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Author: Lisa B. English Publisher: Springer Science & Business Media ISBN: 1592592856 Category : Science Languages : en Pages : 380
Book Description
The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms—such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules—has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.
Author: Lisa B. English Publisher: Springer Science & Business Media ISBN: 1592592856 Category : Science Languages : en Pages : 380
Book Description
The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms—such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules—has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.
Author: Armen M. Boldi Publisher: CRC Press ISBN: 1420009273 Category : Science Languages : en Pages : 363
Book Description
Traditionally, the search for new compounds from natural products has been a time- and resource-intensive process. The recent application of combinatorial methods and high-throughput synthesis has allowed scientists to generate a range of new molecular structures from natural products and observe how they interact with biological targets. Combinato
Author: Shmuel Cabilly Publisher: Springer Science & Business Media ISBN: 1592595715 Category : Science Languages : en Pages : 320
Book Description
During the course of evolution, an imbalance was created between the rate of vertebrate genetic adaptation and that of the lower forms of living organisms, such as bacteria and viruses. This imbalance has given the latter the advantage of generating, relatively quickly, molecules with unexpected structures and features that carry a threat to vertebrates. To compensate for their weakness, vertebrates have accelerated their own evolutionary processes, not at the level of whole organism, but in specialized cells containing the genes that code for antibody molecules or for T-cell receptors. That is, when an immediate requirement for molecules capable of specific interactions arose, nature has preferred to speed up the mode of Darwinian evolution in pref- ence to any other approach (such as the use of X-ray diffraction studies and computergraphic analysis). Recently, Darwinian rules have been adapted for test tube research, and the concept of selecting molecules having particular characteristics from r- dom pools has been realized in the form of various chemical and biological combinatorial libraries. While working with these libraries, we noticed the interesting fact that when combinatorial libraries of oligopeptides were allowed to interact with different selector proteins, only the actual binding sites of these proteins showed binding properties, whereas the rest of the p- tein surface seemed "inert. " This seemingly common feature of protein- having no extra potential binding sites--was probably selected during evolution in order to minimize nonspecific interactions with the surrounding milieu.
Author: Stephen R. Wilson Publisher: John Wiley & Sons ISBN: 9780471126874 Category : Medical Languages : en Pages : 286
Book Description
The new time-saving revolution in drug discovery. Combinatorial chemistry, a method for synthesizing millions of chemical compounds much faster than usual, is becoming one of the most useful technical tools available to chemists and researchers working today. Using current advances in computer and laboratory techniques, combinatorial chemistry has freed professionals from the drudgery of piecemeal experimental work and opened new creative possibilities for experimentation. Combinatorial Chemistry: Synthesis and Application details critical aspects of the technique, featuring the work of some of the world's leading chemists, many of whom played a key role in its development. Including examples of both solution-phase and solid-phase approaches as well as the full complement of organic chemistry technologies currently available, the book describes: * Concepts and terms of combinatorial chemistry * Polymer-supported synthesis of organic compounds * Macro beads as microreactors * Solid-phase methods in combinatorial chemistry * Encoded combinatorial libraries, including Rf-encoding of synthesis beads * Strategies for combinatorial libraries of oligosaccharides * Combinatorial libraries of peptides, proteins, and antibodies using biological systems. While combinatorial chemistry originated in peptide chemistry, this volume has deliberately focused on nonpeptide organic applications, illustrating the technique's wide uses. Combinatorial Chemistry introduces organic, medicinal, and pharmaceutical chemists as well as biochemists to this exciting, cost-effective, and practical technique, which has unlocked creative potential for the next millennium.
Author: Pierfausto Seneci Publisher: John Wiley & Sons ISBN: 0471460737 Category : Science Languages : en Pages : 653
Book Description
A unique, integrated look at solid-phase synthesis and advances in combinatorial chemistry and technologies The last decade has seen a rapid expansion in combinatorial technologies, a field where chemistry disciplines intersect with automation, statistics, and information science, as well as certain biological disciplines. Reflecting these multidisciplinary trends, this new work provides a comprehensive overview of the most important aspects of solid-phase synthesis (SPS), combinatorial chemistry, and related combinatorial technologies. It clearly demonstrates how SPS and combinatorial chemistry have extended their application from the pharmaceutical arena to new areas, including biotechnology, material sciences, catalysis, and agrochemical industries, and explores in detail strategies for planning, designing, preparing, and testing of combinatorial libraries in various disciplines. Designed to meet the needs of both experienced combinatorial chemists and newcomers to the field, Solid-Phase Synthesis and Combinatorial Technologies: * Surveys the most recent developments in SPS and combinatorial chemistry * Explains the entire process, from determining the need for a library to the details necessary for synthesis of the library * Discusses choice of format, size, and the rationale behind the design of each synthetic step * Surveys the analytical techniques and the purification methods used to characterize and purify combinatorial libraries * Employs a large number of examples to illustrate important concepts * Includes problems geared toward applying acquired knowledge and designing the steps to SPS/library synthesis * Describes the quality control and activity screening of combinatorial libraries for various applications * Features a detailed bibliography of more than 1,700 relevant sources
Author: Stanislav Miertus Publisher: CRC Press ISBN: 0824758374 Category : Medical Languages : en Pages : 616
Book Description
Several books on the market cover combinatorial techniques, but they offer just a limited perspective of the field, focusing on selected aspects without examining all approaches and integrated technologies. Combinatorial Chemistry and Technologies: Methods and Applications answers the demand for a complete overview of the field, covering all of the methodologies used in the design, synthesis, and screening of molecular libraries. Now in its second edition, this volume updates prior content and explores new areas such as catalysis, applications in biotechnology, and current ICS-UNIDO activities. Topics include the generation of molecular diversity by chemical methods using solution- and solid-phase chemistries, biological approaches for the production and screening of peptides, antibody and oligonucleotide libraries, and the application of computer-assisted approaches to guide library synthesis. The book establishes the link between combinatorial chemistry and molecular modeling and illustrates the importance of economics and patenting in combinatorial technologies. Valuable to technologists and researchers as an introductory survey on the many aspects of combinatorial chemistry and combinatorial technology, Combinatorial Chemistry and Technologies: Methods and Applications offers an overview of a field that promises broad applicability in the identification of new drugs, as well as in diagnostics, new materials, and catalysis.
Author: Günther Jung Publisher: John Wiley & Sons ISBN: 352761351X Category : Science Languages : en Pages : 634
Book Description
The story of success goes on and on - with a new book on combinatorial chemistry, edited by Gunther Jung! Combinatorial chemistry is a proven time- and resource-saving synthetic method of outstanding importance for industrial processes. Compound libraries help to save time and money, especially in the search for new drugs, and therefore play a pivotal role in solving the problem of the worldwide increasing demand for new and more active drugs. Not only substances, which are of interest for pharmaceutical chemistry, but also materials, catalysts, and biomolecules such as DNA or oligosaccharides are readily available with high structural diversities. The broad scope of combinatorial sciences is reflected by this book, edited by Gunther Jung: The synthetic methods discussed range from solid-phase to solution-phase synthesis, from preparations of small molecules such as amines or alcohols to those of complex biomolecules. Feasible methods, efficient techniques, new trends in automation, and state-of-the-art fast instrumental analytical and screening methods are presented with many practical tips and tricks for everybody working in combinatorial chemistry. This is the book written by specialists for specialists and for everyone aspiring to become an insider! It is an indispensible source of information for researchers working in organic synthesis, catalysis, biochemistry, and biotechnology, pharmaceutical and clinical chemistry, material sciences, and analytical chemistry.
Author: Stanislav Miertus Publisher: CRC Press ISBN: 1420027840 Category : Medical Languages : en Pages : 597
Book Description
Several books on the market cover combinatorial techniques, but they offer just a limited perspective of the field, focusing on selected aspects without examining all approaches and integrated technologies. Combinatorial Chemistry and Technologies: Methods and Applications answers the demand for a complete overview of the field, covering all of the
Author: Robert A. Goodnow, Jr. Publisher: John Wiley & Sons ISBN: 1118487680 Category : Science Languages : en Pages : 495
Book Description
This book comprehensively describes the development and practice of DNA-encoded library synthesis technology. Together, the chapters detail an approach to drug discovery that offers an attractive addition to the portfolio of existing hit generation technologies such as high-throughput screening, structure-based drug discovery and fragment-based screening. The book: Provides a valuable guide for understanding and applying DNA-encoded combinatorial chemistry Helps chemists generate and screen novel chemical libraries of large size and quality Bridges interdisciplinary areas of DNA-encoded combinatorial chemistry – synthetic and analytical chemistry, molecular biology, informatics, and biochemistry Shows medicinal and pharmaceutical chemists how to efficiently broaden available "chemical space" for drug discovery Provides expert and up-to-date summary of reported literature for DNA-encoded and DNA-directed chemistry technology and methods
Author: Lisa B. English
Author: Lisa B. English
Author: Armen M. Boldi
Author: Shmuel Cabilly
Author: Stephen R. Wilson
Author: Allan Geoffrey Skillman
Author: Pierfausto Seneci
Author: Stanislav Miertus
Author: Günther Jung
Author: Stanislav Miertus
Author: Robert A. Goodnow, Jr.