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High-Throughput Fluorescence Polarization Assay for the Enzymatic Activity of GTPase-Activating Protein of ADP-Ribosylation Factor (ARFGAP)
- Source :
- SLAS Discovery. 16:717-723
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- GTPase-activating proteins of ADP-ribosylation factors (ARFGAPs) play key cellular roles in vesicle production and trafficking, adhesion, migration, and development. Dysfunctional regulation of ARFGAPs has been implicated in various diseases, including cancer, Alzheimer disease, and autism. Unfortunately, there are few mechanistic details describing how ARFGAPs contribute to disease states. In this regard, it would be extremely helpful to have a set of small molecules that selectively and directly modulate specific ARFGAPs as probes to dissect ARFGAP-regulated cell signaling under various conditions. Currently, such probes are lacking, and their identification is hampered by the lack of a suitable high-throughput assay to monitor ARFGAP activity. Here, the authors describe and validate a robust high-throughput assay using fluorescence polarization to monitor the ability of diverse ARFGAPs to enhance the capacity of ARF1 to hydrolyze guanosine triphosphate.
- Subjects :
- Cell signaling
GTPase-activating protein
ADP ribosylation factor
High-throughput screening
Fluorescence Polarization
Biology
Guanosine triphosphate
Biochemistry
Analytical Chemistry
Small Molecule Libraries
Enzyme activator
chemistry.chemical_compound
Animals
Humans
GTPase-Activating Proteins
Membrane Proteins
High-Throughput Screening Assays
Rats
Cell biology
Enzyme Activation
Membrane protein
chemistry
Molecular Medicine
ADP-Ribosylation Factor 1
Biotechnology
Subjects
Details
- ISSN :
- 24725552
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- SLAS Discovery
- Accession number :
- edsair.doi.dedup.....b818ccc297d4ed4b7c1998ff25f5f357