Top ▲

tankyrase

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 3108

Nomenclature: tankyrase

Family: Poly ADP-ribose polymerases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1327 8p23.1 TNKS tankyrase
Mouse - 1320 8 21.16 cM Tnks tankyrase, TRF1-interacting ankyrin-related ADP-ribose polymerase
Rat - 1317 16q12.2 Tnks tankyrase
Previous and Unofficial Names Click here for help
tankyrase, TRF1-interacting ankyrin-related ADP-ribose polymerase | PARP5a | tankyrase 1 | ARTD5 | TNKS1 | PARP-5a
Database Links Click here for help
Alphafold
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.4.2.30

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 21 [PMID: 34141085] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 4
pIC50 8.4 (IC50 4x10-9 M) [4]
compound 5 [Tomassi et al., 2020] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 5
pIC50 8.2 (IC50 6.1x10-9 M) [5]
AZ1366 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 2
pIC50 8.1 (IC50 7x10-9 M) [2]
RK-287107 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.43x10-8 M) [3]
NVP‐TNKS656 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 1
pIC50 7.8 (IC50 1.55x10-8 M) [1]
MC2050 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 5
pIC50 6.7 (IC50 2.18x10-7 M) [5]
Immuno Process Associations
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0000209 protein polyubiquitination IDA

References

Show »

1. Cheung AK, Chin DN, Fan J, Miller-Moslin KM, Shultz MD, Smith TD, Tomlinson RC, Toure B-B, Visser MS. (2013) Novel 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors. Patent number: WO2013012723A1. Assignee: Novartis Ag, Chen, Zhuoliang. Priority date: 13/07/2011. Publication date: 24/01/2013.

2. Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA, Dishington AP, Gingipalli L, Gu C, Hawkins JL et al.. (2015) Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology. ACS Med Chem Lett, 6 (3): 254-9. [PMID:25815142]

3. Mizutani A, Yashiroda Y, Muramatsu Y, Yoshida H, Chikada T, Tsumura T, Okue M, Shirai F, Fukami T, Yoshida M et al.. (2018) RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model. Cancer Sci, 109 (12): 4003-4014. [PMID:30238564]

4. Qin D, Lin X, Liu Z, Chen Y, Zhang Z, Wu C, Liu L, Pan Y, Laquerre S, Emery J et al.. (2021) Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors. ACS Med Chem Lett, 12 (6): 1005-1010. [PMID:34141085]

5. Tomassi S, Pfahler J, Mautone N, Rovere A, Esposito C, Passeri D, Pellicciari R, Novellino E, Pannek M, Steegborn C et al.. (2020) From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. ACS Med Chem Lett, [Articles ASAP]. DOI: 10.1021/acsmedchemlett.9b00654

How to cite this page

Poly ADP-ribose polymerases: tankyrase. Last modified on 07/07/2021. Accessed on 30/11/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3108.