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The Organic Chemistry of Drug Design and Drug Action
Author | : Richard B. Silverman |
Publisher | : Academic Press |
Total Pages | : 537 |
Release | : 2014-03-29 |
Genre | : Medical |
ISBN | : 0123820316 |
The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition includes updates to all chapters, including new examples and references. It reflects significant changes in the process of drug design over the last decade and preserves the successful approach of the previous editions while including significant changes in format and coverage. This text is designed for undergraduate and graduate students in chemistry studying medicinal chemistry or pharmaceutical chemistry; research chemists and biochemists working in pharmaceutical and biotechnology industries. - Updates to all chapters, including new examples and references - Chapter 1 (Introduction): Completely rewritten and expanded as an overview of topics discussed in detail throughout the book - Chapter 2 (Lead Discovery and Lead Modification): Sections on sources of compounds for screening including library collections, virtual screening, and computational methods, as well as hit-to-lead and scaffold hopping; expanded sections on sources of lead compounds, fragment-based lead discovery, and molecular graphics; and deemphasized solid-phase synthesis and combinatorial chemistry - Chapter 3 (Receptors): Drug-receptor interactions, cation-p and halogen bonding; atropisomers; case history of the insomnia drug suvorexant - Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug discovery and enzyme synthesis - Chapter 5 (Enzyme Inhibition and Inactivation): New case histories: - for competitive inhibition, the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor, imatinib - for transition state analogue inhibition, the purine nucleoside phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the mechanism of the multisubstrate analog inhibitor isoniazid - for slow, tight-binding inhibition, the dipeptidyl peptidase-4 inhibitor, saxagliptin - Chapter 7 (Drug Resistance and Drug Synergism): This new chapter includes topics taken from two chapters in the previous edition, with many new examples - Chapter 8 (Drug Metabolism): Discussions of toxicophores and reactive metabolites - Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of antibody–drug conjugates
Small-Molecule Inhibitors of Protein-Protein Interactions
Author | : Lyubomir Vassilev |
Publisher | : Springer Science & Business Media |
Total Pages | : 180 |
Release | : 2011-01-18 |
Genre | : Medical |
ISBN | : 3642170838 |
In this volume, the editors have collected the knowledgeable insights of a number of leaders in this field - researchers who have achieved success in addressing the difficult problem of inhibiting protein-protein interactions. These researchers describe their unique approaches, and share experiences, results, thoughts, and opinions. The content of the articles is rich, and in terms of scope ranges from generalized approaches to specific case studies. There are various focal points, including methodologies and the molecules themselves. Ultimately, there are numerous lessons to be taken away from this collection, and the editors hope that this snapshot of the current state of the art in developing protein-protein inhibitors not only pays tribute to the past successes, but also generates excitement about the future potential of this field
Peptides
Author | : Norbert Sewald |
Publisher | : Wiley-VCH Verlag GmbH |
Total Pages | : 562 |
Release | : 2002-01-01 |
Genre | : Science |
ISBN | : 9783527304059 |
Peptides play a decisive role in many physiological processes, whether as neurotransmitters, hormones or antibiotics. The rapid developments in peptide research over the past few decades make it almost impossible for newcomers to gain an overview. This means an easily comprehensible yet concise introduction is vital. This unique work covers all the important aspects of this wide-ranging field in one handy volume. On the basis of the fundamental chemical and structural properties of peptides, this reference runs the gamut from analysis, the occurrence and biological importance of peptides, via chemical, biochemical and genetic methods of peptide synthesis, right up to peptide libraries, peptide design and their role in drug research. Yet this book offers much more than a mere overview of the latest level of research. An encyclopedic appendix with valuable data on more than 500 biological relevant peptides and proteins, a comprehensive register and details of further literature references make this the ideal reference for all questions regarding peptide research. For newcomers and specialists alike. On the basis of the fundamental chemical and structural properties of peptides, this reference runs the gamut from analysis, the occurrence and biological importance of peptides.
Supramolecular Protein Chemistry
Author | : Peter B Crowley |
Publisher | : Royal Society of Chemistry |
Total Pages | : 329 |
Release | : 2020-12-09 |
Genre | : Science |
ISBN | : 1788019806 |
Building on decades of “host-guest” research, recent years have seen a surge of activity in water-soluble supramolecular receptors for protein recognition and assembly. Progress has been particularly rich in the area of calixarenes, cucurbiturils and molecular tweezers. Emerging applications include controlled protein assembly in solution, crystal engineering, supramolecular control of catalysis (both in vitro and in vivo), as well as novel mechanisms of protein-interaction inhibition with relevance to amyloids and disease. One challenge at the interface of supramolecular chemistry and protein science is to increase interaction and collaboration between chemists and biochemists/structural biologists.This book addresses the exciting interface of supramolecular chemistry and protein science. Chapters cover supramolecular approaches to protein recognition, assembly and regulation. Principles outlined will highlight the opportunities that are readily accessible to collaborating chemists and biochemists, enriching the breadth and scope of this multidisciplinary field. Supramolecular Protein Chemistry will be of particular interest to graduate students and researchers working in supramolecular chemistry, protein science, self-assembly, biomaterials, biomedicine and biotechnology.
Inhibitors of Protein–Protein Interactions
Author | : Ali Tavassoli |
Publisher | : Royal Society of Chemistry |
Total Pages | : 357 |
Release | : 2020-12-07 |
Genre | : Science |
ISBN | : 178801569X |
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.
Peptidomimetics I
Author | : William D. Lubell |
Publisher | : Springer |
Total Pages | : 322 |
Release | : 2017-06-29 |
Genre | : Science |
ISBN | : 3319491199 |
The series Topics in Heterocyclic Chemistry presents critical reviews on present and future trends in the research of heterocyclic compounds. Overall the scope is to cover topics dealing with all areas within heterocyclic chemistry, both experimental and theoretical, of interest to the general heterocyclic chemistry community. The series consists of topic related volumes edited by renowned editors with contributions of experts in the field. All chapters from Topics in Heterocyclic Chemistry are published Online First with an individual DOI. In references, Topics in Heterocyclic Chemistry is abbreviated as Top Heterocycl Chem and cited as a journal.
Essentials of Medical Biochemistry
Author | : Chung Eun Ha |
Publisher | : Academic Press |
Total Pages | : 600 |
Release | : 2011-01-28 |
Genre | : Science |
ISBN | : 0080916880 |
Expert biochemist N.V. Bhagavan's new work condenses his successful Medical Biochemistry texts along with numerous case studies, to act as an extensive review and reference guide for both students and experts alike. The research-driven content includes four-color illustrations throughout to develop an understanding of the events and processes that are occurring at both the molecular and macrolecular levels of physiologic regulation, clinical effects, and interactions. Using thorough introductions, end of chapter reviews, fact-filled tables, and related multiple-choice questions, Bhagavan provides the reader with the most condensed yet detailed biochemistry overview available. More than a quick survey, this comprehensive text includes USMLE sample exams from Bhagavan himself, a previous coauthor. - Clinical focus emphasizing relevant physiologic and pathophysiologic biochemical concepts - Interactive multiple-choice questions to prep for USMLE exams - Clinical case studies for understanding basic science, diagnosis, and treatment of human diseases - Instructional overview figures, flowcharts, and tables to enhance understanding