Thapsigargin—From Traditional Medicine to Anticancer Drug

Autor: Katarzyna Gach-Janczak, Anna Janecka, Agata Jaskulska
Rok vydání: 2020
Předmět:
0301 basic medicine
Review
Pharmacology
Sesquiterpene lactone
sarcoplasmic/endoplasmic reticulum Ca2+ ATPase
lcsh:Chemistry
prostate-specific membrane antigen
chemistry.chemical_compound
0302 clinical medicine
Neoplasms
lcsh:QH301-705.5
Thapsia
Spectroscopy
chemistry.chemical_classification
Molecular Structure
biology
cytotoxin
apoptosis
Biological activity
General Medicine
Prodrug
Endoplasmic Reticulum Stress
Computer Science Applications
Thapsia (plant)
anticancer activity
030220 oncology & carcinogenesis
cardiovascular system
prodrug
Thapsigargin
SERCA
Antineoplastic Agents
Catalysis
Inorganic Chemistry
03 medical and health sciences
thapsigargin
prostate-specific antigen
Humans
Physical and Theoretical Chemistry
Molecular Biology
unfold protein response
Endoplasmic reticulum
Organic Chemistry
biology.organism_classification
030104 developmental biology
lcsh:Biology (General)
lcsh:QD1-999
chemistry
mipsagargin
Apoptosis
Unfolded Protein Response
Medicine
Traditional
Zdroj: International Journal of Molecular Sciences
International Journal of Molecular Sciences, Vol 22, Iss 4, p 4 (2021)
ISSN: 1422-0067
DOI: 10.3390/ijms22010004
Popis: A sesquiterpene lactone, thapsigargin, is a phytochemical found in the roots and fruits of Mediterranean plants from Thapsia L. species that have been used for centuries in folk medicine to treat rheumatic pain, lung diseases, and female infertility. More recently thapsigargin was found to be a potent cytotoxin that induces apoptosis by inhibiting the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump, which is necessary for cellular viability. This biological activity encouraged studies on the use of thapsigargin as a novel antineoplastic agent, which were, however, hampered due to high toxicity of this compound to normal cells. In this review, we summarized the recent knowledge on the biological activity and molecular mechanisms of thapsigargin action and advances in the synthesis of less-toxic thapsigargin derivatives that are being developed as novel anticancer drugs.
Databáze: OpenAIRE
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