Peptide And Peptidomimetic Therapeutics

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Peptide and Peptidomimetic Therapeutics

Author : Nir Qvit
Publisher : Academic Press
ISBN 13 : 0128204478
Total Pages : 792 pages
Book Rating : 4.1/5 (282 download)

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Book Synopsis Peptide and Peptidomimetic Therapeutics by : Nir Qvit

Download or read book Peptide and Peptidomimetic Therapeutics written by Nir Qvit and published by Academic Press. This book was released on 2022-09-22 with total page 792 pages. Available in PDF, EPUB and Kindle. Book excerpt: Peptide and Peptidomimetic Therapeutics: From Bench to Beside offers applied, evidence-based instruction on developing and applying peptide therapeutics in disease treatment, driving drug discovery, and improving patient care. Here, researchers, clinicians and students will find tools to harness the full power of peptides and peptidomimetics and improve bioavailability, stability, efficiency and selectivity of new therapeutics and their application in treatment plans. More than 20 leaders in the field share their approaches for identifying and advancing peptide and peptidomimetic therapeutics. Topics examined run from "bench to bedside," beginning with fundamental peptide science, protein-protein interactions and peptide synthesis. Later chapters examine modes for peptide drug delivery, including cell penetration peptide and peptidomimetic delivery, as well as the targeting of specific disease types, peptide therapeutics as applied to infectious disease, cancer, metabolic disorders, neurodegenerative disorders, and skin disorders, and antiparasitic and immunosuppressive peptidomimetics. - Helps researchers and clinicians harness the full of power of peptides and peptidomimetics in their daily work and drug discovery - Features chapters running from "bench to bedside, providing a thorough grounding in fundamental peptide science, drug delivery methods, and targeting of specific disease types - Features chapter contributions from international leaders in peptide science and drug development

Advances in Peptide and Peptidomimetic Design Inspiring Basic Science and Drug Discovery

Author : Henry I. Mosberg
Publisher : MDPI
ISBN 13 : 3039282883
Total Pages : 406 pages
Book Rating : 4.0/5 (392 download)

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Book Synopsis Advances in Peptide and Peptidomimetic Design Inspiring Basic Science and Drug Discovery by : Henry I. Mosberg

Download or read book Advances in Peptide and Peptidomimetic Design Inspiring Basic Science and Drug Discovery written by Henry I. Mosberg and published by MDPI. This book was released on 2020-03-13 with total page 406 pages. Available in PDF, EPUB and Kindle. Book excerpt: Advances in Peptide and Peptidomimetic Design Inspiring Basic Science and Drug Discovery is a book dedicated to Prof. Victor J. Hruby on the occasion of his 80th birthday. This book includes twenty contributions from authors representing diverse multidisciplinary fields of scientific expertise, and is focused on the extraordinary potential of peptides and peptidomimetics as a surging therapeutic modality and as tools for basic research and technology development.

Mid-size Drugs Based on Peptides and Peptidomimetics

Author : Hirokazu Tamamura
Publisher : Springer
ISBN 13 : 981107691X
Total Pages : 113 pages
Book Rating : 4.8/5 (11 download)

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Book Synopsis Mid-size Drugs Based on Peptides and Peptidomimetics by : Hirokazu Tamamura

Download or read book Mid-size Drugs Based on Peptides and Peptidomimetics written by Hirokazu Tamamura and published by Springer. This book was released on 2018-01-16 with total page 113 pages. Available in PDF, EPUB and Kindle. Book excerpt: This brief describes studies conducted by the authors on mid-size drugs utilizing peptides and peptidomimetics, and on the development of anti-HIV agents. Peptides are important biological molecules and have various physiological actions. Peptide-based drug discovery may help bring about the development of useful medicines that are highly safe and show potent pharmacological effects in small doses. Recently, it has been shown that there is an important drug-like space in the mid-sized region between low- and high-molecular-weight compounds. Thus, mid-size drugs such as peptide compounds are being focused on. To date, several peptidomimetics that mimic primary, secondary, and tertiary structures of peptides have been developed to maintain and improve biological activities and actions of peptides. In this book, the features and advantages of mid-size drugs are described in detail. In addition, the merits of utilizing peptidomimetics in the development of mid-size drugs are referred to. Understanding such peptide-derived mid-size drugs will lead to a comprehensive expansion of medicinal chemistry.

Peptide-based Drug Discovery

Author : Ved Srivastava
Publisher : Royal Society of Chemistry
ISBN 13 : 1782627324
Total Pages : 589 pages
Book Rating : 4.7/5 (826 download)

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Book Synopsis Peptide-based Drug Discovery by : Ved Srivastava

Download or read book Peptide-based Drug Discovery written by Ved Srivastava and published by Royal Society of Chemistry. This book was released on 2017-06-26 with total page 589 pages. Available in PDF, EPUB and Kindle. Book excerpt: With potentially high specificity and low toxicity, biologicals offer promising alternatives to small-molecule drugs. Peptide therapeutics have again become the focus of innovative drug development efforts backed up by a resurgence of venture funds and small biotechnology companies. What does it take to develop a peptide-based medicine? What are the key challenges and how are they overcome? What are emerging therapeutics for peptide modalities? This book answers these questions with a holistic story from molecules to medicine, combining the themes of design, synthesis and clinical applications of peptide-based therapeutics and biomarkers. Chapters are written and edited by leaders in the field from industry and academia and they cover the pharmacokinetics of peptide therapeutics, attributes necessary for commercially successful metabolic peptides, medicinal chemistry strategies for the design of peptidase-resistant peptide analogues, disease classes for which peptide therapeutic are most relevant, and regulatory issues and guidelines. The critical themes covered provide essential background information on what it takes to develop peptide-based medicine from a chemistry perspective and views on the future of peptide drugs. This book will be a valuable resource not only as a reference book for the researcher engaged in academic and pharmaceutical setting, from basic research to manufacturing and from organic chemistry to biotechnology, but also a valuable resource to graduate students to understand discovery and development process for peptide-based medicine.

Peptidomimetics in Organic and Medicinal Chemistry

Author : Antonio Guarna
Publisher : John Wiley & Sons
ISBN 13 : 1119950600
Total Pages : 334 pages
Book Rating : 4.1/5 (199 download)

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Book Synopsis Peptidomimetics in Organic and Medicinal Chemistry by : Antonio Guarna

Download or read book Peptidomimetics in Organic and Medicinal Chemistry written by Antonio Guarna and published by John Wiley & Sons. This book was released on 2014-04-07 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt: A peptidomimetic is a small protein-like chain designed to mimic a peptide with adjusted molecular properties such as enhanced stability or biological activity. It is a very powerful approach for the generation of small-molecule-based drugs as enzyme inhibitors or receptor ligands. Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature. Topics covered include the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery.

Handbook of In Vivo Chemistry in Mice

Author : Katsunori Tanaka
Publisher : John Wiley & Sons
ISBN 13 : 3527344322
Total Pages : 560 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Handbook of In Vivo Chemistry in Mice by : Katsunori Tanaka

Download or read book Handbook of In Vivo Chemistry in Mice written by Katsunori Tanaka and published by John Wiley & Sons. This book was released on 2020-04-27 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: Provides timely, comprehensive coverage of in vivo chemical reactions within live animals This handbook summarizes the interdisciplinary expertise of both chemists and biologists performing in vivo chemical reactions within live animals. By comparing and contrasting currently available chemical and biological techniques, it serves not just as a collection of the pioneering work done in animal-based studies, but also as a technical guide to help readers decide which tools are suitable and best for their experimental needs. The Handbook of In Vivo Chemistry in Mice: From Lab to Living System introduces readers to general information about live animal experiments and detection methods commonly used for these animal models. It focuses on chemistry-based techniques to develop selective in vivo targeting methodologies, as well as strategies for in vivo chemistry and drug release. Topics include: currently available mouse models; biocompatible fluorophores; radionuclides for radiodiagnosis/radiotherapy; live animal imaging techniques such as positron emission tomography (PET) imaging; magnetic resonance imaging (MRI); ultrasound imaging; hybrid imaging; biocompatible chemical reactions; ligand-directed nucleophilic substitution chemistry; biorthogonal prodrug release strategies; and various selective targeting strategies for live animals. -Completely covers current techniques of in vivo chemistry performed in live animals -Describes general information about commonly used live animal experiments and detection methods -Focuses on chemistry-based techniques to develop selective in vivo targeting methodologies, as well as strategies for in vivo chemistry and drug release -Places emphasis on material properties required for the development of appropriate compounds to be used for imaging and therapeutic purposes in preclinical applications Handbook of In Vivo Chemistry in Mice: From Lab to Living System will be of great interest to pharmaceutical chemists, life scientists, and organic chemists. It will also appeal to those working in the pharmaceutical and biotechnology industries.

Peptide and Protein Drug Analysis

Author : Ronald Reid
Publisher : CRC Press
ISBN 13 : 9781420001334
Total Pages : 926 pages
Book Rating : 4.0/5 (13 download)

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Book Synopsis Peptide and Protein Drug Analysis by : Ronald Reid

Download or read book Peptide and Protein Drug Analysis written by Ronald Reid and published by CRC Press. This book was released on 1999-11-12 with total page 926 pages. Available in PDF, EPUB and Kindle. Book excerpt: Furthering efforts to simulate the potency and specificity exhibited by peptides and proteins in healthy cells, this remarkable reference supplies pharmaceutical scientists with a wealth of techniques for tapping the enormous therapeutic potential of these molecules-providing a solid basis of knowledge for new drug design. Provides a broad, comprehensive overview of peptides and proteins as mediators of cell movement, proliferation, differentiation, and communication. Written by more than 50 leading international authorities, Peptides and Protein Drug Analysis discusses strategies for dealing with the complexity of peptides and proteins in conformational flexibility and amino acid sequence variability analyzes drug formulations facilitated by solid-phase peptide synthesis and recombinant DNA technology examines chemical purity analysis by high-pressure chromatographic, capillary electrophoretic, gel electrophoretic, and isoelectric focusing methods highlights drug design elements derived from protein folding, bioinformatics, and computational chemistry demonstrates uses of unnatural mutagenesis and combinatorial chemistry explores mass spectrometry, protein sequence, and carbohydrate analysis illustrates bioassays and other new functional analysis methods surveys spectroscopic techniques such as ultraviolet, fluorescence, Fourier transform infrared, and nuclear magnetic resonance (NMR) addresses ways of distinguishing between levels of therapeutic and endogenous agents in cells reviews structural analysis tools such as ultracentrifugation and light, X-ray, and neutron scattering and more! Featuring over 3400 bibliographic citations and more than 500 tables, equations, and illustrations, Peptide and Protein Drug Analysis is a must-read resource for pharmacists; pharmacologists; analytical, organic, and pharmaceutical chemists; cell and molecular biologists; biochemists; and upper-level undergraduate and graduate students in these disciplines.

Practical Medicinal Chemistry with Macrocycles

Author : Eric Marsault
Publisher : John Wiley & Sons
ISBN 13 : 1119092566
Total Pages : 617 pages
Book Rating : 4.1/5 (19 download)

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Book Synopsis Practical Medicinal Chemistry with Macrocycles by : Eric Marsault

Download or read book Practical Medicinal Chemistry with Macrocycles written by Eric Marsault and published by John Wiley & Sons. This book was released on 2017-09-12 with total page 617 pages. Available in PDF, EPUB and Kindle. Book excerpt: Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations

Cosmetic Dermatology

Author : Zoe Diana Draelos
Publisher : John Wiley & Sons
ISBN 13 : 111865546X
Total Pages : 34 pages
Book Rating : 4.1/5 (186 download)

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Book Synopsis Cosmetic Dermatology by : Zoe Diana Draelos

Download or read book Cosmetic Dermatology written by Zoe Diana Draelos and published by John Wiley & Sons. This book was released on 2015-10-14 with total page 34 pages. Available in PDF, EPUB and Kindle. Book excerpt: Back for a new edition, Zoe Draelos' outstanding resource to cosmetic dermatology again provides a highly-illustrated, clinical guide to the full range of cosmetic skin treatments. Bringing together experts from research, industry, surgery and practice, it is structured in four distinct parts for easy navigation by the busy clinician: Basic Concepts - giving an overview of the physiology pertinent to cosmetic dermatology and the delivery systems by which treatments can take effect; Hygiene Products - evaluating cleansing and moisturising products; Adornment - looking at aesthetic techniques such as cosmetics, nail protheses and hair treatment; Antiaging - ie, injectables, resurfacing and skin contouring techniques, and the rapidly growing area of Cosmeceuticals. With over 300 high-quality images and key summary boxes throughout, this new edition incorporates the newest procedural innovations in this rapidly developing field. Perfect for all dermatologists, especially those specialising in cosmetic dermatology and whether hospital-based or in private practice, it provides the complete cosmetic regimen for your patients and will be an indispensable tool to consult over and over again.

Antiviral Drug Discovery and Development

Author : Xinyong Liu
Publisher : Springer Nature
ISBN 13 : 9811602670
Total Pages : 357 pages
Book Rating : 4.8/5 (116 download)

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Book Synopsis Antiviral Drug Discovery and Development by : Xinyong Liu

Download or read book Antiviral Drug Discovery and Development written by Xinyong Liu and published by Springer Nature. This book was released on 2021-07-13 with total page 357 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book summarizes state-of-the-art antiviral drug design and discovery approaches starting from natural products to de novo design, and provides a timely update on recently approved antiviral drugs and compounds in advanced clinical development. Special attention is paid to viral infections with a high impact on the world population or highly relevant from the public health perspective (HIV, hepatitis C, influenza virus, etc.). In these chapters, limitations associated with adverse effects and emergence of drug resistance are discussed in detail. In addition to classical antiviral strategies, chapters will be dedicated to discuss the non-classical drug development strategies to block viral infection, for instance, allosteric inhibitors, covalent antiviral agents, or antiviral compounds targeting protein–protein interactions. Finally, current prospects for producing broad-spectrum antiviral inhibitors will be also addressed. The book is distinctive in providing the most recent update in the rapidly evolving field of antiviral therapeutics. Authoritative reviews are written by international scientists well known for their contributions in their topics of research, which makes this book suitable for researchers not only within the antiviral research community but also attractive to a broad audience in the drug discovery field. This book covers molecular structures and biochemical mechanisms mediating the antiviral effects, while discussing various ligand design strategies, which include traditional medicinal chemistry, computational chemistry, and chemical biology approaches. The book provides a comprehensive review of antiviral drug discovery and development approaches, particularly focusing on current innovations and future trends.

Fmoc Solid Phase Peptide Synthesis

Author : W. Chan
Publisher : OUP Oxford
ISBN 13 : 0199637245
Total Pages : 371 pages
Book Rating : 4.1/5 (996 download)

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Book Synopsis Fmoc Solid Phase Peptide Synthesis by : W. Chan

Download or read book Fmoc Solid Phase Peptide Synthesis written by W. Chan and published by OUP Oxford. This book was released on 1999-12-16 with total page 371 pages. Available in PDF, EPUB and Kindle. Book excerpt: Since the publication of Atherton and Sheppard's volume, the technique of Fmoc solid-phase peptide synthesis has matured considerably and is now the standard approach for the routine production of peptides. The focus of this new volume is much broader, and covers the essential procedures.

Innovative Dosage Forms

Author : Yogeshwar Bachhav
Publisher : John Wiley & Sons
ISBN 13 : 3527343962
Total Pages : 470 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Innovative Dosage Forms by : Yogeshwar Bachhav

Download or read book Innovative Dosage Forms written by Yogeshwar Bachhav and published by John Wiley & Sons. This book was released on 2019-12-04 with total page 470 pages. Available in PDF, EPUB and Kindle. Book excerpt: Teaches future and current drug developers the latest innovations in drug formulation design and optimization This highly accessible, practice-oriented book examines current approaches in the development of drug formulations for preclinical and clinical studies, including the use of functional excipients to enhance solubility and stability. It covers oral, intravenous, topical, and parenteral administration routes. The book also discusses safety aspects of drugs and excipients, as well as regulatory issues relevant to formulation. Innovative Dosage Forms: Design and Development at Early Stage starts with a look at the impact of the polymorphic form of drugs on the preformulation and formulation development. It then offers readers reliable strategies for the formulation development of poorly soluble drugs. The book also studies the role of reactive impurities from the excipients on the formulation shelf life; preclinical formulation assessment of new chemical entities; and regulatory aspects for formulation design. Other chapters cover innovative formulations for special indications, including oncology injectables, delayed release and depot formulations; accessing pharmacokinetics of various dosage forms; physical characterization techniques to assess amorphous nature; novel formulations for protein oral dosage; and more. -Provides information that is essential for the drug development effort -Presents the latest advances in the field and describes in detail innovative formulations, such as nanosuspensions, micelles, and cocrystals -Describes current approaches in early pre-formulation to achieve the best in vivo results -Addresses regulatory and safety aspects, which are key considerations for pharmaceutical companies -Includes case studies from recent drug development programs to illustrate the practical challenges of preformulation design Innovative Dosage Forms: Design and Development at Early Stage provides valuable benefits to interdisciplinary drug discovery teams working in industry and academia and will appeal to medicinal chemists, pharmaceutical chemists, and pharmacologists.

Inhibitors of Protein–Protein Interactions

Author : Ali Tavassoli
Publisher : Royal Society of Chemistry
ISBN 13 : 178801569X
Total Pages : 357 pages
Book Rating : 4.7/5 (88 download)

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Book Synopsis Inhibitors of Protein–Protein Interactions by : Ali Tavassoli

Download or read book Inhibitors of Protein–Protein Interactions written by Ali Tavassoli and published by Royal Society of Chemistry. This book was released on 2020-12-07 with total page 357 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein-protein interactions (PPI) are at the heart of the majority of cellular processes, and are frequently dysregulated or usurped in disease. Given this central role, the inhibition of PPIs has been of significant interest as a means of treating a wide variety of diseases. However, there are inherent challenges in developing molecules capable of disrupting the relatively featureless and large interfacial areas involved. Despite this, there have been a number of successes in this field in recent years using both traditional drug discovery approaches and innovative, interdisciplinary strategies using novel chemical scaffolds. This book comprehensively covers the various aspects of PPI inhibition, encompassing small molecules, peptidomimetics, cyclic peptides, stapled peptides and macrocycles. Illustrated throughout with successful case studies, this book provides a holistic, cutting-edge view of the subject area and is ideal for chemical biologists and medicinal chemists interested in developing PPI inhibitors.

Nanostructures for Novel Therapy

Author : Denisa Ficai
Publisher : Elsevier
ISBN 13 : 0323461484
Total Pages : 908 pages
Book Rating : 4.3/5 (234 download)

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Book Synopsis Nanostructures for Novel Therapy by : Denisa Ficai

Download or read book Nanostructures for Novel Therapy written by Denisa Ficai and published by Elsevier. This book was released on 2017-02-25 with total page 908 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nanostructures for Novel Therapy: Synthesis, Characterization and Applications focuses on the fabrication and characterization of therapeutic nanostructures, in particular, synthesis, design, and in vitro and in vivo therapeutic evaluation. The chapters provide a cogent overview of recent therapeutic applications of nanostructured materials that includes applications of nanostructured materials for wound healing in plastic surgery and stem cell therapy. The book explores the promise for more effective therapy through the use of nanostructured materials, while also assessing the challenges their use might pose from both an economic and medicinal point of view. This innovative look at how nanostructured materials are used in therapeutics will be of great benefit to researchers, providing a greater understanding of the different ways nanomaterials could improve medical treatment, along with a discussion of the obstacles that need to be overcome in order to guarantee widespread availability. - Outlines how the characteristics of nanostructures made from different materials gives particular properties that can be successfully used in therapeutics - Compares the properties of different nanostructures, allowing medicinal chemists and engineers to select which are most appropriate for their needs - Highlights new uses of nanostructures within the therapeutic field, enabling the discovery of new, more effective drugs

Structure-based Design of Drugs and Other Bioactive Molecules

Author : Arun K. Ghosh
Publisher : John Wiley & Sons
ISBN 13 : 3527333657
Total Pages : 474 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Structure-based Design of Drugs and Other Bioactive Molecules by : Arun K. Ghosh

Download or read book Structure-based Design of Drugs and Other Bioactive Molecules written by Arun K. Ghosh and published by John Wiley & Sons. This book was released on 2014-08-11 with total page 474 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use numerous examples of recently developed drugs to present "best practice" methods in structurebased drug design with both newcomers and practicing researchers in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design. This book is aimed at new and active medicinal chemists, biochemists, pharmacologists, natural product chemists and those working in drug discovery in the pharmaceutical industry. It is highly recommended as a desk reference to guide students in medicinal and chemical sciences as well as to aid researchers engaged in drug design today.

Chemical Epigenetics

Author : Antonello Mai
Publisher : Springer Nature
ISBN 13 : 3030429822
Total Pages : 569 pages
Book Rating : 4.0/5 (34 download)

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Book Synopsis Chemical Epigenetics by : Antonello Mai

Download or read book Chemical Epigenetics written by Antonello Mai and published by Springer Nature. This book was released on 2020-03-31 with total page 569 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.

Small Molecule Drug Discovery

Author : Andrea Trabocchi
Publisher : Elsevier
ISBN 13 : 0128183500
Total Pages : 358 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Small Molecule Drug Discovery by : Andrea Trabocchi

Download or read book Small Molecule Drug Discovery written by Andrea Trabocchi and published by Elsevier. This book was released on 2019-11-23 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: Small Molecule Drug Discovery: Methods, Molecules and Applications presents the methods used to identify bioactive small molecules, synthetic strategies and techniques to produce novel chemical entities and small molecule libraries, chemoinformatics to characterize and enumerate chemical libraries, and screening methods, including biophysical techniques, virtual screening and phenotypic screening. The second part of the book gives an overview of privileged cyclic small molecules and major classes of natural product-derived small molecules, including carbohydrate-derived compounds, peptides and peptidomimetics, and alkaloid-inspired compounds. The last section comprises an exciting collection of selected case studies on drug discovery enabled by small molecules in the fields of cancer research, CNS diseases and infectious diseases. The discovery of novel molecular entities capable of specific interactions represents a significant challenge in early drug discovery. Small molecules are low molecular weight organic compounds that include natural products and metabolites, as well as drugs and other xenobiotics. When the biological target is well defined and understood, the rational design of small molecule ligands is possible. Alternatively, small molecule libraries are being used for unbiased assays for complex diseases where a target is unknown or multiple factors contribute to a disease pathology. - Outlines modern concepts and synthetic strategies underlying the building of small molecules and their chemical libraries useful for drug discovery - Provides modern biophysical methods to screening small molecule libraries, including high-throughput screening, small molecule microarrays, phenotypic screening and chemical genetics - Presents the most advanced chemoinformatics tools to characterize the structural features of small molecule libraries in terms of chemical diversity and complexity, also including the application of virtual screening approaches - Gives an overview of structural features and classification of natural product-derived small molecules, including carbohydrate derivatives, peptides and peptidomimetics, and alkaloid-inspired small molecules