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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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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.

Keywords

pharmacology --- toxicology

Drug Discovery and Development - Present and Future

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ISBN: 9789533076157 Year: Pages: 542 DOI: 10.5772/1179 Language: English
Publisher: InTechOpen
Subject: Therapeutics
Added to DOAB on : 2019-10-03 07:51:48

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Drug discovery and development process aims to make available medications that are safe and effective in improving the length and quality of life and relieving pain and suffering. However, the process is very complex, time consuming, resource intensive, requiring multi-disciplinary expertise and innovative approaches. There is a growing urgency to identify and develop more effective, efficient, and expedient ways to bring safe and effective products to the market. The drug discovery and development process relies on the utilization of relevant and robust tools, methods, models, and validated biomarkers that are predictive of clinical effects in terms of diagnosis, prevention, therapy, and prognosis. There is a growing emphasis on translational research, a bidirectional bench to the bedside approach, in an effort to improve the process efficiency and the need for further innovations. The authors in the book discuss the current and evolving state of drug discovery and development.

Topics on Drug Metabolism

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ISBN: 9789535100997 Year: Pages: 308 DOI: 10.5772/1180 Language: English
Publisher: InTechOpen
Subject: Therapeutics
Added to DOAB on : 2019-10-03 07:51:48

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In order to avoid late-stage drug failure due to factors such as undesirable metabolic instability, toxic metabolites, drug-drug interactions, and polymorphic metabolism, an enormous amount of effort has been expended by both the pharmaceutical industry and academia towards developing more powerful techniques and screening assays to identify the metabolic profiles and enzymes involved in drug metabolism. This book presents some in-depth reviews of selected topics in drug metabolism. Among the key topics covered are: the interplay between drug transport and metabolism in oral bioavailability; the influence of genetic and epigenetic factors on drug metabolism; impact of disease on transport and metabolism; and the use of novel microdosing techniques and novel LC/MS and genomic technologies to predict the metabolic parameters and profiles of potential new drug candidates.

Recent Advances in Novel Drug Carrier Systems

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ISBN: 9789535108108 9789535142683 Year: Pages: 514 DOI: 10.5772/2889 Language: English
Publisher: InTechOpen
Subject: Pharmacy and materia medica
Added to DOAB on : 2019-10-03 07:51:49

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This contribution book collects reviews and original articles from eminent experts working in the interdisciplinary arena of novel drug delivery systems and their uses. From their direct and recent experience, the readers can achieve a wide vision on the new and ongoing potentialities of different drug delivery systems. Since the advent of analytical techniques and capabilities to measure particle sizes in nanometer ranges, there has been tremendous interest in the use of nanoparticles for more efficient methods of drug delivery. On the other hand, this reference discusses advances in the design, optimization, and adaptation of gene delivery systems for the treatment of cancer, cardiovascular, pulmonary, genetic, and infectious diseases, and considers assessment and review procedures involved in the development of gene-based pharmaceuticals.

Epileptology - The Modern State of Science

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ISBN: 9789535126980 9789535126997 Year: Pages: 278 DOI: 10.5772/61409 Language: English
Publisher: InTechOpen
Subject: Neurology --- Pediatrics
Added to DOAB on : 2019-10-03 07:51:49

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Epilepsy seems to represent one of the most frequent neurological diseases and occurs in about 1% of the general population. Although epilepsy is known since antiquity, the precise data on its pathogenesis and effective treatment are still collected and nowadays represents an interest for neurologists and psychiatrists. Being a neurological disease, epilepsy is characterized by a broad palette of comorbid psychiatric disorders (affective and anxiety disorders, psychoses) that reduce the quality of life. Moreover, the risk of suicidal attempts in persons with epilepsy is much higher than in general population that once again increases the actuality of epilepsy research in many aspects. The book contains 13 chapters written by different authors from all over the world on different topics, including phenomenology, pathogenesis, and treatment in epilepsy. The modern data on these topics may be helpful for many specialists in the domain of epileptology.

Pain Relief - From Analgesics to Alternative Therapies

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ISBN: 9789535131878 9789535131885 Year: Pages: 362 DOI: 10.5772/63264 Language: English
Publisher: InTechOpen
Subject: Pharmacy and materia medica
Added to DOAB on : 2019-10-03 07:51:50

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Since the beginning of times, pain treatment has been the motive of research giving birth to multiple groups of pharmacological families and therapies. Pain perception is a construction built over the biological phenomenon of signal transduction surrounded by different factors such as gender, age, and sociocultural status, among others. The concept of pain as the solely biological manifestation of defense is nowadays considered as a narrow-minded view of this topic. In this regard concepts such as newborns feel no pain or older people complain about everything therefore should not be paid attention when referring pain, are being left behind in the understanding that pain alleviation is a human right and everybody feeling pain should be helped for its relief. This book comprises many aspects of pain treatment and the drugs involved in it. From old analgesics with new mechanisms of action for pain alleviation to analgesics potential for diminishing oxidative stress; from pharmacological therapies to electrical ones, going through alternative medicine; and from pain treatment in dentistry to chronic pain therapies, also boarding the treatment of migraine, different experts share their knowledge on the topic.

Seizures

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ISBN: 9781789230048 9781789230055 Year: Pages: 184 DOI: 10.5772/65137 Language: English
Publisher: InTechOpen
Subject: Neurology --- Pediatrics
Added to DOAB on : 2019-10-03 07:51:51

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This book contains selected peer-reviewed articles that cover novel information on epileptic seizure and psychogenic non-epileptic seizures written by international researchers. In this book, we discuss self-reporting technologies for supporting epilepsy treatment. We also discuss about the diagnostic testing in epilepsy genetic clinical practice. Clinical aspects related to diagnosis in patients presenting psychogenic non-epileptic seizures vs. epileptic seizures and neurocysticercosis are discussed as well. We delivered novel aspects about the treatment for pseudoseizures. In another chapter, the authors estimated the prevalence of ischemic stroke in epileptic patients presenting subarachnoid neurocysticercosis and ischemic stroke frequency among HIV-positive patients, and finally other authors discuss autoimmune epilepsy, its new development, and its future directions. We are looking forward with confidence and pride to the remarkable role that this book will play for a new vision and mission.

Capsaicin and its Human Therapeutic Development

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ISBN: 9781789235203 9781789235210 Year: Pages: 124 DOI: 10.5772/intechopen.73124 Language: English
Publisher: InTechOpen
Subject: Therapeutics
Added to DOAB on : 2019-10-03 07:51:51

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The enormous field of this topic is clearly shown by the following facts: during the last ten years (2007-2016) around 500 papers/ year and 523 review articles are listed in the PubMed database on capsaicin, and over 200/year are under keywords of ""capsaicin human"". Recently, two major studies on the mortality of consumers of spicy food containing capsaicin and nonconsumers (over 350000 men and women aged 30-79 with heart disease, cancer, and stroke at baseline over 3.5 million person-years, 2004-2013) showed that the relative risk in total mortality was reduced by 14% in 10 diverse geographic areas of China (2015). Similarly, in the USA, (16,179 participants during over 2,70,000 person/year with the median of 18.9 years) the total mortality was reduced by 13% in populations consuming hot chili (2017). Recently, the book series ""Progress in Drug Research"" the 68th volume dealt for the first time on ""Capsaicin as a Therapeutic Molecule"" (Springer, Basel, 2014). Five excellent chapters are found in this book dealing with procedures of capsaicin from capsicum plants, emerging technologies to improve capsaicin delivery, capsaicinoid diversity and its human food preference, capsaicin and lipid metabolism, and predictors in treatment response to capsaicin. The results of these observations clearly indicate that the capsaicin research has changed direction to include human medical treatment with capsaicin. The book gathers knowledge from experts in basic and clinical sciences, pharmacologists, in the nutrition and food industry, in the drug industry, technologists, plant cultivators, as well as experts across a wide scale of medical branches.

Molecular Insight of Drug Design

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ISBN: 9781789236323 9781789236330 Year: Pages: 130 DOI: 10.5772/intechopen.71744 Language: English
Publisher: InTechOpen
Subject: Therapeutics
Added to DOAB on : 2019-10-03 07:51:51

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The approaches in drug design are mainly comprised of these three multidisciplinary sciences. First, Bioinformatics has successfully gather biological data in form of biomolecular sequences, in order to construct knowledge on drug and vaccine design. It is of considerable importance for drug designers to comprehend the utilization of bioinformatics tools for resolving their research questions. Second, Nanotechnology has made possible the design and delivery of the nano-based drug. Third, Pharmaceutical Chemistry made it possible to investigate the adsorption, distribution, metabolism, and toxicology of the drug candidates in a fine-grained resolution.

Drug Discovery - Concepts to Market

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ISBN: 9781789236965 9781789236972 Year: Pages: 192 DOI: 10.5772/intechopen.70151 Language: English
Publisher: InTechOpen
Subject: Therapeutics
Added to DOAB on : 2019-10-03 07:51:52

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The book ""Drug Discovery - Concepts to Market"" is a collection of reviewed and relevant research chapters, offering a comprehensive overview of recent developments in the latest drug discovery trends that have been revolutionized with up-to-date technological developments. This book comprises single chapters authored by various researchers and edited by an expert active in the drug development research area. All chapters are independently complete but united under a common research study topic. This publication aims to provide a thorough overview of the latest research efforts in this field from international authors and open new possible research paths for further novel developments.

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