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Scientists synthesize long-sought-after anticancer agent
Yale University ^ | January 31, 2011 | Unknown

Posted on 01/31/2011 1:14:28 PM PST by decimon

New Haven, Conn.—A team of Yale University scientists has synthesized for the first time a chemical compound called lomaiviticin aglycon, leading to the development of a new class of molecules that appear to target and destroy cancer stem cells.

Chemists worldwide have been interested in lomaiviticin's potential anticancer properties since its discovery in 2001. But so far, they have been unable to obtain significant quantities of the compound, which is produced by a rare marine bacterium that cannot be easily coaxed into creating the molecule. For the past decade, different groups around the world have been trying instead to synthesize the natural compound in the lab, but without success.

Now a team at Yale, led by chemist Seth Herzon, has managed to create lomaiviticin aglycon for the first time, opening up new avenues of exploration into novel chemotherapies that could target cancer stem cells, thought to be the precursors to tumors in a number of different cancers including ovarian, brain, lung, prostate and leukemia. Their discovery appears online today in the Journal of the American Chemical Society.

"About three quarters of anticancer agents are derived from natural products, so there's been lots of work in this area," Herzon said. "But this compound is structurally very different from other natural products, which made it extremely difficult to synthesize in the lab."

In addition to lomaiviticin aglycon, Herzon's team also created smaller, similar molecules that have proven extremely effective in killing ovarian stem cells, said Gil Mor, M.D., a researcher at the Yale School of Medicine who is collaborating with Herzon to test the new class of molecules' potential as a cancer therapeutic.

The scientists are particularly excited about lomaiviticin aglycon's potential to kill ovarian cancer stem cells because the disease is notoriously resistant to Taxol and Carboplatin, two of the most common chemotherapy drugs. "Ovarian cancer has a high rate of recurrence, and after using chemotherapy to fight the tumor the first time, you're left with resistant tumor cells that tend to keep coming back," Mor explained. "If you can kill the stem cells before they have the chance to form a tumor, the patient will have a much better chance of survival – and there aren't many potential therapies out there that target cancer stem cells right now."

Herzon's team, which managed to synthesize the molecule in just 11 steps starting from basic chemical building blocks, has been working on the problem since 2008 and spent more than a year on just one step of the process involving the creation of a carbon-carbon bond. It was an achievement that many researchers deemed impossible, but while others tried to work around having to create that bond by using other techniques, the team's persistence paid off.

"A lot of blood, sweat and tears went into creating that bond," Herzon said. "After that, the rest of the process was relatively easy."

Next, the team will continue to analyze the compound to better understand what's happening to the stem cells at the molecular level. The team hopes to begin testing the compounds in animals shortly.

"This is a great example of the synergy between basic chemistry and the applied sciences," Herzon said. "Our original goal of synthesizing this natural product has led us into entirely new directions that could have broad impacts in human medicine."

###

Other authors of the paper include Liang Lu, Christina M. Woo and Shivajirao L. Gholap, all of Yale University.


TOPICS: Health/Medicine; Science
KEYWORDS:

1 posted on 01/31/2011 1:14:31 PM PST by decimon
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To: neverdem; DvdMom; grey_whiskers; Ladysmith; Roos_Girl; Silentgypsy

Ping


2 posted on 01/31/2011 1:15:12 PM PST by decimon
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To: decimon

Why am I seeing “Omega Man” and “I am legend” flashing before my eyes?


3 posted on 01/31/2011 1:23:17 PM PST by enraged
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To: decimon

Here’s hoping....


4 posted on 01/31/2011 1:31:12 PM PST by Silentgypsy
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To: enraged

“I am Legend” was my first thought as well...


5 posted on 01/31/2011 1:32:44 PM PST by eyrish69 (Yellowstone Wolves - Smoke a Pack a Day!!!)
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To: decimon

[ In addition to lomaiviticin aglycon, Herzon’s team also created smaller, similar molecules that have proven extremely effective in killing ovarian stem cells, ]

Hmm, can you say, “Depopulation vaccine”......

If course the progressives would sell it to us as a “good idea”.....

The people who want to depopulate the planet scare me... and they are willing to use any tool to do so.


6 posted on 01/31/2011 1:35:02 PM PST by GraceG
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To: decimon

How would success in this area affect the pharmaceutical industry? I knew a fella who patented some photovoltaic cell thingy and GM kept trying to buy his patent, ostensibly in order to suppress it. (Is this considered hijacking a thread? I’m trying to behave better, but some things make me think of other things....)


7 posted on 01/31/2011 1:36:48 PM PST by Silentgypsy
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To: decimon
Go Elis!!!


8 posted on 01/31/2011 2:00:17 PM PST by Daffynition ( Live EACH DAY as if it were your last, but EXPECT that there still may be a tomorrow.)
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To: GraceG

Forgive me, perhaps I’m being dense, but since I just lost my best friend to cancer two weeks ago I’m pretty enthusiastic about a new chemical that appears to target and kill cancer cells. What is wrong with that and how do you see that using it would depopulate the world? Just the opposite, I’d think—if we have fewer people dying of cancer we’ll have more people on earth. I don’t see how that’s a bad thing, and I just wish they’d come up with this a few years ago. Could you clarify? Are you really suggesting these people did so much research not because they want to cure cancer but because they secretly want us all to die? If you could make the connection for me I’d be most grateful.


9 posted on 01/31/2011 2:13:54 PM PST by ottbmare (off-the-track Thoroughbred mare)
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To: Silentgypsy
How would success in this area affect the pharmaceutical industry?

Dunno. The field of oncology is big even without pharmaceuticals.

10 posted on 01/31/2011 2:25:33 PM PST by decimon
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To: Silentgypsy

PM me and tell me more about it.


11 posted on 01/31/2011 2:48:59 PM PST by Niuhuru (The Internet is the digital AIDS; adapting and successfully destroying the MSM host.)
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To: decimon

I have a background in organic synthesis and I can appreciate the difficulties in a project like this.


12 posted on 01/31/2011 3:22:38 PM PST by ol painless (ol' painless is out of the bag)
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To: ol painless
I have a background in organic synthesis and I can appreciate the difficulties in a project like this.

If the anti-cancer properties were discovered in 2001 then it took about nine years to reproduction. I guess that's good.

13 posted on 01/31/2011 3:29:54 PM PST by decimon
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To: GraceG
Grace, I think there is a word missing in this statement....

"... proven extremely effective in killing ovarian stem cells..."

I think the word that is missing is "killing ovarian cancer stem cells.

As an ovarian cancer survivor I would be really happy for them to develop this particular drug.

14 posted on 01/31/2011 4:33:33 PM PST by Grammy ( TSA “We handle more packages than UPS.”)
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To: Grammy

I have a friend who was diagnosed with ovarian cancer probably a couple of years ago. She chose to forego traditional treatments and is doing it herself. So far, so good.


15 posted on 01/31/2011 5:04:07 PM PST by Conservativegreatgrandma
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