BibliographicReference 300228

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Type: Bibliographic resource
Type of document: Journal article
BibLvlCode: AS
Title: Macrophilones from the marine hydroid Macrorhynchia philippina can inhibit ERK cascade signaling
Abstract: Six new macrophilone-type pyrroloiminoquines were isolated and identified from an extract of the marine hydroid Macrorhynchia philippina. The proton-deficient and heteroatom-rich structures of macrophilones B–G (2–7) were elucidated by spectroscopic analysis and comparison of their data with those of the previously reported metabolite macrophilone A (1). Compounds 1–7 are the first pyrroloiminoquines to be reported from a hydroid. The macrophilones were shown to inhibit the enzymatic conjugation of SUMO to peptide substrates, and macrophilones A (1) and C (3) exhibit potent and selective cytotoxic properties in the NCI-60 anticancer screen. Bioinformatic analysis revealed a close association of the cytotoxicity profiles of 1 and 3 with two known B-Raf kinase inhibitory drugs. While compounds 1 and 3 showed no kinase inhibitory activity, they resulted in a dramatic decrease in cellular protein levels of selected components of the ERK signal cascade. As such, the chemical scaffold of the macrophilones could provide small-molecule therapeutic leads that target the ERK signal transduction pathway.
WebOfScience code: https://www.webofscience.com/wos/woscc/full-record/WOS:000440505900022
Bibliographic citation: Yan, P.; Ritt, D.A.; Zlotkowski, K.; Bokesch, H.R.; Reinhold, W.C.; Schneekloth, J.S.; Morrison, D.K.; Gustafson, K.R. (2018). Macrophilones from the marine hydroid Macrorhynchia philippina can inhibit ERK cascade signaling. J. Nat. Prod. 81(7): 1666-1672. https://dx.doi.org/10.1021/acs.jnatprod.8b00343
Topic: Marine
Is peer reviewed: true

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