نتایج جستجو برای: uncompetitive inhibitor

تعداد نتایج: 211497  

2017
Narin Kirikyali Jonathan Wood Ian F Connerton

β-xylosidases catalyse the hydrolysis of short chain xylooligosaccharides from their non-reducing ends into xylose. In this study we report the heterologous expression of Aspergillus oryzae β-xylosidase (XylA) in Pichia pastoris under the control of the glyceraldehyde-3-phosphate dehydrogenase promoter. The recombinant enzyme was optimally active at 55°C and pH 4.5 with Km and Vmax values of 1....

Journal: :The Biochemical journal 1989
R G Jackson N S Gee C I Ragan

myo-Inositol monophosphatase is inhibited by the arginine-specific reagent phenylglyoxal. The rate of inactivation is decreased in the presence of Pi, a competitive inhibitor of the enzyme. The effect of Pi is dependent on the presence of Mg2+, but is unaffected by Li+, an uncompetitive inhibitor. In the absence of Mg2+, the substrate, Ins(1)P, binds to the enzyme but is not converted into prod...

2002
THOMAS S. SOPER WANDA M. JONES BRAD LERNER MOSHE TROP JAMES M. MANNING

Purified D-amino acid transaminase from Bacillus sphaericus catalyzes an (~,/3 elimination from the D isomer of pchloroalanine to yield equivalent amounts of pyruvate, chloride, and ammonia; the L isomer of chloroalanine is not a substrate for this transaminase. During the /I elimination there is a synchronous loss in enzyme activity; the Kinact for /I-chloroalanine was estimated to be about 10...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2013
John T Barr Jeffrey P Jones

The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2-dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in huma...

2012

The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in human...

2012

The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in human...

2017
Vinayak Singh Stefano Donini Angela Pacitto Claudia Sala Ruben C. Hartkoorn Neeraj Dhar Gyorgy Keri David B. Ascher Guillaume Mondésert Anthony Vocat Andréanne Lupien Raphael Sommer Hélène Vermet Sophie Lagrange Joe Buechler Digby F. Warner John D. McKinney Janos Pato Stewart T. Cole Tom L. Blundell Menico Rizzi Valerie Mizrahi

VCC234718, a molecule with growth inhibitory activity against Mycobacterium tuberculosis (Mtb), was identified by phenotypic screening of a 15344-compound library. Sequencing of a VCC234718-resistant mutant identified a Y487C substitution in the inosine monophosphate dehydrogenase, GuaB2, which was subsequently validated to be the primary molecular target of VCC234718 in Mtb. VCC234718 inhibits...

2015
Jay M. Sage Anthony J. Cura Kenneth P. Lloyd Anthony Carruthers

23 GLUT1 is the primary glucose transport protein of the cardiovascular system and astroglia. A 24 recent study proposes that caffeine uncompetitive inhibition of GLUT1 results from interactions 25 at an exofacial GLUT1 site. Intracellular ATP is also an uncompetitive GLUT1 inhibitor and 26 shares structural similarities with caffeine suggesting that caffeine acts at the previously 27 character...

2012

The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in human...

2012

The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in human...

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