1elb
From Proteopedia
(New page: 200px<br /><applet load="1elb" size="450" color="white" frame="true" align="right" spinBox="true" caption="1elb, resolution 2.1Å" /> '''ANALOGOUS INHIBITORS ...) |
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| - | [[Image:1elb.gif|left|200px]]<br /><applet load="1elb" size=" | + | [[Image:1elb.gif|left|200px]]<br /><applet load="1elb" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1elb, resolution 2.1Å" /> | caption="1elb, resolution 2.1Å" /> | ||
'''ANALOGOUS INHIBITORS OF ELASTASE DO NOT ALWAYS BIND ANALOGOUSLY'''<br /> | '''ANALOGOUS INHIBITORS OF ELASTASE DO NOT ALWAYS BIND ANALOGOUSLY'''<br /> | ||
==Overview== | ==Overview== | ||
| - | It has been assumed that the structure of a single inhibitor complex is | + | It has been assumed that the structure of a single inhibitor complex is sufficient to define the available subsites of an enzyme that has a unique binding site and a uniquely defined mode for ligand binding--the specificity for these subsites can thus be probed by kinetic experiments. Elastase is an enzyme for which these traditional assumptions, which underlie such structural and kinetic studies, do not hold. Three new crystal structures of elastase complexed to chemically similar inhibitors with similar binding affinities reveal a diversity of binding modes as well as two new subsites on elastase. The existence of multiple binding sites and different binding modes for such similar inhibitors indicates that researchers must proceed with caution when using kinetics to map out protein subsites. |
==About this Structure== | ==About this Structure== | ||
| - | 1ELB is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa] with CA and SO4 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Pancreatic_elastase Pancreatic elastase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.36 3.4.21.36] Full crystallographic information is available from [http:// | + | 1ELB is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa] with <scene name='pdbligand=CA:'>CA</scene> and <scene name='pdbligand=SO4:'>SO4</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Pancreatic_elastase Pancreatic elastase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.36 3.4.21.36] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1ELB OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Ding, X.]] | [[Category: Ding, X.]] | ||
[[Category: Mattos, C.]] | [[Category: Mattos, C.]] | ||
| - | [[Category: Petsko, G | + | [[Category: Petsko, G A.]] |
[[Category: Rasmussen, B.]] | [[Category: Rasmussen, B.]] | ||
[[Category: Ringe, D.]] | [[Category: Ringe, D.]] | ||
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[[Category: hydrolase(serine proteinase)]] | [[Category: hydrolase(serine proteinase)]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:28:55 2008'' |
Revision as of 10:28, 21 February 2008
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ANALOGOUS INHIBITORS OF ELASTASE DO NOT ALWAYS BIND ANALOGOUSLY
Overview
It has been assumed that the structure of a single inhibitor complex is sufficient to define the available subsites of an enzyme that has a unique binding site and a uniquely defined mode for ligand binding--the specificity for these subsites can thus be probed by kinetic experiments. Elastase is an enzyme for which these traditional assumptions, which underlie such structural and kinetic studies, do not hold. Three new crystal structures of elastase complexed to chemically similar inhibitors with similar binding affinities reveal a diversity of binding modes as well as two new subsites on elastase. The existence of multiple binding sites and different binding modes for such similar inhibitors indicates that researchers must proceed with caution when using kinetics to map out protein subsites.
About this Structure
1ELB is a Single protein structure of sequence from Sus scrofa with and as ligands. Active as Pancreatic elastase, with EC number 3.4.21.36 Full crystallographic information is available from OCA.
Reference
Analogous inhibitors of elastase do not always bind analogously., Mattos C, Rasmussen B, Ding X, Petsko GA, Ringe D, Nat Struct Biol. 1994 Jan;1(1):55-8. PMID:7656008
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