Antonello Mai
YOU?
Author Swipe
View article: A Combined SIRT5 Activation and SIRT3 Inhibition Prevents Breast Cancer Spheroids Growth by Reducing HIF-1α and Mitophagy
A Combined SIRT5 Activation and SIRT3 Inhibition Prevents Breast Cancer Spheroids Growth by Reducing HIF-1α and Mitophagy Open
Background/Objectives: Metabolic reprogramming is an essential feature of tumors. Mitochondrial sirtuins SIRT3 and SIRT5 differently regulate glutamine metabolism with SIRT5 inhibiting glutaminase (GLS) and SIRT3 increasing glutamate dehyd…
View article: Structural snapshots of Pseudomonas aeruginosa LptB2FG and LptB2FGC reveal insights into lipopolysaccharide recognition and transport
Structural snapshots of Pseudomonas aeruginosa LptB2FG and LptB2FGC reveal insights into lipopolysaccharide recognition and transport Open
Gram-negative bacteria are intrinsically resistant to many antibiotics because of densely packed lipopolysaccharides (LPS) in the outer leaflet of their outer membrane (OM), which acts as a highly effective barrier towards the spontaneous …
View article: Quinoline-Based DNA Methyltransferase Inhibitors Featuring Basic Side Chains: Design, Synthesis, and Insight in Biochemical and Anticancer Cell Properties
Quinoline-Based DNA Methyltransferase Inhibitors Featuring Basic Side Chains: Design, Synthesis, and Insight in Biochemical and Anticancer Cell Properties Open
The quinoline DNMT inhibitors 4-21, incorporating basic chains, were designed, synthesized, and evaluated for their ability to inhibit DNMT1 and DNMT3A/3L by directly measuring DNA methylation. Pharmacomodulation yielded nanomolar inhibito…
View article: Discovery of First-in-Class Carbonic Anhydrase/Histone Deacetylase Dual Inhibitors with Antiproliferative Activity in Cancer Cells
Discovery of First-in-Class Carbonic Anhydrase/Histone Deacetylase Dual Inhibitors with Antiproliferative Activity in Cancer Cells Open
This study reports in vitro evidence supporting a new class of compounds capable of independently targeting the tumor-associated human (h) carbonic anhydrase (CA; EC 4.2.1.1) and histone deacetylase (HDAC; EC 3.5.1.98) isoforms as first-in…
View article: Brain wide engraftment of human monocytes induces neurodegeneration and cognitive dysfunction
Brain wide engraftment of human monocytes induces neurodegeneration and cognitive dysfunction Open
Transplantation of peripherally derived myeloid cells in combination with microglia depletion is increasingly being examined as a potential therapy for various neurological disorders.1-9 However, primitive yolk sac derived microglia and de…
View article: Benzodeazaoxaflavin Sirtuin Inhibitors Inhibit <i>Schistosoma mansoni</i> Sirt2 and Cause Phenotypic Changes and Lethality in Schistosomula and Adult Worm Stages
Benzodeazaoxaflavin Sirtuin Inhibitors Inhibit <i>Schistosoma mansoni</i> Sirt2 and Cause Phenotypic Changes and Lethality in Schistosomula and Adult Worm Stages Open
Schistosomiasis, a neglected tropical disease caused by trematodes of Schistosoma genus, urgently requires new treatments due to praziquantel's limited efficacy against juvenile worms as well as the threat of drug resistance. In this study…
View article: Additional Cover
Additional Cover Open
Cover legend: The cover image is based on the article A Xanthine Derivative With Novel Heat Shock Protein 90‐Alpha Inhibitory and Senolytic Properties by Sandra Atlante et al., https://doi.org/10.1111/acel.70047. [Image: see text]
View article: Advancements in Hydrazide-Based HDAC Inhibitors: A Review of Recent Developments and Therapeutic Potential
Advancements in Hydrazide-Based HDAC Inhibitors: A Review of Recent Developments and Therapeutic Potential Open
Histone deacetylase (HDAC) impairment is strongly related to various cancers as well as neurodegenerative and inflammatory diseases. Considering HDACs' crucial role as drug targets, over the past decade, the development of HDAC inhibitors …
View article: Tranylcypromine-Based LSD1 Inhibitors as Useful Agents to Reduce Viability of <i>Schistosoma mansoni</i>
Tranylcypromine-Based LSD1 Inhibitors as Useful Agents to Reduce Viability of <i>Schistosoma mansoni</i> Open
Schistosoma infections remain a major public health issue mainly in tropical and subtropical regions. While Praziquantel is the primary treatment for schistosomiasis, its limitations include resistance development and poor efficacy against…
View article: Cardioprotection Through Pharmacological Activation of Sirtuin 5 in a Murine Model of Acute Myocardial Infarction
Cardioprotection Through Pharmacological Activation of Sirtuin 5 in a Murine Model of Acute Myocardial Infarction Open
SIRT5 pharmacological agonism emerges as a novel cardioprotective target, leading to RISK pathway activation and mitochondria-related metabolic effects, converging at salvaging ischemic myocardium from I/R injury.
View article: Neutrophils shape the therapeutic efficacy of sirtuin 1 activity modulators in murine influenza virus infection
Neutrophils shape the therapeutic efficacy of sirtuin 1 activity modulators in murine influenza virus infection Open
Sirtuin 1 (Sirt1), a class III histone deacetylase, is a key regulator of gene expression in various immune cell types, including neutrophils, during infection and acute inflammation. Herein, we studied the effect of the Sirt1 activator (S…
View article: An improved multiplex RT–quantitative PCR assay can reveal sex-specific activity of transmission-blocking drugs on <i>ex vivo</i> gametocytes from <i>Plasmodium falciparum</i> asymptomatic infections
An improved multiplex RT–quantitative PCR assay can reveal sex-specific activity of transmission-blocking drugs on <i>ex vivo</i> gametocytes from <i>Plasmodium falciparum</i> asymptomatic infections Open
Objectives To develop a multiplex RT–quantitative PCR (RT–qPCR) assay to quantify sex-specific Plasmodium falciparum gametocyte transcripts (pfCCp4, pfMGET), for evaluating the impact of drug treatments on gametocyte viability for malaria …
View article: Development of C646‐Based Proteolysis Targeting Chimeras Degraders of the Lysine Acetyltransferases CBP and p300
Development of C646‐Based Proteolysis Targeting Chimeras Degraders of the Lysine Acetyltransferases CBP and p300 Open
The alteration of the lysine acetyltransferase activity and protein–protein interactions of the transcriptional co‐activators CREB‐binding protein (CBP) and p300 is linked to the development of both solid and hematological cancers. To targ…
View article: A Xanthine Derivative With Novel Heat Shock Protein 90‐Alpha Inhibitory and Senolytic Properties
A Xanthine Derivative With Novel Heat Shock Protein 90‐Alpha Inhibitory and Senolytic Properties Open
The accumulation of senescent cells contributes to aging and related diseases; therefore, discovering safe senolytic agents—compounds that selectively eliminate senescent cells—is a critical priority. Heat shock protein 90 (HSP90) inhibito…
View article: An Amazing 30-Year Journey around the DABO Family: A Medicinal Chemistry Lesson on a Versatile Class of Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors
An Amazing 30-Year Journey around the DABO Family: A Medicinal Chemistry Lesson on a Versatile Class of Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors Open
Since the emergence of AIDS, the non-nucleoside HIV-1 RT inhibitors (NNRTIs) have attracted the attention of scientists and clinicians due to their high potency and specificity combined with low toxicity. 3,4-Dihydro-2-alkoxy-6-benzyl-4-ox…
View article: Design of Benzyl-triazolopyrimidine-Based NADPH Oxidase Inhibitors Leads to the Discovery of a Potent Dual Covalent NOX2/MAOB Inhibitor
Design of Benzyl-triazolopyrimidine-Based NADPH Oxidase Inhibitors Leads to the Discovery of a Potent Dual Covalent NOX2/MAOB Inhibitor Open
NADPH oxidases (NOXs) are enzymes dedicated to reactive oxygen species (ROS) production and are implicated in cancer, neuroinflammation, and neurodegenerative diseases. VAS2870 is a covalent inhibitor of mainly NOX2 and NOX5. It alkylates …
View article: Dual manifestation of Dupuytren's contracture: A bilateral case analysis with clinical implications
Dual manifestation of Dupuytren's contracture: A bilateral case analysis with clinical implications Open
Dupuytren's disease is a chronic fibroproliferative disorder of the hand, characterised by progressive contracture of the fingers, which can significantly impair functionality. This article presents a unique case of post-surgical recurrenc…
View article: The inhibitory effects of Remodelin on murine myoblasts differentiation
The inhibitory effects of Remodelin on murine myoblasts differentiation Open
Summary Myoblasts differentiation is a highly regulated and complex process leading to the formation of fused and aligned mature myotubes. Growing interest in the role of epigenetics in muscle differentiation has highlighted epi-modulators…
View article: Lateral forehead flap in oral reconstruction: A case report
Lateral forehead flap in oral reconstruction: A case report Open
Introduction: Lateral Forehead flap is very versatile as it represents a good choice for reparation of different types of nose and oral cavity defects and provides an optimal, aesthetic, and functional outcome. In era of free transfer tiss…
View article: Off-Target Inhibition of Human Dihydroorotate Dehydrogenase (<i>h</i>DHODH) Highlights Challenges in the Development of Fat Mass and Obesity-Associated Protein (FTO) Inhibitors
Off-Target Inhibition of Human Dihydroorotate Dehydrogenase (<i>h</i>DHODH) Highlights Challenges in the Development of Fat Mass and Obesity-Associated Protein (FTO) Inhibitors Open
FTO, an N 6-methyladenosine (m6A) and N 6,2'-O-dimethyladenosine (m6Am) RNA demethylase, is a promising target for treating acute myeloid leukemia (AML) due to the significant anticancer activity of its inhibitors in preclinical models. He…
View article: Penoscrotal elephantiasis after treatment of prostate cancer: A case report
Penoscrotal elephantiasis after treatment of prostate cancer: A case report Open
Penoscrotal elephantiasis (EPS) is a terminal state of lymphoedema defined by a progressive histopathological state characterized by chronic inflammatory fibromatosis of the subdermal and dermal connective tissue caused by lymphatic and ve…
View article: Immune checkpoint inhibitors in advanced gastroesophageal adenocarcinoma: a series of patient-level meta-analyses in different programmed death-ligand 1 subgroups
Immune checkpoint inhibitors in advanced gastroesophageal adenocarcinoma: a series of patient-level meta-analyses in different programmed death-ligand 1 subgroups Open
In PD-L1low HER-2 negative GEAC, the benefit of first-line ICI is modest, yet significant. Further translational work is warranted to better select patients who could benefit from immunotherapy in this setting. Meanwhile, alternative thera…
View article: Epigenetic modulation of sirt1 and sirt6 in cardiovascular diseases: unraveling autophagy regulation and endothelial function
Epigenetic modulation of sirt1 and sirt6 in cardiovascular diseases: unraveling autophagy regulation and endothelial function Open
Background Heart failure (HF) and cardiovascular diseases (CVD) still represent major causes of death. Dysmetabolic conditions led by epigenetic alterations play a major role as CVD triggers, expecially those related to the modulation and …
View article: Activation and inhibition of sirtuins: From bench to bedside
Activation and inhibition of sirtuins: From bench to bedside Open
The sirtuin family comprises seven NAD + ‐dependent enzymes which catalyze protein lysine deacylation and mono ADP‐ribosylation. Sirtuins act as central regulators of genomic stability and gene expression and control key processes, includi…
View article: HDAC3 genetic and pharmacologic inhibition radiosensitizes fusion positive rhabdomyosarcoma by promoting DNA double-strand breaks
HDAC3 genetic and pharmacologic inhibition radiosensitizes fusion positive rhabdomyosarcoma by promoting DNA double-strand breaks Open
Radiotherapy (RT) plays a critical role in the management of rhabdomyosarcoma (RMS), the prevalent soft tissue sarcoma in childhood. The high risk PAX3-FOXO1 fusion-positive subtype (FP-RMS) is often resistant to RT. We have recently demon…