Page last updated: 2024-10-24

protein tyrosine phosphatase activator activity

Definition

Target type: molecularfunction

Binds to and increases the activity of a phosphotyrosine phosphatase, an enzyme which catalyzes of the removal of a phosphate group from a tyrosyl phenolic group of a protein. [GOC:ai, ISBN:0198506732]

Protein tyrosine phosphatase activator activity describes the ability of a molecule to enhance or stimulate the activity of protein tyrosine phosphatases (PTPs). PTPs are a large family of enzymes that play crucial roles in cellular signaling by removing phosphate groups from tyrosine residues on proteins. This dephosphorylation process can reverse the effects of protein kinases, which add phosphate groups to proteins, and thus regulate a wide range of cellular processes, including cell growth, differentiation, metabolism, and immune responses.

PTPs are typically inactive in their unphosphorylated state and become active upon phosphorylation. However, some molecules, such as certain proteins or small molecules, can bind to PTPs and induce conformational changes that activate the enzyme without requiring phosphorylation. These molecules are referred to as PTP activators.

The molecular mechanisms by which PTP activators exert their effects vary depending on the specific activator and PTP. Some activators may bind to the catalytic site of the PTP and directly enhance its catalytic activity, while others may bind to other regions of the PTP, causing conformational changes that indirectly activate the enzyme.

PTP activators have emerged as potential therapeutic targets for a variety of diseases, including cancer, diabetes, and inflammatory diseases. By modulating the activity of PTPs, activators could potentially restore proper cellular signaling and treat these disorders.

For example, activators of the PTP SHP-2 have shown promise in treating cancer by promoting apoptosis (programmed cell death) in tumor cells. Similarly, activators of the PTP PTEN, a tumor suppressor gene, could potentially inhibit tumor growth and metastasis.

The study of PTP activators is an ongoing area of research with significant implications for understanding cellular signaling and developing novel therapies for a range of diseases.'
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Proteins (2)

ProteinDefinitionTaxonomy
Serine/threonine-protein phosphatase 2A activatorA serine/threonine-protein phosphatase 2A regulatory subunit B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15257]Homo sapiens (human)
Insulin-like growth factor-binding protein 3An insulin-like growth factor-binding protein 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P17936]Homo sapiens (human)

Compounds (2)

CompoundDefinitionClassesRoles
Tautomycincarboxylic ester
nbi 31772NBI 31772: an insulin-like growth factor-binding protein ligand; structure in first source

NBI-31772 : An isoquinoline substituted by 3,4-dihydroxybenzoyl, carboxy, hydroxy, and hydroxy groups at positions 1, 3, 6, and 7, respectively. It is a potent inhibitor of insulin-like growth factor-1 binding protein (IGFBP).
aromatic ketone;
benzenediols;
hydroxy monocarboxylic acid;
isoquinolines;
tetrol
insulin-like growth factor-binding protein inhibitor