A5046076121- Click Chemistry and Applications
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Trypanosoma species research and implications
- Fluorine in Organic Chemistry
- Synthesis and Reactivity of Heterocycles
- Biological Stains and Phytochemicals
- Synthesis and Biological Evaluation
- Alzheimer's disease research and treatments
- Porphyrin and Phthalocyanine Chemistry
- Research on Leishmaniasis Studies
- Monoclonal and Polyclonal Antibodies Research
- Parasite Biology and Host Interactions
- 14-3-3 protein interactions
- Synthesis and Reactions of Organic Compounds
- Biochemical and Molecular Research
- RNA and protein synthesis mechanisms
- Respiratory viral infections research
- Advanced Fluorescence Microscopy Techniques
- Microtubule and mitosis dynamics
- Liver Disease Diagnosis and Treatment
- Digestive system and related health
- Parkinson's Disease Mechanisms and Treatments
- Retinoids in leukemia and cellular processes
- Photochromic and Fluorescence Chemistry
University of California, San Diego
2020-2025
Center for Discovery
2020-2023
University of Montana
2023
Génétique Moléculaire Génomique Microbiologie
2015
Institut National des Sciences Appliquées Rouen Normandie
2014
Université de Rouen Normandie
2014
Normandie Université
2014
Laboratoire COBRA
2014
Centre National de la Recherche Scientifique
2014
Metabolic dysfunction-associated steatotic liver disease (MASLD) is a multifactorial chronic that can progress to metabolic steatohepatitis (MASH) and fibrosis, ultimately leading cirrhosis hepatocellular carcinoma. Oxidative stress believed play an important role in the development of MASH. Small aminothiol compounds such as cysteamine its oxidized precursor, cystamine, are known pleiotropic exhibit relatively potent antioxidant other effects. Herein, we evaluate efficacy well two...
Epicocconone is a natural latent fluorophore that widely used in biotechnology because of its large Stokes shift and lack fluorescence unconjugated state. However, the low photostability quantum yields epicocconone have limited wider use, absence total synthesis, this limitation has been long-standing problem. Here we report general strategy for synthesis analogues relies on 2-iodoxybenzoic acid-mediated dearomatization replacement triene tail product by an aromatic ring. This design element...
Studies in tau and Aβ plaque transgenic mouse models demonstrated that brain-penetrant microtubule (MT)-stabilizing compounds, including the 1,2,4-triazolo[1,5-a]pyrimidines, hold promise as candidate treatments for Alzheimer's disease related neurodegenerative tauopathies. Triazolopyrimidines have already been investigated anticancer agents; however, antimitotic activity of these compounds does not always correlate with stabilization MTs cells. Indeed, previous studies from our laboratories...
We identify the prolyl-tRNA synthetase (PRS) inhibitor halofuginone 1 , a compound in clinical trials for anti-fibrotic and anti-inflammatory applications 2 as potent of SARS-CoV-2 infection replication. The interaction spike protein with cell surface heparan sulfate (HS) promotes viral entry 3 . find that reduces HS biosynthesis, thereby reducing binding, pseudotyped virus, authentic infection. Halofuginone also potently suppresses replication post-entry is 1,000-fold more than Remdesivir 4...
Microtubule (MT)-stabilizing 1,2,4-triazolo[1,5-a]pyrimidines (TPDs) hold promise as candidate therapeutics for Alzheimer's disease (AD) and other neurodegenerative conditions. However, depending on the choice of substituents around TPD core, these compounds can elicit markedly different cellular phenotypes that likely arise from interaction congeners with either one or two spatially distinct binding sites within tubulin heterodimers (i.e., seventh site vinca site). In present study, we...
Fluorinated alcohols and phenols are potentially useful as bioisosteres of the carboxylic acid functional group. To enable a direct comparison properties fluorinated surrogates with those other commonly used, non-fluorinated bioisosteres, we conducted structure-property relationship (SPR) study based on matched molecular pair (MMP) analyses. A series representative examples have been characterized by experimentally determining physicochemical properties, such acidity (pK
Abstract The hallmark pathologies of the Alzheimer's disease (AD) brain are amyloid beta (Aβ)‐containing senile plaques and neurofibrillary tangles formed from microtubule (MT)‐binding tau protein. Tau becomes hyperphosphorylated disengages MTs in AD, with evidence resulting MT structure/function defects. Brain‐penetrant MT‐stabilizing compounds can normalize axonal transport mouse models pathology, thereby reducing neuron loss decreasing pathology. dysfunction is also observed dystrophic...
Tubulin and microtubules (MTs) are potential protein targets to treat parasitic infections our previous studies have shown that the triazolopyrimidine (TPD) class of MT-active compounds hold promise as antitrypanosomal agents. MT-targeting TPDs include structurally related but functionally diverse congeners interact with mammalian tubulin at either one or two distinct interfacial binding sites; namely, seventh vinca sites, which found within between α,β-tubulin heterodimers, respectively....
Intraneuronal inclusions composed of tau protein are found in Alzheimer's disease (AD) and other tauopathies. Tau normally binds microtubules (MTs), its disengagement from MTs misfolding AD is thought to result MT abnormalities. We previously identified triazolopyrimidine-containing MT-stabilizing compounds that provided benefit mouse models herein describe the characterization efficacy testing an optimized candidate, CNDR-51997.
Schistosomiasis is a parasitic disease that affects approximately 200 million people in developing countries. Current treatment relies on just one partially effective drug, and new drugs are needed. Tubulin microtubules (MTs) essential constituents of the cytoskeleton all eukaryotic cells considered potential drug targets to treat infections. The α- β-tubulin Schistosoma mansoni have ∼96% ∼91% sequence identity their respective human tubulins, suggesting compounds which bind mammalian...
Tubulin and microtubules (MTs) are potential protein targets to treat parasitic infections our previous studies have shown that the triazolopyrimidine (TPD) class of MT- active compounds hold promise as antitrypanosomal agents. MT-targeting TPDs include structurally related but functionally diverse congeners interact with mammalian tubulin at either one or two distinct interfacial binding sites; namely, seventh vinca sites, which found within between α,β-tubulin heterodimers, respectively....