Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1

The inducible enzyme microsomal prostaglandin E synthase 1 (MPGES1) is a glutathione-dependent prostaglandin H2 isomerase that has been implicated in a variety of inflammatory diseases and several forms of cancer. While there are currently no available drugs that selectively inhibit its activity, M...

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Main Author:	Prage, Edward B
Other Authors:	Richard N Armstrong
Format:	Others
Language:	en
Published:	VANDERBILT 2012
Subjects:	Chemistry
Online Access:	http://etd.library.vanderbilt.edu/available/etd-02202012-105424/

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spelling	ndltd-VANDERBILT-oai-VANDERBILTETD-etd-02202012-1054242013-01-08T17:16:50Z Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1 Prage, Edward B Chemistry The inducible enzyme microsomal prostaglandin E synthase 1 (MPGES1) is a glutathione-dependent prostaglandin H2 isomerase that has been implicated in a variety of inflammatory diseases and several forms of cancer. While there are currently no available drugs that selectively inhibit its activity, MPGES1 represents a promising therapeutic target. The aim of the research described here is to analyze the structural implications of the interaction of MPGES1 with different types of inhibitors. The structural dynamics determination technique hydrogen/deuterium exchange mass spectrometry was utilized to locate spatially distinct inhibitor binding sites within the enzyme. The method was also used, coupled with biochemical techniques, to defined the modes of inhibition of MPGES1 by the cyclopentenone 15-deoxy-Δ12,14-prostaglandin J2. Richard N Armstrong VANDERBILT 2012-02-21 text application/pdf http://etd.library.vanderbilt.edu/available/etd-02202012-105424/ http://etd.library.vanderbilt.edu/available/etd-02202012-105424/ en unrestricted I hereby certify that, if appropriate, I have obtained and attached hereto a written permission statement from the owner(s) of each third party copyrighted matter to be included in my thesis, dissertation, or project report, allowing distribution as specified below. I certify that the version I submitted is the same as that approved by my advisory committee. I hereby grant to Vanderbilt University or its agents the non-exclusive license to archive and make accessible, under the conditions specified below, my thesis, dissertation, or project report in whole or in part in all forms of media, now or hereafter known. I retain all other ownership rights to the copyright of the thesis, dissertation or project report. I also retain the right to use in future works (such as articles or books) all or part of this thesis, dissertation, or project report.
collection	NDLTD
language	en
format	Others
sources	NDLTD
topic	Chemistry
spellingShingle	Chemistry Prage, Edward B Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1
description	The inducible enzyme microsomal prostaglandin E synthase 1 (MPGES1) is a glutathione-dependent prostaglandin H2 isomerase that has been implicated in a variety of inflammatory diseases and several forms of cancer. While there are currently no available drugs that selectively inhibit its activity, MPGES1 represents a promising therapeutic target. The aim of the research described here is to analyze the structural implications of the interaction of MPGES1 with different types of inhibitors. The structural dynamics determination technique hydrogen/deuterium exchange mass spectrometry was utilized to locate spatially distinct inhibitor binding sites within the enzyme. The method was also used, coupled with biochemical techniques, to defined the modes of inhibition of MPGES1 by the cyclopentenone 15-deoxy-Δ12,14-prostaglandin J2.
author2	Richard N Armstrong
author_facet	Richard N Armstrong Prage, Edward B
author	Prage, Edward B
author_sort	Prage, Edward B
title	Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1
title_short	Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1
title_full	Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1
title_fullStr	Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1
title_full_unstemmed	Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1
title_sort	structural studies of inhibition of the human inducible prostaglandin e synthase mpges1
publisher	VANDERBILT
publishDate	2012
url	http://etd.library.vanderbilt.edu/available/etd-02202012-105424/
work_keys_str_mv	AT prageedwardb structuralstudiesofinhibitionofthehumaninducibleprostaglandinesynthasempges1
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Structural Studies of Inhibition of the Human Inducible Prostaglandin E Synthase MPGES1

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