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1ya4

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{{STRUCTURE_1ya4| PDB=1ya4 | SCENE= }}
{{STRUCTURE_1ya4| PDB=1ya4 | SCENE= }}
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'''Crystal Structure of Human Liver Carboxylesterase 1 in complex with tamoxifen'''
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===Crystal Structure of Human Liver Carboxylesterase 1 in complex with tamoxifen===
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==Overview==
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Human carboxylesterase 1 (hCE1) exhibits broad substrate specificity and is involved in xenobiotic processing and endobiotic metabolism. We present and analyze crystal structures of hCE1 in complexes with the cholesterol-lowering drug mevastatin, the breast cancer drug tamoxifen, the fatty acyl ethyl ester (FAEE) analogue ethyl acetate, and the novel hCE1 inhibitor benzil. We find that mevastatin does not appear to be a substrate for hCE1, and instead acts as a partially non-competitive inhibitor of the enzyme. Similarly, we show that tamoxifen is a low micromolar, partially non-competitive inhibitor of hCE1. Further, we describe the structural basis for the inhibition of hCE1 by the nanomolar-affinity dione benzil, which acts by forming both covalent and non-covalent complexes with the enzyme. Our results provide detailed insights into the catalytic and non-catalytic processing of small molecules by hCE1, and suggest that the efficacy of clinical drugs may be modulated by targeted hCE1 inhibitors.
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(as it appears on PubMed at http://www.pubmed.gov), where 16081098 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16081098}}
==About this Structure==
==About this Structure==
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[[Category: Hydrolase domain]]
[[Category: Hydrolase domain]]
[[Category: Tamoxifen complex]]
[[Category: Tamoxifen complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:03:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:37:44 2008''

Revision as of 13:37, 28 July 2008

Image:1ya4.png

Template:STRUCTURE 1ya4

Crystal Structure of Human Liver Carboxylesterase 1 in complex with tamoxifen

Template:ABSTRACT PUBMED 16081098

About this Structure

1YA4 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural insights into drug processing by human carboxylesterase 1: tamoxifen, mevastatin, and inhibition by benzil., Fleming CD, Bencharit S, Edwards CC, Hyatt JL, Tsurkan L, Bai F, Fraga C, Morton CL, Howard-Williams EL, Potter PM, Redinbo MR, J Mol Biol. 2005 Sep 9;352(1):165-77. PMID:16081098

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