Page last updated: 2024-10-24

frizzled binding

Definition

Target type: molecularfunction

Binding to a frizzled (fz) receptor. [GOC:ceb]

Frizzled binding refers to the interaction of a protein with a member of the Frizzled (FZD) family of transmembrane receptors. These receptors are essential components of the Wnt signaling pathway, a crucial developmental signaling cascade involved in a wide range of biological processes, including cell fate determination, cell proliferation, and tissue patterning. Wnt proteins, a family of secreted glycoproteins, bind to Frizzled receptors, initiating a complex intracellular signaling cascade that ultimately regulates gene expression.

The molecular function of Frizzled binding can be described as follows:

1. **Ligand Recognition and Binding:** Frizzled receptors possess a large extracellular domain that serves as a binding site for Wnt proteins. This binding is highly specific, with different Wnt proteins exhibiting distinct affinities for specific Frizzled receptors.

2. **Conformational Changes:** Upon Wnt binding, Frizzled receptors undergo conformational changes. These changes are essential for initiating downstream signaling events.

3. **Recruitment of Co-receptors:** Frizzled receptors often require the presence of co-receptors, such as low-density lipoprotein receptor-related protein 6 (LRP6), to fully activate Wnt signaling. These co-receptors interact with Frizzled receptors, stabilizing the complex and facilitating the recruitment of downstream signaling molecules.

4. **Activation of Intracellular Signaling Cascades:** Wnt binding to Frizzled receptors leads to the activation of intracellular signaling pathways. These pathways involve a complex interplay of protein interactions and modifications, ultimately resulting in the regulation of gene expression.

5. **Regulation of Gene Expression:** Wnt signaling, triggered by Frizzled binding, influences the expression of genes involved in various developmental and cellular processes. This includes genes regulating cell fate determination, cell proliferation, cell migration, and tissue patterning.

Frizzled binding, therefore, plays a critical role in the intricate regulatory network of Wnt signaling, influencing a wide range of biological processes essential for proper development and homeostasis.'
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Proteins (4)

ProteinDefinitionTaxonomy
Protein Wnt-3aA protein Wnt-3a that is encoded in the genome of human. [PRO:DNx, UniProtKB:P56704]Homo sapiens (human)
MyocilinA myocilin that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99972]Homo sapiens (human)
Secreted frizzled-related protein 1A secreted frizzled-related protein 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8N474]Homo sapiens (human)
Proto-oncogene Wnt-3A proto-oncogene Wnt-3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P56703]Homo sapiens (human)

Compounds (10)

CompoundDefinitionClassesRoles
4-[(2,4,6-triamino-5-pyrimidinyl)azo]benzoic acidbenzoic acids
iwr-1 exoIWR-1-exo : A dicarboximide having an exo bridged phthalimide structure, substituted at nitrogen by a 4-(quinolin-8-ylcarbamoyl)benzoyl group. It is a weak axin stabilizer, an analogue of IWR-1-endo.bridged compound;
dicarboximide
axin stabilizer
1-(4-hydroxyphenyl)-3-(3-methoxyphenyl)thioureathioureas
apigeninChamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.trihydroxyflavoneantineoplastic agent;
metabolite
2',3,4-trihydroxychalcone2',3,4-trihydroxychalcone: structure given in first sourcecatechols;
chalcones
gw-5074
WAY-316606WAY-316606 : A sulfonamide resulting from the formal condensation of the sulfonic acid group of 5-(phenylsulfonyl)-2-(trifluoromethyl)benzenesulfonic acid with the primary amino group of piperidin-4-amine. An inhibitor of secreted Frizzled-Related Protein-1 (sFRP-1).(trifluoromethyl)benzenes;
piperidines;
secondary amino compound;
sulfonamide;
sulfone
secreted frizzled-related protein 1 inhibitor
CCT251545CCT251545 : A chloropyridine that is 3-chloropyridine substituted by a 1-oxo-2,8-diazaspiro[4.5]decan-8-yl group and a 4-(1-methyl-1H-pyrazol-4-yl)phenyl group at positions 4 and 5, respectively. It is an orally bioavailable inhibitor of Wnt signaling (IC50 = 5 nM) and a potent and selective chemical probe for cyclin-dependent kinases CDK8 and CDK19.

CCT251545: a Wnt signaling inhibitor; structure in first source
azaspiro compound;
chloropyridine;
pyrazoles
antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
Wnt signalling inhibitor
xav939XAV939 : A thiopyranopyrimidine in which a 7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine skeleton is substituted at C-4 by a hydroxy group and at C-2 by a para-(trifluoromethyl)phenyl group.

XAV939: selectively inhibits beta-catenin-mediated transcription; structure in first source
(trifluoromethyl)benzenes;
thiopyranopyrimidine
tankyrase inhibitor
nvp-tnks656