Results 81 to 90 of about 4,995,094 (293)

Microfluidic Nano‐Assembly of Red‐Blood‐Cell (RBC) Lipids and Components for Engineering Extracellular Vesicles

open access: yesAdvanced Healthcare Materials, EarlyView.
Engineered red blood cell‐derived extracellular vesicles (eRBCEVs) are synthesized via controlled microfluidic assembly from native RBC lipids, enabling tunable encapsulation of proteins, nucleic acids, nanoparticles, and viral vectors. The platform demonstrates reproducible nanoscale architecture, preserved membrane composition, and functional cargo ...
Chiranth K. Nagaraj   +23 more
wiley   +1 more source

TOLLIP Inhibits Psoriasis Progression via Suppressing PKM2‐Mediated Glycolysis in Keratinocytes

open access: yesAdvanced Science, EarlyView.
In this study, we identify TOLLIP as a critical regulator of psoriasis pathogenesis through its modulation of glycolytic metabolism. Our findings establish the TOLLIP‐PKM2‐glycolysis axis as a key mechanism linking metabolic reprogramming to psoriasis pathogenesis, and propose TOLLIP as a promising therapeutic target.
Xiuhuan Jiang   +11 more
wiley   +1 more source

Design and Engineering of an Artificial Bifunctional N‐Deacetylase/N‐Sulfotransferase for the Biosynthesis of N‐Sulfated Heparosan

open access: yesAdvanced Science, EarlyView.
An artificial bifunctional N‐deacetylase/N‐sulfotransferase was engineered in Escherichia coli by combining screened N‐deacetylases with an NST domain. The integrated engineering strategy improved enzyme performance. The optimized enzyme efficiently converted heparosan into N‐sulfated heparosan, addressing a key bottleneck in microbial heparin ...
Xintong Xi   +8 more
wiley   +1 more source

The Action of Positive Allosteric Modulators of the GABAAR Can Be Reversed by Novel Spiro Barbiturates [PDF]

open access: yes
GABAARs are pentameric ligand-gated ion channels that play a major role in mediating inhibition in the CNS. They are the target of many widely used positive allosteric modulators (PAMs) of GABAARs such as general anesthetics, sedatives, antiepileptics ...
Keith W., Miller   +4 more
core   +2 more sources

Systematic Position Mapping of Split CRISPR‐Cas12a Activators Enables Highly Sensitive miRNA Detection and Cancer Cell Stratification

open access: yesAdvanced Science, EarlyView.
ABSTRACT Amplification‐free Cas12a diagnostics with split crRNA enable rapid and programmable target recognition, yet insufficient understanding of DNA activator architecture prevents predictable control over trans‐cleavage activity and sensitivity. Here we systematically map over 200 split DNA activator configurations by introducing nicks at every ...
Xiaoyan Tang   +8 more
wiley   +1 more source

The mGluR2 Positive Allosteric Modulator, AZD8529, and Cue-Induced Relapse to Alcohol Seeking in Rats

open access: yes, 2016
Group II metabotropic glutamate receptors (mGluR2 and mGluR3) may control relapse of alcohol seeking, but previously available Group II agonists were unable to discriminate between mGluR2 and mGluR3.
Augier, Eric,   +11 more
core   +1 more source

Cancer‐Associated BCL‐2 Mutants Reveal Mechanisms Towards Venetoclax Resistance

open access: yesAdvanced Science, EarlyView.
Venetoclax (VEN) resistance in chronic lymphocytic leukemia arises from diverse BCL2 mutations. We map mechanisms contributing to VEN resistance across common BCL‐2 variants. G101V and D103Y reduce drug binding and increase sequestration of pro‐apoptotic proteins. V156D blocks VEN allosterically.
Jonas Aufdermauer   +9 more
wiley   +1 more source

Flavonoids as positive allosteric modulators of α7 nicotinic receptors

open access: yesNeuropharmacology, 2019
The use of positive allosteric modulators (PAM) of α7 nicotinic receptors is a promising therapy for neurodegenerative, inflammatory and cognitive disorders. Flavonoids are polyphenolic compounds showing neuroprotective, anti-inflammatory and pro-cognitive actions. Besides their well-known antioxidant activity, flavonoids trigger intracellular pathways
Beatriz Elizabeth Nielsen   +2 more
openaire   +4 more sources

Computational analysis of negative and positive allosteric modulator binding and function in metabotropic glutamate receptor 5 (in)activation

open access: yes, 2014
Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets because of their involvement in several neurological disease states, and mGluR5 in particular is a subtype whose controlled allosteric modulation, both ...
Dalton, James A. R.   +3 more
core   +1 more source

Pyrazole‐Derived Antibacterial Compounds Effectively Treat Methicillin‐Resistant Staphylococcus Aureus Infections by Inhibiting Aspartate Transcarbamoylase

open access: yesAdvanced Science, EarlyView.
This study unveils a novel antibacterial mechanism against MRSA, in which the compound Py‐27 selectively targets and inhibits aspartate transcarbamoylase (ATCase), a key enzyme in pyrimidine synthesis. This inhibition disrupts DNA replication, induces oxidative damage, leading to potent bactericidal activity.
Xiaorong Yang   +11 more
wiley   +1 more source

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