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Enzyme Inhibitors

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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.

Enzyme activation.

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This book is an introduction to the language of systems biology, which is spoken among many disciplines, from biology to engineering. Authors Thomas Sauter and Marco Albrecht draw on a multidisciplinary background and evidence-based learning to facilitate the understanding of biochemical networks, metabolic modeling and system dynamics. Their pedagogic approach briefly highlights core ideas of concepts in a broader interdisciplinary framework to guide a more effective deep dive thereafter. The learning journey starts with the purity of mathematical concepts, reveals its power to connect biological entities in structure and time, and finally introduces physics concepts to tightly align abstraction with reality. This workbook is all about self-paced learning, supports the flipped-classroom concept, and kick-starts with scientific evidence on studying. Each chapter comes with links to external YouTube videos, learning checklists, and Integrated real-world examples to gain confidence in thinking across scientific perspectives. The result is an integrated approach that opens a line of communication between theory and application, enabling readers to actively learn as they read. This overview of capturing and analyzing the behavior of biological systems will interest adherers of systems biology and network analysis, as well as related fields such as bioinformatics, biology, cybernetics, and data science.

Biomathematics. --- Enzyme kinetics. --- Metabolism.

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Enzyme activation --- Phagocytosis --- Phosphoinositides

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Immunoassay techniques have become essential in various fields of pure and applied research. This volume of the well known Laboratory Techniques series will be of assistance to those who have plans or are making efforts to develop ultrasensitive enzyme immunoassays for antigens and antibodies. The volume describes factors limiting the sensitivity of noncompetitive solid phase enzyme immunoassays, methods to overcome difficulties limiting sensitivities, methods to perform ultrasensitive enzyme immunoassays as rapidly as possible, and protocols of enzyme labeling and enzyme assays as

Enzymes --- Enzyme activity --- antibodies --- Immunoenzyme techniques --- Enzyme-linked immunosorbent assay --- Molecular biology --- Technique. --- ELISA --- Enzyme immunoassay --- Enzyme labeled antibody technique --- Enzyme labeled immunoassay --- Enzyme linked immunoassay --- Enzyme linked immunospecific assay --- Immunoassay, Enzyme --- Immunoenzymometric assay --- Immunoenzyme technique --- Solid-phase analysis