Poly (ADP-ribose) Polymerase 5A (PARP5A) Human Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Poly (ADP-ribose) polymerase 5A (PARP5A, also known as Tankyrase 1, TNKS1, ARTD5) is a member of the PARP family and catalyzes the transfer of an ADP-ribose from the co-substrate NAD+ on a target protein. PARP5A consists of an N-terminal HPS domain, 24 ankyrin repeats, a SAM domain, and a carboxy-terminal PARP catalytic domain. PARP5A shares a high sequence identity with PARP5B, and both regulate telomere maintenance, Wnt/β-catenin signaling, and DNA repair, involved in various cellular functions. PARylation of TRF1 by PARP5 results in the degradation of TRF1, enabling telomere elongation. Coinhibition of PARP5 and telomerase synergistically shorten telomere length in gastric cancer cells. PARP5 activity also promotes Wnt/β-catenin pathway and combined treatment with a Wnt/PARP5 inhibitor reduced nuclear β-catenin and repressed tumor growth.
Family:
DNA Repair & Mitotic Regulation
Class:
Other
Protein Name:
PARP5A
Uniprot Number:
O95271
Protein Aliases:
ARTD5
Gene Name:
TNKS
Gene ID:
8658
Gene Aliases:
TIN1, TINF1, TNKS1, PARP-5a, PARP5A, pART5, ARTD5
Accession Number:
NM_003747
Organism:
Human
Construct Details:
fragment, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrophotometry
Platform:
Plate reader
Measured Response:
Absorbance
Testing Information
Procedure Summary:
Human recombinant protein PARP5A expressed in Sf9 cells is used. 100 ng histone proteins are coated on a 96-well plate. Test compound and/or vehicle is preincubated with 0.1 µg/ml enzyme for 15 minutes at 25°C in Tris-HCl buffer pH 7.4. The reaction is initiated by addition of 100 µM spiked biotinylated NAD+ plus NAD+ for another 60 minutes reaction time. Streptavidin-HRP is added and followed by addition of the TMB substrate to produce color that can be measured at 450 nm on a spectrophotometer. Compounds are screened at 10 µM.
Substrate:
100 µM NAD+
Incubation:
60 min at 25°C
Control Inhibitor:
XAV-939
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
PARP Screen LeadHunter Panel - TW
Item: PP317
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