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PI(3) Kinases

Revealing the delta lady

A Corrigendum to this article was published on 01 April 2010

This article has been updated

Phosphoinositide 3-OH kinases (PI(3)Ks) are important lipid signaling enzymes and exciting drug targets for a number of human diseases. The first, much anticipated crystal structure of the delta isoform of PI(3)K provides surprising new insights into the selectivity of inhibitors for this versus other PI(3)K isoforms and facilitates the design of improved drugs.

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Figure 1: PI(3)Kδ-selective propeller-shaped inhibitors exploit a flexible specificity pocket in PI(3)Kδ that is not opened upon the binding of flat pan-specific PI(3)K inhibitors.

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  • 02 March 2010

    In the version of this article initially published, there was an error in the chemical structure of IC87114 that arose from the coordinates used to generate Figure 1a. The corrected structure has been deposited by Berndt et al. to the Protein Data Bank (PDB code 2X38). Figure 1a and the PDB code in the figure legend have been corrected in the HTML and PDF versions of the article.


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Correspondence to Paul Workman or Rob L M van Montfort.

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Competing interests

P.W. and R.L.M.M. are employees of The Institute of Cancer Research, which has a commercial interest in the development of PI(3)K inhibitors, and operates a rewards-to-inventors scheme. P.W. has been involved in a commercial collaboration with Yamanouchi (now Astellas Pharma) and with Piramed Pharma, and intellectual property arising from the program has been licensed to Genentech. P.W. was a scientific founder of, consultant to, and Scientific Advisory Board member of Piramed Pharma; is a scientific founder of, consultant to, and Scientific Advisory Board member and Main Board member of Chroma Therapeutics; and was formerly an employee of AstraZeneca. R.L.M.M. is a former employee of Astex Therapeutics.

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Workman, P., van Montfort, R. Revealing the delta lady. Nat Chem Biol 6, 82–83 (2010).

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