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3ddu
From Proteopedia
| 3ddu, resolution 1.56Å () | |||||||||
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| Sites: | , , , , , and | ||||||||
| Ligands: | , , | ||||||||
| Gene: | PREP, PEP (Homo sapiens) | ||||||||
| Activity: | Prolyl oligopeptidase, with EC number 3.4.21.26 | ||||||||
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
Prolyl Oligopeptidase with GSK552
We report the synthesis and in vitro activity of a series of novel pyrrolidinyl pyridones and pyrazinones as potent inhibitors of prolyl oligopeptidase (POP). Within this series, compound 39 was co-crystallized within the catalytic site of a human chimeric POP protein which provided a more detailed understanding of how these inhibitors interacted with the key residues within the catalytic pocket.
Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP)., Haffner CD, Diaz CJ, Miller AB, Reid RA, Madauss KP, Hassell A, Hanlon MH, Porter DJ, Becherer JD, Carter LH, Bioorg Med Chem Lett. 2008 Aug 1;18(15):4360-3. Epub 2008 Jun 24. PMID:18606544
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
3DDU is a 1 chain structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
- Haffner CD, Diaz CJ, Miller AB, Reid RA, Madauss KP, Hassell A, Hanlon MH, Porter DJ, Becherer JD, Carter LH. Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP). Bioorg Med Chem Lett. 2008 Aug 1;18(15):4360-3. Epub 2008 Jun 24. PMID:18606544 doi:10.1016/j.bmcl.2008.06.067
Page seeded by OCA on Mon Feb 16 14:41:08 2009
