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Author: Zhong Qi Li
Publisher:
ISBN:
Category :
Languages : en
Pages : 530
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Book Description
Author: Zhong Qi Li
Publisher:
ISBN:
Category :
Languages : en
Pages : 530
Get Book Here
Book Description
Author: Landon R. Whitby
Publisher:
ISBN:
Category : Combinatorial chemistry
Languages : en
Pages : 446
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Book Description
Protein-protein interactions (PPIs) are essential components in cellular signaling pathways as well as important viral processes such as infection, replication, and immune suppression. The many uncharacterized PPIs involved in such interaction networks often represent compelling therapeutic drug targets. To date, however, the main strategies for discovery of small molecule modulators of PPIs are limited to structurally characterized targets. Recent developments in peptide secondary structure mimetics have yielded effective designs, however, very few screening libraries of such mimetics currently exist that can be used to interrogate PPI targets. We initiated a program to prepare a comprehensive small molecule library designed to mimic the three major recognition motifs that mediate PPIs ([alpha]-helix, [beta]-turn, [beta]-strand). Three libraries built around templates designed to mimic each such secondary structure and substituted with all triplet combinations of groups representing the 20 natural amino acid side chains would contain a member capable of mimicking the key interaction residues of most targetable PPIs. We present herein the results of the design, synthesis, and validation of an 8,000 member [alpha]-helix mimetic library and a 4,200 member [beta]-turn mimetic library. The screening of these libraries is expected not only to provide lead structures against [alpha]-helix- or [beta]-turn-mediated interactions, even if the nature of the interaction is unknown, but also yield key insights into the recognition motif ([alpha]-helix or [beta]-turn), and identify the key residues mediating the interaction. Consistent with this expectation, screening of the libraries against p53/MDM2 and HIV-1 gp41 ([alpha]-helix mimetic library) or the opioid receptors ([beta]-turn mimetic library) led to the discovery of library members that mimic the known endogenous ligands. These efforts led to the discovery of high affinity [alpha]-helix mimetics (Ki = 0.7 [micro]M) against HIV-1 gp41 as well as high affinity and selective [beta]-turn mimetics (Ki = 80 nM) against the [kappa]-opioid receptor. The studies herein suggest that the use of such comprehensive libraries of peptide secondary structure mimetics, built around effective molecular scaffolds, constitutes a powerful method of interrogating PPIs, providing small molecule modulators of PPI networks for therapeutic target validation, lead compound discovery, and identification of modulators of biological processes for study.
Author: G.E. Schulz
Publisher: Springer Science & Business Media
ISBN: 1461261376
Category : Science
Languages : en
Pages : 328
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Book Description
New textbooks at all levels of chemistry appear with great regularity. Some fields like basic biochemistry, organic reaction mechanisms, and chemical thermodynamics are well represented by many excellent texts, and new or revised editions are published sufficiently often to keep up with progress in research. However, some areas of chemistry, especially many of those taught at the graduate level, suffer from a real lack of up-to-date textbooks. The most serious needs occur in fields that are rapidly changing. Textbooks in these subjects usually have to be written by scientists actually involved in the research which is advancing the field. It is not often easy to persuade such individuals to set time aside to help spread the knowledge they have accumulated. Our goal, in this series, is to pinpoint areas of chemistry where recent progress has outpaced what is covered in any available textbooks, and then seek out and persuade experts in these fields to produce relatively concise but instructive introductions to their fields. These should serve the needs of one semester or one quarter graduate courses in chemistry and biochemistry. In some cases the availability of texts in active research areas should help stimulate the creation of new courses.
Author: Gregory A. Petsko
Publisher: New Science Press
ISBN: 0878936637
Category : Proteins
Languages : en
Pages : 220
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Book Description
Each title in the 'Primers in Biology' series is constructed on a modular principle that is intended to make them easy to teach from, to learn from, and to use for reference.
Author: G.D. Fasman
Publisher: Springer Science & Business Media
ISBN: 1461315719
Category : Science
Languages : en
Pages : 796
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Book Description
The prediction of the conformation of proteins has developed from an intellectual exercise into a serious practical endeavor that has great promise to yield new stable enzymes, products of pharmacological significance, and catalysts of great potential. With the application of predic tion gaining momentum in various fields, such as enzymology and immunology, it was deemed time that a volume be published to make available a thorough evaluation of present methods, for researchers in this field to expound fully the virtues of various algorithms, to open the field to a wider audience, and to offer the scientific public an opportunity to examine carefully its successes and failures. In this manner the practitioners of the art could better evaluate the tools and the output so that their expectations and applications could be more realistic. The editor has assembled chapters by many of the main contributors to this area and simultaneously placed their programs at three national resources so that they are readily available to those who wish to apply them to their personal interests. These algorithms, written by their originators, when utilized on pes or larger computers, can instantaneously take a primary amino acid sequence and produce a two-or three-dimensional artistic image that gives satisfaction to one's esthetic sensibilities and food for thought concerning the structure and function of proteins. It is in this spirit that this volume was envisaged.
Author: Daniel Chasman
Publisher: CRC Press
ISBN: 0824748166
Category : Medical
Languages : en
Pages : 534
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Book Description
This text offers in-depth perspectives on every aspect of protein structure identification, assessment, characterization, and utilization, for a clear understanding of the diversity of protein shapes, variations in protein function, and structure-based drug design. The authors cover numerous high-throughput technologies as well as computational methods to study protein structures and residues. A valuable reference, this book reflects current trends in the effort to solve new structures arising from genome initiatives, details methods to detect and identify errors in the prediction of protein structural models, and outlines challenges in the conversion of routine processes into high-throughput platforms.
Author: Jesko Koehnke
Publisher: Royal Society of Chemistry
ISBN: 1782625283
Category : Science
Languages : en
Pages : 392
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Book Description
This book provides the reader with a comprehensive view of the state-of-the-art of cyclic peptides, from construction to utility in biology and drug discovery.
Author: Ken Tse-yau Lau
Publisher:
ISBN:
Category :
Languages : en
Pages : 178
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Author: Natalya Kurochkina
Publisher: Springer
ISBN: 9811366012
Category : Science
Languages : en
Pages : 276
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Book Description
This book will consider principles of the organization of protein molecules, the relationships between primary, secondary, and tertiary structure, the determinants of protein conformation, and the applications of structure determination and structure modeling in biomedical research.
Author: Henrik Bohr
Publisher: IOS Press
ISBN: 9784274022630
Category : Distance geometry
Languages : en
Pages : 364
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Book Description
