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Showing 1 to 20 of 90 for “"Chymotrypsin"”.
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Kinetics and mechanism of alpha-chymotrypsin catalyzed reactions.
The principle of microscopic reversibility was formulated for elementary reactions at equilibrium. It follows from the principle that for any elementary reaction the favored reaction path in one direction must be the reverse of that in the opposite reaction, and that the ratio of rate constants is …
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Folding Studies on Mutants of Chymotrypsin Inhibitor 2
… at the helix N-terminus and hydrophobic core of Chymotrypsin Inhibitor 2 (CI2) have been studied. All mutants adhere to a two-state model for protein folding , and are destabilised relative to wild-type. Mutation of N-cap residue S31 to Ala or Gly destabilises CI2 by nearly 1 kcal mol-1, with …
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The Application of a Reporter Group to α-Chymotrypsin
… This potential reporter group was attached to chymotrypsin by a covalent bond to a methionine residue. It was demonstrated that substrates perturb the spectrum of the reporter-modified chymotrypsin and that the spectral perturbations have characteristics related to a tentative but consistent …
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Theoretical and experimental studies of slowly deacylating alpha-chymotrypsin acyl enzymes
The differential deacylation rates for alpha-chymotrypsin beta-phenyl acyl enzymes 13 and 14 have been studied using the techniques of molecular mechanics and molecular dynamics. These studies indicate that the ketone side-chain of slowly deacylating acyl enzyme 13 is hydrogen bonded to the NH of …
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2-Pyranones as Suicide Inhibitors for Alpha-Chymotrypsin: I. A Structure-Activity Study of the 6-Halo-2-Pyranones. Ii. 5-Halomethyl-2-Pyranones as Inhibitors of Chymotrypsin
… of 6-halo-2-pyranones as suicide inhibitors of chymotrypsin. In the 6-chloro-2-pyranone series, substitution in the 3- position of the pyrone by either ethyl or n-butyl produced poor binding relative to 3-benzyl-6-chloro-2-pyranone, and no inactivation. Increasing the aromatic area of the …
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Activity of Analogs of Anticancer Drugs on the Serine Protease Enzymes Subtilisin and Chymotrypsin
… partly responsible for the anticancer activity. Chymotrypsin and subtilisin are serine proteases that have a histidine residue in the active site. We are investigating the inhibition of the digestive enzymes chymotrypsin and subtilisin by analogs of the anticancer drug cisplatin and trying to …
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Design and Synthesis of Enzyme Activated Irreversible Inactivators for Proteases. Suicide Inactivation of Chymotrypsin
Strategies directed toward the synthesis of halo-enol lactones have been investigated. The catalytic mercury induced lactonization of acetylenic acids has been studied, and shown to proceed via a mercuronium intermediate, to give enol lactones in good yield. This methodology was adapted to afford …
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INHIBITION OF THE SERINE PROTEASE CHYMOTRYPSIN BY A SILANEDIOL PEPTIDE MIMIC: ASYMMETRIC SYNTHESIS AND INHIBITION STUDIES
… and inhibition of the serine protease α- chymotrypsin by silanediol structures and the development of an efficient method to install the stereochemistry at the P1’ position of the inhibitor. In the first part, the silanediol 67 was synthesized as a potential α-chymotrypsin inhibitor, …
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Halo enol lactone and protio enol lactone inhibitors of alpha-chymotrypsin: Mechanism and stereospecific behavior of inhibition
A kinetic study of inactivation of $\alpha$-chymotrypsin by enol lactones was performed. Halo enol lactones, 3-(1-naphthyl)-6(E)-(iodomethylene)tetrahydro-2-pyranone ($\alpha$Np6I) and 3-phenyl-6(E)-(bromomethylene)tetrahydro-2-pyranone ($\alpha$Ph6Br), showed burst kinetics in the inactivation of …
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Halo Enol Lactones as Enzyme-Activated Irreversible Inhibitors of Chymotrypsin: Their Synthesis, Kinetics, and Mechanism of Inactivation (Suicide Substrates)
… inhibitors or suicide substrates for (alpha)-chymotrypsin. Acyl transfer to the active site serine generates a halo methyl ketone that remains tethered in the catalytic site during the lifetime of the acyl enzyme, available for reaction with an enzymatic nucleophile. To investigate the …
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PART I. STEREOELECTRONIC EFFECTS IN PHOSPHATE ESTERS. PART II. PROTON NUCLEAR MAGNETIC RESONANCE STUDY ON THE BINDING OF TRANS-CINNAMALDEHYDE TO ALPHA-CHYMOTRYPSIN.
… ON THE BINDING OF TRANS-CINNAMALDEHYDE TO ALPHA-CHYMOTRYPSIN.
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Understanding the determinants for substrate recognition, regulation of enzymatic activity and the development of broad-spectrum inhibitors of coronavirus 3-chymotrypsin-like proteases
… anti-coronaviral therapeutics. Viral encoded 3-Chymotrypsin-like protease (3CLpro) is essential for viral polyprotein processing to release non-structural proteins that form the replicase complex machinery for viral genome replication. Due to its indispensable role in coronaviral replication, …
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Halo Enol Lactones as Enzyme-Activated Irreversible Inhibitors of Alpha-Chymotrypsin: I. The Effect of Lactone Substitution Pattern. Ii. Alpha - Amino-Functionalized Lactones
… irreversible (suicide) inhibitors for (alpha)-chymotrypsin with the activities of the corresponding (alpha)-substituted lactones. The 4-phenyl-5(E)-(iodomethylidene) tetrahydro-2-furanone, the 4-phenyl-5(E)-(iodomethylidene)dihydro-2-furanone, the …
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1-Acylamido boronic acids and Difluoroborane analogs of amino acids: Synthesis and biological activity of transition state analogs for Chymotrypsin and Elastase (inhibition, esters)
… inhibitors of the serine proteases (alpha)-chymotrypsin and elastase. These inhibitors were designed to resemble N-acyl phenylalanine, phenylglycine (as chymotrypsin inhibitors), alanine, valine, and isoleucine (as elastase inhibitors) and have boron sybstituted for the carboxy terminus …
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Genetic, biochemical, and molecular studies of the Bowman-Birk inhibitors in the genus Glycine Willd
… and cvs. Kunitz and Williams 82. The BBI (chymotrypsin inhibitor activity) inherited as a quantitative/multigenic trait with 18-34% of the F$\sb2$ progeny exceeding the high parent (cv. Kunitz) in their activity suggesting a transgressive nature of inheritance. A ""new"" electrophoretic …
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Solid-State 17O NMR as a New Probe to Study Acyl-Enzyme Intermediates
… intermediates: p-N,N-dimethylaminobenzoyl-chymotrypsin (DAB-CHT), trans¬¬-¬o-methoxycinnamoyl-chymotrypsin (oMC-CHT), and trans-p-methoxycinnamoyl-chymotrypsin (pMC-CHT). At pH 7.8, the three acyl-enzyme intermediates were found to undergo hydrolysis (deacylation) with the following rate …
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Modification of soybean proteins by immobilized proteases
Trypsin and alpha-chymotrypsin were immobilized on nylon pellets or porous glass by covalent methods to change molecular properties and functional characteristics of soybean proteins. The amount of trypsin immobilized on nylon pellets using the glutaraldehyde method was high when the pellets were …
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Chemistry at liquid-liquid interfaces: con- and counter-current extraction and biologically active membranes in microchannels
… active membranes that are reactive to chymotrypsin are synthesized and studied. It is found that these polyamide membranes can be synthesized within the microchannel and have shown reactivity toward chymotrypsin. The result of the reaction with chymotrypsin leads to a breakdown in the …
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Photochemical harpoons: covalent labels for multi-protein complexes
… inhibits hydrolase enzymes such as trypsin and chymotrypsin along with the common organophosphate target acetylcholine esterase. PSP is also suspected of affecting many other cell functions and may interact with a large number of cellular proteins. In this work phenyl saligenin phosphate has …
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