Target intelligence / Profile preview

Sarcoplasmic reticulum calcium-transporting ATPase (SERCA)

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

Overview

The **Sarcoplasmic reticulum calcium-transporting ATPase (SERCA)** is an ATP-dependent membrane pump found in the sarcoplasmic reticulum (SR) of muscle cells and the endoplasmic reticulum (ER) of other cells. It maintains low cytosolic calcium levels by actively transporting calcium ions from the cytosol into the SR, which is essential for muscle relaxation after contraction and for a wide array of cellular processes dependent on intracellular calcium signaling. SERCA is regulated by small transmembrane peptides, such as phospholamban and sarcolipin, as well as recently described micropeptides. Dysregulation of SERCA activity is implicated in diseases including heart failure, muscular disorders, and neurodegenerative conditions, making it an important therapeutic target[1][3][5][8].

Other names
Sarcoendoplasmic reticulum calcium ATPaseSarcoplasmic/endoplasmic reticulum Ca^2+-ATPaseSR Ca^2+-ATPaseATP2A1 (gene)ATP2A2 (gene)Calcium ATPase
02

Mechanism of action

Inhibition or modulation of SERCA activity alters calcium uptake into the sarcoplasmic reticulum, thereby affecting cytosolic calcium levels, muscle contraction, and cellular signaling[3][8].

03

Biological functions

Regulation of intracellular calcium homeostasisMuscle contraction and relaxationSignal transductionCell metabolism
04

Disease associations

Cardiovascular diseaseMuscular disorders (e.g., heart failure, recurrent exertional rhabdomyolysis)Neurodegenerative diseaseOther conditions associated with abnormal calcium handling
05

Safety considerations

Inhibition of SERCA can cause impaired muscle relaxation, cardiac dysfunction, and cell death due to calcium overload[1][3]Non-specific modulation may disturb systemic calcium homeostasis
06

Interacting drugs

Thapsigargin (inhibitor)

2 more in the full profile.

07

Biomarkers

SERCA expression/activity (used in some heart failure research and stratification)Phospholamban and sarcolipin expression, which regulate SERCA activity[5]

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