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dc.contributorWichita State University. Department of Chemistryen_US
dc.contributor.authorGroutas, William C.en_US
dc.contributor.authorVenkataraman, Radhikaen_US
dc.contributor.authorBrubaker, Michael J.en_US
dc.contributor.authorStanga, Michael A.en_US
dc.date.accessioned2012-02-06T17:17:25Z
dc.date.available2012-02-06T17:17:25Z
dc.date.issued1991-04-30en_US
dc.identifier2021604en_US
dc.identifier0370623en_US
dc.identifierHL 38048en_US
dc.identifier.citationBiochemistry. 1991 Apr 30; 30(17): 4132-6.en_US
dc.identifier.issn0006-2960en_US
dc.identifier.urihttp://hdl.handle.net/10057/4421
dc.descriptionFull text of this article is not available in SOAR.en_US
dc.description.abstractA series of phosphate esters derived from N-hydroxysuccinimide and 3-alkyl-N-hydroxysuccinimide have been synthesized and found to be potent time-dependent irreversible inhibitors of human leukocyte elastase (HLE). The observed inhibitory activity in this series of compounds correlated well with the known preference of HLE for substrates with small hydrophobic side chains. Maximum potency was reached when a favorable aromatic interaction involving a phenyl group present in the inhibitor and an aromatic residue located in the vicinity of the S2' subsite was operative. 31P NMR spectroscopy was used to probe the mechanism of action of these compounds. Direct evidence is presented in support of a mechanism involving phosphorylation of the active site serine. These compounds constitute a new class of hydrolytically stable phosphorylating agents.en_US
dc.description.sponsorshipNHLBI NIH HHSen_US
dc.format.extent4132-6en_US
dc.language.isoengen_US
dc.publisherAmerican Chemical Societyen_US
dc.relation.ispartofseriesBiochemistryen_US
dc.sourceNLMen_US
dc.subjectResearch Support, U.S. Gov't, P.H.S.en_US
dc.subject.lcshEsters/pharmacologyen_US
dc.subject.lcshPancreatic Elastase/metabolismen_US
dc.subject.lcshPhosphates/pharmacologyen_US
dc.subject.lcshSuccinimides/pharmacologyen_US
dc.subject.meshBinding Sitesen_US
dc.subject.meshChymotrypsin/antagonists & inhibitorsen_US
dc.subject.meshEsters/chemistryen_US
dc.subject.meshHumansen_US
dc.subject.meshKineticsen_US
dc.subject.meshLeukocyte Elastaseen_US
dc.subject.meshMagnetic Resonance Spectroscopyen_US
dc.subject.meshPancreatic Elastase/antagonists & inhibitorsen_US
dc.subject.meshPhosphates/chemistryen_US
dc.subject.meshPhosphorylationen_US
dc.subject.meshSerine Proteinase Inhibitorsen_US
dc.subject.meshSubstrate Specificityen_US
dc.subject.meshSuccinimides/chemistryen_US
dc.titleInhibition of human leukocyte elastase by phosphate esters of N-hydroxysuccinimide and its derivatives: direct observation of a phosphorylated enzyme by 31P nuclear magnetic resonance spectroscopyen_US
dc.typeArticleen_US
dc.coverage.spacialUnited Statesen_US
dc.description.versionpeer revieweden_US
dc.rights.holderCopyright © 1991 American Chemical Societyen_US


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