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Curcumin is a potent DNA hypomethylation agent.
Molecular docking of the interaction of curcumin and DNMT1 suggested that curcumin covalently blocks the catalytic thiolate of C1226 of DNMT1 to exert its inhibitory effect. This was validated byExpand
ZIP8 regulates host defense through zinc-mediated inhibition of NF-κB.
Activation of the transcription factor NF-κB is essential for innate immune function and requires strict regulation. The micronutrient zinc modulates proper host defense, and zinc deficiency isExpand
Cryo-EM structure of the protein-conducting ERAD channel Hrd1 in complex with Hrd3
TLDR
Hrd1 is the crucial membrane component for retro-translocation, but it is unclear whether it forms a protein-conducting channel. Expand
Modulation of DNA Methylation by a Sesquiterpene Lactone Parthenolide
Hypermethylation of 5′-cytosine-guanosine islands of tumor suppressor genes resulting in their silencing has been proposed to be a hallmark of various tumors. Modulation of DNA methylation with DNAExpand
HDAC6 deacetylates and ubiquitinates MSH2 to maintain proper levels of MutSα.
MutS protein homolog 2 (MSH2) is a key DNA mismatch repair protein. It forms the MSH2-MSH6 (MutSα) and MSH2-MSH3 (MutSβ) heterodimers, which help to ensure genomic integrity. MutSα not onlyExpand
Negative Allosteric Modulators That Target Human α4β2 Neuronal Nicotinic Receptors
Allosteric modulation of neuronal nicotinic acetylcholine receptors (nAChRs) is considered to be one of the most promising approaches for therapeutics. We have previously reported on theExpand
Ca2+/Calmodulin-Dependent Protein Kinase II–Based Regulation of Voltage-Gated Na+ Channel in Cardiac Disease
Background— Human gene variants affecting ion channel biophysical activity and/or membrane localization are linked to potentially fatal cardiac arrhythmias. However, the mechanism for many humanExpand
Carborane Clusters in Computational Drug Design: A Comparative Docking Evaluation Using AutoDock, FlexX, Glide, and Surflex
TLDR
AutoDock, Glide, FlexX, and Surflex proved to be comparably efficient in the docking of closo- and nido-carboranyl antifolates into the active site of a human dihydrofolate reductase. Expand
Low active loading of cargo into engineered extracellular vesicles results in inefficient miRNA mimic delivery
ABSTRACT Extracellular vesicles (EVs) hold great potential as novel systems for nucleic acid delivery due to their natural composition. Our goal was to load EVs with microRNA that are synthesized byExpand
Effect of Novel Negative Allosteric Modulators of Neuronal Nicotinic Receptors on Cells Expressing Native and Recombinant Nicotinic Receptors: Implications for Drug Discovery
Allosteric modulation of nAChRs is considered to be one of the most promising approaches for drug design targeting nicotinic acetylcholine receptors (nAChRs). We have reported previously on theExpand
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