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Showing 1 - 25 of 53 matches in All departments

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
R2,999 R2,395 Discovery Miles 23 950 Save R604 (20%) Shipped within 7 - 12 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
R2,879 R2,279 Discovery Miles 22 790 Save R600 (21%) Shipped within 7 - 12 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.

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
R2,989 R2,386 Discovery Miles 23 860 Save R603 (20%) Shipped within 7 - 12 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.

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
R3,001 R2,398 Discovery Miles 23 980 Save R603 (20%) Shipped within 7 - 12 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.

Drug Metabolism Prediction (Hardcover): Johannes Kirchmair Drug Metabolism Prediction (Hardcover)
Johannes Kirchmair; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R3,526 R2,795 Discovery Miles 27 950 Save R731 (21%) Shipped within 7 - 12 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.

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, …
R3,319 R2,678 Discovery Miles 26 780 Save R641 (19%) Shipped within 7 - 12 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, …
R3,627 R2,869 Discovery Miles 28 690 Save R758 (21%) Shipped within 7 - 12 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.

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
R5,257 R4,670 Discovery Miles 46 700 Save R587 (11%) Shipped within 7 - 12 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.

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, …
R3,224 R2,588 Discovery Miles 25 880 Save R636 (20%) Shipped within 7 - 12 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.

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
R4,557 R3,653 Discovery Miles 36 530 Save R904 (20%) Shipped within 7 - 12 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.

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
R4,449 R3,549 Discovery Miles 35 490 Save R900 (20%) Shipped within 7 - 12 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
R4,451 R3,956 Discovery Miles 39 560 Save R495 (11%) Shipped within 7 - 12 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, …
R3,247 R2,611 Discovery Miles 26 110 Save R636 (20%) Shipped within 7 - 12 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
R2,999 R2,673 Discovery Miles 26 730 Save R326 (11%) Shipped within 7 - 12 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
R3,618 R2,861 Discovery Miles 28 610 Save R757 (21%) Shipped within 7 - 12 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
R4,352 R3,458 Discovery Miles 34 580 Save R894 (21%) Shipped within 7 - 12 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.

High-Throughput Screening in Drug Discovery (Hardcover): Jorg Huser High-Throughput Screening in Drug Discovery (Hardcover)
Jorg Huser; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R4,439 R3,539 Discovery Miles 35 390 Save R900 (20%) Shipped within 7 - 12 working days

Backed by leading authorities, this is a professional guide to successful compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for correct data evaluation. Chapter authors from leading pharmaceutical companies as well as from Harvard University discuss such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results.

For both academics and professionals in the pharma and biotech industries working on small molecule screening.

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
R4,865 R3,845 Discovery Miles 38 450 Save R1,020 (21%) Shipped within 7 - 12 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.

Microwaves in Organic and Medicinal Chemistry (Hardcover, 2nd, Completely Revised and Enlarged Edition): C.Oliver Kappe,... Microwaves in Organic and Medicinal Chemistry (Hardcover, 2nd, Completely Revised and Enlarged Edition)
C.Oliver Kappe, Alexander Stadler, Doris Dallinger; Series edited by Raimund Mannhold, Hugo Kubinyi, …
R4,087 R3,288 Discovery Miles 32 880 Save R799 (20%) Shipped within 7 - 12 working days

Tailored to the needs of medicinal and natural products chemists, the second edition of this unique handbook brings the contents up to speed, almost doubling the amount of chemical information with an additional volume. As in the predecessor, a short introductory section covers the theoretical background and evaluates currently available instrumentation and equipment. The main part of the book then goes on to systematically survey the complete range of published microwave-assisted synthesis methods from their beginnings in the 1990s to mid-2011, drawing on data from more than 5,000 reports and publications. Throughout, the focus is on those reactions, reagents and reaction conditions that work, and that are the most relevant for medicinal and natural products chemistry. A much expanded section is devoted to combinatorial, high-throughput and flow chemistry methods.

Virtual Screening - Principles, Challenges, and Practical Guidelines (Hardcover): Christoph Sotriffer Virtual Screening - Principles, Challenges, and Practical Guidelines (Hardcover)
Christoph Sotriffer; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R4,424 R3,095 Discovery Miles 30 950 Save R1,329 (30%) Shipped within 7 - 13 working days

Drug discovery is all about finding small molecules that interact in a desired way with larger molecules, namely proteins and other macromolecules in the human body. If the three-dimensional structures of both the small and large molecule are known, their interaction can be tested by computer simulation with a reasonable degree of accuracy. Alternatively, if active ligands are already available, molecular similarity searches can be used to find new molecules. This virtual screening can even be applied to compounds that have yet to be synthesized, as opposed to "real" screening that requires cost- and labor-intensive laboratory testing with previously synthesized drug compounds. Unique in its focus on the end user, this is a real "how to" book that does not presuppose prior experience in virtual screening or a background in computational chemistry. It is both a desktop reference and practical guide to virtual screening applications in drug discovery, offering a comprehensive and up-to-date overview. Clearly divided into four major sections, the first provides a detailed description of the methods required for and applied in virtual screening, while the second discusses the most important challenges in order to improve the impact and success of this technique. The third and fourth, practical parts contain practical guidelines and several case studies covering the most important scenarios for new drug discovery, accompanied by general guidelines for the entire workflow of virtual screening studies. Throughout the text, medicinal chemists from academia, as well as from large and small pharmaceutical companies report on their experience and pass on priceless practical advice on how to make best use of these powerful methods.

Fragment-based Drug Discovery - Lessons and Outlook (Hardcover): Daniel A. Erlanson, Wolfgang Jahnke Fragment-based Drug Discovery - Lessons and Outlook (Hardcover)
Daniel A. Erlanson, Wolfgang Jahnke; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R3,121 R2,509 Discovery Miles 25 090 Save R612 (20%) Shipped within 7 - 12 working days

From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.

Bioisosteres in Medicinal Chemistry (Hardcover): Nathan Brown Bioisosteres in Medicinal Chemistry (Hardcover)
Nathan Brown; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R2,998 R2,372 Discovery Miles 23 720 Save R626 (21%) Shipped within 7 - 12 working days

Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section.

Transporters as Drug Targets (Hardcover): Gerhard F. Ecker, Rasmus P. Clausen, Harald H. Sitte Transporters as Drug Targets (Hardcover)
Gerhard F. Ecker, Rasmus P. Clausen, Harald H. Sitte; Series edited by Raimund Mannhold, Gerd Folkers, …
R2,893 R2,293 Discovery Miles 22 930 Save R600 (21%) Shipped within 7 - 12 working days

As opposed to other books on the topic, this volume is unique in also covering emerging transporter targets. Following a general introduction to the importance of targeting transporter proteins with drugs, the book systematically presents individual transporter classes and explains their pharmacology and physiology. The text covers all transporter families with known or suspected importance as drug targets, including neurotransmitter transporters, ABC transporters, glucose transporters and organic ion transporters. The final part discusses recent advances in structural studies of transport proteins, assay methods for transport activity, and the systems biology of transporters and their regulation. With its focus on drug development issues, this authoritative overview is required reading for researchers in industry and academia targeting transport proteins for the treatment of disease.

Molecular Drug Properties - Measurement and Prediction (Hardcover): Raimund Mannhold Molecular Drug Properties - Measurement and Prediction (Hardcover)
Raimund Mannhold; Series edited by Hugo Kubinyi, Gerd Folkers
R4,215 R3,746 Discovery Miles 37 460 Save R469 (11%) Shipped within 7 - 12 working days

This first systematic overview for more than a decade is tailor-made for the medicinal chemist. All the chapters are written by experienced drug developers and include practical examples from real drug candidates. Following an introduction to global drug properties and their impact on drug research, screening and combinatorial chemistry libraries, this handbook demonstrates the best and fastest way to estimate those properties most relevant for the efficiency and pharmacokinetic performance of a drug molecule: lipophilicity, solubility, electronic properties and conformation

Pharmacokinetics and Metabolism in Drug Design (Hardcover, 3rd Edition): Dennis A. Smith, Charlotte Allerton, Hugo Kubinyi, Han... Pharmacokinetics and Metabolism in Drug Design (Hardcover, 3rd Edition)
Dennis A. Smith, Charlotte Allerton, Hugo Kubinyi, Han Van De Waterbeemd, Han Walker, …
R2,592 R2,086 Discovery Miles 20 860 Save R506 (20%) Shipped within 7 - 12 working days

In this new edition of a bestseller, all the contents have been brought upto- date by addressing current standards and best practices in the assessment and prediction of ADMET properties. Although the previous chapter layout has been retained, substantial revisions have been made, with new topics such as pro-drugs, active metabolites and transporters covered in detail in a manner useful to the Drug Discovery scientist. The authors discuss the parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. Uniquely comprehensive, the book relates physicochemistry and chemical structure to pharmacokinetic properties and ultimately drug efficacy and safety. While aimed at all those dealing professionally with the development and application of pharmaceutical substances, the readily comprehensible style makes this book equally suitable for students of pharmacy and related subjects.

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