{"doi":"10.3390/ijms22010004","title":"Thapsigargin—From Traditional Medicine to Anticancer Drug","abstract":"<jats:p>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.</jats:p>","journal":"International Journal of Molecular Sciences","year":2020,"id":606129,"datarank":0.7401710899696038,"base_score":4.9344739331306915,"endowment":4.9344739331306915,"self_citation_contribution":0.7401710899696038,"citation_network_contribution":0.0,"self_endowment_contribution":0.7401710899696038,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":138,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1555849,"name":"Anna Ewa Janecka","orcid":null,"position":1,"is_corresponding":false},{"id":1555850,"name":"Katarzyna Gach-Janczak","orcid":"0000-0002-3129-4158","position":2,"is_corresponding":false},{"id":1555848,"name":"Agata Jaskulska","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Thapsigargin—From Traditional Medicine to Anticancer Drug","abstract":"<jats:p>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.</jats:p>","is_dataset_classified":null,"base_score":4.9344739331306915,"endowment":4.9344739331306915,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"33374919","pmcid":"PMC7792614","openalex_id":"https://openalex.org/W3116541429","authors":[],"funders":[{"funder_name":"National Science Centre, Poland","grant_id":"No 2015/17/D/NZ3/02226","title":null}],"total_grants":1,"fwci":6.1134,"citation_percentile":0.97672496,"influential_citations":0,"citation_trend":[{"year":2021,"count":14},{"year":2022,"count":25},{"year":2023,"count":43},{"year":2024,"count":20},{"year":2025,"count":22},{"year":2026,"count":14}],"oa_status":"gold","license":"cc-by","oa_locations":[{"url":"https://www.mdpi.com/1422-0067/22/1/4/pdf?version=1608635960","host_type":"journal"},{"url":"https://www.mdpi.com/1422-0067/22/1/4/pdf?version=1608635960","host_type":"publisher"},{"url":"https://www.mdpi.com/1422-0067/22/1/4/pdf","host_type":"publisher"},{"url":"https://doi.org/10.3390/ijms22010004","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/33374919","host_type":"repository"},{"url":"https://doaj.org/article/99bbd25b6a48458e82e8c88fe3fe0722","host_type":"repository"},{"url":"http://europepmc.org/pmc/articles/PMC7792614","host_type":"repository"},{"url":"https://dx.doi.org/10.3390/ijms22010004","host_type":"repository"},{"url":"https://www.ncbi.nlm.nih.gov/pmc/articles/7792614","host_type":"repository"},{"url":"https://europepmc.org/articles/PMC7792614","host_type":"Europe_PMC"},{"url":"https://europepmc.org/articles/PMC7792614?pdf=render","host_type":"Europe_PMC"}],"fields_of_study":["Plant biochemistry and biosynthesis","Allelopathy and phytotoxic interactions","Essential Oils and Antimicrobial Activity","Antineoplastic Agents","Apoptosis","Endoplasmic Reticulum Stress","Humans","Medicine, Traditional","Molecular Structure","Neoplasms","Thapsia","Thapsigargin","Unfolded Protein Response"],"mesh_terms":["Antineoplastic Agents","Humans","Medicine, Traditional","Neoplasms","Molecular Structure","Apoptosis","Thapsigargin","Thapsia","Unfolded Protein Response","Endoplasmic Reticulum Stress"],"keywords":["Thapsigargin","SERCA","Endoplasmic reticulum","Pharmacology","Sesquiterpene lactone","Medicine","Phytochemical","Chemistry","ATPase","Biology","Traditional medicine","Biochemistry","Sesquiterpene","Stereochemistry","Enzyme","Apoptosis","Cytotoxin","Prostate-specific antigen","Prostate-specific membrane antigen","Anticancer activity","Prodrug","Sarcoplasmic/endoplasmic Reticulum Ca2+ Atpase","Unfold Protein Response","Mipsagargin"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[{"name":"nct"}],"source":"live","citation_network_status":"fetched"},"created_at":"2026-07-30T03:56:49.413154Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}