| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 7802251 | European Journal of Medicinal Chemistry | 2012 | 9 Pages |
Abstract
⺠Substrate-Activity-Screening is applied to a tyrosine kinase. ⺠The substrate efficiency of a tetrapeptide was optimized using a modular approach. ⺠Substrates were then converted into inhibitors by replacement of the tyrosine. ⺠A correlation between substrate SAR and inhibitor SAR was confirmed. ⺠We obtained a low single-digit micromolar substrate-site inhibitor of IGF-1R.
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Organic Chemistry
Authors
Julien Chapelat, Frédéric Berst, Andreas L. Marzinzik, Henrik Moebitz, Peter Drueckes, Joerg Trappe, Doriano Fabbro, Dieter Seebach,