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:12/7/2016)... ... ... AlignLife clinics nationwide are giving back to their communities by collecting toys ... gifts wrapped tightly under a Christmas Tree. AlignLife hopes to spread the joy ... In exchange for generous donations, customers will receive a gift in return. Anyone ...
(Date:12/7/2016)... Honolulu, HI (PRWEB) , ... December 07, 2016 ... ... Dermatology is proud to announce that its fully redesigned website, which launched October ... well as a sleek responsive design and easy-to-navigate layout. Visitors and patients can ...
(Date:12/7/2016)... (PRWEB) , ... December 07, 2016 , ... ... Top 20 Marketing Campaign Winner in the Folio: Marketing Awards competition. Live From ... the year’s best in pioneering, inventive, and ultimately successful projects undertaken by the ...
(Date:12/7/2016)... AZ (PRWEB) , ... December ... ... ElectroMedical Technologies, announced its newest portable bioelectronic medicine device WellnessPro Plus for ... WellnessPro Plus substantially enhances the WellnessPro platform by expanding the treatment modalities ...
(Date:12/7/2016)... ... 2016 , ... “Walking With God: Inspirational Lessons from My Life's Journey”: ... be aware of God's direction in their lives. “Walking With God: Inspirational Lessons from ... active church leader. , Sanford says, “I enjoy sharing the true stories ...
Breaking Medicine News(10 mins):
(Date:12/6/2016)... N.Y. , Dec. 6, 2016  Licenders is bringing their ... This new location in Park Slope at 203 13 th ... Brooklyn clientele. "Our goal is to ... treatment plans are designed to get children right back to class ... are 100% all natural and safe for the whole family," Licenders ...
(Date:12/6/2016)... 2016  "Blood Tests replace Surgical Biopsies. Single ... The Diagnostic, Monitoring and Screening Test opportunities are ... occurring using in vitro blood testing to identify ... backing, has announced a single blood test to ... than the market. New technology that definitively identifies ...
(Date:12/6/2016)... 6, 2016 Diabetes & Obesity Drug Development ... obesity disease cluster is currently dominated by therapeutics indicated ... diabetes mellitus (T2DM), and the majority of the pipeline, ... is attributable to these indications. While products indicated for ... there are a large number of these products in ...
Breaking Medicine Technology: