2023
Design, synthesis, and biological testing of biphenylmethyloxazole inhibitors targeting HIV-1 reverse transcriptase
Carter Z, Hollander K, Spasov K, Anderson K, Jorgensen W. Design, synthesis, and biological testing of biphenylmethyloxazole inhibitors targeting HIV-1 reverse transcriptase. Bioorganic & Medicinal Chemistry Letters 2023, 84: 129216. PMID: 36871704, PMCID: PMC10278203, DOI: 10.1016/j.bmcl.2023.129216.Peer-Reviewed Original Research
2013
Quantitative full time course analysis of nonlinear enzyme cycling kinetics
Cao W, De La Cruz EM. Quantitative full time course analysis of nonlinear enzyme cycling kinetics. Scientific Reports 2013, 3: 2658. PMID: 24029878, PMCID: PMC3772379, DOI: 10.1038/srep02658.Peer-Reviewed Original ResearchConceptsKinetic time coursesProduct inhibitionSteady-state enzyme kinetic parametersReaction schemeEnzymology approachReaction productsReversible bindingEnzyme kinetic parametersProduct releasePractical general methodKinetic parametersEnzyme inhibitionGeneral methodProductsEnzyme systemEnzymatic parameters
2012
Angiotensin-converting enzyme inhibition or mineralocorticoid receptor blockade do not affect prevalence of atrial fibrillation in patients undergoing cardiac surgery*
Pretorius M, Murray KT, Yu C, Byrne JG, Billings FT, Petracek MR, Greelish JP, Hoff SJ, Ball SK, Mishra V, Body SC, Brown NJ. Angiotensin-converting enzyme inhibition or mineralocorticoid receptor blockade do not affect prevalence of atrial fibrillation in patients undergoing cardiac surgery*. Critical Care Medicine 2012, 40: 2805-2812. PMID: 22824930, PMCID: PMC3588582, DOI: 10.1097/ccm.0b013e31825b8be2.Peer-Reviewed Original ResearchConceptsAcute renal failureAngiotensin-converting enzyme inhibitorMineralocorticoid receptor blockadePostoperative atrial fibrillationMineralocorticoid receptor antagonistsAtrial fibrillationPlacebo groupSpironolactone groupRenal failureCardiac surgeryReceptor blockadeReceptor antagonistEnzyme inhibitorsDouble-blind placebo-controlled studyAngiotensin-Converting Enzyme InhibitionPrevalence of hypotensionElective cardiac surgeryPlacebo-controlled studyRenin-angiotensin systemNormal sinus rhythmEnzyme inhibitionRamipril groupSpironolactone useHospital stayPrimary endpoint
2008
17&bgr;-Estradiol Increases Basal but Not Bradykinin-Stimulated Release of Active t-PA in Young Postmenopausal Women
Pretorius M, van Guilder GP, Guzman RJ, Luther JM, Brown NJ. 17&bgr;-Estradiol Increases Basal but Not Bradykinin-Stimulated Release of Active t-PA in Young Postmenopausal Women. Hypertension 2008, 51: 1190-1196. PMID: 18259028, PMCID: PMC2673569, DOI: 10.1161/hypertensionaha.107.105627.Peer-Reviewed Original ResearchConceptsYounger postmenopausal womenT-PA antigenEffect of angiotensinPostmenopausal womenT-PA releaseActive t-PAT-PAAntigen releasePlasminogen activator inhibitor-1 antigenTissue-type plasminogen activator releaseNet t-PA releaseForearm blood flowPlasminogen activator releaseEnzyme inhibitionCrossover studyIntraarterial infusionBasal releaseVascular releaseTreatment periodFibrinolytic functionPlaceboBlood flowActivator releaseAngiotensinAntigenBradykinin Type 2 Receptor BE1 Genotype Influences Bradykinin-Dependent Vasodilation During Angiotensin-Converting Enzyme Inhibition
Van Guilder GP, Pretorius M, Luther JM, Byrd JB, Hill K, Gainer JV, Brown NJ. Bradykinin Type 2 Receptor BE1 Genotype Influences Bradykinin-Dependent Vasodilation During Angiotensin-Converting Enzyme Inhibition. Hypertension 2008, 51: 454-459. PMID: 18180402, PMCID: PMC2581632, DOI: 10.1161/hypertensionaha.107.102574.Peer-Reviewed Original ResearchMeSH KeywordsAdultAngiotensin-Converting Enzyme InhibitorsBlood PressureBradykininDrug SynergismEnalaprilatEndothelium, VascularFemaleForearmGenotypeHumansInjections, Intra-ArterialMaleMethacholine ChlorideNitroprussidePolymorphism, GeneticReceptor, Bradykinin B2Regional Blood FlowSex FactorsTissue Plasminogen ActivatorVascular ResistanceVasodilationVasodilator AgentsConceptsForearm blood flowT-PA releaseForearm vascular resistanceVascular resistanceBlood flowBlood pressureTissue-type plasminogen activator releaseBasal forearm blood flowAngiotensin-Converting Enzyme InhibitionGenotype groupsNet t-PA releaseReceptor-mediated vasodilationBasal forearm vascular resistanceSystolic blood pressureBody mass indexIntra-arterial bradykininEffect of bradykininDegradation of bradykininPlasminogen activator releaseEnzyme inhibitionMass indexVascular responsesActivator releaseBradykininWhite American subjects
2007
Dipeptidyl Peptidase IV in Angiotensin-Converting Enzyme Inhibitor–Associated Angioedema
Byrd JB, Touzin K, Sile S, Gainer JV, Yu C, Nadeau J, Adam A, Brown NJ. Dipeptidyl Peptidase IV in Angiotensin-Converting Enzyme Inhibitor–Associated Angioedema. Hypertension 2007, 51: 141-147. PMID: 18025295, PMCID: PMC2749928, DOI: 10.1161/hypertensionaha.107.096552.Peer-Reviewed Original ResearchConceptsEnzyme (ACE) inhibitor-associated angioedemaDipeptidyl peptidase IV activityHistory of angiotensinPeptidase IV activityControl subjectsSubstance PDipeptidyl peptidase IVEnzyme inhibitorsLife-threatening adverse effectsAngiotensin converting enzyme (ACE) inhibitorsEnzyme inhibitionAbsence of angiotensinPrevalence of smokingSera of patientsCase-control studyPeptidase IVSubstrates of angiotensinTissue edemaAssociated angioedemaAminopeptidase P activityVascular permeabilityAngioedemaAngiotensinAminopeptidase N activityAmino-terminal degradation
2006
Endogenous NO Regulates Plasminogen Activator Inhibitor-1 During Angiotensin-Converting Enzyme Inhibition
Brown NJ, Muldowney JA, Vaughan DE. Endogenous NO Regulates Plasminogen Activator Inhibitor-1 During Angiotensin-Converting Enzyme Inhibition. Hypertension 2006, 47: 441-448. PMID: 16432054, DOI: 10.1161/01.hyp.0000202478.79587.1a.Peer-Reviewed Original ResearchMeSH KeywordsAdultAldosteroneAngiotensin-Converting Enzyme InhibitorsArginineDouble-Blind MethodDrug CombinationsEnzyme InhibitorsFemaleFibrinolysisHemodynamicsHumansInfusions, IntravenousMaleMiddle AgedNG-Nitroarginine Methyl EsterNitric OxideNitric Oxide SynthasePlasminogen Activator Inhibitor 1ProdrugsRamiprilReference ValuesRenin-Angiotensin SystemConceptsPlasminogen activator inhibitor-1Plasminogen activator inhibitor-1 antigenActivator inhibitor-1Salt-replete subjectsL-arginineFibrinolytic balanceInhibitor-1Angiotensin-Converting Enzyme InhibitionNO precursor L-argininePlasminogen activator inhibitor antigenTissue-type plasminogen activator antigenEffect of angiotensinPrecursor L-argininePlasminogen activator antigenNO synthase inhibitorEnzyme inhibitionT-PA activityRenin activityD-dimerInhibitor antigenNormal subjectsSynthase inhibitorEnzyme inhibitorsT-PAAntigen
2005
Angiotensin-Converting Enzyme Inhibition Increases Basal Vascular Tissue Plasminogen Activator Release in Women But Not in Men
Pretorius M, Luther JM, Murphey LJ, Vaughan DE, Brown NJ. Angiotensin-Converting Enzyme Inhibition Increases Basal Vascular Tissue Plasminogen Activator Release in Women But Not in Men. Arteriosclerosis Thrombosis And Vascular Biology 2005, 25: 2435-2440. PMID: 16166566, DOI: 10.1161/01.atv.0000186185.13977.94.Peer-Reviewed Original ResearchMeSH KeywordsAdultAge FactorsAngiotensin-Converting Enzyme InhibitorsBlood PressureBradykininEnalaprilatFemaleHumansLuteal PhaseMaleMethacholine ChlorideMiddle AgedNitroprussideParasympathomimeticsPeptide FragmentsPeptidyl-Dipeptidase APostmenopausePremenopauseRegional Blood FlowSex CharacteristicsTissue Plasminogen ActivatorVasodilator AgentsConceptsT-PA releaseForearm blood flowBasal t-PA releaseNet t-PA releaseTissue plasminogen activator releasePostmenopausal womenPlasminogen activator releaseOlder menPremenopausal womenMenopausal statusActivator releaseIntra-arterial enalaprilatEffect of ACEIEndogenous bradykininHormone replacementExogenous bradykininBlood flowACEIBradykininEnalaprilatWomenYoung menMenEnzyme inhibitionRelease
2004
Chapter 5 Enzyme Inhibition and Inactivation
Silverman R. Chapter 5 Enzyme Inhibition and Inactivation. 2004, 227-321. DOI: 10.1016/b978-0-08-051337-9.50010-9.Peer-Reviewed Original ResearchNoncovalent interactionsIrreversible enzyme inhibitorsCovalent bondsLead compoundsRational discoveryEnzyme inhibitionCompoundsEnzyme targetsReversible inhibitorTarget enzymeEnzyme inhibitorsIrreversible inhibitorDrug synergismBondsMechanisms of resistanceAntibiotic interactionsMechanism of actionEnzymeDrug resistance
2003
Angiotensin-Converting Enzyme Inhibition Increases Human Vascular Tissue-Type Plasminogen Activator Release Through Endogenous Bradykinin
Pretorius M, Rosenbaum D, Vaughan DE, Brown NJ. Angiotensin-Converting Enzyme Inhibition Increases Human Vascular Tissue-Type Plasminogen Activator Release Through Endogenous Bradykinin. Circulation 2003, 107: 579-585. PMID: 12566370, DOI: 10.1161/01.cir.0000046268.59922.a4.Peer-Reviewed Original ResearchMeSH KeywordsAdultAngiotensin-Converting Enzyme InhibitorsBlood Flow VelocityBradykininBradykinin Receptor AntagonistsDose-Response Relationship, DrugEnalaprilatEndothelium, VascularFemaleFibrinolysisForearmHumansInfusions, Intra-ArterialMaleMethacholine ChlorideMuscarinic AgonistsRegional Blood FlowSmokingTissue Plasminogen ActivatorVascular ResistanceConceptsForearm blood flowNet t-PA releaseT-PA releaseEndothelial t-PA releaseHoe 140T-PA responseEndogenous bradykininACE inhibitionExogenous bradykininTissue-type plasminogen activator releaseReceptor antagonist HOE 140Angiotensin-Converting Enzyme InhibitionBradykinin receptor antagonist HOE 140Effects of enalaprilatIntra-arterial enalaprilatIntra-arterial infusionPlasminogen activator releaseEnzyme inhibitionFBF responseVascular resistanceBlood flowActivator releaseEnalaprilatBradykininMethacholine
2000
An analysis of the catalytic cycle of HIV-1 reverse transcriptase: opportunities for chemotherapeutic intervention based on enzyme inhibition.
Furman P, Painter G, Anderson K. An analysis of the catalytic cycle of HIV-1 reverse transcriptase: opportunities for chemotherapeutic intervention based on enzyme inhibition. Current Pharmaceutical Design 2000, 6: 547-67. PMID: 10788596, DOI: 10.2174/1381612003400777.Peer-Reviewed Original ResearchConceptsCatalytic cycleIntrinsic binding affinityHIV-1 reverse transcriptaseCatalytic complexChemical catalysisBinding affinityCatalysisMolecular forcesReverse transcriptase inhibitorsAllosteric siteClasses of approved drugsNon-nucleoside reverse transcriptase inhibitorsTranscriptase inhibitorsNucleoside reverse transcriptase inhibitorsSite of inhibitionEnzyme inhibitionReverse transcriptaseAlternative substratesEnzyme
1999
Comparative Effect of Angiotensin-Converting Enzyme Inhibition and Angiotensin II Type 1 Receptor Antagonism on Plasma Fibrinolytic Balance in Humans
Brown N, Agirbasli M, Vaughan D. Comparative Effect of Angiotensin-Converting Enzyme Inhibition and Angiotensin II Type 1 Receptor Antagonism on Plasma Fibrinolytic Balance in Humans. Hypertension 1999, 34: 285-290. PMID: 10454455, DOI: 10.1161/01.hyp.34.2.285.Peer-Reviewed Original ResearchMeSH KeywordsAdultAldosteroneAngiotensin IIAngiotensin Receptor AntagonistsAngiotensin-Converting Enzyme InhibitorsAntihypertensive AgentsBlood PressureData Interpretation, StatisticalDiet, Sodium-RestrictedFemaleFibrinolysisHeart RateHumansIsoquinolinesLosartanMalePlasminogen Activator Inhibitor 1QuinaprilReninRenin-Angiotensin SystemTetrahydroisoquinolinesTissue Plasminogen ActivatorConceptsPlasminogen activator inhibitor-1PAI-1 antigenTissue plasminogen activatorACE inhibitorsFibrinolytic balanceAldosterone systemAngiotensin II type 1 receptor antagonismAngiotensin II type 1 receptor antagonistAngiotensin-Converting Enzyme InhibitionType 1 receptor antagonistPlasma PAI-1 antigenPAI-1 antigen concentrationsAntigen concentrationEquivalent hypotensive dosesPlasma fibrinolytic balancePlasma renin activityAngiotensin II formationLow salt intakePAI-1 activityClass of drugsTPA antigen concentrationsActivator inhibitor-1Enzyme inhibitionLosartan treatmentQuinapril treatment
1993
Alteration of rat liver endoplasmic reticulum Ca2+-ATPase thiol integrity by ciprofibrate, a peroxisome proliferator
Bennett A, Williams G. Alteration of rat liver endoplasmic reticulum Ca2+-ATPase thiol integrity by ciprofibrate, a peroxisome proliferator. Biochemical Pharmacology 1993, 45: 2093-2098. PMID: 8512590, DOI: 10.1016/0006-2952(93)90021-n.Peer-Reviewed Original Research
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