Identification and development of mPGES-1 inhibitors: where we are at?
Microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal synthase responsible for the synthesis of the pro-tumorigenic prostaglandin E(2) (PGE(2)). mPGES-1 is overexpressed in a wide variety of cancers. Since its discovery in 1997 by Bengt Samuelsson and collaborators, the enzyme has been the...
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Published in | Future medicinal chemistry Vol. 3; no. 15; p. 1909 |
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Main Authors | , |
Format | Journal Article |
Language | English |
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England
01.11.2011
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Abstract | Microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal synthase responsible for the synthesis of the pro-tumorigenic prostaglandin E(2) (PGE(2)). mPGES-1 is overexpressed in a wide variety of cancers. Since its discovery in 1997 by Bengt Samuelsson and collaborators, the enzyme has been the object of over 200 peer-reviewed articles. Although today mPGES-1 is considered a validated and promising therapeutic target for anticancer drug discovery, challenges in inhibitor design and selectivity are such that up to this date there are only a few published records of small-molecule inhibitors targeting the enzyme and exhibiting some in vivo anticancer activity. This review summarizes the structures, and the in vitro and in vivo activities of these novel mPGES-1 inhibitors. Challenges that have been encountered are also discussed. |
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AbstractList | Microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal synthase responsible for the synthesis of the pro-tumorigenic prostaglandin E(2) (PGE(2)). mPGES-1 is overexpressed in a wide variety of cancers. Since its discovery in 1997 by Bengt Samuelsson and collaborators, the enzyme has been the object of over 200 peer-reviewed articles. Although today mPGES-1 is considered a validated and promising therapeutic target for anticancer drug discovery, challenges in inhibitor design and selectivity are such that up to this date there are only a few published records of small-molecule inhibitors targeting the enzyme and exhibiting some in vivo anticancer activity. This review summarizes the structures, and the in vitro and in vivo activities of these novel mPGES-1 inhibitors. Challenges that have been encountered are also discussed. |
Author | Meuillet, Emmanuelle J Chang, Hui-Hua |
Author_xml | – sequence: 1 givenname: Hui-Hua surname: Chang fullname: Chang, Hui-Hua organization: Arizona Cancer Center, University of Arizona, Tucson, AZ 85724, USA – sequence: 2 givenname: Emmanuelle J surname: Meuillet fullname: Meuillet, Emmanuelle J |
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SubjectTerms | Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Intramolecular Oxidoreductases - antagonists & inhibitors Intramolecular Oxidoreductases - chemistry Intramolecular Oxidoreductases - metabolism Microsomes - enzymology Models, Molecular Neoplasms - drug therapy Neoplasms - enzymology Prostaglandin-E Synthases Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology |
Title | Identification and development of mPGES-1 inhibitors: where we are at? |
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