Inhibition of yeast cytosine deaminase by 5-bromo-2-pyrimidinone and its covalent hydrate
Yeast cytosine deaminase (EC 3.5.4.1) is inhibited by 5‐bromo‐2‐pyrimidinone. In aqueous solution at neutral pH three forms of this compound (the anion, the parent, and the covalent hydrate) are in equilibrium. Experiments were undertaken in order to determine the relative contributions of these thr...
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Veröffentlicht in: | European journal of biochemistry 1986, Vol.156 (2), p.297-300 |
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description | Yeast cytosine deaminase (EC 3.5.4.1) is inhibited by 5‐bromo‐2‐pyrimidinone. In aqueous solution at neutral pH three forms of this compound (the anion, the parent, and the covalent hydrate) are in equilibrium. Experiments were undertaken in order to determine the relative contributions of these three forms to the observed inhibition. The anion makes little or no contribution. Both the parent and the covalent hydrate inhibit the enzyme, with the Ki for the hydrate being 0.2–0.02 times that of the parent. In the presence of stoichiometric concentrations of the enzyme, the equilibrium between parent and hydrate is displaced towards the hydrate; however, the hydration is not catalyzed by cytosine deaminase. |
doi_str_mv | 10.1111/j.1432-1033.1986.tb09581.x |
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In aqueous solution at neutral pH three forms of this compound (the anion, the parent, and the covalent hydrate) are in equilibrium. Experiments were undertaken in order to determine the relative contributions of these three forms to the observed inhibition. The anion makes little or no contribution. Both the parent and the covalent hydrate inhibit the enzyme, with the Ki for the hydrate being 0.2–0.02 times that of the parent. In the presence of stoichiometric concentrations of the enzyme, the equilibrium between parent and hydrate is displaced towards the hydrate; however, the hydration is not catalyzed by cytosine deaminase.</description><identifier>ISSN: 0014-2956</identifier><identifier>EISSN: 1432-1033</identifier><identifier>DOI: 10.1111/j.1432-1033.1986.tb09581.x</identifier><identifier>PMID: 3516692</identifier><identifier>CODEN: EJBCAI</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>5-bromo-2-pyrimidinone ; Applied sciences ; bakers yeast ; cytosine ; Cytosine Deaminase ; enzyme activity ; Exact sciences and technology ; Hydrogen-Ion Concentration ; inhibition ; Kinetics ; Nucleoside Deaminases - antagonists & inhibitors ; Other techniques and industries ; Pyrimidinones - pharmacology ; Saccharomyces cerevisiae ; Saccharomyces cerevisiae - enzymology</subject><ispartof>European journal of biochemistry, 1986, Vol.156 (2), p.297-300</ispartof><rights>1987 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4757-93efee1a05a4fbf09178ad6b753fcb259b9766d891202164fde14ee47899575d3</citedby><cites>FETCH-LOGICAL-c4757-93efee1a05a4fbf09178ad6b753fcb259b9766d891202164fde14ee47899575d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,777,781,4010,27904,27905,27906</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8108866$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3516692$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kornblatt, M.J</creatorcontrib><creatorcontrib>Tee, O.S</creatorcontrib><title>Inhibition of yeast cytosine deaminase by 5-bromo-2-pyrimidinone and its covalent hydrate</title><title>European journal of biochemistry</title><addtitle>Eur J Biochem</addtitle><description>Yeast cytosine deaminase (EC 3.5.4.1) is inhibited by 5‐bromo‐2‐pyrimidinone. In aqueous solution at neutral pH three forms of this compound (the anion, the parent, and the covalent hydrate) are in equilibrium. Experiments were undertaken in order to determine the relative contributions of these three forms to the observed inhibition. The anion makes little or no contribution. Both the parent and the covalent hydrate inhibit the enzyme, with the Ki for the hydrate being 0.2–0.02 times that of the parent. In the presence of stoichiometric concentrations of the enzyme, the equilibrium between parent and hydrate is displaced towards the hydrate; however, the hydration is not catalyzed by cytosine deaminase.</description><subject>5-bromo-2-pyrimidinone</subject><subject>Applied sciences</subject><subject>bakers yeast</subject><subject>cytosine</subject><subject>Cytosine Deaminase</subject><subject>enzyme activity</subject><subject>Exact sciences and technology</subject><subject>Hydrogen-Ion Concentration</subject><subject>inhibition</subject><subject>Kinetics</subject><subject>Nucleoside Deaminases - antagonists & inhibitors</subject><subject>Other techniques and industries</subject><subject>Pyrimidinones - pharmacology</subject><subject>Saccharomyces cerevisiae</subject><subject>Saccharomyces cerevisiae - enzymology</subject><issn>0014-2956</issn><issn>1432-1033</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1986</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVkU1v1DAQhi0EKtvCT0BECPWW4G_HXBBULVSqxKH0wMmykzH1KokXOwvNv8erjfaOLz7MM--MHyP0juCGlPNh2xDOaE0wYw3RrWxmh7VoSfP0DG1OpedogzHhNdVCvkTnOW8xxlJLdYbOmCBSarpBP2-nx-DCHOJURV8tYPNcdcscc5ig6sGOYbIZKrdUonYpjrGm9W5JYQx9mGJh7NRXYc5VF__YAaa5elz6ZGd4hV54O2R4vd4X6OHm-sfVt_ru-9fbq893dceVULVm4AGIxcJy7zzWRLW2l04J5jtHhXZaSdm3mlBMieS-B8IBuGq1Fkr07AJdHnN3Kf7eQ57NGHIHw2AniPtsCC9mWoEL-PEIdinmnMCbXXmGTYsh2By8mq05yDMHeebg1axezVNpfrNO2bsR-lPrKrLU3691mzs7-GSnLuQT1hLctlIW7NMR-xsGWP5jAXNz_eWealUS3h4TvI3G_kplyMM9xYSVrxZCcMr-AVU4njg</recordid><startdate>1986</startdate><enddate>1986</enddate><creator>Kornblatt, M.J</creator><creator>Tee, O.S</creator><general>Blackwell Publishing Ltd</general><general>Blackwell</general><scope>FBQ</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QL</scope><scope>C1K</scope><scope>M7N</scope></search><sort><creationdate>1986</creationdate><title>Inhibition of yeast cytosine deaminase by 5-bromo-2-pyrimidinone and its covalent hydrate</title><author>Kornblatt, M.J ; Tee, O.S</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4757-93efee1a05a4fbf09178ad6b753fcb259b9766d891202164fde14ee47899575d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1986</creationdate><topic>5-bromo-2-pyrimidinone</topic><topic>Applied sciences</topic><topic>bakers yeast</topic><topic>cytosine</topic><topic>Cytosine Deaminase</topic><topic>enzyme activity</topic><topic>Exact sciences and technology</topic><topic>Hydrogen-Ion Concentration</topic><topic>inhibition</topic><topic>Kinetics</topic><topic>Nucleoside Deaminases - antagonists & inhibitors</topic><topic>Other techniques and industries</topic><topic>Pyrimidinones - pharmacology</topic><topic>Saccharomyces cerevisiae</topic><topic>Saccharomyces cerevisiae - enzymology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kornblatt, M.J</creatorcontrib><creatorcontrib>Tee, O.S</creatorcontrib><collection>AGRIS</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><jtitle>European journal of biochemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kornblatt, M.J</au><au>Tee, O.S</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibition of yeast cytosine deaminase by 5-bromo-2-pyrimidinone and its covalent hydrate</atitle><jtitle>European journal of biochemistry</jtitle><addtitle>Eur J Biochem</addtitle><date>1986</date><risdate>1986</risdate><volume>156</volume><issue>2</issue><spage>297</spage><epage>300</epage><pages>297-300</pages><issn>0014-2956</issn><eissn>1432-1033</eissn><coden>EJBCAI</coden><abstract>Yeast cytosine deaminase (EC 3.5.4.1) is inhibited by 5‐bromo‐2‐pyrimidinone. In aqueous solution at neutral pH three forms of this compound (the anion, the parent, and the covalent hydrate) are in equilibrium. Experiments were undertaken in order to determine the relative contributions of these three forms to the observed inhibition. The anion makes little or no contribution. Both the parent and the covalent hydrate inhibit the enzyme, with the Ki for the hydrate being 0.2–0.02 times that of the parent. In the presence of stoichiometric concentrations of the enzyme, the equilibrium between parent and hydrate is displaced towards the hydrate; however, the hydration is not catalyzed by cytosine deaminase.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>3516692</pmid><doi>10.1111/j.1432-1033.1986.tb09581.x</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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subjects | 5-bromo-2-pyrimidinone Applied sciences bakers yeast cytosine Cytosine Deaminase enzyme activity Exact sciences and technology Hydrogen-Ion Concentration inhibition Kinetics Nucleoside Deaminases - antagonists & inhibitors Other techniques and industries Pyrimidinones - pharmacology Saccharomyces cerevisiae Saccharomyces cerevisiae - enzymology |
title | Inhibition of yeast cytosine deaminase by 5-bromo-2-pyrimidinone and its covalent hydrate |
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