2jbj
From Proteopedia
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|PDB= 2jbj |SIZE=350|CAPTION= <scene name='initialview01'>2jbj</scene>, resolution 2.19Å | |PDB= 2jbj |SIZE=350|CAPTION= <scene name='initialview01'>2jbj</scene>, resolution 2.19Å | ||
|SITE= <scene name='pdbsite=AC1:Zn+Binding+Site+For+Chain+A'>AC1</scene>, <scene name='pdbsite=AC2:Zn+Binding+Site+For+Chain+A'>AC2</scene>, <scene name='pdbsite=AC3:Ca+Binding+Site+For+Chain+A'>AC3</scene>, <scene name='pdbsite=AC4:Cl+Binding+Site+For+Chain+A'>AC4</scene>, <scene name='pdbsite=AC5:Nag+Binding+Site+For+Chain+A'>AC5</scene>, <scene name='pdbsite=AC6:Nag+Binding+Site+For+Chain+A'>AC6</scene>, <scene name='pdbsite=AC7:Nag+Binding+Site+For+Chain+A'>AC7</scene>, <scene name='pdbsite=AC8:Nag+Binding+Site+For+Chain+A'>AC8</scene>, <scene name='pdbsite=BC1:Nag+Binding+Site+For+Chain+A'>BC1</scene>, <scene name='pdbsite=BC2:Nag+Binding+Site+For+Chain+A'>BC2</scene>, <scene name='pdbsite=BC3:Nag+Binding+Site+For+Chain+A'>BC3</scene>, <scene name='pdbsite=BC4:Nag+Binding+Site+For+Chain+A'>BC4</scene>, <scene name='pdbsite=BC5:Nag+Binding+Site+For+Chain+A'>BC5</scene>, <scene name='pdbsite=BC6:Nag+Binding+Site+For+Chain+A'>BC6</scene>, <scene name='pdbsite=BC7:Bma+Binding+Site+For+Chain+A'>BC7</scene>, <scene name='pdbsite=BC8:Man+Binding+Site+For+Chain+A'>BC8</scene> and <scene name='pdbsite=BC9:G88+Binding+Site+For+Chain+A'>BC9</scene> | |SITE= <scene name='pdbsite=AC1:Zn+Binding+Site+For+Chain+A'>AC1</scene>, <scene name='pdbsite=AC2:Zn+Binding+Site+For+Chain+A'>AC2</scene>, <scene name='pdbsite=AC3:Ca+Binding+Site+For+Chain+A'>AC3</scene>, <scene name='pdbsite=AC4:Cl+Binding+Site+For+Chain+A'>AC4</scene>, <scene name='pdbsite=AC5:Nag+Binding+Site+For+Chain+A'>AC5</scene>, <scene name='pdbsite=AC6:Nag+Binding+Site+For+Chain+A'>AC6</scene>, <scene name='pdbsite=AC7:Nag+Binding+Site+For+Chain+A'>AC7</scene>, <scene name='pdbsite=AC8:Nag+Binding+Site+For+Chain+A'>AC8</scene>, <scene name='pdbsite=BC1:Nag+Binding+Site+For+Chain+A'>BC1</scene>, <scene name='pdbsite=BC2:Nag+Binding+Site+For+Chain+A'>BC2</scene>, <scene name='pdbsite=BC3:Nag+Binding+Site+For+Chain+A'>BC3</scene>, <scene name='pdbsite=BC4:Nag+Binding+Site+For+Chain+A'>BC4</scene>, <scene name='pdbsite=BC5:Nag+Binding+Site+For+Chain+A'>BC5</scene>, <scene name='pdbsite=BC6:Nag+Binding+Site+For+Chain+A'>BC6</scene>, <scene name='pdbsite=BC7:Bma+Binding+Site+For+Chain+A'>BC7</scene>, <scene name='pdbsite=BC8:Man+Binding+Site+For+Chain+A'>BC8</scene> and <scene name='pdbsite=BC9:G88+Binding+Site+For+Chain+A'>BC9</scene> | ||
| - | |LIGAND= <scene name='pdbligand= | + | |LIGAND= <scene name='pdbligand=BMA:BETA-D-MANNOSE'>BMA</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=G88:(2S)-2-(PHOSPHONOMETHYL)PENTANEDIOIC+ACID'>G88</scene>, <scene name='pdbligand=MAN:ALPHA-D-MANNOSE'>MAN</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> |
| - | |ACTIVITY= [http://en.wikipedia.org/wiki/Glutamate_carboxypeptidase_II Glutamate carboxypeptidase II], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.17.21 3.4.17.21] | + | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Glutamate_carboxypeptidase_II Glutamate carboxypeptidase II], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.17.21 3.4.17.21] </span> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1z8l|1Z8L]], [[2c6c|2C6C]], [[2c6g|2C6G]], [[2c6p|2C6P]], [[2cij|2CIJ]], [[2jbk|2JBK]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2jbj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2jbj OCA], [http://www.ebi.ac.uk/pdbsum/2jbj PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2jbj RCSB]</span> | ||
}} | }} | ||
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==Overview== | ==Overview== | ||
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. | 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== | ||
| - | Known diseases associated with this structure: Myocardial infarcation, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=602855 602855]] | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Hilgenfeld, R.]] | [[Category: Hilgenfeld, R.]] | ||
[[Category: Mesters, J R.]] | [[Category: Mesters, J R.]] | ||
| - | [[Category: CA]] | ||
| - | [[Category: CL]] | ||
| - | [[Category: G88]] | ||
| - | [[Category: NAG]] | ||
| - | [[Category: ZN]] | ||
[[Category: alternative splicin]] | [[Category: alternative splicin]] | ||
[[Category: alternative splicing]] | [[Category: alternative splicing]] | ||
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[[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 Mon Mar 31 03:55:46 2008'' |
Revision as of 00:55, 31 March 2008
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| , resolution 2.19Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | , , , , , , , , , , , , , , , and | ||||||
| Ligands: | , , , , , , | ||||||
| Activity: | Glutamate carboxypeptidase II, with EC number 3.4.17.21 | ||||||
| Related: | 1Z8L, 2C6C, 2C6G, 2C6P, 2CIJ, 2JBK
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
MEMBRANE-BOUND GLUTAMATE CARBOXYPEPTIDASE II (GCPII) IN COMPLEX WITH 2-PMPA (2-PHOSPHONOMETHYL-PENTANEDIOIC ACID)
Overview
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.
About this Structure
2JBJ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
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 Mon Mar 31 03:55:46 2008
Categories: Glutamate carboxypeptidase II | Homo sapiens | Single protein | Henning, K. | Hilgenfeld, R. | Mesters, J R. | Alternative splicin | Alternative splicing | 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
