A5065983701- Click Chemistry and Applications
- Advanced biosensing and bioanalysis techniques
- Enzyme function and inhibition
- Protein Degradation and Inhibitors
- Receptor Mechanisms and Signaling
- RNA Interference and Gene Delivery
- Ubiquitin and proteasome pathways
- Glycosylation and Glycoproteins Research
- Protein Tyrosine Phosphatases
- Immunotherapy and Immune Responses
- Virus-based gene therapy research
- Histone Deacetylase Inhibitors Research
- Protein Kinase Regulation and GTPase Signaling
- bioluminescence and chemiluminescence research
- Amino Acid Enzymes and Metabolism
- Peptidase Inhibition and Analysis
- Neuroscience and Neuropharmacology Research
- Estrogen and related hormone effects
- Cytokine Signaling Pathways and Interactions
- Hormonal Regulation and Hypertension
- Advanced Biosensing Techniques and Applications
- Monoclonal and Polyclonal Antibodies Research
- Biotin and Related Studies
Novartis (Switzerland)
2016-2021
Novartis Institutes for BioMedical Research
2017-2021
GlaxoSmithKline (United Kingdom)
2009-2010
We are introducing a new approach to evaluate cellular uptake of drugs and drug candidates into living cells. The is based on converting the protein target given class compounds fluorescent biosensor. By measuring binding different their cognate biosensor in live cells comparing these values those measured vitro, concentrations can be ranked. demonstrate that our strategy enables evaluation cytosol 2 classes inhibitors using two sensor designs; first, sensors comprising self-labeling SNAP...
Abstract To study the behavior of MDM2‐p53 inhibitors in a disease‐relevant cellular model, we have developed and validated set bioorthogonal probes that can be fluorescently labeled cells used high‐content screening assays. By using automated image analysis with single‐cell resolution, could visualize intracellular target binding compounds by co‐localization quantify upregulation upon inhibition an osteosarcoma model. Additionally, high‐throughput assay to occupancy non‐tagged competition...
Peptides constitute an important class of drugs for the treatment multiple metabolic, oncological, and neurodegenerative diseases, several hundred novel therapeutic peptides are currently in preclinical clinical stages development. However, many leads fail to advance clinically because poor cellular membrane tissue permeability. Therefore, assessment ability a peptide cross membranes is critical when developing peptide-based therapeutics. Current methods assess permeability limited by...
To study the behavior of MDM2-p53 inhibitors in a disease-relevant cellular model, we have developed and validated set bioorthogonal probes that can be fluorescently labeled cells used high-content screening assays. By using automated image analysis with single-cell resolution, could visualize intracellular target binding compounds by co-localization quantify upregulation upon inhibition an osteosarcoma model. Additionally, high-throughput assay to occupancy non-tagged competition identify...
ABSTRACT Targeted protein degradation is a rapidly developing therapeutic modality that promises lower dosing and enhanced selectivity as compared to traditional occupancy-driven inhibitors, the potential modulate historically intractable targets. While well-characterized E3 ligases CRBN VHL have been successfully redirected degrade numerous proteins, there are approximately 600 predicted additional family members may offer improved activity, substrate selectivity, and/or tissue...