Oxidative folding and preparation of α-conotoxins for use in high-throughput structure-activity relationship studies

2012 ◽  
Vol 19 (1) ◽  
pp. 16-24 ◽  
Author(s):  
Reena Gyanda ◽  
Jayati Banerjee ◽  
Yi-Pin Chang ◽  
Angela M. Phillips ◽  
Lawrence Toll ◽  
...  
Keyword(s):  
High Throughput ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Oxidative Folding ◽  
Structure Activity

High-Throughput Chemical Modification of Oligonucleotides for Systematic Structure–Activity Relationship Evaluation

2014 ◽  
Vol 25 (12) ◽  
pp. 2222-2232 ◽  
Author(s):  
Daniel Zewge ◽  
Francis Gosselin ◽  
Denise M. Kenski ◽  
Jenny Li ◽  
Vasant Jadhav ◽  
...  
Keyword(s):  
Chemical Modification ◽  
High Throughput ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Systematic Structure

scholarly journals Trypanothione Reductase High-Throughput Screening Campaign Identifies Novel Classes of Inhibitors with Antiparasitic Activity

2009 ◽  
Vol 53 (7) ◽  
pp. 2824-2833 ◽  
Author(s):  
Georgina A. Holloway ◽  
William N. Charman ◽  
Alan H. Fairlamb ◽  
Reto Brun ◽  
Marcel Kaiser ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Trypanothione Reductase ◽  
Antiparasitic Activity ◽  
Class A ◽  
Structure Activity ◽  
Metabolic Properties

ABSTRACT High-throughput screening of 100,000 lead-like compounds led to the identification of nine novel chemical classes of trypanothione reductase (TR) inhibitors worthy of further investigation. Hits from five of these chemical classes have been developed further through different combinations of preliminary structure-activity relationship rate probing and assessment of antiparasitic activity, cytotoxicity, and chemical and in vitro metabolic properties. This has led to the identification of novel TR inhibitor chemotypes that are drug-like and display antiparasitic activity. For one class, a series of analogues have displayed a correlation between TR inhibition and antiparasitic activity. This paper explores the process of identifying, investigating, and evaluating a series of hits from a high-throughput screening campaign.

scholarly journals Development and Validation of a high-throughput Structure-Activity Relationship Assay for the hERG Potassium Channel

2012 ◽  
Vol 102 (3) ◽  
pp. 330a
Author(s):  
Daniel J. Gillie ◽  
Steven J. Novick ◽  
Brian T. Donovan ◽  
Lisa A. Payne ◽  
Claire Townsend
Keyword(s):  
Potassium Channel ◽  
High Throughput ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Development And Validation
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