Target intelligence / Profile preview

Calcium-transporting ATPase (Ca-ATPase) (Ca-ATPase)

Target
Ca-ATPase
Molecular classification
Enzyme, Transporter, P-type ATPase
01

Overview

Calcium-transporting ATPases (Ca-ATPases) are a family of P-type ATPases that maintain low cytosolic calcium levels by actively transporting Ca2+ ions across membranes using energy from ATP hydrolysis [UniProt, PubMed]. This family includes the Sarcoplasmic/Endoplasmic Reticulum Calcium ATPase (SERCA), the Plasma Membrane Calcium ATPase (PMCA), and the Secretory Pathway Calcium ATPase (SPCA) [UniProt, StatPearls]. SERCA is a critical regulator of cardiac contractility, pumping calcium back into the sarcoplasmic reticulum to initiate muscle relaxation; its downregulation is a hallmark of heart failure [PubMed, NIH]. PMCA extrudes calcium into the extracellular space, playing a vital role in global calcium signaling and blood pressure regulation [PubMed]. Because of their central role in calcium signaling, Ca-ATPases are significant therapeutic targets; for instance, SERCA2a activation by drugs like istaroxime is pursued to treat heart failure [PubMed], while SERCA inhibition is explored in cancer therapy via prodrugs like mipsagargin [PubMed]. However, modulating these pumps requires precision to avoid disrupting essential calcium-dependent processes or inducing arrhythmias [PubMed].

Other names
Calcium pumpSarcoplasmic/endoplasmic reticulum calcium ATPasePlasma membrane calcium ATPaseSecretory pathway calcium ATPaseSERCAPMCASPCAATP2AATP2BATP2C
02

Mechanism of action

Active transport of calcium ions across biological membranes against a concentration gradient, powered by the hydrolysis of ATP [UniProt, PubMed].

03

Biological functions

Calcium homeostasis [UniProt]Muscle relaxation [PubMed]Signal transduction [StatPearls]Protein folding [UniProt]Apoptosis regulation [PubMed]
04

Disease associations

Heart failure [PubMed]Darier disease [NIH]Hailey-Hailey disease [NIH]Cancer [PubMed]Hypertension [PubMed]
05

Safety considerations

Arrhythmogenic potential [PubMed]Endoplasmic reticulum stress [PubMed]Cytotoxicity [PubMed]Off-target inhibition of related ATPases [PubMed]
06

Interacting drugs

Istaroxime [PubMed]

5 more in the full profile.

07

Biomarkers

Phospholamban phosphorylation status [PubMed]Cytosolic calcium transients [PubMed]SERCA2a protein expression levels [PubMed]NT-proBNP [PubMed]

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