Target type: cellularcomponent
An integrin complex that comprises one alpha8 subunit and one beta1 subunit. [PMID:12297042]
Integrin alpha8-beta1, also known as α8β1, is a transmembrane protein complex that plays a crucial role in cell-cell and cell-matrix interactions. The cellular component of this complex comprises the following:
1. **Extracellular Domain:**
- **α8 Subunit:** The extracellular domain of the α8 subunit consists of a large, globular head region that binds to specific extracellular matrix (ECM) ligands. This region is further subdivided into the following domains:
- **β-propeller:** This domain is composed of seven blade-like structures that provide a scaffold for ligand binding.
- **I-like domain:** This domain contains a metal ion-dependent adhesion site (MIDAS) that facilitates the binding of divalent cations, such as magnesium or manganese, which are essential for ligand recognition.
- **α-helical domain:** This domain extends from the I-like domain and contributes to ligand binding and interactions with the β1 subunit.
- **β1 Subunit:** The extracellular domain of the β1 subunit is also a globular head region that interacts with the α8 subunit and participates in ligand binding. It consists of:
- **β-propeller:** Similar to the α8 subunit, the β1 subunit contains a β-propeller domain.
- **Hybrid domain:** This domain combines features of both the β-propeller and I-like domains.
- **Cys-rich domain:** This domain is enriched in cysteine residues and plays a role in protein stability and conformation.
2. **Transmembrane Domain:**
- Both the α8 and β1 subunits contain a transmembrane domain that anchors the complex to the cell membrane. These domains are composed of hydrophobic amino acids that interact with the phospholipid bilayer of the cell membrane.
3. **Cytoplasmic Domain:**
- **α8 Subunit:** The cytoplasmic domain of the α8 subunit is relatively short and interacts with intracellular signaling molecules, particularly those involved in cell migration and adhesion.
- **β1 Subunit:** The cytoplasmic domain of the β1 subunit is larger and more complex than that of the α8 subunit. It contains a series of binding sites for various intracellular proteins, including:
- **Focal adhesion kinase (FAK):** FAK is a key regulator of cell adhesion and signaling.
- **Talin:** Talin links integrins to the actin cytoskeleton, which is responsible for cell shape and movement.
- **Kindlin:** Kindlin proteins are involved in integrin activation and clustering.
These intracellular interactions enable integrin α8-β1 to participate in a variety of cellular processes, including cell adhesion, migration, differentiation, and signal transduction.'
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Protein | Definition | Taxonomy |
---|---|---|
Integrin beta-1 | An integrin beta-1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P05556] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
haloperidol | haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279) | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
1,3-ditolylguanidine | 1,3-ditolylguanidine: structure given in first source; a selective ligand for the sigma binding sites in the brain | toluenes | |
tirofiban | tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group. Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME. | L-tyrosine derivative; piperidines; sulfonamide | anticoagulant; fibrin modulating drug; platelet glycoprotein-IIb/IIIa receptor antagonist |
arginyl-glycyl-aspartic acid | arginyl-glycyl-aspartic acid: amino acid sequence of basic unit of widespread cellular recognition system | oligopeptide | |
arginyl-glycyl-aspartyl-serine | arginyl-glycyl-aspartyl-serine: corresponds to cell attachment site of fibronectin; located near carboxyl-terminal region of alpha-chain of fibrinogen; inhibits platelet aggregation & fibrinogen binding to activated platelets | ||
glycyl-arginyl-glycyl-aspartyl-serine | glycyl-arginyl-glycyl-aspartyl-serine: synthetic peptide from fibronectins; inhibits experimental metastasis of murine melanoma cells | ||
d-arg-gly-asp-trp | arginyl-glycyl-aspartyl-tryptophan: a synthetic RGD-containing peptide | ||
l 738167 | L 738167: structure in first source | ||
cilengitide | Cilengitide: an alphaVbeta3 integrin antagonist that paralyzes cancer cells | oligopeptide | |
l 734217 | L 734217: fibrinogen receptor antagonist; structure given in first source | ||
cyclopamine | piperidines | glioma-associated oncogene inhibitor | |
arginyl-glycyl-aspartyl-phenylalanine | |||
cyclic(arg-gly-asp-d-phe-val) | |||
mk-0429 | |||
mocetinostat | mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11). mocetinostat: undergoing phase II clinical trials for treatment of cancer | aminopyrimidine; benzamides; pyridines; secondary amino compound; secondary carboxamide; substituted aniline | antineoplastic agent; apoptosis inducer; autophagy inducer; cardioprotective agent; EC 3.5.1.98 (histone deacetylase) inhibitor; hepatotoxic agent |
tr 14035 | N-(2,6-dichlorobenzoyl)-4-(2',6'-bismethoxyphenyl)phenylalanine: TR-14035 is the (L)-isomer; an antagonist of both alpha4beta1 and beta7 integrins; structure in first source | ||
bio 1211 | BIO 1211: integrin alpha4beta1 inhibitor; structure in first source |