Page last updated: 2024-10-24

regulation of protein tyrosine kinase activity

Definition

Target type: biologicalprocess

Any process that modulates the rate, frequency, or extent of protein tyrosine kinase activity. [GOC:dph, GOC:tb]

Protein tyrosine kinases (PTKs) are a family of enzymes that catalyze the phosphorylation of tyrosine residues on target proteins. This phosphorylation event can alter the activity, localization, and interactions of these target proteins, playing a crucial role in a wide range of cellular processes, including cell growth, differentiation, proliferation, and survival.

The regulation of PTK activity is a tightly controlled process involving multiple layers of mechanisms:

1. **Regulation by upstream signaling molecules:** PTKs are often activated by upstream signaling molecules, such as growth factors, cytokines, and hormones. These molecules bind to their specific receptors, triggering a cascade of downstream signaling events that ultimately activate the PTK.

2. **Autophosphorylation:** Many PTKs possess intrinsic kinase activity and can autophosphorylate themselves. This autophosphorylation event can create binding sites for other signaling molecules, leading to further activation and downstream signaling.

3. **Scaffolding proteins:** Scaffolding proteins can bring together multiple signaling molecules, including PTKs, their substrates, and regulatory proteins, facilitating efficient signal transduction and localized activation of PTKs.

4. **Adaptor proteins:** Adaptor proteins can act as intermediaries, linking PTKs to their substrates or other signaling molecules, thereby mediating their activity.

5. **Inhibitory proteins:** A number of inhibitory proteins can directly bind to PTKs and prevent their activity. These inhibitors can act by blocking the active site of the kinase, preventing substrate binding, or by inducing conformational changes that inhibit kinase activity.

6. **Post-translational modifications:** PTKs can be regulated by post-translational modifications, such as phosphorylation, ubiquitination, and acetylation. These modifications can influence the activity, stability, and localization of PTKs.

7. **Subcellular localization:** PTKs are often localized to specific subcellular compartments, such as the plasma membrane, cytoplasm, or nucleus. This localization can affect their accessibility to substrates and regulatory molecules, influencing their activity.

8. **Feedback loops:** PTKs can be regulated by feedback loops, where their activity can influence the expression or activity of upstream or downstream signaling molecules, creating a closed loop of regulation.

Overall, the regulation of PTK activity is a complex and dynamic process involving a network of interacting proteins and signaling pathways. This intricate regulation ensures that PTKs are activated only when and where needed, preventing aberrant signaling and maintaining cellular homeostasis.'
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Proteins (1)

ProteinDefinitionTaxonomy
Receptor-type tyrosine-protein phosphatase CA receptor-type tyrosine-protein phosphatase C that is encoded in the genome of human. [PRO:CNA, UniProtKB:P08575]Homo sapiens (human)

Compounds (10)

CompoundDefinitionClassesRoles
4-hydroxyphenylglyoxylic acid4-hydroxyphenylglyoxylate : Conjugate base of 4-hydroxyphenylglyoxylic acid.

4-hydroxyphenylglyoxylic acid: RN given refers to parent cpd
phenols
5-iodo-2-(oxaloamino)benzoic acidorganoiodine compound
9,10-phenanthrenequinone9,10-phenanthrenequinone: structurephenanthrenes
oleanolic acidhydroxy monocarboxylic acid;
pentacyclic triterpenoid
plant metabolite
1,2-naphthoquinone1,2-naphthoquinone : The parent structure of the family of 1,2-naphthoquinones, in which the oxo groups of the quinone moiety are at positions 1 and 2 of the naphthalene ring. It is a metabolite of naphthalene and is found in diesel exhaust particles.

naphthalene-1,2-dione: structure given in first source
1,2-naphthoquinonesaryl hydrocarbon receptor agonist;
carcinogenic agent
cryptotanshinonecryptotanshinone: from Salvia miltiorrhizaabietane diterpenoidanticoronaviral agent
2-(oxaloamino)benzoic acid(oxaloamino)benzoic acid
illudalic acidilludalic acid: isolated from Clitocybe illudens; structure in first source
3-(1-(3-(biphenyl-4-ylamino)-3-oxopropyl)-1h-1,2,3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1h-indole-5-carboxylic acid3-(1-(3-(biphenyl-4-ylamino)-3-oxopropyl)-1H-1,2,3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1H-indole-5-carboxylic acid: an SHP2 inhibitor; structure in first source
variabilinvariabilin: an RGD-containing antagonist of glycoprotein IIb-IIIa from the hard tick, Dermacentor variabilis; amino acid sequence given in first source