009

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

scientific article

P300/CBP associated factor regulates nitroglycerin-dependent arterial relaxation by N(ε)-lysine acetylation of contractile proteins

scientific journal 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 activation of SIRT6 triggers lethal autophagy in human cancer cells

scientific article published on 24 September 2018

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

scientific article

Pharmacological inhibition of HDAC6 attenuates endothelial barrier dysfunction induced by thrombin

scientific article published on 21 April 2011

Pharmacological inhibition of lysine-specific demethylase 1 (LSD1) induces global transcriptional deregulation and ultrastructural alterations that impair viability in Schistosoma mansoni

scientific article published on 01 July 2020

Photoactivable peptides for identifying enzyme–substrate and protein–protein interactions

scientific article published on 13 December 2010

Polymyxins and quinazolines are LSD1/KDM1A inhibitors with unusual structural features

scientific article

Progress in the Development of Lysine Methyltransferase SETD8 Inhibitors.

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

Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity

scientific article

Protein recognition by short peptide reversible inhibitors of the chromatin-modifying LSD1/CoREST lysine demethylase

scientific article

Proteomic profile of differentially expressed plasma proteins from dystrophic mice and following suberoylanilide hydroxamic acid treatment.

scientific article published on 11 November 2009

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

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

scientific article published in June 2018

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

Pyrrolobenzodiazepines and related systems. 2. Synthesis and biological properties of isonoraptazepine derivatives

scientific article published in November 1992

Pyrrylphenylethanones related to cathinone and lefetamine: synthesis and pharmacological activities

scientific article (publication date: July 1992)

Quinoline derivative MC1626, a putative GCN5 histone acetyltransferase (HAT) inhibitor, exhibits HAT-independent activity against Toxoplasma gondii

scientific article published on 18 December 2006

Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells

scientific article published on 06 February 2014

RIP1-HAT1-SirT complex identification and targeting in treatment and prevention of cancer.

scientific article published on 13 March 2018

Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)

scientific article published on 18 August 2020

Researches on antibacterial and antifungal agents, X. Synthesis and antifungal activities of 1-(p-methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)azoles and some related products.

scientific article

Reversible acetylation regulates vascular endothelial growth factor receptor-2 activity

scientific article

Role of endogenous reverse transcriptase in murine early embryo development

scientific article published in November 2003

SIRT5 regulation of ammonia-induced autophagy and mitophagy

scientific article published in January 2015

Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect.

scientific article

Screen of pseudopeptidic inhibitors of human sirtuins 1-3: two lead compounds with antiproliferative effects in cancer cells

scientific article

Screening assays for epigenetic targets using native histones as substrates

scientific article published on 30 September 2011

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

Selective targeting of HDAC1/2 elicits anticancer effects through Gli1 acetylation in preclinical models of SHH Medulloblastoma.

scientific article published on 09 March 2017

Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile

scientific article published on 19 January 2011

Sirt4: A Multifaceted Enzyme at the Crossroads of Mitochondrial Metabolism and Cancer

scientific article published on 15 April 2020

Sirtinol treatment reduces inflammation in human dermal microvascular endothelial cells

scientific article

Sirtuin function in aging heart and vessels

scientific article published on 09 January 2015

Sirtuin functions and modulation: from chemistry to the clinic

scientific article

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

Sirtuin modulators: where are we now? A review of patents from 2015 to 2019

scientific article published on 13 April 2020

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

scientific article published on 19 October 2018

Slow-, tight-binding HIV-1 reverse transcriptase non-nucleoside inhibitors highly active against drug-resistant mutants

scientific article published on 01 April 2007

Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations

scientific article published on 27 February 2007

Small-Molecule Chromatin-Modifying Agents: Therapeutic Applications ⬇️

scientific article published on April 1, 2010

Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties

scientific article published on November 2006

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

Specific control of pancreatic endocrine β- and δ-cell mass by class IIa histone deacetylases HDAC4, HDAC5, and HDAC9

scientific article

Statins and Histone Deacetylase Inhibitors Affect Lamin A/C - Histone Deacetylase 2 Interaction in Human Cells

scientific article published on 31 January 2019

Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules

scientific article

Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules

article

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

scientific article published on 27 March 2017

Structure-Reactivity Relationships on Substrates and Inhibitors of the Lysine Deacylase Sirtuin 2 from Schistosoma Mansoni (SmSirt2)

Structure-Reactivity Relationships on Substrates and Inhibitors of the Lysine Deacylase Sirtuin 2 from Schistosoma mansoni (SmSirt2)

scientific article published on 20 September 2019

Structure-activity relationship studies on new DABOS: effect of substitutions at pyrimidine C-5 and C-6 positions on anti-HIV-1 activity

scientific article

Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase

scientific article

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

scientific article

Substrate-induced stable enzyme-inhibitor complex formation allows tight binding of novel 2-aminopyrimidin-4(3H)-ones to drug-resistant HIV-1 reverse transcriptase mutants

scientific article published in September 2008

Synthesis and Biological Properties of Novel, Uracil-Containing Histone Deacetylase Inhibitors

scientific article published on 01 October 2006

Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.

scientific article published on August 1995

Synthesis and biological characterization of amidopropenyl hydroxamates as HDAC inhibitors

scientific article published on August 2010

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 N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors

scientific article published in January 2010

Synthesis and biological evaluation of enantiomerically pure pyrrolyl-oxazolidinones as a new class of potent and selective monoamine oxidase type A inhibitors

scientific article

Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains

scientific article

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

scientific article published on July 2007

Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.

scientific article published on March 2004

Synthesis and structure--activity relationship of new cytotoxic agents targeting human glutathione-S-transferases

scientific article

Synthesis of new disoxaril analogues with potent and selective anti-human rhinovirus 14 activity

scientific article published in 1991

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 Histone Demethylases: A New Avenue for the Fight against Cancer ⬇️

scientific article published on June 1, 2011

Targeting Lysine Deacetylases (KDACs) in Parasites

scientific article

Targeting epigenetics in drug discovery

scientific article published in March 2014

Targeting histone acetylation/deacetylation in parasites: an update (2017-2020)

scientific article published on 29 June 2020

Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors

scientific article published on 4 January 2018

Targeting the anti-apoptotic Bcl-2 family proteins: machine learning virtual screening and biological evaluation of new small molecules

scientific article published on 28 February 2022

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 Histone Acetylase Activator Pentadecylidenemalonate 1b Rescues Proliferation and Differentiation in the Human Cardiac Mesenchymal Cells of Type 2 Diabetic Patients

scientific article published on 23 January 2014

The Innovative Potential of Statins in Cancer: New Targets for New Therapies

scientific article published on 18 June 2020

The Pan-Sirtuin Inhibitor MC2494 Regulates Mitochondrial Function in a Leukemia Cell Line

scientific article published on 21 May 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

The emerging role of epigenetics in human autoimmune disorders

The emerging role of histone lysine demethylases in prostate cancer

scientific article

The emerging role of lysine methyltransferase SETD8 in human diseases ⬇️

scientific article

The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases.

scientific article

The histone deacetylase inhibitor suberoylanilide hydroxamic acid reduces cardiac arrhythmias in dystrophic mice

scientific article published on 17 February 2010

The histone methyltransferase EZH2 as a druggable target in SHH medulloblastoma cancer stem cells

scientific article published on 2 August 2017

The relevance of Ki calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor.

scientific article published on 5 May 2017

The therapeutic uses of chromatin-modifying agents

scientific article published on June 2007

Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity

scientific article published in December 2016

Transcriptomic and genomic studies classify NKL54 as a histone deacetylase inhibitor with indirect influence on MEF2-dependent transcription

scientific article published on 01 March 2022

Tranylcypromine-Based LSD1 Inhibitors: Structure-Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation

scientific article published on 14 February 2020

Trends of LSD1 inhibitors in viral infections.

scientific article

Tumour-specific metabolic adaptation to acidosis is coupled to epigenetic stability in osteosarcoma cells

scientific article published on 15 March 2016

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

scientific article

p300/CBP-associated factor selectively regulates the extinction of conditioned fear

scientific article

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

scientific article published on 25 March 2013

α,γ-Diketocarboxylic Acids and Their Esters Act as Carbonic Anhydrase IX and XII Selective Inhibitors

scientific article published on 19 February 2019

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