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Coupled Enzyme Activity and Thermal Shift Screening of the Maybridge Rule of 3 Fragment Library Against Trypanosoma brucei Choline Kinase; A Genetically Validated Drug Target (Book chapter)

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ISBN: 9789535109068 Year: DOI: 10.5772/52668 Language: English
Publisher: IntechOpen Grant: Wellcome Trust - 067441
Subject: Medicine (General)
Added to DOAB on : 2019-01-17 11:47:01
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Abstract

In this study we interrogate 630 compounds of the Maybridge Rule of 3 Fragment Library for compounds that interact with, and inhibit TbCK. The Maybridge Rule of 3 Fragment Library is a small collection of quantifiable diverse, pharmacophoric rich, chemical entities that comply with the following criteria; MW ≤ 300, cLogP ≤ 3, H-Bond Acceptors ≤ 3, H-Bond Donors ≤ 3, Rotatable bonds (Flexibility Index) ≤ 3, Polar Surface Area ≤ 60 Å2 and aqueous solubility ≥ 1 mM using LogS and high purity (≥ 95%). Comparisons between two different screening methods, a coupled enzyme activity assay and differential scanning fluorimetry, has allowed identification of compounds that interact and inhibit the T. brucei choline kinase, several of which possess selective trypanocidal activity. Screening of a comparatively small fragment library by two different screening methods has allowed identification of several compounds that interact with and inhibit TbCK, a genetically validated drug target against African sleeping sickness. Some of the inhibitory fragments were also selectively trypanocidal, considering these are relatively simple molecules with no optimization, finding low μΜ inhibitors is very encouraging. Moreover some of the morphological phenotypes of these trypanocidal compounds include cell-cycle arrests similar to those observed for the TbCK conditional knockout grown under permissive conditions.

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pharmacology --- toxicology

New Insights into Toxicity and Drug Testing

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ISBN: 9789535109464 Year: Pages: 254 DOI: 10.5772/55886 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:49

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This book ""New Insights into Toxicity and Drug Testing"" covers all emerging technologies (profiling technologies, 3D cultures, next generation sequencing etc.), available methods and models to evaluate candidate drugs and medicinal plants with reference to toxicity, drug testing and development. This book is an original contribution of experts from different parts of the globe and the in-depth information will be a significant resource for scientists and physicians who are directly dealing with drugs / medicines and human life.

Aflatoxins - Recent Advances and Future Prospects

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ISBN: 9789535109044 9789535142553 Year: Pages: 408 DOI: 10.5772/2500 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:49

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This book is broadly divided into five sections and 17 chapters, highlighting recent advances in aflatoxin research from epidemiology to molecular genomics and control measures, biocontrol approaches, modern analytical techniques, economic concerns and underlying mechanisms of contamination processes. This book will update readers on several cutting-edge aspects of aflatoxins research with useful up-to-date information for mycologists, toxicologists, microbiologists, agriculture scientists, plant pathologists and pharmacologists, who may be interest to understanding of the impact, significance and recent advances within the field of of aflatoxins with a focus on control strategy.

Using Old Solutions to New Problems - Natural Drug Discovery in the 21st Century

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ISBN: 9789535111580 9789535142454 Year: Pages: 426 DOI: 10.5772/46069 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:49

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The medicinal use of plants, animals and microorganisms has been a part of human evolution and likely began before recorded history. Is it possible that this knowledge can be used to create powerful new drugs and solve some of the human health problems facing us today? This book is a collection of an expert team of agronomists, chemists, biologists and policy makers who discuss some of the processes involved in developing a naturally-sourced bioactive compound into a drug therapy. These experts define a natural compound and elucidate the processes required to find, extract and define a naturally-derived bioactive molecule. Finally, they describe the necessity for understanding the fundamental mechanisms of disease before applying bioactive molecules in bioassay-guided drug discovery platforms.

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