Practical Medicinal Chemistry with Macrocycles


Book Description

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




AACR 2019 Proceedings: Abstracts 2749-5314


Book Description

American Association for Cancer Research 2019 Proceedings: Abstracts 2749-5314 - Part B




CPP, Cell-Penetrating Peptides


Book Description

In this book, a summary and update of the most important areas of cell-penetrating peptides (CPP) research are presented, while raising relevant questions for further development. The CPP sequences are presented and discussed throughout the book. The methods for testing CPP mechanisms are discussed in detail. Various approaches for the testing of endocytotic pathways of CPP uptake are also described. Different CPP uptake experiments are compared since it is becoming clear that it is often best to apply several methods in a complementary manner in order to most comprehensively evaluate CPP uptake mechanisms due to the complexity of these processes. A brief summary of functionality issues of CPPs, both in vitro and in vivo, is discussed. Therapeutic potential of CPPs and commercial developments are discussed. The present, second edition of this book is the updated and expanded version of the first edition, published in 2019. The development of the field of cell-penetrating peptides in these five years has been obvious and exciting. This second edition of the book has been partly reorganized and comprehensively expanded with the exciting research in 2019-2023. Around 2500 novel scientific articles have become available, most of them are reviewed in the second edition. Additional rapidly growing areas of high impact presented in this second edition are therapeutic developments (Chapter 16) and delivery of oligonucleotides and proteins/peptides (Chapters 5 and 6) including novel reports on genome editing with CPP assistance. Also, several additional examples are available now on clinical trials using CPPs (Chapter 15). The book is written for researchers and students in the field.




Handbook of In Vivo Chemistry in Mice


Book Description

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.




Cell-Penetrating Peptides


Book Description

Cell-Penetrating Peptides The definitive reference on the rational design of cell-penetrating peptides enables readers to develop tailor-made peptides for their specific needs. In recent years, cell-penetrating peptides (CPPs) have become valuable tools for the cellular delivery of proteins, nucleic acids, and drugs. These small peptide sequences can be artificially designed and synthesized with custom-made characteristics to mediate the efficient and non-toxic transport of biomolecules, drugs, or nanoparticles into the cell. Cell-Penetrating Peptides: Design, Development, and Applications provides an up-to-date account of the development and use of CPPs for delivering membrane-impermeable bioactive molecules into cells. Bringing together contributions from leading researchers from around the world, this comprehensive volume describes the characteristics and mechanisms of CPPs as well as their application in both medicine, biotechnology and agriculture. Covers rational design and development of cell-penetrating peptides for use in cellular delivery of small molecule drugs, proteins, nucleic acids, and nanoparticles Presents the chemical and biological characteristics of CPP action in vitro and in vivo Describes the structure and design principles of both synthetic and naturally occurring CPPs Discusses key medical applications of CPPs such as oral delivery, intranasal delivery, and clinical trials Cell-Penetrating Peptides: Design, Development, and Applications is an essential resource for biochemists, medicinal chemists, molecular biologists, biotechnologists, and researchers studying CPPs in both academia and industry.




Surface-Enhanced Raman Scattering


Book Description

Surface-Enhanced Raman Spectroscopy: Principles, Experiments, and Applications is a comprehensive, up to date, and balanced treatment of the theoretical and practical aspects of Surface-Enhanced Raman Scattering (SERS), a useful branch of spectroscopy for several areas of science. This book describes the basic principles of SERS, including SERS mechanisms, performing SERS measurements, and interpreting data. Also emphasized are applications in electrochemistry; catalysis; surface processing and corrosion; Self-Assemble-Layer and L-B Films; polymer science; biology; medicine and drug analysis; sensors; fuel cells; forensics; and archaeology. It is an essential guide for student and professional analytical chemists.




Peptide Synthesis


Book Description

Peptide synthesis includes an array of techniques and procedures that enable the preparation of materials ranging from small peptides to large proteins. Many synthetic peptides have commercial and pharmaceutical applications, however, the synthesis of these peptides is a difficult task. This book addresses the common problems relating to the synthesis and applications of synthetic peptides. It discusses novel methods for the efficient synthesis of long chain and difficult peptide sequences and presents detailed analysis of various aspects of solid phase peptide synthesis. It also includes a section on antimicrobial peptides.




Cell-Penetrating Peptides


Book Description

Divided into three parts this volume summarizes the most important areas of Cell-Penetrating Peptides (CPP) research . Part one briefly presents the historical background of CPP studies and the classifications of the available CPPs, and then summarizes the approaches for prediction of novel CPPs. Part two mainly describes the methods for studies of “naked” CPPs, that is, CPPs without conjugated cargos. Last but not least part three presents a representative and brief summary of functionality issues of CPPs, both in vitro and in vivo. As a volume in the highly successful Methods in Molecular Biology series, chapters contain introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Concise and easy-to-use, Cell-Penetrating Peptides: Methods and Protocols, Second Edition hopes to raise relevant questions for further development.




Fmoc Solid Phase Peptide Synthesis


Book Description

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.




Handbook of Cell-Penetrating Peptides


Book Description

Since the first Handbook of Cell-Penetrating Peptides was prepared in 2001, the wealth of new information on the use of these peptides as transport systems has in fact served to confound the field. The constant internal change in the field of cell-penetrating peptides (CPPs) is due to recent research uncovering apparent ambiguities in cellular upta