| Autor: |
Cancilla MT; Sunesis Pharmaceuticals, Inc., 395 Oyster Point Boulevard, Suite 400, South San Francisco, CA 94080, USA., He MM, Viswanathan N, Simmons RL, Taylor M, Fung AD, Cao K, Erlanson DA |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jul 15; Vol. 18 (14), pp. 3978-81. Date of Electronic Publication: 2008 Jun 10. |
| DOI: |
10.1016/j.bmcl.2008.06.011 |
| Abstrakt: |
We demonstrate a fragment-based lead discovery method that combines site-directed ligand discovery with dynamic combinatorial chemistry. Our technique targets dynamic combinatorial screening to a specified region of a protein by using reversible disulfide chemistry. We have used this technology to rapidly identify inhibitors of the drug target Aurora A that span the purine-binding site and the adaptive pocket of the kinase. The binding mode of a noncovalent inhibitor has been further characterized through crystallography. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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