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Comment
. 2013 Nov 21;20(11):1309-10.
doi: 10.1016/j.chembiol.2013.11.002.

Two birds with one stone: dual p110δ and p110γ inhibition

Klaus Okkenhaug  1
Affiliations
Comment

Two birds with one stone: dual p110δ and p110γ inhibition

Klaus Okkenhaug. Chem Biol. .

Abstract

In this issue of Chemistry & Biology, Winkler and colleagues describe the discovery and preclinical development of IPI-145, a new inhibitor of the phosphoinositide 3-kinase (PI3K) isoforms p110δ and p110γ that have entered clinical trials.

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Figures

Figure 1
Figure 1. Chemical structure and PI3K isoform selectivity of GS-1101, IPI-145 and IPI-3063
Structures and cellular IC50 values (nM) against the PI3K p110α, p110β, p110δ and p110γ isoforms as reported by Winkler et al, in this issue. PI3K activity, as determined by Akt phosphorylation, was measured in SCOV cells stimulated with serum (p110α), 786-0 cells stimulated with serum (p110β), RAJI cells stimulated with anti-IgM (p110δ) or RAW264.7 cells stimulated with C5a (p110γ). Enzymatic IC50 values (nM) measured in presence of 3 mM ATP are shown in brackets for GS-1101 and IPI-145.
See this image and copyright information in PMC

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