Navigation Links
Scientists solve mystery of polyketide drug formation
Date:4/1/2008

Irvine, Calif., April 1, 2008 Many top-selling drugs used to treat cancer and lower cholesterol are made from organic compounds called polyketides, which are found in nature but historically difficult for chemists to alter and reproduce in large quantities.

For the first time, scientists at UC Irvine have discovered how polyketides form their ringlike shape, making it easier for chemists to manipulate them into new drugs.

The key, they found, is an enzyme called aromatase/cyclase, which forms a C-shape mold in which polyketides can form one molecule at a time. By changing this mold, chemists can control the size and shape of the polyketide, resulting in the formation of new drugs.

Almost every polyketide has rings in its chemical structure, and if we can control ring formation, we can produce more polyketide drugs, said Sheryl Tsai, lead author of this study and an assistant professor of molecular biology and biochemistry and chemistry at UCI. Until now, polyketide ring formation was a mystery that hampered our efforts to produce new drugs.

The research appears online this week in the Proceedings of the National Academy of Sciences.

Polyketide-based drugs and products account for more than $35 billion in sales annually. They include antibiotics that can cure a bacteria infection (tetracycline and erythromycin); anti-cancer drugs used in chemotherapy (doxorubicin and mithramycin); anti-oxidants that help prevent cancer and promote heart strength (EGCG and resverastrol); and drugs that lower cholesterol levels (Zocor). Green tea and red wine also contain beneficial polyketides.

Polyketides are made naturally by bacteria, fungi, plants and marine animals. Those organisms produce polyketides to kill their predators, be it another bacteria or fungi. They can produce different types of polyketides that kill different types of enemies.

Because bacteria do not have arthritis or diabetes, they would not evolutionally select polyketides that could be used for arthritis or diabetes treatment, Tsai said. But we can coax the bacteria to do precisely that, if we can control the ring formation in the polyketides.

Prior to this study, it was not known how nature controls the polyketide ring shape, which is essential for antibiotic and anti-cancer properties.

By using molecular cloning and chemical biology techniques, Tsai and her scientific team discovered that the aromatase/cyclase enzyme has a pocket that shapes the polyketide, promoting a unique ring pattern.

Said Tsai: We hope this will lead to the development of new drugs in such areas as cancer therapeutics, obesity treatment and stem cell research.


'/>"/>

Contact: Jennifer Fitzenberger
jfitzen@uci.edu
949-824-3969
University of California - Irvine
Source:Eurekalert

Related medicine news :

1. Scientists Uncover How HIV Hides Inside Cells
2. Scientists: New technique identifies molecular biomarkers for disease
3. Princeton Professor David W. C. MacMillan Lectured WuXi PharmaTech Scientists
4. NewYork-Presbyterian/Columbia physician-scientists present at ACCs 57th Annual Scientific Session
5. Dental scientists convene in Dallas
6. Eminent scientists to lecture in Dallas
7. Scientists learn whats up with a class of retinal cells in mice
8. Scientists Isolate Organism That Causes Disfiguring Tropical Disease
9. Scientists uncover how superbug Staph aureus resists our natural defenses
10. Signaling protein helps limit damage in heart attack, Jefferson scientists show
11. Scripps Florida scientists develop a process to disrupt hepatitis C virion production
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:8/18/2017)... ... August 18, 2017 , ... Radabaugh & Associates, a ... communities in North-Central West Virginia, is embarking on a cooperative charity effort with ... area. , The Chestnut Mountain Ranch (CMR) is a Christ-centered boarding school for ...
(Date:8/18/2017)... ... 2017 , ... The Brian Gifford Agency, an Indiana-based firm providing asset protection ... Campagna Academy in a charity drive to provide for at-risk children and teens in ... Academy is a nonprofit organization that has offered critical programs to at-risk and foster ...
(Date:8/18/2017)... ... 2017 , ... “Emotions are sacred, valid, honored, encouraged. This is the memo ... Generation Mindful. To help change the mindset of parents and educators from punitive to ... the Time-In Toolkit, which launched on Kickstarter 3 weeks ago and fully funded in ...
(Date:8/18/2017)... ... 18, 2017 , ... Alcovit, a lime-flavored beverage that rids the body of ... its product now available through Jet.com. , After 25 years of development, the ... is designed to quickly detox the body thereby avoiding alcohol-induced hangovers. Whether you’re having ...
(Date:8/18/2017)... ... ... “Our Mountains to Climb: A Journey of Love and Faith Through Trials”: ... faith they shared to overcome struggles in life. “Our Mountains to Climb: A Journey ... Corcoran, a retired teacher and happily married since 1999; the author’s personal experiences drive ...
Breaking Medicine News(10 mins):
(Date:8/17/2017)... , August 17, 2017 DarioHealth ... Company with mobile health and big data solutions, ... agreements with domestic and non-U.S. investors for the ... and shares of the Company,s newly designated Series ... offerings. The Company expects to conduct a closing ...
(Date:8/15/2017)... HOUSTON , Aug. 15, 2017   Mostyn Law ... in Houston, Texas . The Mostyn Law ... the past 2 years. That is why Mostyn Law ... Texas to show its appreciation. Blood supplies ... to fall 5% short of hospital needs in August. That is ...
(Date:8/15/2017)... Aug. 15, 2017  Axium Pharmaceuticals Inc., the creator of the drug ... in the beginning stages of an IPO. The ... with the average cost of a prescription epilepsy drug being $450.00-$1200.00 for ... AXIUM PHARMACEUTICALS, INC ... Another staggering figure is the fact that Americans spent ...
Breaking Medicine Technology: