Page last updated: 2024-10-24

protein phosphatase 2B binding

Definition

Target type: molecularfunction

Binding to a protein phosphatase 2B. [GOC:jl]

Protein phosphatase 2B (PP2B), also known as calcineurin, is a calcium/calmodulin-dependent serine/threonine protein phosphatase. It plays a critical role in various cellular processes, including signal transduction, gene expression, neuronal function, and immune responses. PP2B binding is crucial for its activation and regulation.

PP2B is composed of two subunits: a catalytic subunit (PP2Bα or PP2Bβ) and a regulatory subunit (calmodulin). The catalytic subunit contains the phosphatase activity, dephosphorylating target proteins. Calmodulin acts as a calcium sensor, binding to the catalytic subunit in response to increased intracellular calcium levels. This calcium-dependent binding activates PP2B, enabling it to dephosphorylate its substrates.

PP2B binding to target proteins is a complex process involving multiple factors. The specific binding site on PP2B varies depending on the interacting protein. In some cases, the binding site is located on the catalytic subunit, while in others, it is on the calmodulin subunit.

The molecular function of PP2B binding can be summarized as follows:

* **Activation:** PP2B binding to calmodulin is essential for its activation. Calcium binding to calmodulin induces a conformational change that exposes the active site of the catalytic subunit, allowing it to dephosphorylate target proteins.
* **Regulation:** PP2B binding to regulatory proteins, such as inhibitor-1 (I-1), can inhibit its activity. I-1 binds to the catalytic subunit, preventing substrate access and inhibiting phosphatase activity.
* **Substrate specificity:** PP2B binding to specific target proteins determines its substrate specificity. The binding interaction can be modulated by post-translational modifications, such as phosphorylation, or by the presence of other interacting proteins.
* **Signal transduction:** PP2B binding to signaling molecules, such as NFAT (nuclear factor of activated T cells), plays a critical role in signal transduction pathways. PP2B dephosphorylates NFAT, allowing it to translocate to the nucleus and regulate gene expression.
* **Cellular processes:** PP2B binding is involved in various cellular processes, including neuronal function, immune responses, muscle contraction, and cell growth.

In summary, PP2B binding is a crucial mechanism for regulating its activity and influencing a wide range of cellular processes.'
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Proteins (3)

ProteinDefinitionTaxonomy
Sodium/hydrogen exchanger 1A sodium/hydrogen exchanger 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P19634]Homo sapiens (human)
Serine/threonine-protein phosphatase 2B catalytic subunit beta isoformA serine/threonine-protein phosphatase 2B catalytic subunit beta isoform that is encoded in the genome of human. [PRO:DNx, UniProtKB:P16298]Homo sapiens (human)
Superoxide dismutase [Cu-Zn]A superoxide dismutase [Cu-Zn] that is encoded in the genome of human. [PRO:DNx, UniProtKB:P00441]Homo sapiens (human)

Compounds (11)

CompoundDefinitionClassesRoles
ethylisopropylamilorideethylisopropylamiloride : A member of the class of pyrazines that is amiloride in which the amino substitutent of the pyrazine ring that is adjacent to the chloro substituent has been substituted by an ethyl group and by an isopropyl group.

ethylisopropylamiloride: structure in first source
aromatic amine;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines;
tertiary amino compound
anti-arrhythmia drug;
neuroprotective agent;
sodium channel blocker
benzotriazolebenzotriazole : The simplest member of the class of benzotriazoles that consists of a benzene nucleus fused to a 1H-1,2,3-triazole ring.

benzotriazole: inhibitor of atmospheric metal corrosion; also component of motion picture film & Neva brake fluid
benzotriazolesenvironmental contaminant;
xenobiotic
amilorideamiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid.

Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)
aromatic amine;
guanidines;
organochlorine compound;
pyrazines
diuretic;
sodium channel blocker
amiloride hydrochlorideamiloride hydrochloride dihydrate : A hydrate that is the dihydrate of amiloride hydrochloride.hydratediuretic;
sodium channel blocker
formylmethionyl-leucyl-phenylalanine methyl esterpeptide
cariporidecariporide: a selective sodium-hydrogen exchange subtype 1 inhibitor; structure in first source
eniporideeniporide: inhibits NHE-1 isoform; structure in first source
zoniporidezoniporide: inhibits sodium-hydrogen exchanger isoform-1 (NHE-1)
sabiporidesabiporide: a NHE-1 inhibitor and a cardioprotective agent; structure in first source
(5-(2-methoxy-5-chloro-5-phenyl)furan-2-ylcarbonyl)guanidine(5-(2-methoxy-5-chloro-5-phenyl)furan-2-ylcarbonyl)guanidine: KR-32570 possesses potent cardioprotective effects in perfused rat hearts, and its effects may be mediated by inhibition of NHE-1, preservation of high-energy phosphates, and inhibition of lipid peroxidation
bi 201335faldaprevir: inhibits hepatitis C virus NS3 protease