| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371310 | Bioorganic & Medicinal Chemistry Letters | 2015 | 4 Pages |
Abstract
5Z-7-Oxozeaenol (5Z7O) is a covalent bonding inhibitor against the several protein kinases (e.g., ERK2 and TAK1) that possess a free cysteine at the gatekeeper-2 position. In addition to this cysteine, MAP2K7 has three other cysteine residues that are candidate for covalent bonding by the inhibitor 5Z7O. The crystal structure of the MAP2K7/5Z7O complex revealed that the inhibitor binds to MAP2K7 at a cysteine residue located at the end of the hinge region and not at the gatekeeper-2 residue. The structural insights into the interaction of 5Z7O with MAP2K7 should aid the development of 5Z7O derivatives with improved potency and selectivity.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Yuri Sogabe, Takashi Matsumoto, Takuma Hashimoto, Yasuyuki Kirii, Masaaki Sawa, Takayoshi Kinoshita,