Umfang:
Online-Ressource (X, 285p. 184 illus., 11 illus. in color, digital)
ISBN:
9783034803649
,
9783034803632
,
303480363X
Serie:
Experientia Supplementum 103
Inhalt:
Satya Prakash Gupta
Inhalt:
Matrix metalloproteinases (MMPs) are proteolytic enzymes that are involved in many physiological and pathological processes. The field of MMP research is very important due to the implications of the distinct paralogs in both human physiology and pathology. Over-activation of these enzymes results in tissue degradation, producing a wide array of disease processes such as rheumatoid arthritis, osteoarthritis, tumor growth and metastasis, multiple sclerosis, congestive heart failure, and others. Thus MMP inhibitors are candidates for therapeutic agents to combat a number of diseases. The present book discusses the design and development of different classes of inhibitors of important classes of MMPs, such as gelatinases and collagenases. The articles focus specifically on structure-activity relationships of all classes of compounds and on their modes of action and specificity of binding with the receptors based on experimental and theoretical studies. These studies constitute a valuable asset for all those involved in drug development.
Anmerkung:
Description based upon print version of record
,
Matrix Metalloproteinase Inhibitors; Specificity of Binding and Structure-Activity Relationships; Preface; Contents; List of Contributers; Chapter 1: Matrix Metalloproteinases; 1.1 Introduction; 1.2 Members of MMP Family; 1.3 Structure and Function of the MMPs; 1.3.1 Propeptide Domain; 1.3.2 Catalytic Domain; 1.3.3 Hemopexin/Vitronectin Domain; 1.4 Overactivation of MMPs and Related Diseases; 1.4.1 Overactivation of MMPs in Cardiovascular Diseases; 1.4.1.1 MMPs and Atherosclerosis; 1.4.1.2 Increased MMPs Activity and the Risk of Restenosis; 1.4.1.3 MMPs in Hypertension
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1.4.1.4 MMPs in Heart Failure1.4.1.5 MMPs in Aortic Aneurysm; 1.4.2 Overactivation of MMPs in Diseases of the Lungs; 1.4.2.1 MMPs in Pulmonary Arterial Hypertension; 1.4.2.2 MMPs Overactivation in COPD; 1.4.2.3 MMPs in Bronchial Asthma; 1.4.2.4 MMPs in Pulmonary Fibrosis; 1.4.3 Overactivation of MMPs in Rheumatic Diseases; 1.4.3.1 MMPs in Rheumatoid Arthritis; 1.4.3.2 MMPs in Systemic Lupus Erythematosus; 1.4.3.3 MMPs in Systemic Sclerosis; 1.4.4 MMPs in Oncogenesis; 1.4.5 MMPs and Diabetes Mellitus; 1.5 Regulation of MMP Activity; 1.5.1 Classes of MMPs Inhibitors
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1.5.1.1 Tissue Inhibitors of Metalloproteinases1.5.1.2 Synthetic Inhibitors of Matrix Metalloproteinases; 1.6 Conclusion; References; Chapter 2: Specificity of Binding with Matrix Metalloproteinases; 2.1 Introduction; 2.2 Classification of MMPs; 2.2.1 Collagenases; 2.2.2 Gelatinases; 2.2.3 Stromelysins; 2.2.4 Matrilysins; 2.2.5 Membrane-Type MMPs; 2.3 3D Structures of MMPs; 2.3.1 Subsites; 2.4 Specificity of Binding with MMPs; 2.4.1 Inhibitors´ Specificity to S1 Subsite; 2.4.2 Mechanism of Binding at S1 Subsite; 2.5 Catalytic Mechanism; 2.6 TIMP-MMP Inhibition Mechanism; 2.7 Conclusion
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ReferencesChapter 3: The Gelatinases and Their Inhibitors: The Structure-Activity Relationships; 3.1 Introduction; 3.2 Gelatinases; 3.2.1 Structure and Function; 3.2.2 Overactivation and Implications; 3.2.3 Specificity of Gelatinases; 3.2.4 Inhibitors of Gelatinases; 3.2.5 SAR and QSAR of Inhibitors; 3.2.6 Implications; 3.3 Conclusion; References; Chapter 4: Advances in Studies on Collagenase Inhibitors; 4.1 Introduction; 4.2 MMP Activation (Activity Regulation); 4.3 Role of Collagenases in the Pathophysiology of Arthritis; 4.4 Catalytic Domain; 4.4.1 Substrate-Binding Groove
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4.4.2 Active Site/Zinc-Binding Site4.5 Collagenase Inhibitors; 4.6 Hydroxamate-Containing Collagenase Inhibitors; 4.6.1 Anthranilic Acid-Based Inhibitors; 4.6.2 Benzodiazepine-, Diazepine-, and Thiazepine-Based Inhibitors; 4.6.3 Piperidine-, Pyrimidine-, and Pyrollidine-Based Sulfonamide Inhibitors; 4.6.4 Phosphonamide-Based Inhibitors; 4.6.5 Imidazolidinone, Quinoline, and Other Heterobicyclic Scaffold-Containing Inhibitors; 4.6.6 Piperazine-Based Inhibitors; 4.6.7 Benzyl Ether, and Biaryl Ethers and Other Analogues
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4.6.8 Arylsulfonyl, Sulfonylglycine, Biphenylsulfonamide, and beta-Sulfone-Based Inhibitors
Weitere Ausg.:
ISBN 9783034803632
Weitere Ausg.:
Buchausg. u.d.T. Matrix metalloproteinase inhibitors Basel : Springer, 2012 ISBN 9783034803632
Sprache:
Englisch
DOI:
10.1007/978-3-0348-0364-9
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