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Exploring new histone deacetylase 6 inhibitors and their effects on reversing the α-tubulin deacetylation and cell morphology changes caused by methamphetamine
Indazole-based HDAC6 inhibitors with novel zinc-binding modifications were synthesized and evaluated to determine their potential to inhibit HDAC6....
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In Silico and In Vitro Antigiardiasic Potential of Grape Pomace Polyphenols Extracted by Hybrid Microwave-Ultrasound Methodology
Grape pomace is an agro-industrial residue with polyphenolic compounds that have different biological activities. There are few reports of the...
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Preparation and Mechanism of the Antitumor Action of a 4H-Aminochromene Compound
We report here studies of the antitumor action of a 4 H -aminochromene compound in a xenograft model of ALK-expressing lung adenocarcinoma in humanized nude...
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ACY-241, an HDAC6 inhibitor, overcomes erlotinib resistance in human pancreatic cancer cells by inducing autophagy
Histone deacetylase 6 (HDAC6) is a promising target for cancer treatment because it regulates cell mobility, protein trafficking, cell growth,...
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Insights into the structure and tubulin-targeted anticancer potential of N-(3-bromobenzyl) noscapine
BackgroundNoscapine is a non-narcotic, antitussive alkaloid isolated from plants of Papaveraceae family. This benzylisoquinoline alkaloid and its...
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Changes in expression of mesothelial BBS genes in 2D and 3D after lithium chloride and ammonium sulphate induction of primary cilium disturbance: a pilot study
BackgroundMalignant pleural mesothelioma (MPM), a rare and aggressive pleural tumor, has significant histological and molecular heterogeneity....
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Antibody–drug conjugates and bispecific antibodies targeting cancers: applications of click chemistry
Engineering approaches using antibody drug conjugates (ADCs) and bispecific antibodies (bsAbs) are designed to overcome the limitations of...
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Current Prospects and Clinical Status of Microalgae Derived Chemotherapeutics
Globally, despite clinical advancements made over a decade, cancer remains a prominent cause of death. Numerous drugs have been chemically...
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Deciphering the Antidiarrheal Mechanisms of Macleaya cordata by Combining Network Pharmacology, Molecular Docking, and Experimental Evaluations
Diarrhea continues to be a major public health problem and is thought to be the cause of 525,000 child fatalities annually. Studies have shown that Mac...
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Mitragynine inhibits hippocampus neuroplasticity and its molecular mechanism
BackgroundMitragynine (MIT), the primary indole alkaloid of kratom ( Mitragyna speciosa ), has been associated with addictive and cognitive decline...
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6′-Sialylactose abolished lipopolysaccharide-induced inflammation and hyper-permeability in endothelial cells
Disruption of the endothelial barrier function and reduction in cell migration leads to endothelial dysfunction. One of the most abundant human milk...
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Anticancer Activity–Structure Relationship of Quinolinone-Core Compounds: An Overall Review
Quinolinone/quinoline is one of the most unique structures in the discovery of heterocycles that have attracted much attention in the field of...
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Inhibition of autophagy with chloroquine dysregulates mitochondrial quality control and energetics in adipocytes
Autophagy is a complex degradation pathway through which damaged or dysfunctional proteins and organelles are removed. Its pharmacological modulators...
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Recent progress in biologically active indole hybrids: a mini review
The indole moiety is one of the most widespread heterocycles found in both natural products and biological systems. Indoles have important biological...
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Human milk oligosaccharides 3′-sialyllactose and 6′-sialyllactose attenuate LPS-induced lung injury by inhibiting STAT1 and NF-κB signaling pathways
Acute lung injury (ALI) is the leading cause of respiratory diseases induced by uncontrolled inflammation and cell death. Lipopolysaccharide (LPS) is...
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Antibody-drug conjugates in cancer therapy: innovations, challenges, and future directions
The emergence of antibody-drug conjugates (ADCs) as a potential therapeutic avenue in cancer treatment has garnered significant attention. By...
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Synthesis, Antiproliferative Activity, and Effect on Carcinoma A549 Cell Microtubules of New Tubuloclustin Analogs
Combretastatin analogs of the antitumor agent tubuloclustin { N -[7-(adamant-2-yloxy)-7-oxoheptanoyl]- N deacetylcolchicine} were prepared via...
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In vivo evaluation of a microtubule PET ligand, [11C]MPC-6827, in mice following chronic alcohol consumption
BackgroundExcessive alcohol consumption is a global health burden and requires a better understanding of its neurobiology. A lower density of brain...
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Antibody drug conjugates as targeted cancer therapy: past development, present challenges and future opportunities
Antibody drug conjugates (ADCs) are promising cancer therapeutics with minimal toxicity as compared to small cytotoxic molecules alone and have shown...
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Synthesis, Antiproliferative, and Molecular Docking Studies of 3-Mercapto-1,2,4-Triazole Derivatives as Combretastatin A-4 Analogs
In the present work, a series of 1,2,4-triazole derivatives are designed as combretastatin A-4 analogs with the 4-nitrophenyl group and different...