Dataset Information

Discovering the Biological Target of 5-epi-Sinuleptolide Using a Combination of Proteomic Approaches.

ABSTRACT: Sinuleptolide and its congeners are diterpenes with a norcembranoid skeleton isolated from the soft coral genus Sinularia. These marine metabolites are endowed with relevant biological activities, mainly associated with cancer development. 5-epi-sinuleptolide has been selected as a candidate for target discovery studies through the application of complementary proteomic approaches. Specifically, a combination of conventional chemical proteomics based on affinity chromatography, coupled with high-resolution mass spectrometry and bioinformatics, as well as drug affinity responsive target stability (DARTS), led to a clear identification of actins as main targets for 5-epi-sinuleptolide. Subsequent in-cell assays, performed with cytochalasin D as reference compound, gave information on the ability of 5-epi-sinuleptolide to disrupt the actin cytoskeleton by loss of actin fibers and formation of F-actin amorphous aggregates. These results suggest the potential application of 5-epi-sinuleptolide as a useful tool in the study of the molecular processes impaired in several disorders in which actin is thought to play an essential role.

SUBMITTER: Morretta E

PROVIDER: S-EPMC5666420 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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Discovering the Biological Target of 5-epi-Sinuleptolide Using a Combination of Proteomic Approaches.

Morretta Elva E Esposito Roberta R Festa Carmen C Riccio Raffaele R Casapullo Agostino A Monti Maria Chiara MC

Marine drugs 20171013 10

Sinuleptolide and its congeners are diterpenes with a norcembranoid skeleton isolated from the soft coral genus <i>Sinularia</i>. These marine metabolites are endowed with relevant biological activities, mainly associated with cancer development. 5-<i>epi</i>-sinuleptolide has been selected as a candidate for target discovery studies through the application of complementary proteomic approaches. Specifically, a combination of conventional chemical proteomics based on affinity chromatography, cou ...[more]

PMID: 29027931

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Dataset Information

Discovering the Biological Target of 5-epi-Sinuleptolide Using a Combination of Proteomic Approaches.

Publications

Discovering the Biological Target of 5-epi-Sinuleptolide Using a Combination of Proteomic Approaches.

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