3LZ6
Guinea Pig 11beta hydroxysteroid dehydrogenase with PF-877423
Summary for 3LZ6
| Entry DOI | 10.2210/pdb3lz6/pdb |
| Descriptor | Corticosteroid 11-beta-dehydrogenase isozyme 1, NADP NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, N-adamantan-2-yl-1-ethyl-D-prolinamide, ... (4 entities in total) |
| Functional Keywords | oxidoreductase-oxidoreductase inhibitor complex, oxidoreductase/oxidoreductase inhibitor |
| Biological source | Cavia porcellus (guinea pig) |
| Cellular location | Endoplasmic reticulum membrane; Single-pass type II membrane protein: Q6QLL4 |
| Total number of polymer chains | 4 |
| Total formula weight | 119229.22 |
| Authors | Pauly, T.A. (deposition date: 2010-03-01, release date: 2011-05-04, Last modification date: 2024-02-21) |
| Primary citation | Cheng, H.,Hoffman, J.,Le, P.,Nair, S.K.,Cripps, S.,Matthews, J.,Smith, C.,Yang, M.,Kupchinsky, S.,Dress, K.,Edwards, M.,Cole, B.,Walters, E.,Loh, C.,Ermolieff, J.,Fanjul, A.,Bhat, G.B.,Herrera, J.,Pauly, T.,Hosea, N.,Paderes, G.,Rejto, P. The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. Bioorg.Med.Chem.Lett., 20:2897-2902, 2010 Cited by PubMed Abstract: The design and development of a series of highly selective pyrrolidine carboxamide 11beta-HSD1 inhibitors are described. These compounds including PF-877423 demonstrated potent in vitro activity against both human and mouse 11beta-HSD1 enzymes. In an in vivo assay, PF-877423 inhibited the conversion of cortisone to cortisol. Structure guided optimization effort yielded potent and stable 11beta-HSD1 selective inhibitor 42. PubMed: 20363126DOI: 10.1016/j.bmcl.2010.03.032 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.84 Å) |
Structure validation
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