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12:00 AM
Apr 25, 2011
 |  BioCentury  |  Emerging Company Profile

Blueprint: Insightful Kinase Inhibitors

Blueprint building new library of very specific kinase inhibitors for cancer

Traditional kinase inhibitor screening approaches for cancer have relied on chemical libraries designed to inhibit other targets or treat different diseases. Blueprint Medicines is looking to change that by building a brand new library of kinase inhibitors that it believes will be more selective and potent than inhibitors developed using the other approaches.

In cancer, mutations in protein kinases can cause aberrant expression of the kinase that leads to uncontrolled cell division and proliferation. Drugs that inhibit these aberrant kinases are the focus of many cancer programs.

"People have done large screening campaigns with chemical scaffolds, but they have come out of existing medicinal chemistry libraries where they started out as inhibitors of kinase 'X,'" said co-founder and CSO David Armistead. "Now they are saying: 'Let's try elsewhere and see if it works.'"

According to Armistead, this means "companies are trying to use inhibitors of other targets that they've worked on in the past and modify the structures of those to build in selectivity and potency."


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