DIRECT OBSERVATION OF ENZYMATIC CATALYTIC STRATEGIES
Project Number5R01GM033851-12
Contact PI/Project LeaderKURZ, LINDA C.
Awardee OrganizationWASHINGTON UNIVERSITY
Description
Abstract Text
The long term goal of our proposed research is to understand at the
molecular level how enzymes achieve their extraordinary catalytic
efficiencies. We seek to do this through direct observation of enzyme-
bound ligands (substrates, intermediates, and transition-state analogs).
We will use techniques (NMR, IR Spectroscopies) sensitive to local bond
distortions, electronic environment, protonation state and other factors
likely to reflect the enzyme's catalytic strategies. We seek to do this
through observations of the effects of perturbations (pH, temperature,
structure of enzyme and ligand) on the standard free energies of enzyme-
bound substrates, intermediates, transition-states and analogs of those
states. We will use techniques (various spectroscopic titrations,
calorimetry, transient kinetics) appropriate for the measurement of
equilibrium and rate constants. We will make quantitative comparisons
(linear free energy relationships) with the effects of these same
perturbations on well-understood model systems leading to an understanding
of the molecular basis of those interactions between substrate and enzyme
which lead to efficient catalysis. We will focus on two groups of enzymes;
the Claisen enzymes (citrate synthase) and the nucleoside aminohydrolases
(adenosine deaminase). The Claisen enzymes are prominent in pathways
requiring carbon-carbon bond formation in the biosynthesis of fats and
cholesterol as well in the energy-yielding pathways of the tricarboxylic
acid cycle and the glyoxylate cycle. These enzymes operate through
activation of a substrate carbonyl together with the stabilization of an
activated form of the acylthioester substrate. Enzymes which catalyze
amino-nucleoside(tide) hydrolysis have more varied but no less vital
roles. Adenosine deaminase is necessary to the integrity of the immune
response. Other enzymes of this class participate in salvage pathways of
purines and pyrimidines or are involved in the maintenance of cellular
energy balance. These enzymes operate through stabilization of tetrahedral
intermediates, a catalytic strategy used by several other important enzyme
groups. The necessary groundwork is near completion and new results are
rapidly accumulating. In previous work, we have identified catalytic
strategies used by the two enzymes. We have developed probes to
specifically detect and quantify the effects of perturbations on the
catalytic apparatus; we have prepared enzymes with single- and multiple-
site changes. We are now prepared to characterize these mutants and to
continue our search for additional strategies in both groups. An
understanding of how enzymes work is necessary to understand at the most
fundamental level the metabolic processes in normal and disease states.
Public Health Relevance Statement
Data not available.
NIH Spending Category
No NIH Spending Category available.
Project Terms
active sitesadenosine deaminaseanimal tissuecalorimetrycarbonyl groupcatalystcitrate synthaseconformationenzyme complexenzyme mechanismenzyme structureenzyme substrateenzyme substrate analogenzyme substrate complexinfrared spectrometrymutantnuclear magnetic resonance spectroscopyoxaloacetatesprotonationthermodynamics
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Publications
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Outcomes
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Clinical Studies
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