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Gene and Protein Information | ||||||
Frizzled family G protein-coupled receptor | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 7 | 574 | 2q33.1 | FZD7 | frizzled class receptor 7 | |
Mouse | 7 | 572 | 1 30.08 cM | Fzd7 | frizzled class receptor 7 | |
Rat | 7 | - | 9 | Fzd7 | frizzled class receptor 7 |
Previous and Unofficial Names |
FzE3 | frizzled family receptor 7 | Fzd7 | Fz7 |
Database Links | |
Alphafold | O75084 (Hs), Q61090 (Mm) |
CATH/Gene3D | 1.10.2000.10 |
ChEMBL Target | CHEMBL3559688 (Hs) |
Ensembl Gene | ENSG00000155760 (Hs), ENSMUSG00000041075 (Mm), ENSRNOG00000016119 (Rn) |
Entrez Gene | 8324 (Hs), 14369 (Mm), 301440 (Rn) |
Human Protein Atlas | ENSG00000155760 (Hs) |
KEGG Gene | hsa:8324 (Hs), mmu:14369 (Mm), rno:301440 (Rn) |
OMIM | 603410 (Hs) |
Pharos | O75084 (Hs) |
RefSeq Nucleotide | NM_003507 (Hs), NM_008057 (Mm) |
RefSeq Protein | NP_003498 (Hs), NP_032083 (Mm) |
UniProtKB | O75084 (Hs), Q61090 (Mm) |
Wikipedia | FZD7 (Hs) |
Natural/Endogenous Ligands |
Wnt |
Download all structure-activity data for this target as a CSV file
Agonist Comments | ||
WNT-3, WNT-3A, WNT-5A and WNT-7A bind to FZD7. Due to the lack of purified and biologically active WNTs hardly any information on the specificity and pharmacology of FZD-WNT interaction is available. Extensive and quantitative binding assays have not been performed with mammalian FZDs. The references above contain data showing the direct activation/interaction of FZD7 by individual WNTs. For additional information see [2]. |
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Monoclonal antibody vantictumab (OMP-18R5) was found to act as an antagonist at FZD7, and was also found to bind to FZD1, FZD2, FZD5 and FZD8 [3]. |
Antibodies | |||||||||||||||||||||||||||||||||||||||||||||||||||
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Immuno Process Associations | ||
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Primary Transduction Mechanisms | |
Transducer | Effector/Response |
Gs family Gi/Go family |
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References: 2 |
Secondary Transduction Mechanisms | |
Transducer | Effector/Response |
Other - See Comments | |
Comments: WNT/β-catenin signaling. | |
References: 2 |
Tissue Distribution | ||||||||
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Expression Datasets | |
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Functional Assays | ||||||||||
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Physiological Functions | ||||||||
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Physiological Consequences of Altering Gene Expression | ||||||||||
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Clinically-Relevant Mutations and Pathophysiology | ||||||||||||||
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1. Bengochea A, de Souza MM, Lefrançois L, Le Roux E, Galy O, Chemin I, Kim M, Wands JR, Trepo C, Hainaut P et al.. (2008) Common dysregulation of Wnt/Frizzled receptor elements in human hepatocellular carcinoma. Br J Cancer, 99 (1): 143-50. [PMID:18577996]
2. Dijksterhuis JP, Petersen J, Schulte G. (2013) WNT/Frizzled signaling: receptor-ligand selectivity with focus on FZD-G protein signaling and its physiological relevance. Br J Pharmacol,. [PMID:24032637]
3. Gurney A, Axelrod F, Bond CJ, Cain J, Chartier C, Donigan L, Fischer M, Chaudhari A, Ji M, Kapoun AM et al.. (2012) Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors. Proc Natl Acad Sci USA, 109 (29): 11717-22. [PMID:22753465]
4. Kim M, Lee HC, Tsedensodnom O, Hartley R, Lim YS, Yu E, Merle P, Wands JR. (2008) Functional interaction between Wnt3 and Frizzled-7 leads to activation of the Wnt/beta-catenin signaling pathway in hepatocellular carcinoma cells. J Hepatol, 48 (5): 780-91. [PMID:18313787]
5. King TD, Zhang W, Suto MJ, Li Y. (2012) Frizzled7 as an emerging target for cancer therapy. Cell Signal, 24 (4): 846-51. [PMID:22182510]
6. Kirikoshi H, Sekihara H, Katoh M. (2001) Up-regulation of Frizzled-7 (FZD7) in human gastric cancer. Int J Oncol, 19 (1): 111-5. [PMID:11408930]
7. Le Grand F, Jones AE, Seale V, Scimè A, Rudnicki MA. (2009) Wnt7a activates the planar cell polarity pathway to drive the symmetric expansion of satellite stem cells. Cell Stem Cell, 4 (6): 535-47. [PMID:19497282]
8. Li C, Wu Y, Wang W, Xu L, Zhou Y, Yue Y, Wu T, Yang M, Qiu Y, Huang M et al.. (2023) Structure-Based Ligand Discovery Targeting the Transmembrane Domain of Frizzled Receptor FZD7. J Med Chem, 66 (17): 11855-11868. [PMID:37669317]
9. Merle P, de la Monte S, Kim M, Herrmann M, Tanaka S, Von Dem Bussche A, Kew MC, Trepo C, Wands JR. (2004) Functional consequences of frizzled-7 receptor overexpression in human hepatocellular carcinoma. Gastroenterology, 127 (4): 1110-22. [PMID:15480989]
10. Nile AH, de Sousa E Melo F, Mukund S, Piskol R, Hansen S, Zhou L, Zhang Y, Fu Y, Gogol EB, Kömüves LG et al.. (2018) A selective peptide inhibitor of Frizzled 7 receptors disrupts intestinal stem cells. Nat Chem Biol, 14 (6): 582-590. [PMID:29632413]
11. Sagara N, Toda G, Hirai M, Terada M, Katoh M. (1998) Molecular cloning, differential expression, and chromosomal localization of human frizzled-1, frizzled-2, and frizzled-7. Biochem Biophys Res Commun, 252 (1): 117-22. [PMID:9813155]
12. Tanaka S, Akiyoshi T, Mori M, Wands JR, Sugimachi K. (1998) A novel frizzled gene identified in human esophageal carcinoma mediates APC/beta-catenin signals. Proc Natl Acad Sci USA, 95 (17): 10164-9. [PMID:9707618]
13. Tycko B, Li CM, Buttyan R. (2007) The Wnt/beta-catenin pathway in Wilms tumors and prostate cancers. Curr Mol Med, 7 (5): 479-89. [PMID:17691963]
14. Ueno K, Hiura M, Suehiro Y, Hazama S, Hirata H, Oka M, Imai K, Dahiya R, Hinoda Y. (2008) Frizzled-7 as a potential therapeutic target in colorectal cancer. Neoplasia, 10 (7): 697-705. [PMID:18592008]
15. von Maltzahn J, Bentzinger CF, Rudnicki MA. (2012) Wnt7a-Fzd7 signalling directly activates the Akt/mTOR anabolic growth pathway in skeletal muscle. Nat Cell Biol, 14 (2): 186-91. [PMID:22179044]
16. Yang L, Wu X, Wang Y, Zhang K, Wu J, Yuan YC, Deng X, Chen L, Kim CC, Lau S et al.. (2011) FZD7 has a critical role in cell proliferation in triple negative breast cancer. Oncogene, 30 (43): 4437-46. [PMID:21532620]
17. Yu H, Ye X, Guo N, Nathans J. (2012) Frizzled 2 and frizzled 7 function redundantly in convergent extension and closure of the ventricular septum and palate: evidence for a network of interacting genes. Development, 139 (23): 4383-94. [PMID:23095888]
18. Zhang W, Lu W, Ananthan S, Suto MJ, Li Y. (2017) Discovery of novel frizzled-7 inhibitors by targeting the receptor's transmembrane domain. Oncotarget, 8 (53): 91459-91470. [PMID:29207657]