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Showing 1 - 25 of 51 matches in All departments

Predictive Toxicology - From Vision to Reality (Hardcover): Friedlieb Pfannkuch, Laura Suter-Dick Predictive Toxicology - From Vision to Reality (Hardcover)
Friedlieb Pfannkuch, Laura Suter-Dick; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R3,250 R3,025 Discovery Miles 30 250 Save R225 (7%) Ships in 10 - 15 working days

Tailored to the needs of scientists developing drugs, chemicals, cosmetics and other products this one-stop reference for medicinal chemists covers all the latest developments in the field of predictive toxicology and its applications in safety assessment. With a keen emphasis on novel approaches, the topics have been tackled by selected expert scientists, who are familiar with the theoretical scientific background as well as with the practical application of current methods. Emerging technologies in toxicity assessment are introduced and evaluated in terms of their predictive power, with separate sections on computer predictions and simulation methods, novel in vitro systems including those employing stem cells, toxicogenomics and novel biomarkers. In each case, the most promising methods are discussed and compared to classical in vitro and in vivo toxicology assays. Finally, an outlook section discusses such forward-looking topics as immunotoxicology assessment and novel regulatory requirements. With its wealth of methodological knowledge and its critical evaluation of modern approaches, this is a valuable guide for toxicologists working in pharmaceutical development, as well as in safety assessment and the regulation of drugs and chemicals.

Scaffold Hopping in Medicinal Chemistry (Hardcover): Nathan Brown Scaffold Hopping in Medicinal Chemistry (Hardcover)
Nathan Brown; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R3,618 R3,010 Discovery Miles 30 100 Save R608 (17%) Ships in 10 - 15 working days

This first systematic treatment of the concept and practice of scaffold hopping shows the tricks of the trade and provides invaluable guidance for the reader's own projects. The first section serves as an introduction to the topic by describing the concept of scaffolds, their discovery, diversity and representation, and their importance for finding new chemical entities. The following part describes the most common tools and methods for scaffold hopping, whether topological, shape-based or structure-based. Methods such as CATS, Feature Trees, Feature Point Pharmacophores (FEPOPS), and SkelGen are discussed among many others. The final part contains three fully documented real-world examples of successful drug development projects by scaffold hopping that illustrate the benefits of the approach for medicinal chemistry. While most of the case studies are taken from medicinal chemistry, chemical and structural biologists will also benefit greatly from the insights presented here.

Drug Metabolism Prediction (Hardcover): Johannes Kirchmair Drug Metabolism Prediction (Hardcover)
Johannes Kirchmair; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R4,268 R3,504 Discovery Miles 35 040 Save R764 (18%) Ships in 10 - 15 working days

The first professional reference on this highly relevant topic, for drug developers, pharmacologists and toxicologists. The authors provide more than a systematic overview of computational tools and knowledge bases for drug metabolism research and their underlying principles. They aim to convey their expert knowledge distilled from many years of experience in the field. In addition to the fundamentals, computational approaches and their applications, this volume provides expert accounts of the latest experimental methods for investigating drug metabolism in four dedicated chapters. The authors discuss the most important caveats and common errors to consider when working with experimental data. Collating the knowledge gained over the past decade, this practice-oriented guide presents methods not only used in drug development, but also in the development and toxicological assessment of cosmetics, functional foods, agrochemicals, and additives for consumer goods, making it an invaluable reference in a variety of disciplines.

Lead Generation - Methods and Strategies (Hardcover): Jorg Holenz, Markus Haeberlein Lead Generation - Methods and Strategies (Hardcover)
Jorg Holenz, Markus Haeberlein; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R6,363 R5,769 Discovery Miles 57 690 Save R594 (9%) Ships in 10 - 15 working days

In this comprehensive two-volume resource on the topic senior lead generation medicinal chemists present a coherent view of the current methods and strategies in industrial and academic lead generation. This is the first book to combine both standard and innovative approaches in comparable breadth and depth, including several recent successful lead generation case studies published here for the first time. Beginning with a general discussion of the underlying principles and strategies, individual lead generation approaches are described in detail, highlighting their strengths and weaknesses, along with all relevant bordering disciplines like e.g. target identification and validation, predictive methods, molecular recognition or lead quality matrices. Novel lead generation approaches for challenging targets like DNA-encoded library screening or chemical biology approaches are treated here side by side with established methods as high throughput and affinity screening, knowledge- or fragment-based lead generation, and collaborative approaches. Within the entire book, a very strong focus is given to highlight the application of the presented methods, so that the reader will be able to learn from real life examples. The final part of the book presents several lead generation case studies taken from different therapeutic fields, including diabetes, cardiovascular and respiratory diseases, neuroscience, infection and tropical diseases. The result is a prime knowledge resource for medicinal chemists and for every scientist involved in lead generation.

Transporters as Drug Carriers - Structure, Function, Substrates (Hardcover): Gerhard F. Ecker, Peter Chiba Transporters as Drug Carriers - Structure, Function, Substrates (Hardcover)
Gerhard F. Ecker, Peter Chiba; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R4,832 R4,531 Discovery Miles 45 310 Save R301 (6%) Ships in 10 - 15 working days

This reference handbook is the first to provide a comprehensive overview, systematically characterizing all known transporters involved in drug elimination and resistance. Combining recent knowledge on all known classes of drug carriers, from microbes to man, it begins with a look at human and mammalian transporters. This is followed by microbial, fungal and parasitic transporters with special attention given to transport across those physiological barriers relevant for drug uptake, distribution and excretion.
As a result, this key resource lays the foundations for understanding and investigating the molecular mechanisms for multidrug resistance in cancer cells, microbial resistance to antibiotics and pharmacokinetics in general.
For anyone working with antibiotics and cancer chemotherapeutics, as well as being of prime interest to biochemists and biophysicists.

Drug Bioavailability - Estimation of Solubility, Permeability, Absorption and Bioavailability (Hardcover, 2nd Edition): Han Van... Drug Bioavailability - Estimation of Solubility, Permeability, Absorption and Bioavailability (Hardcover, 2nd Edition)
Han Van De Waterbeemd, Bernard Testa; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R5,388 R5,022 Discovery Miles 50 220 Save R366 (7%) Ships in 10 - 15 working days

The gold standard for industrial research now completely revised in line with current trends in the field, with all contributions extensively updated or rewritten.
In 21 chapters readers can benefit from the key working knowledge of today's leading pharmaceutical companies, including Pfizer, AstraZeneca, and Roche. Drug developers from industry and academia present all the factors governing drug bioavailability, complete with practical examples and real-life data.
Part I focuses on in vitro and in vivo measurements of physicochemical properties, such as membrane permeability and ionization. Part II discusses solubility and gastrointestinal absorption, while the third part is devoted to metabolism and excretory mechanisms. The much revised and expanded part IV surveys current in silico approaches to predict drug properties needed to estimate the bioavailability of any new drug candidate. The final part shows how poor bioavailability may be improved by various approaches during the development process.
No other publication offers the same level of treatment on this crucial topic in modern drug development.

In vivo Models for Drug Discovery (Hardcover): Jose M. Vela, Rafael Maldonado, Michel Hamon In vivo Models for Drug Discovery (Hardcover)
Jose M. Vela, Rafael Maldonado, Michel Hamon; Series edited by Raimund Mannhold, Hugo Kubinyi, …
R3,540 R3,283 Discovery Miles 32 830 Save R257 (7%) Ships in 10 - 15 working days

This one-stop reference is the first to present the complete picture -- covering all relevant organisms, from single cells to mammals, as well as all major disease areas, including neurological disorders, cancer and infectious diseases.
Addressing the needs of the pharmaceutical industry, this unique handbook adopts a broad perspective on the use of animals in the early part of the drug development process, including regulatory rules and limitations, as well as numerous examples from real-life drug development projects.
After a general introduction to the topic, the expert contributors from research-driven pharmaceutical companies discuss the basic considerations of using animal models, including ethical issues. The main part of the book systematically surveys the most important disease areas for current drug development, from cardiovascular to endocrine disorders, and from infectious to neurological diseases. For each area, the availability of animal models for target validation, hit finding and lead profiling is reviewed, backed by numerous examples of both successes and failures among the use of animal models. The whole is rounded off with a discussion of perspectives and challenges.
Key knowledge for drug researchers in industry as well as academia.

Protein-Ligand Interactions (Hardcover): Holger Gohlke Protein-Ligand Interactions (Hardcover)
Holger Gohlke; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R3,631 R3,357 Discovery Miles 33 570 Save R274 (8%) Ships in 10 - 15 working days

Innovative and forward-looking, this volume focuses on recent achievements in this rapidly progressing field and looks at future potential for development. The first part provides a basic understanding of the factors governing protein-ligand interactions, followed by a comparison of key experimental methods (calorimetry, surface plasmon resonance, NMR) used in generating interaction data. The second half of the book is devoted to insilico methods of modeling and predicting molecular recognition and binding, ranging from first principles-based to approximate ones. Here, as elsewhere in the book, emphasis is placed on novel approaches and recent improvements to established methods. The final part looks at unresolved challenges, and the strategies to address them. With the content relevant for all drug classes and therapeutic fields, this is an inspiring and often-consulted guide to the complexity of protein-ligand interaction modeling and analysis for both novices and experts.

Epigenetic Targets in Drug Discovery (Hardcover): Wolfgang Sippl, Manfred Jung Epigenetic Targets in Drug Discovery (Hardcover)
Wolfgang Sippl, Manfred Jung; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R4,380 R3,700 Discovery Miles 37 000 Save R680 (16%) Ships in 10 - 15 working days

Fueled by the expertise of a team of international specialist authors, this first reference on the booming topic covers everything a drug researcher needs to know about targeting epigenetic mechanisms of disease.
The first part of the book surveys current methodologies for finding and validating drug candidates that act via epigenetic mechanisms. The second part systematically surveys known and suspected drug targets within the epigenetic machinery, including the discovery and development of vorinostat, the first marketed epigenetic drug.

Antitargets - Prediction and Prevention of Drug Side Effects (Hardcover): Roy J. Vaz, Thomas Klabunde Antitargets - Prediction and Prevention of Drug Side Effects (Hardcover)
Roy J. Vaz, Thomas Klabunde; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R4,706 R4,420 Discovery Miles 44 200 Save R286 (6%) Ships in 10 - 15 working days

This practice-oriented handbook surveys current knowledge on the prediction and prevention of adverse drug reactions related to off-target activity of small molecule drugs. It is unique in collating the current approaches into a single source, and includes several highly instructive case studies that may be used as guidelines on how to improve drug development projects.
With its large section on ADME-related effects, this is key knowledge for every drug developer.

Drug Selectivity - An Evolving Concept in Medicinal Chemistry (Hardcover): Norbert Handler Drug Selectivity - An Evolving Concept in Medicinal Chemistry (Hardcover)
Norbert Handler; Series edited by Helmut Buschmann, Raimund Mannhold, J?rg Holenz
R3,787 R3,381 Discovery Miles 33 810 Save R406 (11%) Ships in 10 - 15 working days

The book "Drug Selectivity - An Evolving Concept in Medicinal Chemistry" provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process. The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist.

Innovative Dosage Forms - Design and Development at Early Stage (Hardcover): Yogeshwar Bachhav Innovative Dosage Forms - Design and Development at Early Stage (Hardcover)
Yogeshwar Bachhav; Series edited by Raimund Mannhold, Helmut Buschmann, J?rg Holenz
R3,648 R3,258 Discovery Miles 32 580 Save R390 (11%) Ships in 10 - 15 working days

Teaches future and current drug developers the latest innovations in drug formulation design and optimization This highly accessible, practice-oriented book examines current approaches in the development of drug formulations for preclinical and clinical studies, including the use of functional excipients to enhance solubility and stability. It covers oral, intravenous, topical, and parenteral administration routes. The book also discusses safety aspects of drugs and excipients, as well as regulatory issues relevant to formulation. Innovative Dosage Forms: Design and Development at Early Stage starts with a look at the impact of the polymorphic form of drugs on the preformulation and formulation development. It then offers readers reliable strategies for the formulation development of poorly soluble drugs. The book also studies the role of reactive impurities from the excipients on the formulation shelf life; preclinical formulation assessment of new chemical entities; and regulatory aspects for formulation design. Other chapters cover innovative formulations for special indications, including oncology injectables, delayed release and depot formulations; accessing pharmacokinetics of various dosage forms; physical characterization techniques to assess amorphous nature; novel formulations for protein oral dosage; and more. -Provides information that is essential for the drug development effort -Presents the latest advances in the field and describes in detail innovative formulations, such as nanosuspensions, micelles, and cocrystals -Describes current approaches in early pre-formulation to achieve the best in vivo results -Addresses regulatory and safety aspects, which are key considerations for pharmaceutical companies -Includes case studies from recent drug development programs to illustrate the practical challenges of preformulation design Innovative Dosage Forms: Design and Development at Early Stage provides valuable benefits to interdisciplinary drug discovery teams working in industry and academia and will appeal to medicinal chemists, pharmaceutical chemists, and pharmacologists.

Antiviral Drug Strategies (Hardcover): Erik De Clercq Antiviral Drug Strategies (Hardcover)
Erik De Clercq; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R3,714 Discovery Miles 37 140 Ships in 10 - 15 working days

By focusing on general molecular mechanisms of antiviral drugs rather than therapies for individual viruses, this ready reference provides the critical knowledge needed to develop entirely novel therapeutics and to target new viruses.
It begins with a general discussion of antiviral strategies, followed by a broad survey of known viral targets, such as reverse transcriptases, proteases, neuraminidases, RNA polymerases, helicases and primases, as well as their known inhibitors. The final section contains several cases studies of recent successful antiviral drug development.
Edited by Erik de Clercq, the world authority on small molecule antiviral drugs, who has developed more new antivirals than anyone else.

Target Discovery and Validation - Methods and Strategies for Drug Discovery (Hardcover): Alleyn T. Plowright Target Discovery and Validation - Methods and Strategies for Drug Discovery (Hardcover)
Alleyn T. Plowright; Series edited by Raimund Mannhold, Helmut Buschmann, J?rg Holenz
R4,912 Discovery Miles 49 120 Ships in 7 - 11 working days

The modern drug developers? guide for making informed choices among the diverse target identification methods Target Discovery and Validation: Methods and Strategies for Drug Discovery offers a hands-on review of the modern technologies for drug target identification and validation. With contributions from noted industry and academic experts, the book addresses the most recent chemical, biological, and computational methods. Additionally, the book highlights techologies that are applicable to ?difficult? targets and drugs directed at multiple targets, including chemoproteomics, activity-based protein profiling, pathway mapping, genome-wide association studies, and array-based profiling. Throughout, the authors highlight a range of diverse approaches, and target validation studies reveal how these methods can support academic and drug discovery scientists in their target discovery and validation research. This resource: -Offers a guide to identifying and validating targets, a key enabling technology without which no new drug development is possible -Presents the information needed for choosing the appropriate assay method from the ever-growing range of available options -Provides practical examples from recent drug development projects, e. g. in kinase inhibitor profiling Written for medicinal chemists, pharmaceutical professionals, biochemists, biotechnology professionals, and pharmaceutical chemists, Target Discovery and Validation explores the current methods for the identification and validation of drug targets in one comrpehensive volume. It also includes numerous practical examples.

Nuclear Receptors as Drug Targets (Hardcover): Eckhard Ottow, Hilmar Weinmann Nuclear Receptors as Drug Targets (Hardcover)
Eckhard Ottow, Hilmar Weinmann; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R5,238 R4,888 Discovery Miles 48 880 Save R350 (7%) Ships in 10 - 15 working days

Nuclear receptors are the site of action for some of the most widely used medications, namely oral contraceptives and related drugs derived from steroid hormones. Recent research has uncovered their pivotal role in a range of human diseases, including diabetes and metabolic syndrome, triggering a new wave of drug discovery efforts focused on this class of molecular targets.
Edited by two experts working at the pioneering pharmaceutical company and major global player in hormone-derived drugs, this handbook systematically treats the drug development aspects of all human nuclear receptors, including such recently characterized receptors as PPAR, FXR and LXR, and modern tools for nuclear receptor research.
With its contributions from authors working at leading pharmaceutical companies around the world providing examples and real-life data from their own experience, this is an invaluable reference for medicinal chemists, biochemists, molecular biologists, pharmacologists and those working in the pharmaceutical industry.

Protein-Protein Interactions in Drug Discovery (Hardcover): Alexander Domling Protein-Protein Interactions in Drug Discovery (Hardcover)
Alexander Domling; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R4,401 R3,359 Discovery Miles 33 590 Save R1,042 (24%) Ships in 10 - 15 working days

Treating protein-protein interactions as a novel and highly promising class of drug targets, this volume introduces the underlying strategies step by step, from the biology of PPIs to biophysical and computational methods for their investigation.
The main part of the book describes examples of protein targets for which small molecule modulators have been developed, covering such diverse fields as cancer, autoimmune disorders and infectious diseases. Tailor-made for the practicing medicinal chemist, this ready reference includes a wide selection of case studies taken straight from the development pipeline of major pharmaceutical companies to illustrate the power and potential of this approach.
From the contents:
* Prediction of intra- and inter-species protein-protein interactions facilitating systems biology studies
* Modulators of protein-protein interactions: The importance of Three-Dimensionality
* Interactive technologies for leveraging the known chemistry of anchor residues
* SH3 Domains as Drug Targets
* P53 MDM2 Antagonists: Towards Non Genotoxic Anticancer Treatments
* Inhibition of LFA-1/ICAM interaction for treatment of autoimmune diseases
* The PIF-binding pocket of AGC kinases
* Peptidic inhibitors of protein-protein interactions for cell adhesion receptors
* The REPLACE Strategy for generating Non-ATP competitive Inhibitors of Cell-Cycle Protein Kinases
and more

Neglected Tropical Diseases - Drug Discovery and Development (Hardcover): David C. Swinney, Michael P. Pollastri Neglected Tropical Diseases - Drug Discovery and Development (Hardcover)
David C. Swinney, Michael P. Pollastri; Series edited by Raimund Mannhold, Helmut Buschmann, J?rg Holenz
R3,372 R3,015 Discovery Miles 30 150 Save R357 (11%) Ships in 10 - 15 working days

A drug discovery reference to the crippling tropical diseases that affect more than 1 billion people. Neglected Tropical Diseases is the first book of its kind to offer a guide that follows the World Health Organization's list of neglected tropical diseases. The authors?all are experts on the topic?address the development of effective treatments for 12 crippling infectious diseases that affect almost 20% of the world's popluation. The book includes information on the common approaches and the most important factors that lead to the development of new drugs for treating tropical diseases. Individual chapters review 12 neglected tropical diseases that are grouped by infectious agent, from viruses to bacteria to eukaryotic parasites. For each of these diseases, the book explains the unmet medical need and explores the current and potential drug discovery strategies. The book also includes information on potential drug compounds derived from natural products. This important book: -Ties together information from different sources for developing novel treatsments forneglected tropical diseases -Is aligned with WHO's initiative to eradicate tropical diseases -Outlines current and potential drugs for treating tropical diseases -Provides a standard reference for the entire field Written for medicinal chemists, pharmaceutical chemists, pharmaceutical industry, virologists, parasitologists, and specialists on tropics medicine, Neglected Tropical Diseases offers an essential guide and a systematic reference for the development of successful treatments for 12 crippling infectious diseases.

Medicinal Chemistry Approaches to Personalized Medicine (Hardcover): Karen Lackey, Bruce Roth Medicinal Chemistry Approaches to Personalized Medicine (Hardcover)
Karen Lackey, Bruce Roth; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R3,630 R2,893 Discovery Miles 28 930 Save R737 (20%) Ships in 10 - 15 working days

Edited by two renowned medicinal chemists who have pioneered the development of personalized therapies in their respective fields, this authoritative analysis of what is already possible is the first of its kind, and the only one to focus on drug development issues. Numerous case studies from the first generation of "personalized drugs" are presented, highlighting the challenges and opportunities for pharmaceutical development. While the majority of these examples are taken from the field of cancer treatment, other key emerging areas, such as neurosciences and inflammation, are also covered. With its careful balance of current and future approaches, this handbook is a prime knowledge source for every drug developer, and one that will remain up to date for some time to come. From the content: * Discovery of Predictive Biomarkers for Anticancer Drugs * Discovery and Development of Vemurafenib * Targeting Basal-Cell Carcinoma * G-Quadruplexes as Therapeutic Targets in Cancer * From Human Genetics to Drug Candidates: An Industrial Perspective on LRRK2 Inhibition as a Treatment for Parkinson's Disease * Therapeutic Potential of Kinases in Asthma * DNA Damage Repair Pathways and Synthetic Lethality * Medicinal Chemistry in the Context of the Human Genome and many more

Phosphodiesterases and Their Inhibitors (Hardcover): Spiros Liras, Andrew S. Bell Phosphodiesterases and Their Inhibitors (Hardcover)
Spiros Liras, Andrew S. Bell; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R3,485 R2,768 Discovery Miles 27 680 Save R717 (21%) Ships in 10 - 15 working days

Written by the pioneers of Viagra, the first blockbuster PDE inhibitor drug.
Beginning with a review of the first wave of phosphodiesterase (PDE) inhibitors, this book focuses on new and emerging PDE targets and their inhibitors. Drug development options for all major human PDE families are discussed and cover diverse therapeutic fields, such as neurological/psychiatric, cardiovascular/metabolic, pain, and allergy/respiratory diseases. Finally, emerging chemotherapeutic applications of PDE inhibitors against malaria and other tropical diseases are discussed.

Early Drug Development - Bringing a Preclinical Candidate to the Clinic 2 Volume Set (Hardcover): Fabrizio Giordanetto Early Drug Development - Bringing a Preclinical Candidate to the Clinic 2 Volume Set (Hardcover)
Fabrizio Giordanetto; Series edited by Raimund Mannhold, Helmut Buschmann, J?rg Holenz
R7,525 R5,987 Discovery Miles 59 870 Save R1,538 (20%) Ships in 10 - 15 working days

This one-stop reference systematically covers key aspects in early drug development that are directly relevant to the discovery phase and are required for first-in-human studies. Its broad scope brings together critical knowledge from many disciplines, ranging from process technology to pharmacology to intellectual property issues. After introducing the overall early development workflow, the critical steps of early drug development are described in a sequential and enabling order: the availability of the drug substance and that of the drug product, the prediction of pharmacokinetics and -dynamics, as well as that of drug safety. The final section focuses on intellectual property aspects during early clinical development. The emphasis throughout is on recent case studies to exemplify salient points, resulting in an abundance of practice-oriented information that is usually not available from other sources. Aimed at medicinal chemists in industry as well as academia, this invaluable reference enables readers to understand and navigate the challenges in developing clinical candidate molecules that can be successfully used in phase one clinical trials.

Reactive Drug Metabolites (Hardcover): Amit S. Kalgutkar, Deepak Dalvie, Dennis A. Smith, R. Scott Obach Reactive Drug Metabolites (Hardcover)
Amit S. Kalgutkar, Deepak Dalvie, Dennis A. Smith, R. Scott Obach; Series edited by Raimund Mannhold, …
R3,903 R3,104 Discovery Miles 31 040 Save R799 (20%) Ships in 10 - 15 working days

Closing a gap in the scientific literature, this first comprehensive introduction to the topic is based on current best practice in one of the largest pharmaceutical companies worldwide. The first chapters trace the development of our understanding of drug metabolite toxicity, covering basic concepts and techniques in the process, while the second part details chemical toxicophores that are prone to reactive metabolite formation. This section also reviews the various drug-metabolizing enzymes that can participate in catalyzing reactive metabolite formation, including a discussion of the structure-toxicity relationships for drugs. Two chapters are dedicated to the currently hot topics of herbal constituents and IADRs. The next part covers current strategies and approaches to evaluate the reactive metabolite potential of new drug candidates, both by predictive and by bioanalytical methods. There then follows an in-depth analysis of the toxicological potential of the top 200 prescription drugs, illustrating the power and the limits of the toxicophore concept, backed by numerous case studies. Finally, a risk-benefit approach to managing the toxicity risk of reactive metabolite-prone drugs is presented. Since the authors carefully develop the knowledge needed, from fundamental considerations to current industry standards, no degree in pharmacology is required to read this book, making it perfect for medicinal chemists without in-depth pharmacology training.

Epigenetic Drug Discovery (Hardcover): Wolfgang Sippl, Manfred Jung Epigenetic Drug Discovery (Hardcover)
Wolfgang Sippl, Manfred Jung; Series edited by Raimund Mannhold, Helmut Buschmann, J?rg Holenz
R4,261 R3,380 Discovery Miles 33 800 Save R881 (21%) Ships in 10 - 15 working days

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.

Data Mining in Drug Discovery (Hardcover): Remy D. Hoffmann, Arnaud Gohier, Pavel Pospisil Data Mining in Drug Discovery (Hardcover)
Remy D. Hoffmann, Arnaud Gohier, Pavel Pospisil; Series edited by Raimund Mannhold, Hugo Kubinyi, …
R4,018 R3,189 Discovery Miles 31 890 Save R829 (21%) Ships in 10 - 15 working days

Written for drug developers rather than computer scientists, this monograph adopts a systematic approach to mining scientifi c data sources, covering all key steps in rational drug discovery, from compound screening to lead compound selection and personalized medicine. Clearly divided into four sections, the first part discusses the different data sources available, both commercial and non-commercial, while the next section looks at the role and value of data mining in drug discovery. The third part compares the most common applications and strategies for polypharmacology, where data mining can substantially enhance the research effort. The final section of the book is devoted to systems biology approaches for compound testing. Throughout the book, industrial and academic drug discovery strategies are addressed, with contributors coming from both areas, enabling an informed decision on when and which data mining tools to use for one's own drug discovery project.

Chemokine Receptors as Drug Targets (Hardcover): Martine J. Smit, Sergio A. Lira, Rob Leurs Chemokine Receptors as Drug Targets (Hardcover)
Martine J. Smit, Sergio A. Lira, Rob Leurs; Series edited by Raimund Mannhold, Hugo Kubinyi, …
R4,390 R3,476 Discovery Miles 34 760 Save R914 (21%) Ships in 10 - 15 working days

Chemokines are hormone-like signaling molecules secreted by cells to signal infection and guide the immune response. Following a decade of basic chemokine research, the pharmaceutical industry has now begun to exploit this crucial signaling pathway for the development of innovative drugs against AIDS, cancer, neural and autoimmune diseases. Here is the first reference focusing on these novel drug development opportunities. Opening with a general introduction on chemokine function and chemokine receptor biology, the second part covers the known implications of these signaling molecules in human diseases, such as cancer, neural disorders, and viral infection, including AIDS. The third part systematically surveys current drug development efforts at targeting individual chemokine receptors, as well as other chemokine interaction partners, including up-to-date reports from the pharmaceutical industry.

Hit and Lead Profiling - Identification and Optimization of Drug-like Molecules (Hardcover): Bernard Faller, Laszlo Urban Hit and Lead Profiling - Identification and Optimization of Drug-like Molecules (Hardcover)
Bernard Faller, Laszlo Urban; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R5,517 R4,356 Discovery Miles 43 560 Save R1,161 (21%) Ships in 10 - 15 working days

The only reference on current methods to generate pharmacokinetic and safety profiles of drug candidates, as well as how they must be balanced against one other for the best selection of candidates for further development.
Following a brief introduction to the necessities of filtering and risk assessment of potential new drug molecules before actual drug development, the two equally important aspects of pharmacological (ADME) and safety (toxicity) profiling are covered in separate parts.
The ADME section covers the profiling of basic physicochemical parameters, such as solubility and permeability, as well as more complex traits, such as the likelihood of drug-drug interactions, metabolic clearance and protein binding properties.
The toxicology part addresses, among others, recent advances in early genetic toxicity testing, bioactivation screening, organ-specific toxicity assays for liver, heart, kidney and blood, as well as profiling for autoimmune reactions.
By addressing both drug efficiency and drug safety, this modern practical reference shows readers how each individual aspect figures in shaping the key decisions on which the entire drug development process hinges. In short, this is a complete toolbox for assessing the risk/benefit ratio for any novel compound during the early drug development stages, using both in vitro and in silico methods.
Both editors are based at one of the leading research-driven pharmaceutical companies, and the authors have been recruited from numerous other global players in the field.
Invaluable know-how for every medicinal chemist and drug developer.

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