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tankyrase 2

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Target id: 3109

Nomenclature: tankyrase 2

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 - 1166 10q23.32 TNKS2 tankyrase 2
Mouse - 1166 19 C2 Tnks2 tankyrase, TRF1-interacting ankyrin-related ADP-ribose polymerase 2
Rat - 1166 1 Tnks2 tankyrase 2
Previous and Unofficial Names Click here for help
tankyrase, TRF1-interacting ankyrin-related ADP-ribose polymerase 2 | tankyrase | ARTD6 | PARP5B | PARP-5b | TANK2
Database Links Click here for help
Alphafold Q9H2K2 (Hs), Q3UES3 (Mm)
BRENDA 2.4.2.30
ChEMBL Target CHEMBL6154 (Hs), CHEMBL3232703 (Mm)
Ensembl Gene ENSG00000107854 (Hs), ENSMUSG00000024811 (Mm), ENSRNOG00000052664 (Rn)
Entrez Gene 80351 (Hs), 74493 (Mm), 309512 (Rn)
Human Protein Atlas ENSG00000107854 (Hs)
KEGG Enzyme 2.4.2.30
KEGG Gene hsa:80351 (Hs), mmu:74493 (Mm), rno:309512 (Rn)
OMIM 607128 (Hs)
Pharos Q9H2K2 (Hs)
RefSeq Nucleotide NM_025235 (Hs), NM_001163635 (Mm), NM_001107607 (Rn)
RefSeq Protein NP_079511 (Hs), NP_001157107 (Mm), NP_001101077 (Rn)
UniProtKB Q9H2K2 (Hs), Q3UES3 (Mm)
Wikipedia TNKS2 (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 5 [Tomassi et al., 2020] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.5 pIC50 7
⤷ pIC50 9.5 (IC50 3x10-10 M) [7]
basroparib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 3
⤷ pIC50 8.5 (IC50 3.2x10-9 M) [3]
NVP‐TNKS656 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 1,6
⤷ pIC50 8.2 (IC50 6x10-9 M) [1,6]
OM-1700 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 8.1 pIC50 8
⤷ pIC50 8.1 (IC50 7x10-9 M) [8]
AZ1366 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 2
⤷ pIC50 8.0 (IC50 1x10-8 M) [2]
RK-287107 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 4
⤷ pIC50 8.0 (IC50 1.06x10-8 M) [4]
compound 21 [PMID: 34141085] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 5
⤷ pIC50 7.2 (IC50 6.31x10-8 M) [5]
MC2050 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 7
⤷ pIC50 6.7 (IC50 1.93x10-7 M) [7]

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. Shultz MD, Cheung AK, Kirby CA, Firestone B, Fan J, Chen CH, Chen Z, Chin DN, Dipietro L, Fazal A et al.. (2013) Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor. J Med Chem, 56 (16): 6495-511. [PMID:23844574]

7. 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

8. Waaler J, Leenders RGG, Sowa ST, Alam Brinch S, Lycke M, Nieczypor P, Aertssen S, Murthy S, Galera-Prat A, Damen E et al.. (2020) Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor. J Med Chem, 63 (13): 6834-6846. [PMID:32511917]

How to cite this page

Poly ADP-ribosylating PARPs: tankyrase 2. Last modified on 19/04/2023. Accessed on 25/04/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3109.