Drugging the P13 kinome
Article Abstract:
The proof of concept for the exciting potential of compounds that simultaneously inhibit P13 kinase p110alpha and mTOR for the treatment of malignant brain tumors (gliomas) is demonstrated. Results indicate that comparison of various compounds for their ability to inhibit glioma cell growth showed that the dual competitive kinase inhibitor PI-103 was the most effective, suggesting that p110alpha cooperates with mTOR in malignant glioma.
Publication Name: Nature Biotechnology
Subject: Business
ISSN: 1087-0156
Year: 2006
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Interaction maps for kinase inhibitors
Article Abstract:
An in vitro essay for determining kinase inhibitor specificity and its use to create 'inhibitor' maps of 20 different kinase inhibitors against 119 different protein kinases is described. Imatinib, an inhibitor of the mutant kinase Bcr-Abl, induces durable complete hematologic responses in 97% of patients with chronic myelogenous leukemia.
Publication Name: Nature Biotechnology
Subject: Business
ISSN: 1087-0156
Year: 2005
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A small molecule-kinase interaction map for clinical kinase inhibitors
Article Abstract:
An efficient way to determine kinase inhibitor specificity by measuring binding of small molecules to the ATP site of kinases is described. The specificity varies widely and is not strongly correlated with chemical structure or identity of the intended target.
Publication Name: Nature Biotechnology
Subject: Business
ISSN: 1087-0156
Year: 2005
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