Results 81 to 90 of about 109,425 (326)

A molecular basis for selective antagonist destabilization of dopamine D3 receptor quaternary organization [PDF]

open access: yes, 2017
The dopamine D3 receptor (D3R) is a molecular target for both first-generation and several recently-developed antipsychotic agents. Following stable expression of this mEGFP-tagged receptor, Spatial Intensity Distribution Analysis indicated that a ...
Caltabiano, Gianluigi   +6 more
core   +2 more sources

Elucidating the monoamine oxidase B inhibitory effect of kaurene diterpenoids from Xylopia aethiopica: An in silico approach.

open access: yesPLoS ONE
Parkinson disease is a neurogenerative disease common in adults and results in different kinds of memory dysfuntions. This study evaluated the monoamine oxidase B (MAO-B) inhibitory potential of kaurane diterpenoids previously isolated from Xylopia ...
Funmilayo Gladys Famuyiwa   +12 more
doaj   +1 more source

Delivery of Multifunctional Microspheres via Intravesical Instillation for Bladder Carcinoma: Therapeutic Potential and Mechanistic Insights

open access: yesAdvanced Healthcare Materials, EarlyView.
PCTM microspheres were successfully synthesized using microfluidic and click chemistry techniques.In Vivo and in vitro experiments have shown that PCTM microspheres have obvious targeting, adhesion, membrane penetration and anti‐tumor properties for bladder tumors.The antitumor mechanism of PCTM microspheres is to indirectly induce S‐stage blockage of ...
Zhaoxiang Lu   +4 more
wiley   +1 more source

Formation and structure of the ferryl [Fe=O] in-termediate in the non-haem iron halogenase SyrB2: classical and QM/MM modelling agree [PDF]

open access: yes, 2017
To rationalise mechanistically the intriguing regio- and chemoselectivity patterns for different substrates of the non-haem iron/2-oxoglutarate dependent halogenase SyrB2, it is crucial to elucidate the structure of the pivotal [FeIV[double bond, length ...
Rugg, G., Senn, H.M.
core   +1 more source

A Molecular Docking and Dynamics Simulation Study on Prevention of Merozoite Red Blood Cell Invasion by Targeting Plasmodium vivax Duffy Binding Protein with Zingiberaceae Bioactive Compounds

open access: yesUniciencia
[Objective] Plasmodium vivax predominantly infects many people in numerous tropical areas, including Southeast Asia, the Western Pacific, the Americas, and the Eastern Mediterranean.
Muhammad Fikri Heikal   +5 more
doaj   +1 more source

DNA Origami‐Templated Aptamer Chiral Structures Realize Cellular Enantioselectivity

open access: yesAdvanced Materials, EarlyView.
Aptamers displayed on tubular DNA origami nanostructures in defined chiral orientations (left‐ or right‐handed) exhibit enantioselective interactions with cell surface target proteins. While the right‐handed configuration supports only transient binding, the left handedness energetically favors protein dimerization and promotes subsequent ...
Tingjie Song   +9 more
wiley   +1 more source

All-atom simulations reveal how single point mutations promote serpin misfolding

open access: yes, 2018
Protein misfolding is implicated in many diseases, including the serpinopathies. For the canonical inhibitory serpin {\alpha}1-antitrypsin (A1AT), mutations can result in protein deficiencies leading to lung disease, and misfolded mutants can accumulate ...
Beccara, Silvio a   +7 more
core   +1 more source

Serotonergic System‐Targeted Nucleic Acid Hydrogel Coordinates Excitability Restoration and Circuit Reconstruction for Spinal Cord Injury Therapy

open access: yesAdvanced Materials, EarlyView.
The study reports a DNA/RNA heteroduplex hydrogel (SeroPTEN‐CG) that undergoes DNase‐mediated hydrogel‐to‐nanogel transition for spinal cord injury therapy by targeting the serotonergic system, combining 5‐hydroxytryptamine (5‐HT)‐mediated excitability restoration to reactivate dormant interneurons with phosphatase and tensin homolog (PTEN)‐targeted ...
Chunlin Li   +19 more
wiley   +1 more source

Substrate-Specific Inhibition Constants for Phospholipase A2 Acting on Unique Phospholipid Substrates in Mixed Micelles and Membranes Using Lipidomics. [PDF]

open access: yes, 2019
Assaying lipolytic enzymes is extremely challenging because they act on water-insoluble lipid substrates, which are normally components of micelles, vesicles, and cellular membranes.
Armando, Aaron   +2 more
core   +6 more sources

Revealing the Acetylcholinesterase Inhibitory Potential of and Its Phytoconstituents: In Vitro and in Silico Approach

open access: yesBioinformatics and Biology Insights, 2022
The inhibition of acetylcholinesterase plays a vital role in the treatment of Alzheimer disease. This study aimed to explore the acetylcholinesterase inhibition potential of Phyllanthus amarus and its phytoconstituents through an in vitro and in silico ...
Kolade O Faloye   +10 more
doaj   +1 more source

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