Development of a Thyroperoxidase Inhibition Assay for High-Throughput Screening

2014 ◽  
Vol 27 (3) ◽  
pp. 387-399 ◽  
Author(s):  
Katie B. Paul ◽  
Joan M. Hedge ◽  
Daniel M. Rotroff ◽  
Michael W. Hornung ◽  
Kevin M. Crofton ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Inhibition Assay

scholarly journals New High-Throughput Fluorimetric Assay for Discovering Inhibitors of UDP-N-Acetylmuramyl-l-Alanine: d-Glutamate (MurD) Ligase

2009 ◽  
Vol 14 (4) ◽  
pp. 412-418 ◽  
Author(s):  
Katja Kristan ◽  
Miha Kotnik ◽  
Marko Oblak ◽  
Uroš Urleb
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Antibacterial Agents ◽  
Enzyme System ◽  
The Novel ◽  
Inhibition Assay ◽  
Structural Class ◽  
Bacterial Enzyme ◽  
Bacterial Peptidoglycan ◽  
Murd Ligase

A novel assay for monitoring the activity of the bacterial enzyme UDP- N-acetylmuramyl-L-alanine:D-glutamate ligase (MurD ligase) is presented. MurD, which belongs to an enzyme family of Mur ligases, is essential for the synthesis of bacterial peptidoglycan and therefore represents an attractive target for the discovery of novel antibacterial agents. The inhibition assay described in this article is amenable to high-throughput screening. It is based on the detection of the accumulation of adenosine 5′-diphosphate (ADP), a product of the reaction catalyzed by MurD ligase, by conversion to a fluorescent signal via a coupled enzyme system, using the ADP Quest™ assay kit from DiscoveRx. The novel assay has been validated by obtaining KM,app values for substrates D-Glu, UDP- N-acetylmuramyl-L-alanine (UMA) and ATP that are in agreement with the data reported in the literature. A counterscreen assay was introduced to eliminate false positives, and some of the known MurD inhibitors have been retested to compare the data measured with different methods. Moreover, a focused library of around 1000 compounds was screened for the inhibition of MurD to assess the performance and robustness of the assay. Finally, a novel MurD inhibitor belonging to a new structural class, with an IC50 value of 105 µM, was discovered. ( Journal of Biomolecular Screening 2009:412-418)

scholarly journals Simple Colorimetric Inhibition Assay of Heme Crystallization for High-Throughput Screening of Antimalarial Compounds

2006 ◽  
Vol 51 (1) ◽  
pp. 350-353 ◽  
Author(s):  
Nguyen Tien Huy ◽  
Dinh Thanh Uyen ◽  
Atsushi Maeda ◽  
Dai Thi Xuan Trang ◽  
Tatsuo Oida ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Colorimetric Assay ◽  
Tween 20 ◽  
Inhibition Assay ◽  
Microplate Reader ◽  
Antimalarial Compounds

ABSTRACT Current assays for screening new antimalarials need initiators of β-hematin formation that require laborious preparation, special devices, and substrates. In this study, based on reduction of heme absorption in β-hematin formation, we developed a simple colorimetric assay using Tween 20 as an initiator and a microplate reader for high-throughput screening of inhibitors of β-hematin formation.

High-throughput screening program for botanical extracts

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
L Hingorani ◽  
NP Seeram ◽  
B Ebersole
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Screening Program ◽  
Botanical Extracts

High throughput screening of microbial biodiversity for the discovery of novel cosmeceutical agents

Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
K Georgousaki ◽  
N DePedro ◽  
AM Chinchilla ◽  
N Aliagiannis ◽  
F Vicente ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Microbial Biodiversity

High throughput screening to investigate Brazilian Cerrado biome plant extract bank chemical diversity

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
LS Espindola ◽  
RG Dusi ◽  
KR Gustafson ◽  
J McMahon ◽  
JA Beutler
Keyword(s):  
High Throughput ◽  
Plant Extract ◽  
High Throughput Screening ◽  
Chemical Diversity ◽  
Brazilian Cerrado ◽  
Cerrado Biome

High-throughput screening revealed a clinically relevant drug to induce sperm motility

2014 ◽  
Author(s):  
Clair Cochrane ◽  
Halil Ruso ◽  
Anthony Hope ◽  
Rosemary G Clarke ◽  
Christopher Barratt ◽  
...  
Keyword(s):  
Sperm Motility ◽  
High Throughput ◽  
High Throughput Screening
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