About My Health Careers Internship MedBlogs Contact us
Medindia LOGIN REGISTER
Advertisement

Researchers Develop New Idea for Targeting the Common Cancer Protein KRAS

by Rukmani Krishna on October 25, 2013 at 12:42 AM
Font : A-A+

 Researchers Develop New Idea for Targeting the Common Cancer Protein KRAS

The results of a study find that patients with cancers driven by the protein KRAS, which are particularly hard to treat, may benefit from small molecules that attach to and disrupt the function of a KRAS-containing protein complex. The results were presented at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, held Oct. 19-23.

Mutant forms of the protein KRAS are found in approximately 30 percent of all cancers. They are responsible for many of the hallmarks of these cancers, and KRAS is, therefore, considered an important therapeutic target. However, attempts to develop clinically useful KRAS-targeted drugs have been unsuccessful.

Advertisement

"KRAS is a molecular switch," said Michael Burns, a doctor of medicine and doctor of philosophy candidate at Vanderbilt School of Medicine in Nashville, Tenn. "In the 'on' state it transmits signals that drive cell growth and survival. In many cancers, KRAS is permanently in the on state, and it is a highly validated therapeutic target.

"KRAS switches from off to on most efficiently when it is attached to a protein called SOS," explained Burns. "Each SOS protein attaches to two KRAS proteins, and we have identified a number of small molecules that bind to a particular part of SOS when it is in a complex with two KRAS proteins. These small molecules disrupt the function of the complex, ultimately causing inhibition of the signaling pathways downstream of KRAS that drive cell growth and survival. Although our data were generated in biochemical assays and cell lines, they suggest a potential way to therapeutically target KRAS, which has not been possible to date."
Advertisement

KRAS switches from off to on during a process called guanine nucleotide exchange, and SOS increases the rate at which this process occurs. Burns and colleagues hypothesized that small molecules that blocked SOS-mediated guanine nucleotide exchange would prevent KRAS switching on and, therefore, inhibit the signaling pathways downstream of KRAS that drive cell growth and survival.

Instead, they found that a number of small molecules that attached to a special pocket in a region of SOS called the CDC25 domain and increased SOS-mediated guanine nucleotide exchange actually inhibited two of the major signaling pathways downstream of KRAS: the MAPK and PI3K signaling pathways.

The researchers are actively investigating why small molecules that increased SOS-mediated guanine nucleotide exchange in biochemical assays blocked signaling downstream of KRAS in cell lines. They are also working to optimize the small molecules before they conduct studies in preclinical models of cancer.

Source: Eurekalert
Advertisement

Advertisement
News A-Z
A B C D E F G H I J K L M N O P Q R S T U V W X Y Z
News Category
What's New on Medindia
Breast Cancer Awareness Month 2021 - It's time to RISE
First-Ever Successful Pig-To-Human Kidney Transplantation
World Osteoporosis Day 2021 -
View all

Medindia Newsletters Subscribe to our Free Newsletters!
Terms & Conditions and Privacy Policy.

More News on:
Cancer and Homeopathy Cancer Facts Cancer Tattoos A Body Art Magical Millets for Your Health Diet and Nutrition Tips for Athletes Nutrition IQ Common Lifestyle Habits that Cause Diseases Health Benefits of Dandelion Plant Immune Checkpoint Inhibitors for Cancer Treatment 
Recommended Reading
Common Lifestyle Habits that Cause Diseases
Cigarette smoking, unhealthy diets, overuse of alcohol, and physical inactivity are some of the most...
Diet and Nutrition Tips for Athletes
Athletes can be physically fit by consuming a well balanced nutritious diet, which keeps them mental...
Health Benefits of Dandelion Plant
What is dandelion? Dandelion greens are nutrition powerhouses with a wide range of health benefits. ...
Immune Checkpoint Inhibitors for Cancer Treatment
Immune checkpoint inhibitors are promising drugs to treat a variety of cancers and the FDA has appro...
Magical Millets for Your Health
Millets are far more nutrient dense than wheat and rice. They are inexpensive and tasty too. Nutriti...
Tattoos A Body Art
Tattoos are a rage among college students who sport it for the ‘cool dude’ or ‘cool babe’ look...

Disclaimer - All information and content on this site are for information and educational purposes only. The information should not be used for either diagnosis or treatment or both for any health related problem or disease. Always seek the advice of a qualified physician for medical diagnosis and treatment. Full Disclaimer

© All Rights Reserved 1997 - 2021

This site uses cookies to deliver our services. By using our site, you acknowledge that you have read and understand our Cookie Policy, Privacy Policy, and our Terms of Use