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Friday, July 31, 2020 | History

2 edition of Inhibition of the RTEM-1 [beta]-lactamase by transition-state analogs. found in the catalog.

Inhibition of the RTEM-1 [beta]-lactamase by transition-state analogs.

Richard Martin

Inhibition of the RTEM-1 [beta]-lactamase by transition-state analogs.

by Richard Martin

  • 328 Want to read
  • 11 Currently reading

Published .
Written in English


The Physical Object
Pagination131 leaves.
Number of Pages131
ID Numbers
Open LibraryOL15411500M
ISBN 100612119688

Analog Synthesis in Drug Design 2. The Design of Enzyme Inhibitors: Transition State Analogs 3. Structure–Absorption–Distribution Relationships: Significance for Drug Design 4. The Role of Charge-Transfer Processes in the Action of Bioactive Materials 5. Approaches to the Rational Combination of Antimetabolites for Cancer Chemotherapy 6. Neuraminidase enzymes are glycoside hydrolase enzymes that cleave (cut) the glycosidic linkages of neuraminic inidase enzymes are a large family, found in a range of organisms. The best-known neuraminidase is the viral neuraminidase, a drug target for the prevention of the spread of influenza infection. The viral neuraminidases are frequently used as antigenic determinants found on.

I. Ojima, in Advances in Metal-Organic Chemistry, Vol. 1 (Ed.: L. S. Liebeskind), Jai Press, Inc., Greenwich, CT, Key Words: ORGANOMETALLICS/GENERAL. The first potent inhibitors are based on the sequence of APP around the β-secretase cleavage site EVNL / DAEF, with the scissile Leu-Asp amide bond being replaced by a hydroxyethylene transition state analogue isostere. In addition, lipophilic sidechains have been incorporated and a crystal structure of such an octapeptidic inhibitor bound in.

  An early inhibitor of BACE1, an aspartic protease, was designed on the basis of a substrate transition-state concept, as well as that of other aspartic proteases, such as renin and HIV protease, which have a substrate transition-state analogue at the P 1 position [10–16]. Phosphoglucomutase (EC ) is an enzyme that transfers a phosphate group on an α-D-glucose monomer from the 1' to the 6' position in the forward direction or the 6' to the 1' position in the reverse direction.. More precisely, it facilitates the interconversion .


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Inhibition of the RTEM-1 [beta]-lactamase by transition-state analogs by Richard Martin Download PDF EPUB FB2

The transition state of ricin A-chain was solved, and powerful transition state analogues designed for in vitro conditions. 72,73 A second generation of inhibitors was designed for Saporin, a related RIP that has robust catalytic activity and inhibitor action at neutral pH.

74 These compounds reflect transition state structure, are the most Inhibition of the RTEM-1 [beta]-lactamase by transition-state analogs. book by: N-Sulfamoylphenylalanine and its derivatives having varied alkyl groups on the terminal amino group were designed rationally as transition state analogue inhibitors for carboxypeptidase A (CPA) and synthesized.

In CPA inhibitory assays the parent compound having the (S)-configuration, i.e., (S)-1a, showed potent inhibitory activity with the Ki value of μM. Its enantiomer was shown to be Cited by:   A considerable effort has been invested in the design and synthesis of transition-state analogue inhibitors of glycosidases, particularly with respect to their potential as therapeutics.

However, their characterization as transition-state mimics is generally based only upon their high affinity. To provide a quantitative evaluation of the mimicry afforded by two commonly used classes of Cited by:   Design of Amino Acid Aldehydes as Transition-State Analogue Inhibitors of Arginase.

Journal of the American Chemical Society(33), DOI: / by: β-Hexosaminidase is an indirect marker of heavy alcohol consumption. β-Hexosaminidase is present in serum mostly as A (αβ), and B (ββ), but other minor forms, such as S (αα), I 1, I 2 (intermediate form), and P (elevated in pregnancy), are also present in serum.

Isoforms I 1, I 2, and P are composed of two β β-hexosaminidase activity in serum represents activities of all. Withers and colleagues observed this phenomenon of enzyme-assisted transition state formation with an inhibitory reactant and the NAG-thiazoline product of test this idea that the O-GlcNAcase activity of NCOAT can convert STZ to a potent transition state analog inhibitor, we incubated.1 M STZ with resin-bound NCOAT, washed the unbound compound from the.

Recent Developments of Transition-State Analogue Glycosidase Inhibitors of Non-Natural Product Origin. Chemical Reviews(2), DOI: /crk.

Adrian Blaser and, Jean-Louis Reymond. Stereoselective Inhibition of α-l-Fucosidases by N-Benzyl Aminocyclopentitols. Transition State Analogues for Nucleotidyl Transfer Reactions: Structure and Stability of Pentavalent Vanadate and Phosphate Ester Dianions.

Stable and functional regeneration of pancreatic beta-cell population in nSTZ-rats treated with tungstate. Vanadate-based transition-state analog inhibitors of Cre–LoxP recombination. Considering that many inhibitors inspired from transition-state analogs during glycosylation catalyzed by α2,3-/α2,6-STs showed much higher inhibitory effects on α2,6-STs rather than α2,3-STs, these results suggested that the donor binding site of α2,6-STs might be quite different from those of α2,3-STs, although both α2,3/α2,6-STs.

Inhibitors of glucosidases I and II have also been studied as potential anti-HIV agents. 6 The HIV viral envelope is composed of a bilipidic layer and a complex protein known as env that consists of glycoproteins gp41 (transmembrane) and gp, the latter being displayed on the viral surface and anchored to gp 7 Glucosidases I and II participate in the formation of gp, through processing.

Because 1-deoxynojirimycin (moranoline) acting as the paradigms of glycosidase inhibitors is known to bind subsite −1 of the corresponding enzymes (13–15), chitin oligosaccharides, (GlcNAc) n, modified with moranoline at their reducing end might be another candidate for the stable transition-state analogue for HEWL.

A focused library of 6,8-dioxaazabicyclo[]-octane peptidomimetic scaffolds was synthesized and assayed towards BACE1 enzyme, resulting in the identification of a thiolactam-containing hit compound possessing IC 50 in the low micromolar range, and confirming the bicyclic acetal portion as a potential transition state analogue in the.

Summary Current evidence implicates the Beta‐amyloid protein as the principal culprit in the pathogenesis of Alzheimer's disease.

Its biogenesis results from the sequential proteolytic cleavage of. A number of hydrazine-containing analogues of inhibitor 1 also inhibited beta-glucosidase and isomaltase slowly, while the amine isofagomine [(3R,4R,5R)-3,4-dihydroxyhydroxymethylpiperidine; inhibitor 5] only inhibited beta-glucosidase slowly.

Inhibitor 1 and related inhibitors were found to leave almond beta-glucosidase with almost. Introduction. Glyoxalase I (GLOI, EC ) is the first and the rate-limiting glutathione (GSH)-dependent enzyme in the glyoxalase system, which functions as a ubiquitous detoxification pathway by catalyzing the conversion of toxic α-oxoaldehydes to nontoxic D-lactate urally, mammalian GLOI is a zinc-containing metalloenzyme with two active sites located at the homodimer interface 2.

Taking these constraints into account, the strategy used to fulfill the criteria requested for optimal recognition of NEP and APN was to design, as inhibitors, transition state analogues to fix the right group in the right position.

The S 1 subsite of APN interacts preferentially with hydrophobic or basic aliphatic chains. ENZYME INHIBITION TRANSITION-STATE INHIBITION The potent transition state analog, Pyrrole 2-carboxylic acid binds to active site of recimase x time more tightly than proline Racemization of proline proceeds through a transition state in which the tetrahedral alfa carbon atom has become trigomonal by loss of a proton 36 Intrinsic kinetic isotope effects report on the bond vibrational status of the labeled reactant atom at the transition state | Transition state analogue—a chemically stable molecule with features of bond lengths, angles and electron density at the van der Waals surface to resemble the actual transition state more closely than it does the.

Full Text; PDF ( K) PDF-Plus ( K) Suppl. data; MgF 3 − and AlF 4 − transition state analogue complexes of yeast phosphoglycerate kinase. Nicole E. McCormick, a Stephanie M. Forget, b Raymond T. Syvitski, b David L. Jakeman a b a College of Pharmacy, Dalhousie University, College Street, Halifax, NS B3H 4R2, Canada.

b Department of Chemistry, Dalhousie University, Coberg. A 'read' is counted each time someone views a publication summary (such as the title, abstract, and list of authors), clicks on a figure, or views or downloads the full-text. A plethora of various classes of NPs were listed as BACE-1 inhibitors in a book chapter by Fang, Sun, Yang, and Guo ().In a review, Konrath, Passos, Klein-Junior, and Henriques () have.All these inhibitors are transition-state analogs.

The crystal structure of the memapsin 2 catalytic unit complexed to a transition-state inhibitor has been solved. The conformation of the enzyme.GD-beta-Galactosidase bound substrates and substrate analog inhibitors less well than did normal beta-galactosidase while planar transition state analog inhibitors were more strongly bound.