Next Article in Journal
Phlorotannins from Ecklonia cava Attenuates Palmitate-Induced Endoplasmic Reticulum Stress and Leptin Resistance in Hypothalamic Neurons
Previous Article in Journal
Cloning, Expression, and Characterization of a New PL25 Family Ulvan Lyase from Marine Bacterium Alteromonas sp. A321
Previous Article in Special Issue
Novel Insights on the Toxicity of Phycotoxins on the Gut through the Targeting of Enteric Glial Cells
Open AccessFeature PaperArticle

Kinase-Based Screening of Marine Natural Extracts Leads to the Identification of a Cytotoxic High Molecular Weight Metabolite from the Mediterranean Sponge Crambe tailliezi

1
Integrative Biology of Marine Models Laboratory (LBI2M), Sorbonne Université, CNRS, UMR 8227, Station Biologique de Roscoff, CS 90074, 29688 Roscoff Cedex, France
2
Department of Chemical Analysis and Drug Quality Control, Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City 70000, Vietnam
3
Marine Natural Products Team, Université Côte d’Azur, CNRS, Institut de Chimie de Nice, UMR 7272, 06108 Nice, France
4
Sorbonne Université, CNRS, Station Biologique de Roscoff, FR 2424, Plateforme de criblage KISSf (Kinase Inhibitor Specialized Screening facility), Place Georges Teissier, 29682 Roscoff, France
5
SeaBeLife Biotech, Place Georges Teissier, 29682 Roscoff, France
*
Authors to whom correspondence should be addressed.
Mar. Drugs 2019, 17(10), 569; https://doi.org/10.3390/md17100569
Received: 6 September 2019 / Revised: 4 October 2019 / Accepted: 7 October 2019 / Published: 9 October 2019
(This article belongs to the Special Issue High-Throughput Screening of Marine Resources)
Regulated cell death (RCD) results from the activation of one or more signal transduction modules both in physiological or pathological conditions. It is now established that RCD is involved in numerous human diseases, including cancer. As regulated cell death processes can be modulated by pharmacological tools, the research reported here aims to characterize new marine compounds acting as RCD modulators. Protein kinases (PKs) are key signaling actors in various RCDs notably through the control of either mitosis (e.g., the PKs Aurora A and B) or necroptosis (e.g., RIPK1 and RIPK3). From the primary screening of 27 various extracts of marine organisms collected in the Mediterranean Sea, an extract and subsequently a purified high molecular weight compound dubbed P3, were isolated from the marine sponge Crambe tailliezi and characterized as a selective inhibitor of PKs Aurora A and B. Furthermore, P3 was shown to induce apoptosis and to decrease proliferation and mitotic index of human osteosarcoma U-2 OS cells. View Full-Text
Keywords: Screening; kinase inhibition; regulated cell death; RIP1-independent cell death; marine natural products; Crambe tailliezi Screening; kinase inhibition; regulated cell death; RIP1-independent cell death; marine natural products; Crambe tailliezi
Show Figures

Graphical abstract

MDPI and ACS Style

Nguyen, T.-N.-D.; Feizbakhsh, O.; Sfecci, E.; Baratte, B.; Delehouzé, C.; Garcia, A.; Moulin, C.; Colas, P.; Ruchaud, S.; Mehiri, M.; Bach, S. Kinase-Based Screening of Marine Natural Extracts Leads to the Identification of a Cytotoxic High Molecular Weight Metabolite from the Mediterranean Sponge Crambe tailliezi. Mar. Drugs 2019, 17, 569.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop