2jbk: Difference between revisions
No edit summary |
No edit summary |
||
| Line 4: | Line 4: | ||
==Overview== | ==Overview== | ||
Human glutamate carboxypeptidase II (GCPII) occurs in the central nervous | Human glutamate carboxypeptidase II (GCPII) occurs in the central nervous system as well as in human prostate (where it is called prostate-specific membrane antigen; PSMA). Inhibitors of the enzyme have been shown to provide neuroprotection, but may also be useful for the detection, imaging and treatment of prostate cancer. Crystal structures were determined of the extracellular part of GCPII (amino-acid residues 44-750) in complex with two potent inhibitors, quisqualate and 2-PMPA (the strongest GCPII inhibitor to date), at resolutions of 3.0 and 2.2 A, respectively. In addition, models were constructed for binding of the inhibitors willardiine, homoibotenate, L-2-amino-4-phosphonobutanoic acid and L-serine-O-sulfate to the S1' site of the enzyme. The common denominator for high-affinity binding to the S1' site is the formation of two strong salt bridges. | ||
==Disease== | ==Disease== | ||
| Line 19: | Line 19: | ||
[[Category: Henning, K.]] | [[Category: Henning, K.]] | ||
[[Category: Hilgenfeld, R.]] | [[Category: Hilgenfeld, R.]] | ||
[[Category: Mesters, J | [[Category: Mesters, J R.]] | ||
[[Category: CA]] | [[Category: CA]] | ||
[[Category: CL]] | [[Category: CL]] | ||
| Line 46: | Line 46: | ||
[[Category: zinc]] | [[Category: zinc]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:01:22 2008'' | ||
Revision as of 19:01, 21 February 2008
|
MEMBRANE-BOUND GLUTAMATE CARBOXYPEPTIDASE II (GCPII) IN COMPLEX WITH QUISQUALIC ACID (QUISQUALATE, ALPHA-AMINO-3,5-DIOXO-1,2,4-OXADIAZOLIDINE-2-PROPANOIC ACID)
OverviewOverview
Human glutamate carboxypeptidase II (GCPII) occurs in the central nervous system as well as in human prostate (where it is called prostate-specific membrane antigen; PSMA). Inhibitors of the enzyme have been shown to provide neuroprotection, but may also be useful for the detection, imaging and treatment of prostate cancer. Crystal structures were determined of the extracellular part of GCPII (amino-acid residues 44-750) in complex with two potent inhibitors, quisqualate and 2-PMPA (the strongest GCPII inhibitor to date), at resolutions of 3.0 and 2.2 A, respectively. In addition, models were constructed for binding of the inhibitors willardiine, homoibotenate, L-2-amino-4-phosphonobutanoic acid and L-serine-O-sulfate to the S1' site of the enzyme. The common denominator for high-affinity binding to the S1' site is the formation of two strong salt bridges.
DiseaseDisease
Known diseases associated with this structure: Myocardial infarcation, susceptibility to OMIM:[602855]
About this StructureAbout this Structure
2JBK is a Single protein structure of sequence from Homo sapiens with , , , and as ligands. Active as Glutamate carboxypeptidase II, with EC number 3.4.17.21 Known structural/functional Sites: , , , , , , , , , , , , , , and . Full crystallographic information is available from OCA.
ReferenceReference
Human glutamate carboxypeptidase II inhibition: structures of GCPII in complex with two potent inhibitors, quisqualate and 2-PMPA., Mesters JR, Henning K, Hilgenfeld R, Acta Crystallogr D Biol Crystallogr. 2007 Apr;63(Pt 4):508-13. Epub 2007, Mar 16. PMID:17372356
Page seeded by OCA on Thu Feb 21 18:01:22 2008
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Glutamate carboxypeptidase II
- Homo sapiens
- Single protein
- Henning, K.
- Hilgenfeld, R.
- Mesters, J R.
- CA
- CL
- NAG
- QUS
- ZN
- Antigen
- Carboxypeptidase
- Dipeptidase
- Glycoprotein
- Hydrolase
- Membrane
- Metal- binding
- Metal-binding
- Metalloprotease
- Multifunctional enzyme
- Naaladase
- Neurodegenerative disease
- Peptidase
- Polymorphism
- Prostate cancer
- Protease
- Psma
- Signal-anchor
- Transmembrane
- Zinc