In the present paper, we review the preclinical development of TG100-115, a PI3K (phosphoinositide 3-kinase) γ/δ isoform-specific inhibitor currently in clinical trials for the reduction of acute MI (myocardial infarction). An overview is presented outlining the pathogenesis of acute MI and the rationale for clinical use of PI3K γ/δ-specific inhibitors in this indication. TG100-115's broad anti-inflammatory activities are described, as well as its ability to discriminate between cellular signalling pathways downstream of receptor tyrosine kinase ligands such as vascular endothelial growth factor. Finally, we review TG100-115's potent cardioprotective activities as revealed in rigorous animal models of acute MI, and, based on these data, this compound's potential for clinical utility.
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April 2007
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Conference Article|
March 20 2007
Isoform-selective PI3K inhibitors as novel therapeutics for the treatment of acute myocardial infarction
J. Doukas;
J. Doukas
1
1TargeGen Inc., 9380 Judicial Drive, San Diego, CA 92121, U.S.A.
1To whom correspondence should be addressed (email jdoukas@targegen.com).
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W. Wrasidlo;
W. Wrasidlo
1TargeGen Inc., 9380 Judicial Drive, San Diego, CA 92121, U.S.A.
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G. Noronha;
G. Noronha
1TargeGen Inc., 9380 Judicial Drive, San Diego, CA 92121, U.S.A.
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E. Dneprovskaia;
E. Dneprovskaia
1TargeGen Inc., 9380 Judicial Drive, San Diego, CA 92121, U.S.A.
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J. Hood;
J. Hood
1TargeGen Inc., 9380 Judicial Drive, San Diego, CA 92121, U.S.A.
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R. Soll
R. Soll
1TargeGen Inc., 9380 Judicial Drive, San Diego, CA 92121, U.S.A.
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Publisher: Portland Press Ltd
Received:
October 30 2006
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2007 The Biochemical Society
2007
Biochem Soc Trans (2007) 35 (2): 204–206.
Article history
Received:
October 30 2006
Citation
J. Doukas, W. Wrasidlo, G. Noronha, E. Dneprovskaia, J. Hood, R. Soll; Isoform-selective PI3K inhibitors as novel therapeutics for the treatment of acute myocardial infarction. Biochem Soc Trans 1 April 2007; 35 (2): 204–206. doi: https://doi.org/10.1042/BST0350204
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