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TitleDiscovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 19, Page 1797-1801, Year 2009
Publish dateJan 8, 2009 (structure data deposition date)
AuthorsRew, Y. / McMinn, D.L. / Wang, Z. / He, X. / Hungate, R.W. / Jaen, J.C. / Sudom, A. / Sun, D. / Tu, H. / Ursu, S. ...Rew, Y. / McMinn, D.L. / Wang, Z. / He, X. / Hungate, R.W. / Jaen, J.C. / Sudom, A. / Sun, D. / Tu, H. / Ursu, S. / Villemure, E. / Walker, N.P. / Yan, X. / Ye, Q. / Powers, J.P.
External linksBioorg. Med. Chem. Lett. / PubMed:19217779
MethodsX-ray diffraction
Resolution2.3 Å
Structure data

PDB-3frj:
Crystal Structure of 11b-Hydroxysteroid Dehydrogenase-1 (11b-HSD1) in Complex with Piperidyl Benzamide Inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.3 Å

Chemicals

ChemComp-NAP:
NADP NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE

ChemComp-A49:
N-{1-[(1-carbamoylcyclopropyl)methyl]piperidin-4-yl}-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsOXIDOREDUCTASE / Endoplasmic reticulum / Glycoprotein / Lipid metabolism / Membrane / NADP / Polymorphism / Signal-anchor / Steroid metabolism / Transmembrane

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