Description

Thapsigargin is a sesquiterpene lactone that is known to inhibit sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA). Through the inhibition of SERCA, thapsigargin promotes the release and eventual depletion of intracellular calcium reserves, leading in turn to calcium influx.

Thapsigargin's ability to regulate calcium influx has been shown to affect several physiological functions. This lactone is known to induce apoptosis by disrupting the ordinary organization of cytoskeletal structures.

Applications

Thapsigargin has played a large role in recent cancer research. Thapsigargin has been shown to be a weak promoter of skin tumors in mice. Intriguingly, however, researchers have also discovered potential uses for it in cancer treatment due to its ability to induce apoptosis. Using specific peptides, thapsigargin can be targeted to individual tumor sites. Studies have also been conducted into thapsigargin's ability to sensitize tumors.