June 3, 2011

GEN Reports On Advances In Novel Protein Kinase Inhibitor Development

Biotech scientists are working on novel protein kinase inhibitors that are targeting a host of conditions ranging from atherosclerosis to neurodegenerative diseases, reports Genetic Engineering & Biotechnology News (GEN). Recent developments in the protein kinase inhibitor field include innovative paradigms for drug development, improved inhibitor profiling and selectivity strategies, and the expansion of disease targets (e.g., Alzheimer disease and traumatic brain injury), according to the June 1 issue of GEN (http://www.genengnews.com/gen-articles/kinase-inhibitor-obstacles-falling/3674/).

"Protein kinases underlie important cellular activities such as proliferation, metabolism, apoptosis, and differentiation, among others," says John Sterling, Editor in Chief of GEN. "They provide an excellent opportunity for a number of promising new drug products."

Researchers at ArQule, for example, are focusing on the inactive state of kinases. They carried out structural and functional studies on inhibitors of the c-Met receptor tyrosine kinase that is implicated in several cancers. The team subsequently co-crystallized their own small molecule inhibitor with inactive c-Met and reportedly discovered a conformation that is distinct from published kinase structures.

Scientists at Celgene are refining the company's in-house kinase selectivity strategy. They used Caliper Life Sciences' ProfilerPro kinase selectivity assay to find selectivity snapshots they were seeking.


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