Small Molecule Drug Discovery

📒Small Molecule Drug Discovery ✍ Andrea Trabocchi

Small Molecule Drug Discovery Book PDF
✏Book Title : Small Molecule Drug Discovery
✏Author : Andrea Trabocchi
✏Publisher : Elsevier
✏Release Date : 2019-11-23
✏Pages : 356
✏ISBN : 9780128183502
✏Available Language : English, Spanish, And French

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✏Small Molecule Drug Discovery Book Summary : 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

Introduction To Biological And Small Molecule Drug Research And Development Book PDF
✏Book Title : Introduction to Biological and Small Molecule Drug Research and Development
✏Author : C. Robin Ganellin
✏Publisher : Academic Press
✏Release Date : 2013-05-07
✏Pages : 472
✏ISBN : 9780123977700
✏Available Language : English, Spanish, And French

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✏Introduction to Biological and Small Molecule Drug Research and Development Book Summary : Introduction to Biological and Small Molecule Drug Research and Development provides, for the first time, an introduction to the science behind successful pharmaceutical research and development programs. The book explains basic principles, then compares and contrasts approaches to both biopharmaceuticals (proteins) and small molecule drugs, presenting an overview of the business and management issues of these approaches. The latter part of the book provides carefully selected real-life case studies illustrating how the theory presented in the first part of the book is actually put into practice. Studies include Herceptin/T-DM1, erythropoietin (Epogen/Eprex/NeoRecormon), anti-HIV protease inhibitor Darunavir, and more. Introduction to Biological and Small Molecule Drug Research and Development is intended for late-stage undergraduates or postgraduates studying chemistry (at the biology interface), biochemistry, medicine, pharmacy, medicine, or allied subjects. The book is also useful in a wide variety of science degree courses, in post-graduate taught material (Masters and PhD), and as basic background reading for scientists in the pharmaceutical industry. For the first time, the fundamental scientific principles of biopharmaceuticals and small molecule chemotherapeutics are discussed side-by-side at a basic level Edited by three senior scientists with over 100 years of experience in drug research who have compiled the best scientific comparison of small molecule and biopharmaceuticals approaches to new drugs Illustrated with key examples of important drugs that exemplify the basic principles of pharmaceutical drug research and development

Target Based Drug Discovery From Protein Structure To Small Molecules By Mcr Chemistry Book PDF
✏Book Title : Target based Drug Discovery from Protein Structure to Small molecules by MCR Chemistry
✏Author :
✏Publisher :
✏Release Date : 2018
✏Pages :
✏ISBN : 9403409584
✏Available Language : English, Spanish, And French

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✏Target based Drug Discovery from Protein Structure to Small molecules by MCR Chemistry Book Summary :

📒Small Molecule Medicinal Chemistry ✍ Werngard Czechtizky

Small Molecule Medicinal Chemistry Book PDF
✏Book Title : Small Molecule Medicinal Chemistry
✏Author : Werngard Czechtizky
✏Publisher : John Wiley & Sons
✏Release Date : 2015-11-02
✏Pages : 528
✏ISBN : 9781118771600
✏Available Language : English, Spanish, And French

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✏Small Molecule Medicinal Chemistry Book Summary : Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs. • Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives • Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches • Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques • Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting

The Science And Business Of Drug Discovery Book PDF
✏Book Title : The Science and Business of Drug Discovery
✏Author : Edward D. Zanders
✏Publisher : Springer Science & Business Media
✏Release Date : 2011-07-08
✏Pages : 397
✏ISBN : 1441999027
✏Available Language : English, Spanish, And French

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✏The Science and Business of Drug Discovery Book Summary : The Science and Business of Drug Discovery is written for those who want to learn about the biopharmaceutical industry and its products whatever their level of technical knowledge. Its aim is to demystify the jargon used in drug development, but in a way that avoids over simplification and the resulting loss of key information. Each of the nineteen chapters is illustrated with figures and tables which clarify some of the more technical points being made. Also included is a drug discovery case history which draws the relevant material together into a single chapter. In recognizing that it is difficult to navigate through the many external resources dealing with drug development, the book has been written to guide the reader towards the most appropriate information sources, including those listed in the two appendices. The following topics are covered: Different types of drugs: from small molecules to stem cells Background to chemistry of small and large molecules Historical background to drug discovery, pharmacology and biotechnology The drug discovery pipeline: from target discovery to marketed medicine Commercial aspects of drug discovery Challenges to the biopharmaceutical industry and its responses Material of specific interest to technology transfer executives, recruiters and pharmaceutical translators.

Exploiting Molecular Diversity Book PDF
✏Book Title : Exploiting Molecular Diversity
✏Author : Wendy A. Warr
✏Publisher :
✏Release Date : 1995
✏Pages : 118
✏ISBN : UCSD:31822023432503
✏Available Language : English, Spanish, And French

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✏Exploiting Molecular Diversity Book Summary : Drug discovery; Intellectual property protection; Molecular structures; Measuring chemical diversity; DIVERSOMER technology; Chemical libraries, etc...

📒Kinase Drug Discovery ✍ Richard A. Ward

Kinase Drug Discovery Book PDF
✏Book Title : Kinase Drug Discovery
✏Author : Richard A. Ward
✏Publisher : Royal Society of Chemistry
✏Release Date : 2011-12
✏Pages : 318
✏ISBN : 9781849731744
✏Available Language : English, Spanish, And French

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✏Kinase Drug Discovery Book Summary : This is the first book to examine the future opportunities and challenges in the development of drugs which target kinases

Introduction To Biological And Small Molecule Drug Research And Development Book PDF
✏Book Title : Introduction to Biological and Small Molecule Drug Research and Development
✏Author : Michael Stocks
✏Publisher : Elsevier Inc. Chapters
✏Release Date : 2013-05-07
✏Pages : 472
✏ISBN : 9780128061930
✏Available Language : English, Spanish, And French

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✏Introduction to Biological and Small Molecule Drug Research and Development Book Summary : Drug discovery of small molecules from target selection through to clinical evaluation is a very complex, challenging but rewarding area of drug discovery. There are many obstacles along the journey from initial hit-finding activities, through optimization of compounds and eventually to delivery of robust candidate drugs (CDs) for clinical evaluation. This chapter presents key issues and literature solutions with respect to the optimization of hits into CDs. Details of the key hit-finding activities namely high-throughput screening, virtual screening, natural products, fragment-based drug discovery and fast-follower approaches are discussed. Key aspects of compound quality such as lipophilicity, solubility, drug metabolism and pharmacokinetic, plasma protein binding and cytochrome P450 inhibition/induction are discussed as well as potential safety liabilities such as human ether-a-go-go related gene, genotoxicity and phospholipidosis, Finally successful hit-to-lead and lead optimization case studies are presented to illustrate and highlight the key principles.

Small Molecule Protein Interactions Book PDF
✏Book Title : Small Molecule Protein Interactions
✏Author : Herbert Waldmann
✏Publisher : Springer Science & Business Media
✏Release Date : 2013-03-09
✏Pages : 228
✏ISBN : 9783662053140
✏Available Language : English, Spanish, And French

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✏Small Molecule Protein Interactions Book Summary : Based on the international workshop on 'Small Molecule - Protein Interactions' held in Berlin, April 24-26, 2002, researchers from industry and academic laboratories describe novel and efficient ways selecting promising new drug targets and developing small molecule inhibitors against them. The structure of the book corresponds to the different aspects of the drug discovery process. All chapters are written by leading experts in the field, who present and discuss the most recent state-of-the-art tools and techniques for the development of novel drugs. The value of the book lies in surveying and summarizing the approaches taken by different companies and institutions giving the reader a balanced view on the use of the latest techniques on the one hand and experience-based assistance in selecting appropriate tools for their own work on the other hand.

Applied Biophysics For Drug Discovery Book PDF
✏Book Title : Applied Biophysics for Drug Discovery
✏Author : Donald Huddler
✏Publisher : John Wiley & Sons
✏Release Date : 2017-10-02
✏Pages : 312
✏ISBN : 9781119099482
✏Available Language : English, Spanish, And French

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✏Applied Biophysics for Drug Discovery Book Summary : 13.2.1 Protein Dynamics of SA WT and S1 Mutant DHFR in Apo and Bound States

Application Of Computational Methods For Kinase Small Molecule Drug Discovery And Design Book PDF
✏Book Title : Application of Computational Methods for Kinase Small Molecule Drug Discovery and Design
✏Author : Abdulkarim Najjar
✏Publisher :
✏Release Date : 2018*
✏Pages :
✏ISBN : OCLC:1099479695
✏Available Language : English, Spanish, And French

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✏Application of Computational Methods for Kinase Small Molecule Drug Discovery and Design Book Summary : Kinase; PKMYT1; PRK1; EGFR; IGF-1R; PDGFR-[beta]; VEDFR2; kinase inhibitors; computer-aided drug design; drug discovery

Introduction To Biological And Small Molecule Drug Research And Development Book PDF
✏Book Title : Introduction to Biological and Small Molecule Drug Research and Development
✏Author : James Samanen
✏Publisher : Elsevier Inc. Chapters
✏Release Date : 2013-05-07
✏Pages : 472
✏ISBN : 9780128061954
✏Available Language : English, Spanish, And French

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✏Introduction to Biological and Small Molecule Drug Research and Development Book Summary : Biotechnology has given rise to a broad range of biotherapies or biologics, including biomolecular drugs, vaccines, cell or gene therapies. This chapter focuses on biomolecular drugs, namely monoclonal antibodies (Mabs), cytokines, tissue growth factors and therapeutic proteins. Prior to the US approval of recombinant human insulin in 1982, biomolecular drugs were extracted from natural sources. The tools of molecular biology have dramatically increased the discovery and development of new biopharmaceuticals. The most obvious difference between small-molecule drugs (SMDs) and biomolecular drugs is size, like the difference in weight between a bicycle and a business jet. SMDs and biomolecular drugs are compared in this chapter by structure, molecular weight, preparation, physicochemical properties, and route of administration, as well as distribution, metabolism, serum half-life, dosing regimen, species reactivity, antigenicity & hypersensitivity, clearance mechanisms, drug–drug interactions, and pharmacology. This chapter reviews the differences and similarities in the various stages of drug discovery and development, with respect to cost, probability of success and cycle time. The clinical metrics of overall clinical success rate, stage-related success rate, and clinical cycle time are examined for SMDs and biomolecular drugs. The hybrid class of peptide drugs tends to be equated with biologics, due to their amino acid content and because oral activity is rare. But peptides truly bridge the gap between small molecules and biologics, in terms of physical properties, range of therapy areas and means of production. This chapter summarizes the similarities and differences of peptide drugs with SMDs and biomolecular drugs. The manner in which these agents compare as products with respect to manufacturing and pricing are considered. Two case studies are presented—the antagonists where small-molecule, peptide and Mab agents have competed in the market, and Her2 inhibitors where small-molecule and Mab agents may ultimately synergize as a combination product. Biomolecular drugs have levelled the playing field. All the “big Pharma” companies now have the capacity to develop both types of drugs. Conversely the larger biotech companies are developing the capacity for small-molecule synthesis. Now, with many blockbuster biologics nearing patent expiration, biosimilars are on the way. It's no longer a question of “choose which type”—one will need to know how to discover and develop either type of drug.

📒Drug Discovery And Development ✍ Omboon Vallisuta

Drug Discovery And Development Book PDF
✏Book Title : Drug Discovery and Development
✏Author : Omboon Vallisuta
✏Publisher : BoD – Books on Demand
✏Release Date : 2015-06-03
✏Pages : 330
✏ISBN : 9789535121282
✏Available Language : English, Spanish, And French

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✏Drug Discovery and Development Book Summary : It is very important for scientists all over the globe to enhance drug discovery research for better human health. This book demonstrates that various expertise are essential for drug discovery including synthetic or natural drugs, clinical pharmacology, receptor identification, drug metabolism, pharmacodynamic and pharmacokinetic research. The following 5 sections cover diverse chapter topics in drug discovery: Natural Products as Sources of Leading Molecules in Drug Discovery; Oncology and Drug Discovery; Receptors Involvement in Drug Discovery; Management and Development of Drugs against Infectious Diseases; Advanced Methodology.

Multifaceted Roles Of Crystallography In Modern Drug Discovery Book PDF
✏Book Title : Multifaceted Roles of Crystallography in Modern Drug Discovery
✏Author : Giovanna Scapin
✏Publisher : Springer
✏Release Date : 2015-02-27
✏Pages : 240
✏ISBN : 9789401797191
✏Available Language : English, Spanish, And French

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✏Multifaceted Roles of Crystallography in Modern Drug Discovery Book Summary : The present work offers a snapshot of the state-of-the-art of crystallographic, analytical, and computational methods used in modern drug design and development. Topics discussed include: drug design against complex systems (membrane proteins, cell surface receptors, epigenetic targets, and ribosomes); modulation of protein-protein interactions; the impact of small molecule structures in drug discovery and the application of concepts such as molecular geometry, conformation, and flexibility to drug design; methodologies for understanding and characterizing protein states and protein-ligand interactions during the drug design process; and monoclonal antibody therapies. These methods are illustrated through their application to problems of medical and biological significance, such as viral and bacterial infections, diabetes, autoimmune disease, and CNS diseases. As approaches to drug discovery have changed over time, so have the methodologies used to solve the varied, new, and difficult problems encountered in drug discovery. In recent years we have seen great progress in the fields of genetics, biology, chemistry, and medicine, but there are still many unmet medical needs, from bacterial infections to cancer to chronic maladies, that require novel, different, or better therapies. This work will be of interest to researchers and policy makers interested in the latest developments in drug design.

Multi Target Pharmacology Of Small Molecule Drugs And First In Class Inhibitors Discovery Book PDF
✏Book Title : Multi target Pharmacology of Small Molecule Drugs and First in class Inhibitors Discovery
✏Author : Da Shi
✏Publisher :
✏Release Date : 2020
✏Pages : 161
✏ISBN : OCLC:1195929015
✏Available Language : English, Spanish, And French

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✏Multi target Pharmacology of Small Molecule Drugs and First in class Inhibitors Discovery Book Summary : This dissertation describes studies into a new drug candidate discovery philosophy and its application to diseases. Over the last several decades, drug discovery has been focusing on one single target modulation. However, due to the high failure rate in drug development, a new philosophy that focusing on multiple drug-target interactions has gained escalating attention in both academia and industry. In this philosophy, drugs, especially small-molecule drugs interact with multiple protein targets in their therapeutic concentrations. In chapter 1, we explored the multi-target pharmacology of cancer drugs. We collected information about multiple targets for each cancer drug along with their experimental effective concentrations or binding activities from multiple sources. We showed that the majority of the cancer drugs had substantial multi-target pharmacology based on our current knowledge. The target subset can further be accentuated and personalized by patient sample-specific expression data. Besides analysis, we also built a web database for the public to access and easily explore the multi-target pharmacology of cancer drugs. To gain a comprehensive multi-target pharmacology, we still need to study new protein targets to further extend the collection of known targets. In chapters 2 and 3, we studied a bacterial transcription factor, RfaH, which may be developed into a new antibacterial target. RfaH is a transcription processivity factor, belonging to a universally conserved transcriptional regulator, NusG/Stp5 family. Unlike other family members, RfaH exerts a distinct structural transformation during its binding to RNA polymerase. We first identified two key residues for the structural transformation through a combined structural and phylogenetic analysis. Then we screened a compound library and identified 3 first-in-class inhibitors for RfaH binding to RNA polymerase. In chapter 4, we developed a novel target for Naegleria fowleri infection, primary amoebic meningoencephalitis (PAM). PAM is a rapid-onset brain infection in humans with over 97% mortality rate. Despite some progress in the treatment of the disease, there is no single, proven, evidence-based treatment with a high probability of cure. The target we developed was ERG2, an isomerase in the ergosterol synthetic pathway. We built a homology model of ERG2 and identified 4 amoebicidal chemicals with low human cell toxicity.

Macrocycles In Drug Discovery Book PDF
✏Book Title : Macrocycles in Drug Discovery
✏Author : Jeremy I Levin
✏Publisher : Royal Society of Chemistry
✏Release Date : 2014-10-16
✏Pages : 499
✏ISBN : 9781849737012
✏Available Language : English, Spanish, And French

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✏Macrocycles in Drug Discovery Book Summary : This book reviews macrocycles in drug discovery, both those of natural origin and semi-synthetic derivatives of natural products, and those designed and synthesized based on principles of medicinal chemistry. The medicinal chemistry of macrocyclic natural products is interesting in itself, but lessons learned from these compounds, in terms of the relationship between structure and desirable physicochemical properties, are now informing the design of fully synthetic macrocyclic drug candidates against a variety of targets including kinases, ATPases, proteases, GPCRs and others. Furthermore, as more non-classical drug targets, such as protein-protein interactions, are pursued in the pharmaceutical industry, macrocyclic molecules are generating increasing interest as they offer a way to provide drug-protein interactions that cover a larger surface area than traditional small molecules. A variety of macrocycles have become important drugs or have been identified as leads to marketed drugs. This text will discuss these compounds, their pharmacology and synthesis, in the context of their broad chemotype as compounds composed of large rings. Providing a wide reaching review of this important area in a single volume, this book will be of interest to biochemists, pharmaceutical scientists and medicinal chemists working in industry or academia.

📒New Drug Development ✍ J. Rick Turner

New Drug Development Book PDF
✏Book Title : New Drug Development
✏Author : J. Rick Turner
✏Publisher : John Wiley & Sons
✏Release Date : 2007-07-27
✏Pages : 270
✏ISBN : 9780470073735
✏Available Language : English, Spanish, And French

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✏New Drug Development Book Summary : This book acquaints students and practitioners in the related fields of pharmaceutical sciences, clinical trials, and evidence-based medicine with the necessary study design concepts and statistical practices to allow them to understand how drug developers plan and evaluate their drug development. Two goals of the book are to make the material accessible to readers with minimal background in research and to be straightforward enough for self-taught purposes. By bringing the topic from the early discovery phase to clinical trials and medical practice, the book provides an indispensable overview of an otherwise confusing and fragmented set of topics. The author’s experience as a respected scientist, teacher of statistics, and one who has worked in the clinical trials arena makes him well suited to write such a treatise.

📒Chemical Genomics ✍ Stefan Jaroch

Chemical Genomics Book PDF
✏Book Title : Chemical Genomics
✏Author : Stefan Jaroch
✏Publisher : Springer Science & Business Media
✏Release Date : 2007-05-26
✏Pages : 179
✏ISBN : 9783540376354
✏Available Language : English, Spanish, And French

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✏Chemical Genomics Book Summary : Chemical genomics is a highly interdisciplinary and very exciting field of research both in academics and in the life sciences industry. The Ernst Schering Research Foundation Workshop 58 was organized to bring together scientific leaders in the field to discuss the implications of chemical genomics for drug discovery. Various aspects of the interface between chemistry and biology are covered in this volume, such as chemogenomics efforts in the pharmaceutical industry, diversity-oriented synthesis, chemogenomic approaches to the study of cell function, screening technologies, and natural products as tools in chemical biology.

Peptide Based Drug Discovery Book PDF
✏Book Title : Peptide based Drug Discovery
✏Author : Ved Srivastava
✏Publisher : Royal Society of Chemistry
✏Release Date : 2017-06-26
✏Pages : 588
✏ISBN : 9781782627326
✏Available Language : English, Spanish, And French

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✏Peptide based Drug Discovery Book Summary : 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.

Protein Surface Recognition Book PDF
✏Book Title : Protein Surface Recognition
✏Author : Ernest Giralt
✏Publisher : John Wiley & Sons
✏Release Date : 2011-07-07
✏Pages : 344
✏ISBN : 9781119957218
✏Available Language : English, Spanish, And French

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✏Protein Surface Recognition Book Summary : A new perspective on the design of molecular therapeutics is emerging. This new strategy emphasizes the rational complementation of functionality along extended patches of a protein surface with the aim of inhibiting protein/protein interactions. The successful development of compounds able to inhibit these interactions offers a unique chance to selectively intervene in a large number of key cellular processes related to human disease. Protein Surface Recognition presents a detailed treatment of this strategy, with topics including: an extended survey of protein-protein interactions that are key players in human disease and biology and the potential for therapeutics derived from this new perspective the fundamental physical issues that surround protein-protein interactions that must be considered when designing ligands for protein surfaces examples of protein surface-small molecule interactions, including treatments of protein-natural product interactions, protein-interface peptides, and rational approaches to protein surface recognition from model to biological systems a survey of techniques that will be integral to the discovery of new small molecule protein surface binders, from high throughput synthesis and screening techniques to in silico and in vitro methods for the discovery of novel protein ligands. Protein Surface Recognition provides an intellectual “tool-kit” for investigators in medicinal and bioorganic chemistry looking to exploit this emerging paradigm in drug discovery.

📒Successful Drug Discovery ✍ János Fischer

Successful Drug Discovery Book PDF
✏Book Title : Successful Drug Discovery
✏Author : János Fischer
✏Publisher : John Wiley & Sons
✏Release Date : 2019-07-20
✏Pages : 272
✏ISBN : 9783527814718
✏Available Language : English, Spanish, And French

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✏Successful Drug Discovery Book Summary : Provides unique insider insight into the current drug development process, and what it takes to achieve success In this fourth volume in the series, inventors and primary developers of drugs that made it to the market continue telling the story of the drugs? discovery and development, and discuss the sometimes twisted route from the first drug candidate molecule to the final marketed one. Beginning with a general section addressing overarching topics for drug discovery, the book offers seven chapters that feature selected case studies describing recently introduced drugs or drug classes. These include small molecule drugs as well as biopharmaceuticals and range across different therapeutic fields. Together, they provide a representative cross-section of the present-day drug development effort. Successful Drug Discovery: Volume 4 covers trends in peptide-based drug discovery and the physicochemical properties of recently approved oral drugs. The section on drug class studies looks at antibody-drug conjugates and the discovery, evolution, and therapeutic potential of dopamine partial agonists. Featured case studies examine the discovery of Etelcalcetide for the treatment of secondary hyper-parathyroidism in patients with chronic kidney disease; the development of Lenvatinib Mesylate; the discovery and development of Venetoclax; and more. -Focuses on recently introduced drugs that have not been featured in any textbooks or general references, including Ocrelizumab, a new generation of anti-CD-20 mAb for the treatment of multiple sclerosis, and Venetoclax, a selective antagonist of BCL-2 -Features personal experiences of successful drug developers from industry and academia -Endorsed and supported by the International Union of Pure and Applied Chemistry (IUPAC) Successful Drug Discovery: Volume 4 provides a fascinating and informative look into the process of drug discovery and would be a great reference for those in the pharmaceutical industry, organic and pharmaceutical chemists, and lecturers in pharmacy.

Natural Small Molecule Drugs From Plants Book PDF
✏Book Title : Natural Small Molecule Drugs from Plants
✏Author : Guan-Hua Du
✏Publisher : Springer
✏Release Date : 2018-11-19
✏Pages : 741
✏ISBN : 9789811080227
✏Available Language : English, Spanish, And French

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✏Natural Small Molecule Drugs from Plants Book Summary : This book discusses 120 types of natural, small-molecule drugs derived from plants. They are grouped into 7 parts according their clinical uses, such as drugs for cardiovascular diseases, for metabolic diseases, for neuropsychiatric diseases, for immune-mediated inflammatory diseases, anti-tumor drugs, and drugs for parasites and bacterial infection. Each chapter systematically summarizes one drug, including its physicochemical properties, sources, pharmacological effects and clinical applications. To help readers understand the drug better, the research and pharmacological activity for each drug is also described, which serves as a salutary lesson for future drug development. Written by frontline researchers, teachers and clinicians working in field of pharmacy and pharmacology it provides an overview of natural, small-molecule drugs derived from plants for researchers in the field.

Small Molecule Scaffold Synthesis One Bead One Compound Library Synthesis And Method Development In Drug Discovery Book PDF
✏Book Title : Small molecule scaffold synthesis one bead one compound library synthesis and method development in drug discovery
✏Author : Seth M. Dixon
✏Publisher :
✏Release Date : 2006
✏Pages : 630
✏ISBN : UCAL:X74600
✏Available Language : English, Spanish, And French

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✏Small molecule scaffold synthesis one bead one compound library synthesis and method development in drug discovery Book Summary :

Pharmaceuticals Drug Development Design And Manufacturing Book PDF
✏Book Title : Pharmaceuticals Drug Development Design and Manufacturing
✏Author : Rodrik Ledger
✏Publisher :
✏Release Date : 2020-09-22
✏Pages : 246
✏ISBN : 1632419009
✏Available Language : English, Spanish, And French

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✏Pharmaceuticals Drug Development Design and Manufacturing Book Summary : A pharmaceutical drug is a compound which is used for the diagnosis, treatment and prevention of a disease. It can be classified depending on the level of control, mode of action, route of administration and therapeutic effects, among others. Some classes of medicine are antibiotics, antipyretics, analgesics, antiseptics, oral contraceptives, tranquilizers, stimulants, etc. The development of pharmaceutical products traverses a number of stages from drug discovery to commercialization. There exists a clear distinction between small molecule drugs and biologic medical products. While small molecule drugs are developed through chemical synthesis; biologic medical products include vaccines, recombinant proteins, gene therapy and cell therapy. This book brings forth some of the most innovative concepts and elucidates the unexplored aspects of pharmaceuticals. It presents researches and studies performed by experts across the globe on potential pharmaceutical agents. With state-of-the-art inputs by acclaimed experts of this field, this book targets students and professionals.

Targeting Protein Protein Interactions By Small Molecules Book PDF
✏Book Title : Targeting Protein Protein Interactions by Small Molecules
✏Author : Chunquan Sheng
✏Publisher : Springer
✏Release Date : 2018-06-26
✏Pages : 329
✏ISBN : 9789811307737
✏Available Language : English, Spanish, And French

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✏Targeting Protein Protein Interactions by Small Molecules Book Summary : This book comprehensively reviews the state-of-the-art strategies developed for protein-protein interaction (PPI) inhibitors, and highlights the success stories in new drug discovery and development. Consisting of two parts with twelve chapters, it demonstrates the design strategies and case studies of small molecule PPI inhibitors. The first part discusses various discovery strategies for small molecule PPI inhibitors, such as high throughput screening, hot spot-based design, computational approaches, and fragment-based design. The second part presents recent advances in small molecule inhibitors, focusing on clinical candidates and new PPI targets. This book has broad appeal and is of significant interest to the pharmaceutical science and medicinal chemistry communities.

📒Epi Informatics ✍ Jose Medina-Franco

Epi Informatics Book PDF
✏Book Title : Epi Informatics
✏Author : Jose Medina-Franco
✏Publisher : Academic Press
✏Release Date : 2016-02-24
✏Pages : 440
✏ISBN : 9780128028094
✏Available Language : English, Spanish, And French

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✏Epi Informatics Book Summary : Epi-Informatics: Discovery and Development of Small Molecule Epigenetic Drugs and Probes features multidisciplinary strategies with strong computational approaches that have led to the successful discovery and/or optimization of compounds that act as modulators of epigenetic targets. This book is intended for all those using or wanting to learn more about computational methodologies in epigenetic drug discovery, including molecular modelers, informaticians, pharmaceutical scientists, and medicinal chemists. With a better understanding of different molecular modeling and cheminformatic approaches, readers can incorporate these techniques into their own drug discovery projects that may involve chemical synthesis and medium- or high-throughput screening. In addition, this book highlights the significance of epigenetic targets to the public health for molecular modelers and chemoinformatians. The goal of this reference is to stimulate ongoing multidisciplinary research and to further improve current computational methodologies and workflows in order to accelerate the discovery and development of epi-drugs and epi-probes. Focuses on the discovery of epi-drugs as candidates to be used in therapy including combined therapies Describes new computational methodologies and screening assays utilizing recent and emerging novel structural data Highlights the discovery, development and optimization of epi-probes, which are molecular probes that elucidate epigenetic mechanisms Includes important topics such as computational-guided optimization of epi-hits, virtual screening to identify novel compounds for epigenetic targets, development and mining of epigenetic molecular databases, SAR modeling of screening data and much more

📒Epigenetic Drug Discovery ✍ Wolfgang Sippl

Epigenetic Drug Discovery Book PDF
✏Book Title : Epigenetic Drug Discovery
✏Author : Wolfgang Sippl
✏Publisher : John Wiley & Sons
✏Release Date : 2019-03-25
✏Pages : 504
✏ISBN : 9783527343140
✏Available Language : English, Spanish, And French

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✏Epigenetic Drug Discovery Book Summary : This broad view of epigenetic approaches in drug discovery combines methods and strategies with individual targets, including new and largely unexplored ones such as sirtuins and methyl-lysine reader proteins. Presented in three parts - Introduction to Epigenetics, General Aspects and Methodologies, and Epigenetic Target Classes - it covers everything any drug researcher would need in order to know about targeting epigenetic mechanisms of disease. Epigenetic Drug Discovery is an important resource for medicinal chemists, pharmaceutical researchers, biochemists, molecular biologists, and molecular geneticists.

📒Translating Molecules Into Medicines ✍ Shobha N. Bhattachar

Translating Molecules Into Medicines Book PDF
✏Book Title : Translating Molecules into Medicines
✏Author : Shobha N. Bhattachar
✏Publisher : Springer
✏Release Date : 2018-07-20
✏Pages : 461
✏ISBN : 3319843036
✏Available Language : English, Spanish, And French

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✏Translating Molecules into Medicines Book Summary : Tackling translational medicine with a focus on the drug discovery development-interface, this book integrates approaches and tactics from multiple disciplines, rather than just the pharmaceutical aspect of the field. The authors of each chapter address the paradox between the molecular understanding of diseases, drug discovery, and drug development. Laying out the detailed trends from various fields, different chapters are dedicated to target engagement, toxicological safety assessments, and the compelling relationship of optimizing early clinical studies with design strategies. The book also highlights the importance of balancing the three pillars: sufficient efficacy, acceptable safety and appropriate pharmacokinetics, all of which are crucial to successful efforts in discovery and development. With discussions regarding the combined approaches of molecular research, personalized medicine, pre-clinical and clinical development, as well as targeted therapies—this compendium is a flexible fit, perfect for professionals in the pharmaceutical industry and related academic fields.

📒Fragment Based Drug Discovery ✍ Edward R. Zartler

Fragment Based Drug Discovery Book PDF
✏Book Title : Fragment Based Drug Discovery
✏Author : Edward R. Zartler
✏Publisher : John Wiley & Sons
✏Release Date : 2008-11-20
✏Pages : 296
✏ISBN : 9780470721568
✏Available Language : English, Spanish, And French

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✏Fragment Based Drug Discovery Book Summary : Fragment-based drug discovery (FBDD) is a new paradigm in drug discovery that utilizes very small molecules - fragments of larger molecules. It is a faster, cheaper, smarter way to do drug discovery, as shown by the number of pharmaceutical companies that have embraced this approach and the biotechnology companies who use fragments as their sole source of drug discovery. Fragment-Based Drug Discovery: A Practical Approach is a guide to the techniques and practice of using fragments in drug screening. The emphasis is on practical guidance, with procedures, case studies, practical tips, and contributions from industry. Topics covered include: an introduction to fragment based drug discovery, why using fragments is a more efficient process than predominant models, and what it means to have a successful FBDD effort. setting up an FBDD project library building and production NMR in fragment screening and follow up application of protein-ligand NOE matching to the rapid evaluation of fragment binding poses target immobilized NMR screening: validation and extension to membrane proteins in situ fragment-based medicinal chemistry: screening by mass spectrometry computational approaches to fragment and substructure discovery and evaluation virtual fragment scanning: current trends, applications and web based tools fragment-based lead discovery using covalent capture methods case study from industry: the identification of high affinity beta-secretase inhibitors using fragment-based lead generation With contributions from industry experts who have successfully set up an industrial fragment-based research program, Fragment-Based Drug Discovery: A Practical Approach offers essential advice to anyone embarking on drug discovery using fragments and those looking for a new approach to screening for drugs.

📒Brain Drug Targeting ✍ William M. Pardridge

Brain Drug Targeting Book PDF
✏Book Title : Brain Drug Targeting
✏Author : William M. Pardridge
✏Publisher : Cambridge University Press
✏Release Date : 2001-05-31
✏Pages : 353
✏ISBN : 0521800773
✏Available Language : English, Spanish, And French

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✏Brain Drug Targeting Book Summary : This challenging 2001 book reviews modern neurotherapeutics from the point of view of drug targeting.