OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Tumor suppressor serine/threonine-protein kinase involved in synaptic plasticity, centriole duplication and G1/S phase transition. Polo-like kinases act by binding and phosphorylating proteins that are already phosphorylated on a specific motif recognized by the POLO box domains. Phosphorylates CPAP, NPM1, RAPGEF2, RASGRF1, SNCA, SIPA1L1 and SYNGAP1. Plays a key role in synaptic plasticity and memory by regulating the Ras and Rap protein signaling: required for overactivity-dependent spine remodeling by phosphorylating the Ras activator RASGRF1 and the Rap inhibitor SIPA1L1 leading to their degradation by the proteasome. Conversely, phosphorylates the Rap activator RAPGEF2 and the Ras inhibitor SYNGAP1, promoting their activity. Also regulates synaptic plasticity independently of kinase activity, via its interaction with NSF that disrupts the interaction between NSF and the GRIA2 subunit of AMPARs, leading to a rapid rundown of AMPAR-mediated current that occludes long term depression. Required for procentriole formation and centriole duplication by phosphorylating CPAP and NPM1, respectively. Its induction by p53/TP53 suggests that it may participate in the mitotic checkpoint following stress.
Family:
Kinase
Sub Family:
Other Protein Kinase
Class:
Protein Ser/Thr
Gene Name:
PLK2
Gene ID:
10769
Gene Aliases:
SNK
Accession Number:
NM_006622
Organism:
Human
Construct Details:
65-409 recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
PLK2/Snk (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2 mg/mL casein, 10 mM Magnesium acetate and [γ-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 120 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in ethanol prior to drying and scintillation counting.
Substrate:
2 mg/mL casein
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 48.1µM )
Incubation:
120 min at Room temperature
Control Inhibitor:
Acid Blank
Test Sample Requirements:
Minimum for 1) Screen: 60 μl of 50X stock based on the top concentration to be tested -OR- 100 μl of 10 mM stock -OR- 1.5 mg (pre-weighed). 2) Dose Response: 80 μl of 50X stock based on the top concentration to be tested -OR- 100 μl of 10 mM stock -OR- 1.5 mg (pre-weighed). (PBS or HBSS prohibited)
Minimum Order Quantity:
2
Turnaround Time
Standard:
6 Business Days
Service Scheduling Note:
Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
KinaseProfiler
Testing Location:
KP - France - Celle L'Evescault
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