Thiostrepton: a novel lead compound against Dengue?

Thiostrepton Focus Biomolecules tebu-bio Catalog # 10-2108

Dengue Virus (DenV) is transmitted by mosquito vectors. It infects 50-100 million people each year and is at the origin of Dengue Fever and the more lethal Dengue Hemorrhagic Fever (DHF) and Shock Syndrome (DSS) leading to an estimated 500,000 cases of DHF and 22 000 deaths. The World Health Organization (WHO) estimates that 40% of the world’s population is at risk of infection.

In the June issue of Journal of Biomolecular Screening, investigators at San Diego State University (Dept of Biology) and Institute Pasteur Korea (Seoul, South Korea) developed a multiplexed cell-based assay for the identification of modulators of pre-membrane processing as a target for the discovery of DenV inhibitors. (1)

The DenV pre-membrane protein (prM) is an essential chaperone for the viral envelope protein which prevents premature fusion with vesicles during viral export. Inhibition of pre-membrane protein cleavage restricts fusion and represents, thus, a novel druggable target.

The new in vitro assay developed in this study, is the first described cell-based assay that monitors DenVprM processing within the classical secretory pathway. In a pilot screen of 1,280 small molecules on that assay, Thiostrepton, a known cyclopeptide Antibiotic and FOXM1 inhibitor,  was identified as a novel positive hit in this assay (IC50=4.94 µM).

The utility of this novel assay has been proven by the identification of Thiostrepton (available at Focus Biomolecules cat. nr 10-2108) which may be a novel lead compound for the discovery of new drugs effective against Dengue Virus.

Thiostrepton Focus Biomolecules tebu-bio Catalog # 10-2108

Thiostrepton – Antibiotic and FOXM1 inhibitor. C72H85N19O18S5 – CAS No: 1393-48-2, 98% by TLC and HPLC at Focus Biomolecules.

 

1- Stolp Z.D. et al. “A Multiplexed Cell-Based Assay for the Identification of Modulators of Pre-Membrane Processing as a Target against Dengue Virus” (2015) J. Biomol. Screen. 20:616-626. DOI: 10.1177/1087057115571247.

Related items

A selection of Abnova’s primary antibodies and ELISA kits in relation to Dengue Fever is available here. A few examples:

 

Dengue Fever Cat. Nr Product Name Application
Antibody for Dengue Virus 157MAB4043 Dengue virus Types 1,2,3,4 monoclonal antibody, clone BDI419 Dot,IF,EIA
Antibodies for Envelope Protein 157MAB8901 Dengue virus E-D3 monoclonal antibody, clone 5j122 ELISA,WB-Re
Antibodies for NS1 protein 157MAB13532 Dengue virus NS1 monoclonal antibody, clone HM026 ELISA,IF,LFIA

 

 

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Philippe Fixe, PhD
Written by Philippe Fixe, PhD
Philippe Fixe is Marketing Director at tebu-bio, passionate about innovation and R&D in Life sciences, Biotechnology, Medical research, Drug discovery, and also a keen photographer.