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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.

Toxicology Studies - Cells, Drugs and Environment

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ISBN: 9789535121404 9789535142201 Year: Pages: 244 DOI: 10.5772/58714 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:49

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The increased exposure to toxins, toxicants and novel drugs has promoted toxicology to become one of the most important areas of research with emerging innovative toxicity testing protocols, techniques, and regulation being placed. Since the bioactivation of many toxins and toxicants and its consequences on human health are not clearly known, this book offers a quick overview of cellular toxicology through the cell, drug and environmental toxicity. This book does not strive to be comprehensive but instead offers a quick overview of principle aspects of toxins and toxicants in order to familiarize the key principles of toxicology. The book is divided into three main sections,; the first one discusses the role of mitochondrial dysfunction, oxidative stress and mitochondrial drug development. The second and third sections bring light to forensic toxicology and drug poisoning followed by environmental toxicity.

Cytotoxicity

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ISBN: 9781789234305 9781789234312 Year: Pages: 278 DOI: 10.5772/intechopen.69919 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:51

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The book Cytotoxicity is aimed to be an essential reading to all medical students, biologists, biochemists and professionals involved in the field of toxicology. This book is a useful and ideal guide for novice researchers interested in learning research methods to study cytotoxic bioactive compounds. The parts of this book describe the replacement and different applications of the cytotoxic agents. All chapters are written by paramount experts in cytotoxicity research. This will hopefully stimulate more research initiatives, funding, and critical insight into the already increasing demand for cytotoxicity researches that have been evidenced worldwide.

Poisoning in the Modern World - New Tricks for an Old Dog?

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ISBN: 9781838807856 9781838807863 9781838807870 Year: Pages: 128 DOI: 10.5772/intechopen.73906 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:53

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Over 400 years ago, Swiss alchemist and physician Paracelsus (1493-1541) cited: ""All substances are poisons; there is none that is not a poison. The right dose differentiates a poison from a remedy."" This is often condensed to: ""The dose makes the poison."" So, why are we overtly anxious about intoxications?In fact, poisons became a global problem with the industrial revolution. Pesticides, asbestos, occupational chemicals, air pollution, and heavy metal toxicity maintain high priority worldwide, especially in developing countries. Children between 0 and 5 years old are the most vulnerable to both acute and chronic poisonings, while older adults suffer from the chronic effects of chemicals. This book aims to raise awareness about the challenges of poisons, to help clinicians understand current issues in toxicology.

Cytotoxicity - Definition, Identification, and Cytotoxic Compounds

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ISBN: 9781789847543 9781789847550 9781839622861 Year: Pages: 118 DOI: 10.5772/intechopen.77899 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:53

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Compensating for cytotoxicity in the multicellular organism by a certain level of cellular proliferation is the primary aim of homeostasis. In addition, the loss of cellular proliferation control (tumorigenesis) is at least as important as cytotoxicity, however, it is a contrasting trauma. With the disruption of the delicate balance between cytotoxicity and proliferation, confrontation with cancer can inevitably occur. This book presents important information pertaining to the molecular control of the mechanisms of cytotoxicity and cellular proliferation as they relate to cancer. It is designed for students and researchers studying cytotoxicity and its control.

Toxicity and Drug Testing

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ISBN: 9789535100041 Year: Pages: 530 DOI: 10.5772/1976 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:48

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Modern drug design and testing involves experimental in vivo and in vitro measurement of the drug candidate's ADMET (adsorption, distribution, metabolism, elimination and toxicity) properties in the early stages of drug discovery. Only a small percentage of the proposed drug candidates receive government approval and reach the market place. Unfavorable pharmacokinetic properties, poor bioavailability and efficacy, low solubility, adverse side effects and toxicity concerns account for many of the drug failures encountered in the pharmaceutical industry. Authors from several countries have contributed chapters detailing regulatory policies, pharmaceutical concerns and clinical practices in their respective countries with the expectation that the open exchange of scientific results and ideas presented in this book will lead to improved pharmaceutical products.

Toxicology - New Aspects to This Scientific Conundrum

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ISBN: 9789535127161 9789535127178 Year: Pages: 218 DOI: 10.5772/62600 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:49

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This edited book, Toxicology - New Aspects to This Scientific Conundrum, is intended to provide an overview on the different xenobiotics employed every day in our anthropogenic activities. We hope that this book will continue to meet the expectations and needs of all interested in the implications for the living species of known and new toxicants and to guide them in the future investigations.

Genotoxicity - A Predictable Risk to Our Actual World

Authors: ---
ISBN: 9781789234183 9781789234190 Year: Pages: 122 DOI: 10.5772/intechopen.69556 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:51

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This book is designed to provide an overview of the different genotoxicants and their effects on living organisms, including humans. The contributions made by the specialists in this field of research are gratefully acknowledged. We hope that the information presented in this book will meet the expectations and needs of all those interested in the different aspects of the genotoxicity field. The publication of this book is of great importance to those scientists, pharmacologists, physicians and veterinarians, as well as engineers, teachers, graduate students and administrators of environmental programmes, who make use of these investigations to understand both the basic and applied genotoxic aspects of known and new xenobiotics, and to guide them in their future investigations.

Botulinum Toxin

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ISBN: 9781789841350 9781789841367 Year: Pages: 154 DOI: 10.5772/intechopen.73809 Language: English
Publisher: IntechOpen
Subject: Public Health
Added to DOAB on : 2019-10-03 07:51:52

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The aim of this book is to ensure a safe understanding and use of botulinum toxin in medicine. Known indications, contraindications, diversity, comparative effects between subtypes, limits, allergies, treatments, adverse reactions, nonresponsiveness, and new investigations will be described. Botulinum toxin can be currently used in nearly every specialty. The main areas in this book are cosmetics and dermatology, as well as dentistry, urology, masseter hypertrophy, chronic pain treatment, and others. The important aim is formation of the knowledge of anatomy, muscles to be treated and their function, risk factors, brand names, associations with operations, and other treatments.

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