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Target validation in drug discovery = 药物发现中的靶标确认 / Brian W. Metcalf and Susan Dillon. —[Reprinted ed.]. — Beijing : Science Press ; [Amsterdam] : Elsevier, 2007.—(63.326/M588(R)) |
Contents
CONTENTS
PREFACE vii
CONTRIBUTORS xi
Ⅰ PHARMACEUTICAL BIOTECHNOLOGY FOR TARGET VALIDATION I
1 Generation of Transgenic Animals 3
2 Target Validation in Chemogenomics 27
Ⅱ TARGET VALIDATION FOR BIOPHARMACEUTICAL DRUG DISCOVERY 41
3 Cetuximab (Erbitux), An Anti-Epidermal Growth Factor Receptor Antibody for the Treatment of Metastatic Colorectal Cancer 43
4 Monoclonal Antibody to HER-2 in Breast Cancer 69
5 Validation of TNF as a Drug Target in Inflammatory Bowel Disease 83
6 Anti-CCL-2/MCP-I: Directed Biologicals for Inflammatory and Malignant Diseases 103
7 Targeting IL-12p40 for Immune-Mediated Disease 12 I
8 The GPllb/llla Antagonist Abciximab for Acute Percutaneous Coronary Intervention 135
Ⅲ VALIDATING TARGETS OF SMALL MOLECULE APPROACHES 153
9 Epidermal Growth Factor Receptor(EGFR) Inhibitor for Oncology: Discovery and Development of Erlotinib 155
10 Progress in Achieving Proof of Concept for p38 Kinase Inhibitors 179
11 IKK-2/NF-KB-Dependent Transcription 199
12 TNF Signaling Pathway Inhibitors for Inflammation-CCR2 Antagonists 223
13 The Discovery of Eltrombopag, An Orally Bioavailable TpoR Agonist 241
14 Orally Bioavailable Glycoprotein llb/llla Antagonists: A Negative Case Study 255
INDEX 269