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
INTEGRA BIOSCIENCES AG

Download Mobile App




Novel Dual-Action Drug Blocks Carcinogenic MYC Oncogene Activity

By LabMedica International staff writers
Posted on 14 Feb 2017
Print article
Image: The crystal structure of the Myc protein in complex with DNA (Photo courtesy of Wikimedia Commons).
Image: The crystal structure of the Myc protein in complex with DNA (Photo courtesy of Wikimedia Commons).
A novel dual-action, low molecular weight drug suppresses the effects of the MYC cancer gene by blocking the action of two key regulatory proteins.

MYC is a regulator gene that codes for a transcription factor. The protein encoded by this gene (Myc) is a multifunctional, nuclear phosphoprotein that plays a role in cell cycle progression, apoptosis, and cellular transformation. A mutated version of MYC is found in many cancers, which causes Myc to be continually expressed. This leads to the unregulated expression of many genes, some of which are involved in cell proliferation, and results in the formation of cancer. Despite the recognition of the role of MYC in cancer, it has proven to very difficult to develop drugs to regulate its activity.

In this regard, investigators at the University of California, San Diego and collaborators at the University of Colorado School of Medicine, and the biopharmaceutical company SignalRx developed a novel dual-action inhibitor that blocks the activity of two key MYC-mediating factors, Phosphoinositide 3-kinase (PI3K) and Bromodomain-containing protein 4 (BRD4).

The investigators reported in the January 30, 2017, online edition of the journal Proceedings of the [U.S.] National Academy of Science that they had used molecular modeling crystal structure and nuclear magnetic resonance imaging, to design a new low molecular weight drug (SF2523) that simultaneously disrupted the two key MYC-mediating factors PI3K and BRD4.

Working with cell culture and mouse models, the investigators showed that the simultaeous inhibition of PI3K and BRD4 blocked MYC expression and activation, promoted MYC degradation, and markedly inhibited cancer cell growth and metastasis.

"Most anti-cancer drugs have a single target. They try to do one thing, such as block a single receptor or signaling pathway," said contributing author Dr. Donald L. Durden, professor of pediatrics at the University of California, San Diego. "This paper is proof-of-concept of a completely different mode of drug discovery clearly separated from the standard practice of one drug, one target. This is a "'first in class" approach to achieve a maximum inhibition of MYC in the treatment of the multitude of cancers known to be driven by the MYC oncogene. These findings suggest that dual-activity inhibitors are a highly promising lead compound for developing new anticancer therapeutics."

Platinum Member
COVID-19 Rapid Test
OSOM COVID-19 Antigen Rapid Test
HLX
Anti-Cyclic Citrullinated Peptide Test
GPP-100 Anti-CCP Kit
New
Gold Member
Systemic Autoimmune Testing Assay
BioPlex 2200 ANA Screen with MDSS

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.