A5076877102- Cannabis and Cannabinoid Research
- Neurotransmitter Receptor Influence on Behavior
- Pharmacological Receptor Mechanisms and Effects
- Cellular Mechanics and Interactions
- Nanofabrication and Lithography Techniques
- Cancer Treatment and Pharmacology
- Synthesis and biological activity
- Neuroscience and Neuropharmacology Research
- Force Microscopy Techniques and Applications
- Utopian, Dystopian, and Speculative Fiction
- Bacteriophages and microbial interactions
- Ubiquitin and proteasome pathways
- Asymmetric Synthesis and Catalysis
- Cell death mechanisms and regulation
- Forensic Toxicology and Drug Analysis
- Advanced Biosensing Techniques and Applications
- Click Chemistry and Applications
- Adenosine and Purinergic Signaling
- Nuclear Structure and Function
- Synthesis and Characterization of Heterocyclic Compounds
- Travel Writing and Literature
- Nicotinic Acetylcholine Receptors Study
- Asthma and respiratory diseases
- HER2/EGFR in Cancer Research
- Synthesis and pharmacology of benzodiazepine derivatives
AstraZeneca (Sweden)
2023
Cancer Research UK Scotland Institute
2015-2019
University of Minnesota
2013
NHS Lanarkshire
2011-2012
Merck (United Kingdom)
2010-2012
Fascin is an actin binding and bundling protein that not expressed in normal epithelial tissues but overexpressed a variety of invasive tumors. It has critical role cancer cell metastasis by promoting migration invasion. Here we report the crystal structures fascin complex with series novel potent inhibitors. Structure-based elaboration these compounds enabled development nanomolar affinities for fascin, good physicochemical properties ability to inhibit fascin-mediated filamentous actin....
Abstract Fascin 1 is an actin-bundling protein that dramatically overexpressed in a variety of invasive tumors and thought to have critical role cancer cell metastasis. However, as drug target it highly challenging due its mechanism protein-protein interaction the lack knowledge around actin-binding sites. Using fragment-based approach, biophysical assay screening X-ray crystallography, we been able identify optimize novel fascin inhibitors. Furthermore developed robust reproducible...
The Sanford-Burnham Medical Research Institute in collaboration with the National Cancer has performed a target-based high-throughput screening (HTS) campaign of ˜149,000 natural product extracts against panel ten apoptosis-inhibiting protein-protein interactions (PPI) that have been implicated human cancer, including proteins Bcl-2, Bcl-B, Bcl-W, Bcl-XL, Bfl-1, Mcl-1, cIAP-1 BIR2 and BIR3 domains, cIAP-2 domains. This joint effort is focused on discovery identification novel product-based...
Chronic cough is a common and persistent symptom of number chronic lung diseases or can also be idiopathic in origin, yet remains an unmet medical need. Cough reflex initiated following activation airway sensory nerve terminals by various different exogenous endogenous stimuli. Targeting this peripheral arm may uncover novel therapeutics. NaV1.7, voltage gated sodium channel, highly expressed on nerves, thought to key signal production propagation. The aim study was determine the...
Abstract The actin-bundling protein fascin 1 is markedly overexpressed in a range of invasive tumors and believed to play critical role cancer cell metastasis. Targeting however very challenging owing its mechanism protein-protein interaction lack knowledge regarding the crucial actin-binding sites. By combining fragment-based approach, biophysical assay screening X-ray crystallography, we have been able identify optimize novel inhibitors that show nanomolar affinity biochemical binding...