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




X-ray Study Explains How Takinib Inhibits TNF-alpha

By LabMedica International staff writers
Posted on 29 Aug 2017
Print article
Image: A molecular model of Takinib, a drug-like molecule that modulates the TNF-alpha inflammatory response, which is at the center of a variety of diseases (Photo courtesy of Duke University).
Image: A molecular model of Takinib, a drug-like molecule that modulates the TNF-alpha inflammatory response, which is at the center of a variety of diseases (Photo courtesy of Duke University).
Takinib, a selective TAK1 inhibiting drug, has been shown to broaden the therapeutic efficacy of TNF-alpha (Tumor necrosis factor-alpha) inhibition for treating cancer and autoimmune diseases.

TAK1 (also known as MAP3K7 or mitogen-activated protein kinase kinase kinase 7) is a key mediator between survival and cell death in TNF-alpha-mediated signaling. TNF-alpha is a cytokine that has a wide variety of functions. It can cause cytolysis of certain tumor cell lines and is a potent pyrogen, causing fever by direct action or by stimulation of interleukin-1 secretion. It can stimulate cell proliferation and induce cell differentiation under certain conditions.

Investigators at Duke University (Durham, NC, USA) recently described the compound Takinib, a potent and selective TAK1 inhibitor that induced apoptosis following TNF-alpha stimulation in cell models of rheumatoid arthritis and metastatic breast cancer.

The investigators used X-ray crystallography to demonstrate that Takinib was an inhibitor of autophosphorylated and non-phosphorylated TAK1 that bound within the ATP-binding pocket and inhibited TAK1 by slowing down the rate-limiting step of TAK1 activation.

Overall, the investigators saw Takinib as an attractive starting point for the development of inhibitors that sensitize cells to TNF-alpha-induced cell death, with general implications for cancer and autoimmune disease treatment.

"The delicate balance between survival and death is often disrupted in disease, and this molecule is able to target the process," said senior author Dr. Timothy Haystead, professor of pharmacology and cancer biology at Duke University. "This compound could potentially enhance the positive parts of TNF-alpha by only targeting tumor cells or inflammatory cells."

The study was published in the August 17, 2017, issue of the journal Cell Chemical Biology.

Related Links:
Duke University

Platinum Member
COVID-19 Rapid Test
OSOM COVID-19 Antigen Rapid Test
Specimen Collection & Transport
Complement 3 (C3) Test
GPP-100 C3 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.