Penn researchers determine structure of binding site of colon-cancer drug and its protein target

(Philadelphia, PA) Researchers at the University of Pennsylvania School of Medicine have determined the precise molecular details of how Erbitux, a recently approved colorectal cancer drug, binds to its target on cancer cells. Knowing this chemical configuration will lead to better drug design for this family of cancer medications.

Colorectal cancer is one of the most frequently diagnosed cancers in men and women, as well as the second-leading cause of cancer-related death, according to the Centers for Disease Control and Prevention. Erbitux works by binding to a protein on the surface of cancer cells, thereby halting excessive cell growth that leads to tumors. Kate Ferguson, PhD, Assistant Professor of Physiology, and colleagues, describe their findings in the April cover article of Cancer Cell.

"By having determined the structure of Erbitux bound to its cellular target receptor, we get new insight into how the drug blocks the receptor's cell growth-promoting activities, and can use this to guide future drug design," says Ferguson.

As is characteristic of many epithelial cancers such as cancers of the head and neck, breast, ovary, lung, and pancreas the surface of cancer cells possess abnormally high levels of epidermal growth factor receptor (EGFR), the protein that interacts with Erbitux. These receptors are made up of three parts: one outside the cell; another passing through the cell membrane; and the third inside the cell. In a cancer cell, an extracellular hormone binds to the outer piece of EGFR, and causes the inside part to kick off a series of reactions that signal the cancerous cell to replicate and divide.

Ferguson and colleagues determined that Erbitux works to halt cell proliferation by blocking EGFR's molecular doorway, disallowing hormones to bind and signal tumor growth. X-ray crystallography provided a snapshot of the interaction between Erbitux and the extracellular component of the cancer cell's receptors. '"/>

Contact: Karen Kreeger
University of Pennsylvania School of Medicine

Page: 1 2

Related biology news :

1. Innovative tagging technique may help researchers better protect fish stocks
2. Penn researchers discover how key protein stops inflammation
3. ASU researchers partner with UOP to make biofuel for military jets a reality
4. Einstein researchers prototype vaccine could provide improved protection against tuberculosis
5. Penn researchers discover pathway that eliminates genetic defects in red blood cells
6. U-M researchers find family of on switches that cause prostate cancer
7. 2007 EURYI: 20 young researchers to receive Nobel Prize-sized awards for breakthrough ideas
8. Pets could be source of multiresistant bacteria infections in humans, MU researchers investigate
9. MGH researchers confirm that bone marrow restores fertility in female mice
10. Smithsonians National Zoo researchers use electronic eggs to help save threatened species
11. U-M researchers identify gene involved in breast cancer

Post Your Comments:

(Date:11/2/2015)... MENLO PARK, Calif. , Nov. 2, 2015 /PRNewswire/ ... to $9 million to provide preclinical development services to ... Under the contract, SRI will provide scientific expertise, modern ... a wide variety of preclinical pharmacology and toxicology studies ... --> --> The PREVENT Cancer Drug ...
(Date:10/29/2015)... RESTON, Va. , Oct. 29, 2015 ... announced today that it has released a new version ... Daon customers in North America ... gains. IdentityX v4.0 also includes a FIDO UAF ... customers are already preparing to activate FIDO features. These ...
(Date:10/29/2015)... 29, 2015 NXTD ) ... focused on the growing mobile commerce market and ... StackCommerce, a leading marketplace to discover and buy ... smart wallet on StackSocial for this holiday season. ... the "Company"), a biometric authentication company focused on ...
Breaking Biology News(10 mins):
(Date:11/27/2015)... , Nov. 27, 2015 /PRNewswire/--  Mallinckrodt plc (NYSE: ... today that it has closed the sale of its ... Guerbet (GBT- NYSE Euronext) in a transaction valued at ... manufacturing facilities and a total of approximately 1,000 employees ... St. Louis area. This entire ...
(Date:11/26/2015)... England , November 26, 2015 ... medical device company specializing in imaging technologies, announced today that ... Commission as part of the Horizon 2020 European Union Framework ... out a large-scale clinical trial in breast cancer. ... http://photos.prnewswire.com/prnh/20151016/277917) , --> --> ...
(Date:11/25/2015)... 25, 2015 Studies reveal the ... plaque and pave the way for more effective treatment for ...     --> --> ... health problems in cats, yet relatively little was understood about ... studies have been conducted by researchers from the WALTHAM Centre ...
(Date:11/25/2015)... ... 25, 2015 , ... A long-standing partnership between the Academy ... been formalized with the signing of a Memorandum of Understanding. , AMA Executive ... Karl Minter and Capt. Albert Glenn Tuesday, November 24, 2015, at AMA Headquarters ...
Breaking Biology Technology:
Cached News: