Navigation Links
Pinning protein could answer provocative cancer question
Date:10/30/2012

HOUSTON -- (Oct. 29, 2012) -- Answers are often elusive in the fight against cancer, and Rice University chemist Zachary Ball is hoping to pin one down -- with pins made of single atoms. The work, which aims to create a drug that's effective against an "undruggable" protein, is one of the first 50 proposals funded under the National Cancer Institute's (NCI) Provocative Questions Project.

The Provocative Questions Project, in its inaugural year, is designed to spur innovative approaches to critical questions that could, if answered, substantially change the way scientists approach cancer research. Ball, assistant professor of chemistry at Rice, and collaborators at Baylor College of Medicine (BCM) are attempting to answer one of 24 questions posed by NCI: "Are there new technologies to inhibit traditionally 'undruggable' target molecules, such as transcription factors, that are required for (cancer)?"

"Most drugs are small molecules that bind tightly to a protein and literally get in the way of it sticking to whatever it might normally interact with, often another protein," Ball said. "Drugs tend to be small molecules because those are the easiest to introduce into cells and because small molecules are particularly effective at binding tightly into the tiny pockets that exist on many proteins."

Unfortunately, there are some proteins that don't have the tiny pockets favored by drug designers. By some estimates, small-molecule drugs are ineffective against as many as 80 percent of the proteins in human cells, including many signaling proteins and a class of proteins called transcription factors that help control basic functions like cell death and cell reproduction. Drugmakers often call these proteins "undruggable."

"Researchers have actually spent a good deal of time and effort looking for drug candidates that are effective against some of these undruggable targets," Ball said. "But the results are generally mediocre, and affinity is a big reason why. Without a classical binding pocket, we tend to see inefficient binding with relatively flat protein surfaces that are not designed to bind drug-like molecules. Our idea is to add well-placed rhodium atoms that will act like pins to hold an otherwise mediocre drug candidate in place."

The NCI project grew out of a collaboration with Michele Redell, assistant professor of internal medicine at BCM, and David Tweardy, professor of medicine and chief of the section of infectious diseases at BCM. Ball, Redell and Tweardy won seed funding in January from the Simmons Family Foundation for a project aimed at developing new drugs to treat acute myeloid leukemia (AML), which afflicts thousands of new patients every year, many of them children.

In particular, the group was interested in modifying a drug candidate compound to improve its effectiveness against STAT3, a transcription regulating protein that has been implicated in AML and numerous other cancers, including gastric, renal, breast, ovarian, skin and brain cancer. STAT3 is an especially compelling area of study because previous research has shown that targeting STAT3 may allow for effective treatment of "multiple drug-resistant" tumors for which available treatments are ineffective.

"The Simmons grant allowed us to gather preliminary evidence to bolster our case for creating a hybrid drug that combines the benefits of both traditional drugs and metal-based drugs," Ball said. "The prior work really strengthened our proposal, and we're hoping to use the two-year 'Provocative Questions' grant to lay the scientific foundations for future translational studies."


'/>"/>

Contact: Jade Boyd
jadeboyd@rice.edu
713-348-6778
Rice University
Source:Eurekalert  

Related medicine news :

1. Salk study finds diabetes raises levels of proteins linked to Alzheimers features
2. Protein regulation linked to intellectual disability
3. Lactation protein suppresses tumors and metastasis in breast cancer
4. Treating Sperm With Missing Protein Might Help Male Fertility
5. Research identifies protein that regulates key fate decision in cortical progenitor cells
6. Cervical cancer and pre-cancer cervical growths require single HPV protein
7. Scripps Research Institute scientists show protein linked to hunger also implicated in alcoholism
8. Hopkins scientists discover how an out-of-tune protein leads to muscle demise in heart failure
9. Protein linked to therapy resistance in breast cancer
10. Well-known protein reveals new tricks
11. Binding sites for LIN28 protein found in thousands of human genes
Post Your Comments:
*Name:
*Comment:
*Email:
Related Image:
Pinning protein could answer provocative cancer question
(Date:10/13/2017)... Abilene, Texas (PRWEB) , ... October 13, 2017 , ... ... publication this week that explains one of the most popular and least understood books ... seems like cryptic and puzzling descriptions that have baffled scholars for centuries. Many have ...
(Date:10/12/2017)... ... October 12, 2017 , ... First Healthcare Compliance (FHC), ... will showcase a range of technology and learning solutions at the 68th Annual ... Expo to be held October 14–18, 2017 at the Mandalay Bay Resort in ...
(Date:10/12/2017)... ... October 12, 2017 , ... The American College of Medical Informatics (ACMI) ... FACMI, during the Opening Session of AMIA’s Annual Symposium in Washington, D.C. AMIA’s ... Morris F. Collen, a pioneer in the field of medical informatics, this prestigious award ...
(Date:10/12/2017)... ... 2017 , ... Leading pediatric oncology experts at Children’s National Health System ... Congress of the International Society of Paediatric Oncology (SIOP) Oct. 12-15. Chaired by ... and Blood Disorders at Children’s National, and Stephen P. Hunger, M.D., Chief of ...
(Date:10/12/2017)... ... October 12, 2017 , ... Vohra Chief ... advancements to physician colleagues, skilled nursing facility medical directors and other clinicians at ... of Wound Care." , "At many of these conferences we get to educate ...
Breaking Medicine News(10 mins):
(Date:9/23/2017)... , Sept. 22, 2017 Janssen Biotech, ... complete response letter from the U.S. Food and Drug ... approval of sirukumab for the treatment of moderately to ... indicates additional clinical data are needed to further evaluate ... to severely active RA. ...
(Date:9/19/2017)... 19, 2017   ZirMed Inc ., a recognized leader ... that it has been ranked #1 by its users for ... Rankings 2017 User Survey. ZirMed was recognized as the top-ranked ... and medical centers over 200 beds and holds one of ... user survey history. ...
(Date:9/12/2017)... PARIS and NEW YORK , Sept. 12, ... ethical performance ratings for global supply chains, has published the first annual ... the CSR performance of more than 20,400 companies evaluated by EcoVadis, based ... years 2015 and 2016. ... EcoVadis Global CSR Risk & Performance Index ...
Breaking Medicine Technology: