We use cookies to understand how you use our site and to improve your experience. This includes personalizing content and advertising. To learn more, click here. By continuing to use our site, you accept our use of cookies. Cookie Policy.

Features Partner Sites Information LinkXpress
Sign In
Advertise with Us
LGC Clinical Diagnostics

Download Mobile App




X-ray Crystallography Study May Lead to New Drugs to Block Cancer Metastasis

By LabMedica International staff writers
Posted on 28 Apr 2016
Print article
Cancer researchers expect that the structure of the enzyme P-Rex1 (PIP3-dependent Rac exchanger 1), which was recently established by X-ray crystallography, will lead to development of a new generation of cancer chemotherapeutic agents to block the processes leading to metastasis.

P-Rex1 is a Rho guanine nucleotide exchange factor synergistically activated by the lipid PIP3 (phosphatidylinositol 3,4,5-trisphosphate) that plays an important role in the metastasis of breast, prostate, and skin cancer, which makes it an attractive therapeutic target. However, the molecular mechanisms behind P-Rex1 regulation have been poorly understood.

Investigators at the University of Michigan (Ann Arbor, USA) used X-ray crystallography to determine structures of the P-Rex1 pleckstrin homology domain (a protein domain of approximately 120 amino acids that occurs in a wide range of proteins involved in intracellular signaling) bound to the headgroup of PIP3.

They reported in the April 14, 2016, online edition of the journal Structure that PIP3 binding to the pleckstrin homology domain was required for P-Rex1 activity in cells but not for membrane localization, which pointed to an allosteric activation mechanism by PIP3.

"P-Rex1 has been an attractive drug target for some time," said senior author Dr. John J.G. Tesmer, professor of pharmacology and biological chemistry at the University of Michigan. "But development of these drugs has been hindered by a lack of understanding of its structure and regulatory mechanisms. Our data have confirmed the location of the binding site, which will greatly assist with the identification or design of small molecules that target this mechanism of activation."

Related Links:
University of Michigan

Platinum Member
COVID-19 Rapid Test
OSOM COVID-19 Antigen Rapid Test
HLX
Anti-Cyclic Citrullinated Peptide Test
GPP-100 Anti-CCP Kit
Gold Member
Real-time PCR System
GentierX3 Series

Print article

Channels

Clinical Chemistry

view channel
Image: Reaching speeds up to 6,000 RPM, this centrifuge forms the basis for a new type of inexpensive, POC biomedical test (Photo courtesy of Duke University)

POC Biomedical Test Spins Water Droplet Using Sound Waves for Cancer Detection

Exosomes, tiny cellular bioparticles carrying a specific set of proteins, lipids, and genetic materials, play a crucial role in cell communication and hold promise for non-invasive diagnostics.... Read more

Molecular Diagnostics

view channel
Image: The study showed the blood-based cancer screening test detects 83% of people with colorectal cancer with specificity of 90% (Photo courtesy of Guardant Health)

Blood Test Shows 83% Accuracy for Detecting Colorectal Cancer

Colorectal cancer is the second biggest cause of cancer deaths among adults in the U.S., with forecasts suggesting 53,010 people might die from it in 2024. While fewer older adults are dying from this... Read more

Hematology

view channel
Image: The Gazelle Hb Variant Test (Photo courtesy of Hemex Health)

First Affordable and Rapid Test for Beta Thalassemia Demonstrates 99% Diagnostic Accuracy

Hemoglobin disorders rank as some of the most prevalent monogenic diseases globally. Among various hemoglobin disorders, beta thalassemia, a hereditary blood disorder, affects about 1.5% of the world's... Read more

Microbiology

view channel
Image: The new platform is designed to perform blood-based diagnoses of nontuberculosis mycobacteria (Photo courtesy of 123RF)

New Blood Test Cuts Diagnosis Time for Nontuberculous Mycobacteria Infections from Months to Hours

Breathing in nontuberculous mycobacteria (NTM) is a common experience for many people. These bacteria are present in water systems, soil, and dust all over the world and usually don't cause any problems.... Read more

Industry

view channel
Image: These new assays are being developed for use on the recently introduced DxI 9000 Immunoassay Analyzer (Photo courtesy of Beckman Coulter)

Beckman Coulter and Fujirebio Expand Partnership on Neurodegenerative Disease Diagnostics

Beckman Coulter Diagnostics (Brea, CA, USA) and Fujirebio Diagnostics (Tokyo, Japan) have expanded their partnership focused on the development, manufacturing and clinical adoption of neurodegenerative... Read more
Copyright © 2000-2024 Globetech Media. All rights reserved.