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Small-molecule agonist AdipoRon alleviates diabetic retinopathy through the AdipoR1/AMPK/EGR4 pathway
BackgroundDiabetes mellitus (DM) is a progressive disease that involves multiple organs due to increased blood glucose, and diabetic retinopathy (DR)...
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Small-molecule discovery through DNA-encoded libraries
The development of bioactive small molecules as probes or drug candidates requires discovery platforms that enable access to chemical diversity and...
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Next-generation neuropeptide Y receptor small-molecule agonists inhibit mosquito-biting behavior
BackgroundFemale Aedes aegypti mosquitoes can spread disease-causing pathogens when they bite humans to obtain blood nutrients required for egg...
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The landscape of small-molecule prodrugs
Prodrugs are derivatives with superior properties compared with the parent active pharmaceutical ingredient (API), which undergo biotransformation...
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Small-Molecule HIV Entry Inhibitors Targeting gp120 and gp41
Interrupting early events in the virus life cycle, such as those prior to the formation of provirus, could effectively prevent HIV-1 infection. HIV-1...
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Biomarkers and Target-Specific Small-Molecule Drugs in Alzheimer’s Diagnostic and Therapeutic Research: From Amyloidosis to Tauopathy
Alzheimer’s disease (AD) is the most common type of human dementia and is responsible for over 60% of diagnosed dementia cases worldwide. Abnormal...
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MM165 - A Small Hybrid Molecule Modulates the Kynurenine Pathway and Attenuates Lipopolysaccharide-Induced Memory Deficits and Inflammation
Cognitive dysfunctions are now recognized as core symptoms of various psychiatric disorders e.g., major depressive disorder. Sustained immune...
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SZC-6, a small-molecule activator of SIRT3, attenuates cardiac hypertrophy in mice
Sirtuin3 (SIRT3), a class III histone deacetylase, is implicated in various cardiovascular diseases as a novel therapeutic target. SIRT3 has been...
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Small-molecule caspase-1 inhibitor CZL80 terminates refractory status epilepticus via inhibition of glutamatergic transmission
Status epilepticus (SE), a serious and often life-threatening medical emergency, is characterized by abnormally prolonged seizures. It is not...
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Beyond the vaccines: a glance at the small molecule and peptide-based anti-COVID19 arsenal
Unprecedented efforts of the researchers have been witnessed in the recent past towards the development of vaccine platforms for the control of the...
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Anti-cytokine therapy and small molecule agents for the treatment of inflammatory bowel disease
Inflammatory bowel disease (IBD), including Crohn disease and ulcerative colitis, with multifactorial etiologies has led to a global...
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Identification of active small-molecule modulators targeting the novel immune checkpoint VISTA
BackgroundCancer immunotherapy has gained increasing popularity as a novel approach to treat cancer. A member of the B7 family, V-domain...
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A small-molecule TLR4 antagonist reduced neuroinflammation in female E4FAD mice
BackgroundAPOE genotype is the greatest genetic risk factor for sporadic Alzheimer’s disease (AD). APOE4 increases AD risk up to 12-fold compared to APOE3...
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Adiponectin receptor agonist AdipoRon modulates human and mouse platelet function
Adiponectin, an adipokine secreted by adipocytes, has anti-atherosclerotic and antithrombotic activities. AdipoRon is synthetic small molecule...
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RORγt agonist enhances anti-PD-1 therapy by promoting monocyte-derived dendritic cells through CXCL10 in cancers
BackgroundThe overall response rate to checkpoint blockade remains unsatisfactory, partially due to the immune-suppressive tumor microenvironment. A...
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Genetic and functional modulation by agonist MRS5698 and allosteric enhancer LUF6000 at the native A3 adenosine receptor in HL-60 cells
The A 3 adenosine receptor (AR) is an important inflammatory and immunological target. However, the underlying mechanisms are not fully understood....
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Bioinformatics driven discovery of small molecule compounds that modulate the FOXM1 and PPARA pathway activities in breast cancer
Our previous studies demonstrated that the FOXM1 pathway is upregulated and the PPARA pathway downregulated in breast cancer (BC), and especially in...
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Emerging Gene and Small Molecule Therapies for the Neurodevelopmental Disorder Angelman Syndrome
Angelman syndrome (AS) is a rare (~1:15,000) neurodevelopmental disorder characterized by severe developmental delay and intellectual disability,...
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Artificial Intelligence Generative Chemistry Design of Target-Specific Scaffold-Focused Small Molecule Drug Libraries
The de novo design of scaffold-focused and target-specific molecular structures using deep learning generative modeling introduces a promising...
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The mGluR2/3 orthosteric agonist LY-404,039 reduces dyskinesia, psychosis-like behaviours and parkinsonism in the MPTP-lesioned marmoset
LY-404,039 is an orthosteric agonist of metabotropic glutamate 2 and 3 receptors (mGluR 2/3 ) that may harbour additional agonist effect at dopamine D 2 ...
