The Design of Synthetic Inhibitors of Thrombin

The Design of Synthetic Inhibitors of Thrombin PDF Author: Goran Claeson
Publisher: Springer Science & Business Media
ISBN: 1489924183
Category : Medical
Languages : en
Pages : 245

Get Book Here

Book Description
In one generation, the numerous factors involved in blood coagulation have become real protein entities, isolated in pure form, expressed by recombinant DNA techniques, and subjected to structure elucidation by the modem methods of physical chemistry, viz. , X-ray diffraction, and NMR, ESR and fluorescence spectroscopy. The major milestone in this field was the breakthrough achieved by W. Bode, R. Huber and their colleagues in 1989 in of human a-thrombin, inhibited with D-Phe-Pro-Arg determining the crystal structure chioromethyl ketone. The availability of this structure will greatly facilitate the interpretation of experiments designed to gain an understanding of the interatomic interactions between this enzyme and fibrinogen and its other substrates. At the same time, it provides a rational basis for the design and synthesis of inhibitors of thrombin, the subject of this symposium. The symposium was organized in four sessions: (1) Structural features of the interaction of thrombin with substrates and inhibitors, (2) Synthetic inhibitors, (3) Hirudin and its analogues, and (4) Pharmacological and clinical considerations. This book contains summaries of most of the papers presented, and takes its rigbful place among two others that provide a comprehensive picture of our current knowledge about thrombin, viz. the 1977 volume entitled "Chemistry and Biology of Thrombin", edited by R. L. Lundblad, J. W. Fenton II, and K. G. Mann, and the 1992 volume entitled "Thrombin: Structure and Function", edited by L. J. Berliner.

The Design of Synthetic Inhibitors of Thrombin

The Design of Synthetic Inhibitors of Thrombin PDF Author: Goran Claeson
Publisher: Springer Science & Business Media
ISBN: 1489924183
Category : Medical
Languages : en
Pages : 245

Get Book Here

Book Description
In one generation, the numerous factors involved in blood coagulation have become real protein entities, isolated in pure form, expressed by recombinant DNA techniques, and subjected to structure elucidation by the modem methods of physical chemistry, viz. , X-ray diffraction, and NMR, ESR and fluorescence spectroscopy. The major milestone in this field was the breakthrough achieved by W. Bode, R. Huber and their colleagues in 1989 in of human a-thrombin, inhibited with D-Phe-Pro-Arg determining the crystal structure chioromethyl ketone. The availability of this structure will greatly facilitate the interpretation of experiments designed to gain an understanding of the interatomic interactions between this enzyme and fibrinogen and its other substrates. At the same time, it provides a rational basis for the design and synthesis of inhibitors of thrombin, the subject of this symposium. The symposium was organized in four sessions: (1) Structural features of the interaction of thrombin with substrates and inhibitors, (2) Synthetic inhibitors, (3) Hirudin and its analogues, and (4) Pharmacological and clinical considerations. This book contains summaries of most of the papers presented, and takes its rigbful place among two others that provide a comprehensive picture of our current knowledge about thrombin, viz. the 1977 volume entitled "Chemistry and Biology of Thrombin", edited by R. L. Lundblad, J. W. Fenton II, and K. G. Mann, and the 1992 volume entitled "Thrombin: Structure and Function", edited by L. J. Berliner.

Casebook in Clinical Pharmacokinetics and Drug Dosing

Casebook in Clinical Pharmacokinetics and Drug Dosing PDF Author: Henry Cohen
Publisher: McGraw Hill Professional
ISBN: 0071832769
Category : Medical
Languages : en
Pages : 300

Get Book Here

Book Description
A STEP-BY-STEP APPROACH TO DESIGNING ACCURATE DOSING REGIMENS Casebook in Pharmacokinetics and Drug Dosing uses real-life cases to teach pharmacy students, pharmacists, and clinical pharmacists how to apply pharmacokinetics to formulate proper dosing regimens. In order to be as clinically relevant as possible, the book not only discusses drugs with readily available therapeutic serum levels, but places equal emphasis on high-alert agents with narrow therapeutic indexes. Each drug chapter is written by clinical pharmacists who have hands-on experience in drug dosing and includes an overview of the drug’s pharmacology, including: Indications Mec hanisms of action Toxicities Pharmacokinetics There is comprehensive review and discussion of each drug's bioavailability, volume of distribution, clearance, half-life, therapeutic drug level monitoring, drug interactions, dosing, and availability. Each chapter is enhanced by numerous patient cases with clear step-by-step answers and explanations. Calculations, equations, and dosing recommendations are provided for each case.

Structural Biology in Drug Discovery

Structural Biology in Drug Discovery PDF Author: Jean-Paul Renaud
Publisher: John Wiley & Sons
ISBN: 1118900502
Category : Medical
Languages : en
Pages : 1437

Get Book Here

Book Description
With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Chemistry and Biology of Heparin and Heparan Sulfate

Chemistry and Biology of Heparin and Heparan Sulfate PDF Author: Hari G. Garg
Publisher: Elsevier
ISBN: 0080529054
Category : Science
Languages : en
Pages : 793

Get Book Here

Book Description
The chemistry, biochemistry and pharmacology of heparin and heparan sulfate have been and continue to be a major scientific undertaking - heparin and its derivative remain important drugs in clinical practice. Chemistry and Biology of Heparin and Heparan Sulfate provides readers with an insight into the chemistry, biology and clinical applications of heparin and heparan sulfate and examines their function in various physiological and pathological conditions. Providing a wealth of useful information, no other tome covers the diversity of topics in the field. Students, doctors, chemists, biochemists, and research scientists will find this book an invaluable source for updating their current knowledge of developments in this area. - Comprehensively reviews all aspects of heparin and heparan sulfate research - Uniquely describes the chemistry, biology and clinical application of heparins and heparan sulfates in one work - Provides an invaluable source of knowledge of current developments for chemists, biochemists, medical doctors, researchers, students and practitioners

Encyclopedia of Heart Diseases

Encyclopedia of Heart Diseases PDF Author: M. Gabriel Khan
Publisher: Elsevier
ISBN: 008045481X
Category : Medical
Languages : en
Pages : 678

Get Book Here

Book Description
The Encyclopedia of Heart Diseases is an accurate and reliable source of in-depth information on the diseases that kill more than 12 million individuals worldwide each year. In fact, cardiovascular diseases are more prevalent than the combined incidence of all forms of cancer, diabetes, asthma and leukemia. In one volume, this Encylopedia thoroughly covers these ailments and also includes in-depth analysis of less common and rare heart conditions to round out the volume's scope. Researchers, clinicians, and students alike will all find this resource an invaluable tool for quick reference before approaching the primary literature.* Coverage of more than 200 topics, including: applied pharmacology of current and experimental cardiac drugs, gene therapy, MRI, electron-beam CT, PET scan put in perspective, cardiac tests costs and justification, and new frontiers in cardiovascular research* More than 150 helpful figures and illustrations!* Dr. Khan is a well-published and respected expert in heart and heart diseases

Anticoagulant Drugs

Anticoagulant Drugs PDF Author: Mojca Božič-Mijovski
Publisher: BoD – Books on Demand
ISBN: 1789236223
Category : Medical
Languages : en
Pages : 122

Get Book Here

Book Description
Anticoagulant drugs are among the most frequently prescribed drugs in everyday clinical practice. In the past decades, several new direct oral anticoagulants were developed that changed the anticoagulant therapy landscape considerably. This book provides an extensive overview of all the known anticoagulants that can be useful for studying different aspects of the haemostatic system or as a starting point for new drug development. It is also a valuable tool for clinicians providing a description of the mode of action and management of therapy for anticoagulant drugs used in everyday clinical practice in different clinical settings, including direct oral anticoagulants dabigatran, rivaroxaban, apixaban and edoxaban.

Structure-based Design of Drugs and Other Bioactive Molecules

Structure-based Design of Drugs and Other Bioactive Molecules PDF Author: Arun K. Ghosh
Publisher: John Wiley & Sons
ISBN: 3527333657
Category : Medical
Languages : en
Pages : 474

Get Book Here

Book Description
Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use numerous examples of recently developed drugs to present "best practice" methods in structurebased drug design with both newcomers and practicing researchers in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design. This book is aimed at new and active medicinal chemists, biochemists, pharmacologists, natural product chemists and those working in drug discovery in the pharmaceutical industry. It is highly recommended as a desk reference to guide students in medicinal and chemical sciences as well as to aid researchers engaged in drug design today.

Combinatorial Library Design and Evaluation

Combinatorial Library Design and Evaluation PDF Author: Arup Ghose
Publisher: CRC Press
ISBN: 1482270765
Category : Medical
Languages : en
Pages : 655

Get Book Here

Book Description
This text traces developments in rational drug discovery and combinatorial library design with contributions from 50 leading scientists in academia and industry who offer coverage of basic principles, design strategies, methodologies, software tools and algorithms, and applications. It outlines the fundamentals of pharmacophore modelling and 3D Qua

Structure-Based Drug Design

Structure-Based Drug Design PDF Author: Pandi Veerapandian
Publisher: Routledge
ISBN: 1351413058
Category : Medical
Languages : en
Pages : 668

Get Book Here

Book Description
Introducing the most recent advances in crystallography, nuclear magnetic resonance, molecular modeling techniques, and computational combinatorial chemistry, this unique, interdisciplinary reference explains the application of three-dimensional structural information in the design of pharmaceutical drugs. Furnishing authoritative analyses by world-renowned experts, Structure-Based Drug Design discusses protein structure-based design in optimizing HIV protease inhibitors and details the biochemical, genetic, and clinical data on HIV-1 reverse transcriptase presents recent results on the high-resolution three-dimensional structure of the catalytic core domain of HIV-1 integrase as a foundation for divergent combination therapy focuses on structure-based design strategies for uncovering receptor antagonists to treat inflammatory diseases demonstrates a systematic approach to the design of inhibitory compounds in cancer treatment reviews current knowledge on the Interleukin-1 (IL-1) system and progress in the development of IL-1 modulators describes the influence of structure-based methods in designing capsid-binding inhibitors for relief of the common cold and much more!

Anesthetic Pharmacology

Anesthetic Pharmacology PDF Author: Alex S. Evers
Publisher: Cambridge University Press
ISBN: 1139497022
Category : Medical
Languages : en
Pages : 2902

Get Book Here

Book Description
In recent years our understanding of molecular mechanisms of drug action and interindividual variability in drug response has grown enormously. Meanwhile, the practice of anesthesiology has expanded to the preoperative environment and numerous locations outside the OR. Anesthetic Pharmacology: Basic Principles and Clinical Practice, 2nd edition, is an outstanding therapeutic resource in anesthesia and critical care: Section 1 introduces the principles of drug action, Section 2 presents the molecular, cellular and integrated physiology of the target organ/functional system and Section 3 reviews the pharmacology and toxicology of anesthetic drugs. The new Section 4, Therapeutics of Clinical Practice, provides integrated and comparative pharmacology and the practical application of drugs in daily clinical practice. Edited by three highly acclaimed academic anesthetic pharmacologists, with contributions from an international team of experts, and illustrated in full colour, this is a sophisticated, user-friendly resource for all practitioners providing care in the perioperative period.