Rutgers pharmaceutical chemist Longqin Hu
(pictured at right) and his colleagues have
developed a new series of compounds for drugs that
have the potential to attack cancer like a
high-tech “smart bomb.” This high-powered
combination of a novel cytotoxin or cell-killing
agent and a precision targeting technology proved
to be as much as 100 times more potent than a
comparable drug currently in clinical trials.
The delivery of the compound is accomplished
with a prodrug – an inert chemical derivative of a
drug that can be activated once it reaches its
destination inside a patient’s body, thereby
safeguarding other body tissues along the way.
Hu’s research employs a new and improved prodrug
package developed by collaborators in England.
Traditional anticancer drugs use accelerated
cell growth as their trigger, which can produce
collateral damage in rapidly replicating normal
cells. “That is how you wind up with the negative
side effects you see in chemotherapy patients,
such as hair loss, nausea and reduced immunities,”
said Hu.
Instead of hitting all cells that grow fast,
the newly reformulated prodrugs use a protein or
enzyme as the activating trigger, guaranteeing a
direct hit on cancerous cells. When researchers
insert a gene for the enzyme into cancer cells,
the cells start to express it, making them an easy
target. The prodrug “bomb” goes off and unleashes
the toxin that spreads to neighboring cells which
ultimately kills the tumor.
The English contingent also developed a
compound that is being evaluated in clinical
trials as another anticancer prodrug. But Hu’s new
compounds appear to be even more potent. The
overseas researchers are now testing the Rutgers
compounds, side by side with their own, delivering
them in the enhanced prodrug packages.
 The High
Performance Liquid Chromatography (HPLC) machine
pictured above in Professor Hu’s laboratory is
an important tool in his pursuit of new and more
effective drugs. HPLC is an analytical method
used in the separation, identification,
purification and quantification of chemical
compounds.
For more information on how HPLC
works, see page 4 of the manufacturer's The
Liquid Chromatography background
document.
|
Initial testing on mammalian hamster cells
shows that after 72 hours of drug exposure, the
Rutgers compounds were as much as 100 times more
effective in inhibiting cell growth.
“Our cytotoxic compounds delivered to the
cancer site in a revamped prodrug form clearly
show great potential, but there are still lots of
tests to be done,” said Hu. “There are many
preclinical studies ahead of us. If everything
goes well, we could see clinical trials in humans
in a couple of years.”
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