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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.

A novel class of quinazolinone derivatives as potent poly(ADP-ribose)polymerase-1 ( PARP-1) inhibitors has been discovered. Key to success was application of a rational discovery strategy involving structure-based design, combinatorial chemistry, and classical SAR for improvement of potency and bioavailability. The new inhibitors were shown to bind to the nicotinamide-ribose binding site (NI site) and the adenosine-ribose binding site (AD site) of NAD+.[1]

References

  1. Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase. Hattori, K., Kido, Y., Yamamoto, H., Ishida, J., Kamijo, K., Murano, K., Ohkubo, M., Kinoshita, T., Iwashita, A., Mihara, K., Yamazaki, S., Matsuoka, N., Teramura, Y., Miyake, H. J. Med. Chem. (2004) [Pubmed]
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