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Advances in chemistry and bioactivity of parthenolide

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Abstract

Review covering up to 07/2019

(−)-Parthenolide is a germacrane sesquiterpene lactone, available in ample amounts from the traditional medical plant feverfew (Tanacetum parthenium). Acting as a covalently reactive compound, it displays anti-inflammatory, redox-modulating, and epigenetic activities, as well as selective cytotoxicity towards cancer stem and progenitor cells. Furthermore, parthenolide was found to modulate microtubule dynamics by interfering with the detyrosination of α-tubulin, a specific posttranslational modification of the cytoskeleton. This review interfaces recently achieved parthenolide syntheses with strategies for bioactivity-based derivatization. Furthermore, chemical probe development from parthenolide is discussed, leading to a qualified summary of reported biological activities and implicated or identified targets. Special emphasis is given to parthenolide-induced microtubule modulation and the recently characterized tubulin carboxypeptidase enzymes involved in nerve (re)growth, cardiac muscle cell function, and metastasis development.

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Publication details

The article was received on 20 Aug 2019 and first published on 25 Nov 2019


Article type: Review Article
DOI: 10.1039/C9NP00049F
Nat. Prod. Rep., 2020, Advance Article

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    Advances in chemistry and bioactivity of parthenolide

    R. R. A. Freund, P. Gobrecht, D. Fischer and H. Arndt, Nat. Prod. Rep., 2020, Advance Article , DOI: 10.1039/C9NP00049F

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