Basic principles of drug discovery and development / Benjamin E. Blass, Temple University School of Pharmacy, Moulder Center for Drug Discovery Research, North Broad Street, Philadelphia, PA, USA.

By:

Blass, Benjamin E [author.]

Material type: Text

TextPublisher: Amsterdam ; Boston : Elsevier/AP, Academic Press is an imprint of Elsevier, [2015]Description: xv, 574 pages : illustrations ; 23 cmContent type:

text

Media type:

unmediated

Carrier type:

volume

ISBN:

9780124115088 (paperback)
012411508X (paperback)

Subject(s):

DDC classification:

615.19 23 B.B.B

LOC classification:

RM301.25 .B59 2015

NLM classification:

2015 G-397
QV 745

Online resources:

Abstract

Contents:

Front Cover; Basic Principles of Drug Discovery and Development; Copyright; Dedication; Contents; Foreword; Chapter 1 -- Drug Discovery and Development: An Overview of Modern Methods and Principles; DRUG DISCOVERY AND DEVELOPMENT FROM 20,000FEET (FIGURE 1.7); TARGET SELECTION: THE FIRST STEP FORWARD; HIT IDENTIFICATION: FINDING A STARTING POINT; IDENTIFY A CLINICAL CANDIDATE: JUGGLING THE PROPERTIES; QUESTIONS; References; Chapter 2 -- The Drug Discovery Process: From Ancient Times to the Present Day; THE AGE OF BOTANICALS: PREINDUSTRIAL DRUG DISCOVERY PAUL EHRLICH: THE FATHER OF MODERN DRUG DISCOVERY10MILESTONES IN DRUG DISCOVERY; THE RISE OF BIOLOGICS AND MACROMOLECULAR THERAPEUTICS; SOCIETAL AND GOVERNMENTAL IMPACTS; REGULATORY MILESTONES; FUTURE DEVELOPMENTS IN DRUG DISCOVERY; QUESTIONS; References; Chapter 3 -- Classical Targets in Drug Discovery; PROTEIN STRUCTURE; ENZYMES; INHIBITION OF ENZYMES; G-PROTEIN-COUPLED RECEPTORS (GPCRS); ION CHANNELS; MEMBRANE TRANSPORT PROTEINS (TRANSPORTERS); EMERGING TARGETS; QUESTIONS; References; Chapter 4 -- In vitro Screening Systems; THE LANGUAGE OF SCREENING: BASIC TERMS; STREPTAVIDIN AND BIOTIN BIOCHEMICAL VERSUS CELLULAR ASSAYSASSAY SYSTEMS AND METHODS OF DETECTION; RADIOLIGAND ASSAY SYSTEMS; ENZYME-LINKED IMMUNOSORBENT ASSAY (ELISA); FLUORESCENCE-BASED ASSAY SYSTEMS; REPORTER GENE ASSAYS; KINETIC FLUORESCENT MEASUREMENT SYSTEMS; LABEL-FREE ASSAY SYSTEMS; ELECTROPHYSIOLOGICAL PATCH CLAMP; GENERAL CONSIDERATION FOR ALL SCREENING METHODS; QUESTIONS; References; Chapter 5 -- Medicinal Chemistry; STRUCTURE-ACTIVITY RELATIONSHIPS AND STRUCTURE-PROPERTY RELATIONSHIPS; THE ROLE OF CHIRALITY; PUSH AND PULL IN STRUCTURE-ACTIVITY RELATIONSHIPS; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS THE PHARMACOPHOREDEVELOPING AN SAR DATA SET; THE STRUCTURE-ACTIVITY RELATIONSHIP CYCLE; BIOISOSTERISM; STRUCTURE-ACTIVITY RELATIONSHIP, SELECTIVITY AND PHYSICOCHEMICAL PROPERTIES; "DRUGLIKE" GUIDELINES; QUESTIONS; References; Chapter 6 -- In vitro ADME and In vivo Pharmacokinetics; ABSORPTION; DISTRIBUTION; ELIMINATION PATHWAYS; IN VITRO ADME SCREENING METHODS; IN VIVO PHARMACOKINETICS; SPECIES SELECTION; QUESTIONS; References; Chapter 7 -- Animal Models of Disease States; SOURCES OF ANIMAL MODELS; VALIDITY OF ANIMAL MODELS; SPECIES SELECTION; NUMBER OF ANIMALS EXEMPLARY ANIMAL MODELS BY DISEASE CATEGORYANIMAL MODELS OF INFECTIOUS DISEASE; ANIMAL MODELS OF ONCOLOGY; QUESTIONS; References; Chapter 8 -- Safety and Toxicology; SOURCES OF TOXICITY; ACUTE VERSUS CHRONIC TOXICITY; CYTOTOXICITY; CARCINOGENICITY, GENOTOXICITY, AND MUTAGENICITY; DRUG-DRUG INTERACTIONS; CARDIOVASCULAR SAFETY AND TOXICOLOGY STUDIES; CENTRAL NERVOUS SYSTEM SAFETY AND TOXICOLOGY STUDIES; IMMUNE SYSTEM MEDIATED SAFETY ISSUES; TERATOGENICITY; IN VIVO TOXICITY AND SAFETY STUDIES; QUESTIONS; References; Chapter 9 -- Basics of Clinical Trials; BEFORE THE CLINIC; DRUG SUPPLY

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Includes biblographical references and indexes.

Front Cover; Basic Principles of Drug Discovery and Development; Copyright; Dedication; Contents; Foreword; Chapter 1 --
Drug Discovery and Development: An Overview of Modern Methods and Principles; DRUG DISCOVERY AND DEVELOPMENT FROM 20,000FEET (FIGURE 1.7); TARGET SELECTION: THE FIRST STEP FORWARD; HIT IDENTIFICATION: FINDING A STARTING POINT; IDENTIFY A CLINICAL CANDIDATE: JUGGLING THE PROPERTIES; QUESTIONS; References; Chapter 2 --
The Drug Discovery Process: From Ancient Times to the Present Day; THE AGE OF BOTANICALS: PREINDUSTRIAL DRUG DISCOVERY PAUL EHRLICH: THE FATHER OF MODERN DRUG DISCOVERY10MILESTONES IN DRUG DISCOVERY; THE RISE OF BIOLOGICS AND MACROMOLECULAR THERAPEUTICS; SOCIETAL AND GOVERNMENTAL IMPACTS; REGULATORY MILESTONES; FUTURE DEVELOPMENTS IN DRUG DISCOVERY; QUESTIONS; References; Chapter 3 --
Classical Targets in Drug Discovery; PROTEIN STRUCTURE; ENZYMES; INHIBITION OF ENZYMES; G-PROTEIN-COUPLED RECEPTORS (GPCRS); ION CHANNELS; MEMBRANE TRANSPORT PROTEINS (TRANSPORTERS); EMERGING TARGETS; QUESTIONS; References; Chapter 4 --
In vitro Screening Systems; THE LANGUAGE OF SCREENING: BASIC TERMS; STREPTAVIDIN AND BIOTIN BIOCHEMICAL VERSUS CELLULAR ASSAYSASSAY SYSTEMS AND METHODS OF DETECTION; RADIOLIGAND ASSAY SYSTEMS; ENZYME-LINKED IMMUNOSORBENT ASSAY (ELISA); FLUORESCENCE-BASED ASSAY SYSTEMS; REPORTER GENE ASSAYS; KINETIC FLUORESCENT MEASUREMENT SYSTEMS; LABEL-FREE ASSAY SYSTEMS; ELECTROPHYSIOLOGICAL PATCH CLAMP; GENERAL CONSIDERATION FOR ALL SCREENING METHODS; QUESTIONS; References; Chapter 5 --
Medicinal Chemistry; STRUCTURE-ACTIVITY RELATIONSHIPS AND STRUCTURE-PROPERTY RELATIONSHIPS; THE ROLE OF CHIRALITY; PUSH AND PULL IN STRUCTURE-ACTIVITY RELATIONSHIPS; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS THE PHARMACOPHOREDEVELOPING AN SAR DATA SET; THE STRUCTURE-ACTIVITY RELATIONSHIP CYCLE; BIOISOSTERISM; STRUCTURE-ACTIVITY RELATIONSHIP, SELECTIVITY AND PHYSICOCHEMICAL PROPERTIES; "DRUGLIKE" GUIDELINES; QUESTIONS; References; Chapter 6 --
In vitro ADME and In vivo Pharmacokinetics; ABSORPTION; DISTRIBUTION; ELIMINATION PATHWAYS; IN VITRO ADME SCREENING METHODS; IN VIVO PHARMACOKINETICS; SPECIES SELECTION; QUESTIONS; References; Chapter 7 --
Animal Models of Disease States; SOURCES OF ANIMAL MODELS; VALIDITY OF ANIMAL MODELS; SPECIES SELECTION; NUMBER OF ANIMALS EXEMPLARY ANIMAL MODELS BY DISEASE CATEGORYANIMAL MODELS OF INFECTIOUS DISEASE; ANIMAL MODELS OF ONCOLOGY; QUESTIONS; References; Chapter 8 --
Safety and Toxicology; SOURCES OF TOXICITY; ACUTE VERSUS CHRONIC TOXICITY; CYTOTOXICITY; CARCINOGENICITY, GENOTOXICITY, AND MUTAGENICITY; DRUG-DRUG INTERACTIONS; CARDIOVASCULAR SAFETY AND TOXICOLOGY STUDIES; CENTRAL NERVOUS SYSTEM SAFETY AND TOXICOLOGY STUDIES; IMMUNE SYSTEM MEDIATED SAFETY ISSUES; TERATOGENICITY; IN VIVO TOXICITY AND SAFETY STUDIES; QUESTIONS; References; Chapter 9 --
Basics of Clinical Trials; BEFORE THE CLINIC; DRUG SUPPLY

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