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View article: Endoscopic Treatment of Staple-Line Leaks After Sleeve Gastrectomy in Patients with Obesity: Which One is the Best Option, if Any? A Systematic Review with Meta-Analysis and Meta-regression
Endoscopic Treatment of Staple-Line Leaks After Sleeve Gastrectomy in Patients with Obesity: Which One is the Best Option, if Any? A Systematic Review with Meta-Analysis and Meta-regression Open
Laparoscopic sleeve gastrectomy (LSG) is the most common bariatric surgery, with staple-line leak (SLL) as its most severe complication. Various endoscopic treatments exist, but no universal algorithm is established. The aim of this paper …
View article: Deficiency of the commensal Bacteroides vulgatus exacerbates skeletal muscle damage in mouse and human models of Duchenne Muscular Dystrophy
Deficiency of the commensal Bacteroides vulgatus exacerbates skeletal muscle damage in mouse and human models of Duchenne Muscular Dystrophy Open
Gut microbiota perturbations are increasingly implicated in skeletal muscle disorders. In this study, we analyzed fecal samples from mice and humans with Duchenne muscular dystrophy (DMD), a severe X-linked myopathy, and found significant …
View article: The Impact of a Quinone Scaffold on Thermo-TRPs Modulation by Dimethylheptyl Phytocannabinoids
The Impact of a Quinone Scaffold on Thermo-TRPs Modulation by Dimethylheptyl Phytocannabinoids Open
Phytocannabinoids (pCBs) from Cannabis sativa represent an important class of bioactive molecules, potentially useful for the treatment of a wide range of diseases. Their efficacy is due to their ability to interact with multiple targets o…
View article: Bioguided Identification of Polymethoxyflavones as Novel Vascular CaV1.2 Channel Blockers from Citrus Peel
Bioguided Identification of Polymethoxyflavones as Novel Vascular CaV1.2 Channel Blockers from Citrus Peel Open
The huge amount of citrus peel produced worldwide represents an economic burden for society. However, this agricultural by-product is a rich source of natural molecules, potentially endowed with interesting pharmacological activities. In t…
View article: Identification of Cannabidiolic and Cannabigerolic Acids as <scp>MTDL AChE</scp>, <scp>BuChE,</scp> and <scp>BACE</scp>‐1 Inhibitors Against Alzheimer's Disease by In Silico, In Vitro, and In Vivo Studies
Identification of Cannabidiolic and Cannabigerolic Acids as <span>MTDL AChE</span>, <span>BuChE,</span> and <span>BACE</span>‐1 Inhibitors Against Alzheimer's Disease by In Silico, In Vitro, and In Vivo Studies Open
Cannabidiolic (CBDA) and cannabigerolic (CBGA) acids are naturally occurring compounds from Cannabis sativa plant, previously identified by us as dual PPARα/γ agonists. Since the development of multitarget‐directed ligands (MTDL) represent…
View article: Eukaryotic Initiation Translation Factor 2A activation by cannabidiolic acid alters the protein homeostasis balance in glioblastoma cells
Eukaryotic Initiation Translation Factor 2A activation by cannabidiolic acid alters the protein homeostasis balance in glioblastoma cells Open
Eukaryotic Initiation Translation Factor 2A (EIF2A) is considered to be primarily responsible for the initiation of translation when a cell is subjected to stressful conditions. However, information regarding this protein is still incomple…
View article: Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists
Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists Open
We report a blueprint for the rational design of G protein coupled receptor (GPCR) ligands with a tailored functional response. The present study discloses the structure-based design of cannabinoid receptor type 2 (CB2R) selecti…
View article: Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich <i>Cannabis sativa</i> L. Chemotype IV
Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich <i>Cannabis sativa</i> L. Chemotype IV Open
The first detailed phytochemical analysis of the cannabigerol (CBG)-rich chemotype IV of Cannabis sativa L. resulted in the isolation of the expected cannabigerolic acid/cannabigerol (CBGA/CBG) and cannabidiolic acid/cannabidiol (CB…
View article: Double-Relief Silver Coins Minted in the Greek Colonies (444–390/340–280/270 BC) of Southern Italy Analysed by XRF
Double-Relief Silver Coins Minted in the Greek Colonies (444–390/340–280/270 BC) of Southern Italy Analysed by XRF Open
A sample of 18 double-relief coins from different poleis of Magna Graecia and ancient Italy has been analysed using a handheld XRF spectrometer directly inside the Museo Provinciale Campano (Capua, Italy). The data analysis shows that (i) …
View article: Flipping the GPCR Switch: Structure–Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists
Flipping the GPCR Switch: Structure–Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists Open
We report the structure-based design of cannabinoid receptor type 2 (CB2R)-selective inverse agonists (S)-1 and (R)-1, which were derived from privileged agonist HU-308 by introduction of a phenyl group at the gem-dimethylheptyl sidechain.…
View article: MA‐XRF analysis of ancient silver coins minted in southern Italy
MA‐XRF analysis of ancient silver coins minted in southern Italy Open
At the Museo Campano (Capua, Italy), eight double‐relief silver coins belonging to southern Italian poleis and dated between the end of the 5th century and the beginning of the 3rd century BC were analysed. These coins are of great interes…
View article: Editorial: “Small molecules targeting transmembrane receptors and ion channels in drug discovery”
Editorial: “Small molecules targeting transmembrane receptors and ion channels in drug discovery” Open
EDITORIAL article Front. Mol. Biosci., 02 May 2023Sec. Structural Biology Volume 10 - 2023 | https://doi.org/10.3389/fmolb.2023.1183713
View article: Data from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability
Data from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability Open
Tumors with microsatellite instability (MSI) are caused by a defective DNA mismatch repair system that leads to the accumulation of mutations within microsatellite regions. Indels in microsatellites of coding genes can result in the synthe…
View article: Table S2 from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability
Table S2 from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability Open
Top Nous-209-derived peptides predicted to bind to HLA-A*02:01.
View article: Supplementary Data from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability
Supplementary Data from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability Open
Fig. S1: Number of immunogenic epitopes in healthy donors vaccinated with viral antigens. Fig. S2: Size distribution of FSPs in Nous-209. Fig. S3: Detection of Nous-209 FSMs in early and late stage MSI tumors. Fig.S4: Mutation allele frequ…
View article: Table S2 from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability
Table S2 from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability Open
Top Nous-209-derived peptides predicted to bind to HLA-A*02:01.
View article: Data from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability
Data from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability Open
Tumors with microsatellite instability (MSI) are caused by a defective DNA mismatch repair system that leads to the accumulation of mutations within microsatellite regions. Indels in microsatellites of coding genes can result in the synthe…
View article: Table S1 from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability
Table S1 from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability Open
List of 1087 FSPs suitable for the inclusion in NOUS-209 vaccine.
View article: Supplementary Data from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability
Supplementary Data from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability Open
Fig. S1: Number of immunogenic epitopes in healthy donors vaccinated with viral antigens. Fig. S2: Size distribution of FSPs in Nous-209. Fig. S3: Detection of Nous-209 FSMs in early and late stage MSI tumors. Fig.S4: Mutation allele frequ…
View article: Table S1 from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability
Table S1 from A Genetic Vaccine Encoding Shared Cancer Neoantigens to Treat Tumors with Microsatellite Instability Open
List of 1087 FSPs suitable for the inclusion in NOUS-209 vaccine.
View article: Marine Natural and Nature-Inspired Compounds Targeting Peroxisome Proliferator Activated Receptors (PPARs)
Marine Natural and Nature-Inspired Compounds Targeting Peroxisome Proliferator Activated Receptors (PPARs) Open
Peroxisome proliferator-activated receptors α, γ and β/δ (PPARα, PPARγ, and PPARβ/δ) are a family of ligand-activated transcriptional factors belonging to the superfamily of nuclear receptors regulating the expression of genes involved in …
View article: Platform Reagents Enable Synthesis of Ligand-Directed Cova-lent Probes: Study of Cannabinoid Receptor 2 in Live Cells
Platform Reagents Enable Synthesis of Ligand-Directed Cova-lent Probes: Study of Cannabinoid Receptor 2 in Live Cells Open
Pharmacological modulation of cannabinoid receptor type 2 (CB2R) holds promise for the treatment of neuroinflammatory disorders, such as Alzheimer’s disease. Despite the importance of CB2R, its expression and downstream signaling are insuf…
View article: 2-pentadecyl-2-oxazoline prevents cognitive and social behaviour impairments in the Amyloid β-induced Alzheimer-like mice model: Bring the α2 adrenergic receptor back into play
2-pentadecyl-2-oxazoline prevents cognitive and social behaviour impairments in the Amyloid β-induced Alzheimer-like mice model: Bring the α2 adrenergic receptor back into play Open
The 2-pentadecyl-2-oxazoline (PEA-OXA) is a natural compound with protective action in neuro-inflammation. We have previously shown that PEA-OXA behaves as an α2 adrenergic receptor (α2AR) antagonist and a putative protean agonist on hista…
View article: Biosynthesis of the Novel Endogenous 15-Lipoxygenase Metabolites N-13-Hydroxy-octodecadienoyl-ethanolamine and 13-Hydroxy-octodecadienoyl-glycerol by Human Neutrophils and Eosinophils
Biosynthesis of the Novel Endogenous 15-Lipoxygenase Metabolites N-13-Hydroxy-octodecadienoyl-ethanolamine and 13-Hydroxy-octodecadienoyl-glycerol by Human Neutrophils and Eosinophils Open
The endocannabinoids 2-arachidonoyl-glycerol and N-arachidonoyl-ethanolamine are lipids regulating many physiological processes, notably inflammation. Endocannabinoid hydrolysis inhibitors are now being investigated as potential anti-infla…
View article: The Combined Effect of Branching and Elongation on the Bioactivity Profile of Phytocannabinoids. Part I: Thermo-TRPs
The Combined Effect of Branching and Elongation on the Bioactivity Profile of Phytocannabinoids. Part I: Thermo-TRPs Open
The affinity of cannabinoids for their CB1 and CB2 metabotropic receptors is dramatically affected by a combination of α-branching and elongation of their alkyl substituent, a maneuver exemplified by the n-pentyl -> α,α-dimethylheptyl (DMH…
View article: Identification and Characterization of Cannabidiol as an OX1R Antagonist by Computational and In Vitro Functional Validation
Identification and Characterization of Cannabidiol as an OX1R Antagonist by Computational and In Vitro Functional Validation Open
The potential, multifaceted therapeutic profile of cannabidiol (CBD), a major constituent derived from the Cannabis sativa plant, covers a wide range of neurological and psychiatric disorders, ranging from anxiety to pediatric epilepsy and…
View article: The (Poly)Pharmacology of Cannabidiol in Neurological and Neuropsychiatric Disorders: Molecular Mechanisms and Targets
The (Poly)Pharmacology of Cannabidiol in Neurological and Neuropsychiatric Disorders: Molecular Mechanisms and Targets Open
Cannabidiol (CBD), the major nonpsychoactive Cannabis constituent, has been proposed for the treatment of a wide panel of neurological and neuropsychiatric disorders, including anxiety, schizophrenia, epilepsy and drug addiction due to the…
View article: Correction to: 2-Pentadecyl-2-oxazoline ameliorates memory impairment and depression-like behaviour in neuropathic mice: possible role of adrenergic alpha2- and H3 histamine autoreceptors
Correction to: 2-Pentadecyl-2-oxazoline ameliorates memory impairment and depression-like behaviour in neuropathic mice: possible role of adrenergic alpha2- and H3 histamine autoreceptors Open
View article: The Endocannabinoid System and PPARs: Focus on Their Signalling Crosstalk, Action and Transcriptional Regulation
The Endocannabinoid System and PPARs: Focus on Their Signalling Crosstalk, Action and Transcriptional Regulation Open
Peroxisome proliferator-activated receptors (PPARs) are a family of nuclear receptors including PPARα, PPARγ, and PPARβ/δ, acting as transcription factors to regulate the expression of a plethora of target genes involved in metabolism, imm…
View article: 2-Pentadecyl-2-oxazoline ameliorates memory impairment and depression-like behaviour in neuropathic mice: possible role of adrenergic alpha2- and H3 histamine autoreceptors
2-Pentadecyl-2-oxazoline ameliorates memory impairment and depression-like behaviour in neuropathic mice: possible role of adrenergic alpha2- and H3 histamine autoreceptors Open