thapsigargin and Soft-Tissue-Neoplasms

The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structure elucidated. By inhibiting the sarco/endoplasmic reticulum Ca(2+) ATPase (SERCA) thapsigargin provokes apoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for either prostate specific antigen (PSA) or prostate specific membrane antigen (PSMA) prodrugs were created, which selectively affect prostate cancer cells or neovascular tissue in tumors. One of the prodrug is currently tested in clinical phase II. The prodrug under clinical trial has been named mipsagargin.

Topics: Animals; Antineoplastic Agents, Phytogenic; Apiaceae; Apoptosis; Cell Proliferation; Enzyme Inhibitors; Humans; Male; Mice; Molecular Structure; Neovascularization, Pathologic; Prodrugs; Prostatic Neoplasms; Sarcoplasmic Reticulum Calcium-Transporting ATPases; Soft Tissue Neoplasms; Thapsigargin