期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 14, 页码 3978-3981出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.011
关键词
dynamic combinatorial chemistry; fragment-based lead discovery; DCC; FBLD; fragment-based; Aurora; kinase; DFG-out; mass-spectrometry; site-directed; cysteine
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. (c) 2008 Elsevier Ltd. All rights reserved.
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