1lyb
From Proteopedia
(New page: 200px<br /> <applet load="1lyb" size="450" color="white" frame="true" align="right" spinBox="true" caption="1lyb, resolution 2.5Å" /> '''CRYSTAL STRUCTURES O...) |
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| - | [[Image:1lyb. | + | [[Image:1lyb.jpg|left|200px]]<br /><applet load="1lyb" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1lyb, resolution 2.5Å" /> | caption="1lyb, resolution 2.5Å" /> | ||
'''CRYSTAL STRUCTURES OF NATIVE AND INHIBITED FORMS OF HUMAN CATHEPSIN D: IMPLICATIONS FOR LYSOSOMAL TARGETING AND DRUG DESIGN'''<br /> | '''CRYSTAL STRUCTURES OF NATIVE AND INHIBITED FORMS OF HUMAN CATHEPSIN D: IMPLICATIONS FOR LYSOSOMAL TARGETING AND DRUG DESIGN'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1LYB is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NAG as [http://en.wikipedia.org/wiki/ligand ligand]. The following page contains interesting information on the relation of 1LYB with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb12_1.html Pepsin]]. Active as [http://en.wikipedia.org/wiki/Cathepsin_D Cathepsin D], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.5 3.4.23.5] Full crystallographic information is available from [http:// | + | 1LYB is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NAG:'>NAG</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. The following page contains interesting information on the relation of 1LYB with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb12_1.html Pepsin]]. Active as [http://en.wikipedia.org/wiki/Cathepsin_D Cathepsin D], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.5 3.4.23.5] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1LYB OCA]. |
==Reference== | ==Reference== | ||
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[[Category: lysosomal aspartic protease]] | [[Category: lysosomal aspartic protease]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:21:12 2008'' |
Revision as of 14:21, 15 February 2008
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CRYSTAL STRUCTURES OF NATIVE AND INHIBITED FORMS OF HUMAN CATHEPSIN D: IMPLICATIONS FOR LYSOSOMAL TARGETING AND DRUG DESIGN
Contents |
Overview
Cathepsin D (EC 3.4.23.5) is a lysosomal protease suspected to play, important roles in protein catabolism, antigen processing, degenerative, diseases, and breast cancer progression. Determination of the crystal, structures of cathepsin D and a complex with pepstatin at 2.5 A resolution, provides insights into inhibitor binding and lysosomal targeting for this, two-chain, N-glycosylated aspartic protease. Comparison with the, structures of a complex of pepstatin bound to rhizopuspepsin and with a, human renin-inhibitor complex revealed differences in subsite structures, and inhibitor-enzyme interactions that are consistent with affinity, differences and structure-activity relationships and suggest strategies, for fine-tuning the specificity of cathepsin D inhibitors. Mutagenesis, studies have identified a phosphotransferase recognition region that is, required for oligosaccharide phosphorylation but is 32 A distant from the, N-domain glycosylation site at Asn-70. Electron density for the crystal, structure of cathepsin D indicated the presence of an N-linked, oligosaccharide that extends from Asn-70 toward Lys-203, which is a key, component of the phosphotransferase recognition region, and thus provides, a structural explanation for how the phosphotransferase can recognize, apparently distant sites on the protein surface.
Disease
Known diseases associated with this structure: Ceroid lipofuscinosis, neuronal, 10 OMIM:[116840]
About this Structure
1LYB is a Single protein structure of sequence from Homo sapiens with as ligand. The following page contains interesting information on the relation of 1LYB with [Pepsin]. Active as Cathepsin D, with EC number 3.4.23.5 Full crystallographic information is available from OCA.
Reference
Crystal structures of native and inhibited forms of human cathepsin D: implications for lysosomal targeting and drug design., Baldwin ET, Bhat TN, Gulnik S, Hosur MV, Sowder RC 2nd, Cachau RE, Collins J, Silva AM, Erickson JW, Proc Natl Acad Sci U S A. 1993 Jul 15;90(14):6796-800. PMID:8393577
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