β-catenin destruction complex proteins

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β-catenin destruction complex proteins

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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The β-catenin destruction multiprotein complex negatively regulates the canonical Wnt signalling pathway by targeting β-catenin for ubiquitination and proteasomal degradation. The complex includes axin, adenomatosis polyposis coli (APC), protein phosphatase 2A (PP2A) and glycogen synthase kinase 3 (GSK3).

Targets

3237

axin 2 Show summary »« Hide summary

Target Id

3237

Nomenclature

axin 2

Previous and unofficial names

axil | conductin

Genes

AXIN2 (Hs), Axin2 (Mm), Axin2 (Rn)

Ensembl ID

ENSG00000168646 (Hs), ENSMUSG00000000142 (Mm), ENSRNOG00000055010 (Rn)

UniProtKB AC

Q9Y2T1 (Hs), O88566 (Mm), AXIN2_RAT (Rn)

Inhibitors

CW85319 (Binding) pK_d 5.2 [2]

Comment

Axin 2 is a component of the β-catenin destruction complex. Mutations in the AXIN2 gene have been linked to the development of oligodontia and colorectal cancer [1,3,5], and in colorectal cancers with defects in DNA mismatch repair genes [4].

References

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1. Callahan N, Modesto A, Meira R, Seymen F, Patir A, Vieira AR. (2009) Axis inhibition protein 2 (AXIN2) polymorphisms and tooth agenesis. Arch Oral Biol, 54 (1): 45-9. [PMID:18790474]

2. Cheng LZ, Huang DL, Tang ZR, Zhang JH, Xiong T, Zhou C, Zhang NX, Fu R, Cheng YX, Wu ZQ. (2023) Pharmacological targeting of Axin2 suppresses cell growth and metastasis in colorectal cancer. Br J Pharmacol, 180 (23): 3071-3091. [PMID:37461816]

3. Lammi L, Arte S, Somer M, Jarvinen H, Lahermo P, Thesleff I, Pirinen S, Nieminen P. (2004) Mutations in AXIN2 cause familial tooth agenesis and predispose to colorectal cancer. Am J Hum Genet, 74 (5): 1043-50. [PMID:15042511]

4. Liu W, Dong X, Mai M, Seelan RS, Taniguchi K, Krishnadath KK, Halling KC, Cunningham JM, Boardman LA, Qian C et al.. (2000) Mutations in AXIN2 cause colorectal cancer with defective mismatch repair by activating beta-catenin/TCF signalling. Nat Genet, 26 (2): 146-7. [PMID:11017067]

5. Marvin ML, Mazzoni SM, Herron CM, Edwards S, Gruber SB, Petty EM. (2011) AXIN2-associated autosomal dominant ectodermal dysplasia and neoplastic syndrome. Am J Med Genet A, 155A (4): 898-902. [PMID:21416598]

How to cite this family page

Database page citation:

β-catenin destruction complex proteins. Accessed on 27/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=1081.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Buneman OP, Faccenda E, Harding SD, Spedding M, Cidlowski JA, Fabbro D, Davenport AP, Striessnig J, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets. Br J Pharmacol. 180 Suppl 2:S1-22.