Highly cytotoxic 1,5-diaryl-1H-imidazoles were studied to clarify the relationship between cytotoxicity and activity as vascular disrupting agents (VDA). All the compounds disorganized the tubulin cytoskeleton, affected endothelial cell morphology and capillary formation in vitro, and caused vessel shutdown and tumor necrosis in vivo, thus confirming their vascular disrupting properties. Nonetheless, the substitution patterns on the imidazole ring, responsible for greater interaction energy with tubulin and higher cytotoxicity, were not associated to greater vascular disrupting activity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm900968s | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Biologically-targeted discovery-replication scan identifies G×G interaction in relation to risk of Barrett's esophagus and esophageal adenocarcinoma.
HGG Adv
January 2025
Department of Epidemiology and Biostatistics, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
Inherited genetics represents an important contributor to risk of esophageal adenocarcinoma (EAC), and its precursor Barrett's esophagus (BE). Genome-wide association studies have identified ∼30 susceptibility variants for BE/EAC, yet genetic interactions remain unexamined. To address challenges in large-scale G×G scans, we combined knowledge-guided filtering and machine learning approaches, focusing on genes with (A) known/plausible links to BE/EAC pathogenesis (n=493) or (B) prior evidence of biological interactions (n=4,196).
View Article and Find Full Text PDFA microanatomical study of the precentral cerebral wall in human fetuses of the second trimester with ventriculomegaly and corpus callosal dysgenesis.
Clin Neurol Neurosurg
December 2024
Department of Anatomy, Kasturba Medical College, Manipal, Manipal Academy of Higher Education, Manipal, Karnataka, India. Electronic address:
Background: The complex structure and function of the cerebrum make it a key focus in neuroscience research. It develops from telencephalic vesicles through processes such as cell growth, division, and migration from the neuroepithelium's ventricular matrix, forming the six-layered isocortex or neocortex. Multipotent neuroepithelial cells give rise to both neuronal and glial precursors, which populate the cerebral cortex.
View Article and Find Full Text PDFEmotional Stress in Cardiac and Vascular Diseases.
Curr Vasc Pharmacol
January 2025
Department of Cardiology, Ippokrateio University Hospital, Athens, Greece.
Introduction/objective: Emotional, mental, or psychological distress, defined as increased symptoms of depression, anxiety, and/or stress, is common in patients with chronic diseases, such as cardiovascular (CV) disease (CVD).
Methods: Literature was reviewed regarding data from studies and meta-analyses examining the impact of emotional stress on the occurrence and outcome of several CVDs (coronary disease, heart failure, hypertension, arrhythmias, stroke). These influences' pathophysiology and clinical spectrum are detailed, tabulated, and pictorially illustrated.
Nanobody-assisted nanoluciferase fragment complementation for in situ measurement and visualization of endogenous protein-protein interaction.
Biosens Bioelectron
December 2024
Shenzhen Bay Laboratory, Shenzhen, 518132, China. Electronic address:
Here, we developed nanobody-assisted nanoluciferase fragment complementation for in situ measurement and visualization of endogenous protein-protein interaction (NanaPPI). When an interaction occurs, primary antibodies for two proteins bring the proximity of secondary nanobody-fused small/large fragment to reassemble into an intact NanoLuc variant, thus transforming interaction events to luminescent signals in situ with high sensitivity. Compared to proximity ligation assay, NanaPPI has a similar signal-to-background ratio, but it is more convenient with faster procedures, easier readout and lower cost.
View Article and Find Full Text PDFBasic Science and Pathogenesis.
Alzheimers Dement
December 2024
Gladstone Institutes, UCSF, San Francisco, CA, USA.
Background: Cerebrovascular alterations and innate immune activation are key features of Alzheimer's disease (AD). However, the mechanisms that link blood-brain barrier disruption to neurodegeneration are poorly understood and well-defined druggable targets at the neurovascular interface are limited.
Method: By developing a multiomic and genetic loss-of-function pipeline, we reported the transcriptomic and global phosphoproteomic landscape of blood-induced microglia activation and the causal role for fibrin in induction of neurodegenerative genes and oxidative stress pathways in innate immune cells.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!