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1Potent, Rationally Designed Inhibitors of Squalene Synthase

SA BILLER,MJ SOFIA,JW ABT,B DELANGE,JK DICKSON,C FORSTER,EM GORDON,T HARRITY,DR MAGNIN,J MARRETTA,LC RICH,CP CIOSEK

The first class of potent inhibitors of squalene synthase is described. The lead inhibitor, ether 10, was discovered as a result of rational design on the basis of a proposed mechanism for the enzymatic reaction. The ether oxygen was positioned to hydrogen bond with a putative active site acid catalyst and was found to make a substantial contribution to the inhibitor-enzyme binding energy. The structural requirements for potent inhibition are discussed.

1992REGULATION OF ISOPENTENOID METABOLISM引用：7

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2The First Potent Inhibitor of Squalene Synthase: a Profound Contribution of an Ether Oxygen to Inhibitor-Enzyme Interaction

SA BILLER,MJ SOFIA,B DELANGE,C FORSTER,EM GORDON,T HARRITY,LC RICH,CP CIOSEK

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTThe first potent inhibitor of squalene synthase: a profound contribution of an ether oxygen to inhibitor-enzyme interactionScott A. Biller, Michael J. Sofia, Barbara DeLange, Cornelia Forster, Eric M. Gordon, Thomas Harrity, Lois C. Rich, and Carl P. Ciosek Jr.Cite this: J. Am. Chem. Soc. 1991, 113, 22, 8522–8524Publication Date (Print):October 1, 1991Publication History Published online1 May 2002Published inissue 1 October 1991https://pubs.acs.org/doi/10.1021/ja00022a050https://doi.org/10.1021/ja00022a050research-articleACS PublicationsRequest reuse permissionsArticle Views168Altmetric-Citations62LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts

1991Journal of the American Chemical Society（1991）引用：102

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3Phosphorus-Containing Inhibitors of Hmg-Coa Reductase .1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxybutanoic Acids - A New Class of Cell-Selective Inhibitors of Cholesterol-Biosynthesis

DS KARANEWSKY,MC BADIA,CP CIOSEK,JA ROBL,MJ SOFIA,LM SIMPKINS,B DELANGE,TW HARRITY,SA BILLER,EM GORDON

AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

1991ChemInform（1991）引用：4

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4Inhibitors Of Squalene Synthetase