Potential new drug blocks pathway of deadliest cancer
Scientists at Cancer Research Technology Ltd (CRT) will present exciting new
findings showing that a potent and selective inhibitor of protein kinase D called
CRT0066101, inhibits the growth of pancreatic tumours.
The research - to be presented by CRT's Dr Christopher Ireson at the American
Association for Cancer Research conference today (Sunday) - was a collaborative
effort between scientists at CRT's discovery laboratories and the University
of Texas MD Anderson Cancer Center. These results show for the first'time that
an inhibitor of PKD can slow the growth of tumours in pancreatic cancer models.
In addition, experiments carried out by CRT have shown that CRT0066101 is also
effective at inhibiting the growth of tumours in a lung cancer model. The scientists
believe that the drug has the potential to treat other cancers too.
PKD is a relatively newly identified family of serine/threonine kinases comprising
PKD1, PKD2 and PKD3. The potential of PKD as a new drug target was discovered
by Enrique Rozengurt, Doreen Cantrell and Peter Parker and funded by Cancer
Research UK. Following this discovery, an intensive drug discovery effort led
by CRT's head of medicinal chemistry, Dr Tony Raynham, culminated in the identification
of CRT0066101 as a lead candidate for pre-clinical studies. Since then, PKD
has been identified as playing a central role in the development of a number
of cancers. In addition to its role in the growth of tumour cells, PKD has also
been shown to play a pivotal role in cell survival and angiogenesis - a process
by which tumours form new blood vessels - which is central to tumour growth
CRT's discovery laboratories director Dr Hamish Ryder said:
"We focused on pancreatic and lung cancer tumours because they
represent cancers with a significant unmet medical need. “The CRT model
of combining promising basic science with the capability of the industrially-focus
Discovery Laboratories gives us a unique opportunity to rapidly develop potential
new molecules to novel targets, and through partnering with industry, explore
the potential to see if one day it might help treat cancer patients in the
Dr Sushovan Guha who leads the laboratory at MD Anderson Cancer Center, said:
"We are very optimistic about CRT0066101's pharmacological potential.
We believe this is the first orally administered small-molecule inhibitor
of PKD with significant biological efficacy in pre-clinical animal models
of pancreatic cancer. My conviction is that we will show the drug can also
prevent the proliferation of cancer cells by blocking their supply of blood
- through neo-angiogenesis. This would mean it offers a double action treatment
but this needs to be proved through further work."