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Title | 2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice. |
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Journal, issue, pages | J. Med. Chem., Vol. 51, Page 2933-2943, Year 2008 |
Publish date | Jan 16, 2008 (structure data deposition date) |
Authors | Johansson, L. / Fotsch, C. / Bartberger, M.D. / Castro, V.M. / Chen, M. / Emery, M. / Gustafsson, S. / Hale, C. / Hickman, D. / Homan, E. ...Johansson, L. / Fotsch, C. / Bartberger, M.D. / Castro, V.M. / Chen, M. / Emery, M. / Gustafsson, S. / Hale, C. / Hickman, D. / Homan, E. / Jordan, S.R. / Komorowski, R. / Li, A. / McRae, K. / Moniz, G. / Matsumoto, G. / Orihuela, C. / Palm, G. / Veniant, M. / Wang, M. / Williams, M. / Zhang, J. |
External links | J. Med. Chem. / PubMed:18419108 |
Methods | X-ray diffraction |
Resolution | 2.69 Å |
Structure data | PDB-3byz: |
Chemicals | ChemComp-NDP: ChemComp-H11: |
Source |
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Keywords | OXIDOREDUCTASE / alpha beta / 3-layer (aba) sandwich / rossmann fold / NAD(P)-binding rossmann-like domain. amino thiazole inhibitor / Endoplasmic reticulum / Glycoprotein / Lipid metabolism / Membrane / Microsome / NADP / Polymorphism / Signal-anchor / Steroid metabolism / Transmembrane / ---- |