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Landscape factors influencing honey bee colony behavior in Southern California commercial apiaries
Colony brood levels, frames of bees (adult bee mass) and internal hive temperature were monitored for 60 colonies for each of two years as they were...
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A general strategy for diversifying complex natural products to polycyclic scaffolds with medium-sized rings
The interrogation of complex biological pathways demands diverse small molecule tool compounds, which can often lead to important therapeutics for...
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Synthesis of novel cytotoxic tetracyclic acridone derivatives and study of their molecular docking, ADMET, QSAR, bioactivity and protein binding properties
Acridone based synthetic and natural products with inherent anticancer activity advancing the research and generating a large number of structurally...
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IMB-T130 targets 3-dehydroquinate synthase and inhibits Mycobacterium tuberculosis
The anti-tuberculosis (TB) agent IMB-T130 was speculated to be a multi-target compound. In this research, we found that IMB-T130 inhibits the...
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Antimicrobial and antioxidant activities of different extracts from Aspergillus unguis SPMD-EGY grown on different media
BackgroundRecently, researchers demonstrate the importance of associated microorganisms as potential sources of bioactive natural products....
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Development of a novel Hsp90 inhibitor NCT-50 as a potential anticancer agent for the treatment of non-small cell lung cancer
Despite the development of advanced therapeutic regimens such as molecular targeted therapy and immunotherapy, the 5-year survival of patients with...
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Thiazole Amides, A Novel Class of Algaecides against Freshwater Harmful Algae
Currently, harmful algal blooms are being one of ever-increasing global environmental problems. Much attention has been paid to the use of natural...
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Cobalt-catalyzed electrooxidative C-H/N-H [4+2] annulation with ethylene or ethyne
Ethylene and ethyne are among the simplest two-carbon building blocks. However, quite limited methods can be applied to incorporate ethylene or...
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Small molecule inhibitors of RAS-effector protein interactions derived using an intracellular antibody fragment
Targeting specific proteināprotein interactions (PPIs) is an attractive concept for drug development, but hard to implement since intracellular...
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The quaternary structure of Thermus thermophilus aldehyde dehydrogenase is stabilized by an evolutionary distinct C-terminal arm extension
Aldehyde dehydrogenases (ALDH) form a superfamily of dimeric or tetrameric enzymes that catalyze the oxidation of a broad range of aldehydes into...
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mGlu1 Receptors Monopolize the Synaptic Control of Cerebellar Purkinje Cells by Epigenetically Down-Regulating mGlu5 Receptors
In cerebellar Purkinje cells (PCs) type-1 metabotropic glutamate (mGlu1) receptors play a key role in motor learning and drive the refinement of...
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A novel benzamine lead compound of histone deacetylase inhibitor ZINC24469384 can suppresses HepG2 cells proliferation by upregulating NR1H4
Histone deacetylases (HDACs) can enzymatically transferred acetyl functional group from protein or lysine residues of histone, so they can regulate...
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A novel retroviral vector system to analyze expression from mRNA with retained introns using fluorescent proteins and flow cytometry
The ability to overcome cellular restrictions that exist for the export and translation of mRNAs with retained introns is a requirement for the...
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Synthetic ligands for PreQ1 riboswitches provide structural and mechanistic insights into targeting RNA tertiary structure
Riboswitches are naturally occurring RNA aptamers that regulate gene expression by binding to specific small molecules. Riboswitches control the...
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Probing ligand recognition of the opioid pan antagonist AT-076 at nociceptin, kappa, mu, and delta opioid receptors through structure-activity relationships
Few opioid ligands binding to the three classic opioid receptor subtypes, mu, kappa and delta, have high affinity at the fourth opioid receptor, the...
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Aminoacyl sulfonamide assembly in SB-203208 biosynthesis
Sulfonamide is present in many important drugs, due to its unique chemical and biological properties. In contrast, naturally occurring sulfonamides...
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Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus
Glucokinase is one of the promising targets for glucose-lowering agents, and the development of GK activators are now considered as one of the most...
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USP7 small-molecule inhibitors interfere with ubiquitin binding
The ubiquitin system regulates essential cellular processes in eukaryotes. Ubiquitin is ligated to substrate proteins as monomers or chains and the...
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KH176 Safeguards Mitochondrial Diseased Cells from Redox Stress-Induced Cell Death by Interacting with the Thioredoxin System/Peroxiredoxin Enzyme Machinery
A deficient activity of one or more of the mitochondrial oxidative phosphorylation (OXPHOS) enzyme complexes leads to devastating diseases, with high...
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Synthesis and anti-obesity effects in vivo of Crotadihydrofuran C as a novel PPARĪ³ antagonist from Crotalaria albida
Crotadihydrofuran C (CC) from the herbs of Crotalaria albida is able to inhibit adipocyte differentiation and lipid accumulation. However, the...
