Results 231 to 240 of about 193,906 (268)

Isoform-specific phosphoinositide 3-kinase inhibitors as therapeutic agents.

Current Opinion in Pharmacology, 2003
The phosphoinositide 3-kinase (PI3K) family of enzymes consists of several closely related isoforms that are thought to have distinct biological roles. Until now, researchers have been frustrated by poor selectivity of the available pharmacological inhibitors, which are unable to distinguish adequately the activities of different PI3K isoforms ...
S. Ward, P. Finan
semanticscholar   +3 more sources

Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold.

Bioorganic & Medicinal Chemistry, 2004
Phosphoinositide 3-kinases (PI3-Ks) are an ubiquitous class of signaling enzymes that regulate diverse cellular processes including growth, differentiation, and motility. Physiological roles of PI3-Ks have traditionally been assigned using two pharmacological inhibitors, LY294002 and wortmannin. Although these compounds are broadly specific for the PI3-
Z. Knight   +7 more
semanticscholar   +3 more sources

Therapeutic potential of phosphoinositide 3-kinase inhibitors

Expert Opinion on Therapeutic Patents, 2004
Originally discovered as oncogene-associated lipid kinases more than 15 years ago, the family of phosphoinositide 3-kinase (PI 3-K) enzymes has recently emerged as an important therapeutic target in human pathophysiology. After more than a decade with only a few inhibitors with low activity, poor isoform or kinase selectivity or unacceptable ...
B. Drees   +3 more
semanticscholar   +2 more sources

Development of first lead structures for phosphoinositide 3-kinase-C2γ inhibitors.

Journal of Medicinal Chemistry, 2015
The importance of complete elucidation of the biological functions of phosphoinositide 3-kinases (PI3K) was realized years ago. They generate 3-phosphoinositides, which are known to function as important second messengers in many inter- and intracellular signaling pathways. However, the functional role of class II PI3Ks is still unclear.
A. Freitag   +8 more
semanticscholar   +3 more sources

Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.

Journal of Medicinal Chemistry, 2011
Of the four class I phosphoinositide 3-kinase (PI3K) isoforms, PI3Kα has justly received the most attention for its potential in cancer therapy. Herein we report our successful approaches to achieve PI3Kα vs PI3Kβ selectivity for two chemical series.
Timothy Heffron   +20 more
semanticscholar   +3 more sources

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