The name derives from platelet and leukocyte C kinase substrate and the KSTR string of amino acids.

[2] Pleckstrins are involved in rearranging the actin cytoskeleton in such processes as platelet activation, erythropoeisis, and cell spreading by extension of filopodia and lamellipodia.

[3] Pleckstrin-1 is believed to become activated by protein kinase C phosphorylation, which results in binding of the membrane lipid phosphatidylinositol 3,4-bisphosphate.

[2] It also occurs in immune cells such as macrophages and neutrophils,[2][3] where it is involved in formation of phagosomes and the secretion of proinflammatory cytokines.

It is also believed to be crucial in the epithelial-to-mesenchymal transition in tumor metastasis, and pleckstrin-2 is known to be overexpressed in a variety of cancers.