Features Partner Sites Information LinkXpress
Sign In
Advertise with Us
RANDOX LABORATORIES

Events

06 Jun 2016 - 09 Jun 2016
22 Jun 2016 - 24 Jun 2016
04 Jul 2016 - 06 Jul 2016

First-in-Class GTPase Inhibitor to Have Applications in Drug Discovery and Fundamental Research

By BiotechDaily International staff writers
Posted on 26 Mar 2013
Print article
A recent paper described the activity of a low molecular weight compound able to selectively inhibit the enzyme Cdc42 in biochemical and cellular assays that are expected to have applications in drug discovery and fundamental research.

Human Cdc42 is a small GTPase of the Rho-subfamily, which regulates signaling pathways that control diverse cellular functions including cell morphology, migration, endocytosis, and cell cycle progression. Overactive Cdc42 has been implicated in the pathology of cancers, immune diseases, and neuronal disorders. While Cdc42 inhibitors would be useful in probing molecular pathways and could have therapeutic potential, previous attempts to develop them have been unsuccessful, as the inhibitors have lacked selectivity and trended towards toxicity.

In the current study investigators at the University of New Mexico (Albuquerque, USA) succeeding in isolating a low molecular weight inhibitor of Cdc42 by high-throughput screening of hundreds of compounds.

They reported in the February 4, 2013, online edition of the Journal of Biological Chemistry that the compound, CID2950007, demonstrated excellent selectivity with no inhibition towards Rho and Rac from the same GTPase family. Biochemical characterization showed that the compound acted as a noncompetitive allosteric inhibitor. When tested in cellular assays, it inhibited Cdc42-related filopodia formation and cell migration.

CID2950007 was also used to clarify the involvement of Cdc42 in the internalization of Sin Nombre virus and the signaling pathway of integrin VLA-4.

“It is an important target in many diseases,” said senior author Dr. Angela Wandinger-Ness professor of pathology at the University of New Mexico. “Cancer is just one. But there were no compounds that target this GTPase. “There is a lot of enthusiasm for a compound like this—because there were not any. This is a first-in-class.”

Related Links:
University of New Mexico


Print article

Channels

Genomics/Proteomics

view channel
Image: A dark field photomicrograph showing the spirochete bacterium Borrelia burgdorferi, the pathogen responsible for causing Lyme disease (Photo courtesy of the CDC).

Statins May Help Block Transmission of Lyme Disease

A recent study found that treatment with cholesterol-lowering statins reduced the number of Borrelia burgdorferi bacteria in rodents, which helped to block transmission of Lyme disease. Lyme disease... Read more

Biochemistry

view channel
Image: A space-filling model of the anticonvulsant drug carbamazepine (Photo courtesy of Wikimedia Commons).

Wastewater May Contaminate Crops with Potentially Dangerous Pharmaceuticals

Reclaimed wastewater used to irrigate crops is contaminated with pharmaceutical residues that can be detected in the urine of those who consumed such produce. Investigators at the Hebrew University... Read more

Lab Technologies

view channel

Huge Modifiable Biomedical Database to Be Available on the Wikidata Site

Genome researchers are exploiting the power of the open Internet community Wikipedia database to create a comprehensive resource for geneticists, molecular biologists, and other interested life scientists. While efficiency in generating scientific data improves almost daily, applying meaningful relationships between... Read more

Business

view channel

European Biotech Agreement to Promote Antigen-Drug Conjugation Technology

Two European biotech companies have joined forces to exploit and commercialize an innovative, site-specific ADC (antigen-drug conjugate) conjugation technology. ProBioGen (Berlin, Germany), a company specializing in the development and manufacture of complex glycoproteins and Eucodis Bioscience (Vienna, Austria), a... Read more
Copyright © 2000-2016 Globetech Media. All rights reserved.