1k4y

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:1k4y.gif|left|200px]]
[[Image:1k4y.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 1k4y |SIZE=350|CAPTION= <scene name='initialview01'>1k4y</scene>, resolution 2.50&Aring;
+
The line below this paragraph, containing "STRUCTURE_1k4y", creates the "Structure Box" on the page.
-
|SITE=
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=4PN:4-PIPERIDINO-PIPERIDINE'>4PN</scene>, <scene name='pdbligand=MAN:ALPHA-D-MANNOSE'>MAN</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Carboxylesterase Carboxylesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.1.1 3.1.1.1] </span>
+
or leave the SCENE parameter empty for the default display.
-
|GENE=
+
-->
-
|DOMAIN=
+
{{STRUCTURE_1k4y| PDB=1k4y | SCENE= }}
-
|RELATEDENTRY=
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1k4y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1k4y OCA], [http://www.ebi.ac.uk/pdbsum/1k4y PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1k4y RCSB]</span>
+
-
}}
+
'''Crystal Structure of Rabbit Liver Carboxylesterase in Complex with 4-piperidino-piperidine'''
'''Crystal Structure of Rabbit Liver Carboxylesterase in Complex with 4-piperidino-piperidine'''
Line 32: Line 29:
[[Category: Potter, P M.]]
[[Category: Potter, P M.]]
[[Category: Redinbo, M R.]]
[[Category: Redinbo, M R.]]
-
[[Category: camptothecin]]
+
[[Category: Camptothecin]]
-
[[Category: esterase]]
+
[[Category: Esterase]]
-
[[Category: hydrolase]]
+
[[Category: Hydrolase]]
-
[[Category: irinotecan]]
+
[[Category: Irinotecan]]
-
[[Category: side door]]
+
[[Category: Side door]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 22:18:55 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:43:30 2008''
+

Revision as of 19:18, 2 May 2008

Image:1k4y.gif

Template:STRUCTURE 1k4y

Crystal Structure of Rabbit Liver Carboxylesterase in Complex with 4-piperidino-piperidine


Overview

Mammalian carboxylesterases cleave the anticancer prodrug CPT-11 (Irinotecan) into SN-38, a potent topoisomerase I poison, and 4-piperidino-piperidine (4PP). We present the 2.5 A crystal structure of rabbit liver carboxylesterase (rCE), the most efficient enzyme known to activate CPT-11 in this manner, in complex with the leaving group 4PP. 4PP is observed bound adjacent to a high-mannose Asn-linked glycosylation site on the surface of rCE. This product-binding site is separated from the catalytic gorge by a thin wall of amino acid side chains, suggesting that 4PP may be released through this secondary product exit pore. The crystallographic observation of a leaving group bound on the surface of rCE supports the 'back door' product exit site proposed for the acetylcholinesterases. These results may facilitate the design of improved anticancer drugs or enzymes for use in viral-directed cancer cotherapies.

About this Structure

1K4Y is a Single protein structure of sequence from Oryctolagus cuniculus. Full crystallographic information is available from OCA.

Reference

Structural insights into CPT-11 activation by mammalian carboxylesterases., Bencharit S, Morton CL, Howard-Williams EL, Danks MK, Potter PM, Redinbo MR, Nat Struct Biol. 2002 May;9(5):337-42. PMID:11967565 Page seeded by OCA on Fri May 2 22:18:55 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1k4y"
Personal tools