Syk inhibitor... new target kinase... pre-clinical characteristics of P505-15

Syk inhibitor... new target kinase... pre-clinical characteristics of P505-15

The selective Syk inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo, and augments the activity of fludarabine in chronic lymphocytic leukemia.

B-cell receptor (BCR) associated kinases including spleen tyrosine kinase (SYK) contribute to the pathogenesis of B-cell malignancies. SYK is persistently phosphorylated in a subset of non-Hodgkin lymphoma (NHL) and chronic lymphocytic leukemia (CLL), and SYK inhibition results in abrogation of downstream kinase activity and apoptosis.

P505-15 (also known as PRT062607) is a novel, highly selective and orally bioavailable small-molecule SYK inhibitor with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.

We evaluated the pre-clinical characteristics of P505-15 in models of NHL and CLL. P505-15 successfully inhibited SYK mediated B-cell receptor signaling and decreased cell viability in NHL and CLL.

jpet.aspetjournals.org/cont...

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~chris

CLL CANADA: cllcanada.ca

CLL Guidelines:

bloodjournal.hematologylibr...

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