Navigation Links
Compounds outsmart solid tumors' malfunctioning machinery
Date:7/17/2013

SAN ANTONIO (July 17, 2013) Molecular biologists in the School of Medicine at The University of Texas Health Science Center San Antonio have found a novel way to fine-tune the activity of cells' protein-disposing machinery, with potentially cancer-fighting effects.

This machinery, the proteasome, is deregulated in cancer. Agents called protease inhibitors are viewed as potential anti-cancer therapies, but they indiscriminately curb proteasome activity, which also includes protein recycling. Such strategy is effective to kill cells in aggressive blood cancers but leads to drug resistance and excessive toxicity in solid tumors.

Fine-tuning

The new strategy may change that. By basically outsmarting the cell's machinery, compounds called allosteric regulators are able to fine-tune the proteasome actions instead of block them. "The result is that cell lines from solid tumors, which are resistant to existing therapy, are sensitive to these agents," said Pawel Osmulski, Ph.D., assistant professor of molecular medicine at the Health Science Center. He and Maria Gaczynska, Ph.D., associate professor of molecular medicine, co-authored a report in Molecular Pharmacology that provides a basis for this approach.

'Highly beneficial'

Deregulation of the proteasome's actions is noted in cancer or during aging and contributes to intracellular pathologies. "It is easy to envision that precise adjusting of the proteasome activities with therapeutic molecules would be highly beneficial in many human conditions," Dr. Osmulski said.

Inhibition and activation

"Allosteric regulators are better than proteasome-affecting agents used in clinics because they do not induce classical drug resistance," Dr. Gaczynska said. "They bind to sites on the proteasome molecule used by natural regulatory proteins. They are more specific and are not restricted to proteasome inhibition but can activate the proteasome under certain conditions."

The new strategy was serendipitously found during experiments with rapamycin, a drug that in a highly publicized study by the UT Health Science Center's Barshop Institute for Longevity and Aging Studies was found to extend life span in mice.

Potential

The Molecular Pharmacology report and follow-up studies describe the unexpected and highly desired effects that rapamycin and similar compounds elicit on the proteasome. Based on these studies, it would be possible to design a new line of proteasome regulators with anti-cancer properties, Drs. Osmulski and Gaczynska said. This work is in progress in their laboratory. Drs. Osmulski and Gaczynska are affiliated with the Barshop Institute and with the Cancer Therapy & Research Center at The University of Texas Health Science Center San Antonio.


'/>"/>

Contact: Will Sansom
sansom@uthscsa.edu
210-567-2579
University of Texas Health Science Center at San Antonio
Source:Eurekalert

Related medicine news :

1. Natural Sciences Repository Publishes Chromatography and Acidic Compounds Resources
2. Compounds activate key cancer enzyme to interfere with tumor formation
3. Taiho Pharmaceutical unveils data on 8 novel anticancer compounds
4. Dirty Drugs and We Know It: Attorneys at Console & Hollawell Comment on ISMP Survey Relating to Contaminated Drug Compounds and the Risks to Consumers
5. Advance in re-engineering photosynthesis to make drugs, compounds or ingredients
6. NIH-supported researchers identify new class of malaria compounds
7. Ginger compounds may be effective in treating asthma symptoms
8. Many solid tumors carry genetic changes targeted by existing compounds
9. Some Whooping Cough Strains Now Outsmarting Vaccine
10. AvePoint Outsmarts the Chaos with Interactive Meetings App for Microsoft SharePoint 2013
11. OHSU research highlights promising strategy to help vaccines outsmart HIV
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:10/13/2017)... ... ... While it’s often important to take certain medications during the night, finding ... identified a solution. , She developed a prototype for MOTION LIGHT-UP PILL BOX to ... the need to turn on a light when taking medication during the night, allowing ...
(Date:10/13/2017)... ... October 13, 2017 , ... ... alumni Hannah Randall, PharmD ‘17, and Jennifer Huggins, PharmD ’17, along with ... for the primary prevention of cardiovascular diseases during the 15th Annual Women’s ...
(Date:10/13/2017)... ... ... The Visiting Nurse Association (VNA) of Somerset Hills is proud to host ... items from across the nation, this holiday-themed event will raise funds and awareness for ... The boutique will be open Saturday, November 4 (10:00 a.m. – 5:00 p.m.) ...
(Date:10/13/2017)... ... October 13, 2017 , ... Talented host, actor ... on sciatica in a new episode of "Success Files," which is an award-winning ... innovation and investigates each subject in-depth with passion and integrity. , Sciatica occurs ...
(Date:10/12/2017)... ... October 12, 2017 , ... First Healthcare ... program management, will showcase a range of technology and learning solutions at the ... Convention and Expo to be held October 14–18, 2017 at the Mandalay Bay ...
Breaking Medicine News(10 mins):
(Date:10/12/2017)... 12, 2017   Divoti USA will engrave ... the standard of the latest FDA requirements, which stipulates new criteria ... Anyone in need of Medical ID jewelry such as Medical ID ... are engraved in terms of the new FDA requirements . ... Divoti offers this dark mark ...
(Date:10/11/2017)... PARK, Calif. , Oct. 11, 2017  BioPharmX ... national scientific team that developed an innovative way to ... quantity of the delivery of new drugs. ... 2017 Fall Clinical Dermatology Conference will show how researchers ... General Hospital, Harvard Medical School used a suite of ...
(Date:10/11/2017)... 2017  True Health, a leader in integrated ... during National Breast Cancer Awareness month to educate ... Research recently published ... more than 10 million American women are at ... or BRCA2 and have not had testing. These mutations ...
Breaking Medicine Technology: