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tankyrase

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Target not currently curated in GtoImmuPdb

Target id: 3108

Nomenclature: tankyrase

Family: Poly ADP-ribosylating PARPs

Contents:

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
ARTD5 | PARP5a | PARP-5a | tankyrase 1 | tankyrase, TRF1-interacting ankyrin-related ADP-ribose polymerase | TNKS1
Database Links Click here for help
Alphafold O95271 (Hs), Q6PFX9 (Mm)
BRENDA 2.4.2.30
ChEMBL Target CHEMBL6164 (Hs), CHEMBL3232702 (Mm)
Ensembl Gene ENSG00000173273 (Hs), ENSMUSG00000031529 (Mm), ENSRNOG00000011625 (Rn)
Entrez Gene 8658 (Hs), 21951 (Mm), 290794 (Rn)
Human Protein Atlas ENSG00000173273 (Hs)
KEGG Enzyme 2.4.2.30
KEGG Gene hsa:8658 (Hs), mmu:21951 (Mm), rno:290794 (Rn)
OMIM 603303 (Hs)
Pharos O95271 (Hs)
RefSeq Nucleotide NM_003747 (Hs), NM_175091 (Mm), NM_001106084 (Rn)
RefSeq Protein NP_003738 (Hs), NP_780300 (Mm), NP_001099554 (Rn)
UniProtKB O95271 (Hs), Q6PFX9 (Mm)
Wikipedia TNKS (Hs)
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 5
⤷ pIC50 8.4 (IC50 4x10-9 M) [5]
basroparib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 3
⤷ pIC50 8.2 (IC50 5.8x10-9 M) [3]
AZ6102 Small molecule or natural product Hs Inhibition 8.2 pIC50 2
⤷ pIC50 8.2 (IC50 6x10-9 M) [2]
Description: Inhibition of enzymatic activity in vitro
compound 5 [Tomassi et al., 2020] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 6
⤷ pIC50 8.2 (IC50 6.1x10-9 M) [6]
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 4
⤷ pIC50 7.8 (IC50 1.43x10-8 M) [4]
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 6
⤷ pIC50 6.7 (IC50 2.18x10-7 M) [6]

References

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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. Kim DY, Kwon YJ, Seo WY, Kim UI, Ahn S, Choi SM, Bang HT, Kim K, Kim JS. (2022) Tankyrase-selective inhibitor STP1002 shows preclinical antitumour efficacy without on-target toxicity in the gastrointestinal tract. Eur J Cancer, 173: 41-51. [PMID:35849876]

4. 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]

5. 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]

6. 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-ribosylating PARPs: tankyrase. Last modified on 19/04/2023. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3108.