Features | Partner Sites | Information | LinkXpress
Sign In
PZ HTL SA
GLOBETECH PUBLISHING LLC
GLOBETECH PUBLISHING LLC

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

By BiotechDaily International staff writers
Posted on 26 Mar 2013
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


comments powered by Disqus

Channels

Genomics/Proteomics

view channel

New Program Encourages Wide Distribution of Genomic Data

A new data sharing program allows genomics researchers and practitioners to analyze, visualize, and share raw sequence data for individual patients or across populations straight from a local browser. The sequencing revolution is providing the raw data required to identify the genetic variants underlying rare diseases... Read more

Lab Technologies

view channel

Experimental Physicists Find Clues into How Radiotherapy Kills Cancer Cells

A new discovery in experimental physics has implications for a better determination of the process in which radiotherapy destroys cancer cells. Dr. Jason Greenwood from Queen’s University Belfast (Ireland) Center for Plasma Physics collaborated with scientists from Italy and Spain on the work on electrons, and published... Read more

Business

view channel

Interest in Commercial Applications for Proteomics Continues to Grow

Increasing interest in the field of proteomics has led to a series of agreements between private proteomic companies and academic institutions as well as deals between pharmaceutical companies and novel proteomics innovator biotech companies. Proteomics is the study of the structure and function of proteins.... Read more
 
Copyright © 2000-2014 Globetech Media. All rights reserved.