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This volume explores detailed methods and experimental protocols evaluating the effect of a compound or a mixture of compounds on the action of enzymes that are significant targets in pharmaceuticals. Consisting of three sections, the book delves into recent biocomputing and bioinformatics protocols, state-of-the art modern biophysical, electrophoretic, and chromatographic methods and high-throughput screening approaches, as well as detailed protocols and examples of the inhibition analysis and evaluation of selected enzymes. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and cutting-edge, Targeting Enzymes for Pharmaceutical Development: Methods and Protocols serves as a vital reference for academics and industry professionals working on expanding our understanding of the wide range of important enzyme targets. The chapter “Enzyme–Ligand Interaction Monitored by Synchrotron Radiation Circular Dichroism” is available open access under a Creative Commons Attribution 4.0 International License via link.springer.com.

Enzims --- Farmacologia molecular --- Biologia molecular --- Farmacologia --- Biocatalitzadors --- Ferments --- Catalitzadors --- Proteïnes --- Coenzims --- Enzims al·lostèrics --- Enzims microbians --- Fibrinolítics --- Hidrolases --- Iduronat-2-sulfatasa --- Inducció enzimàtica --- Isoenzims --- Malt --- Metal·loenzims --- Oxidoreductases --- Transferases --- Biocatàlisi --- Fermentació --- Pharmaceutical chemistry. --- Enzymology. --- Medicinal chemistry. --- Pharmaceutics. --- Medicinal Chemistry. --- Chemistry, Medical and pharmaceutical --- Chemistry, Pharmaceutical --- Drug chemistry --- Drugs --- Medical chemistry --- Medicinal chemistry --- Pharmacochemistry --- Chemistry --- Biochemistry --- Enzymes --- Enzimologia --- Bioquímica clínica --- Química farmacèutica --- Farmacoquímica --- Química dels medicaments --- Química mèdica --- Química patològica --- Química terapèutica --- Farmàcia --- Química --- Matèria mèdica --- Medicaments --- Química combinatòria --- Bioquímica de les malalties --- Bioquímica mèdica --- Bioquímica patològica --- Patobioquímica --- Bioquímica --- Bioquímica clínica veterinària --- Química clínica --- Enzimologia clínica

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Proteases and their involvement in cancer progression have been well addressed and documented; however, the emerging premise presented within this book is that Heparanase is a master regulator of aggressive cancer phenotypes and crosstalk with the tumor microenvironment. This endoglycosidase contributes to tumor-mediated remodeling of the extracellular matrix and cell surfaces, augmenting the bioavailability of pro-tumorigenic and pro-inflammatory growth factors and cytokines that are bound to Heparan sulfate. Compelling evidence ties Heparanase with all steps of tumor progression including tumor initiation, growth, angiogenesis, metastasis, and chemoresistance, supporting the notion that Heparanase is an important contributor to the poor outcome of cancer patients and a validated target for therapy. Unlike Heparanase, heparanase-2, a close homolog of Heparanase, lacks enzymatic activity, inhibits Heparanase, and regulates selected genes that promote normal differentiation and tumor suppression. Written by internationally recognized leaders in Heparanase biology, this volume presents a comprehensive understanding of Heparanase’s multifaceted activities in cancer, inflammation, diabetes and other diseases, as well as its related clinical applications to scientists, clinicians and advanced students in cell biology, tumor biology and oncology.

Cancer research. --- Oncology  . --- Molecular biology. --- Cancer Research. --- Oncology. --- Molecular Medicine. --- Molecular biochemistry --- Molecular biophysics --- Biochemistry --- Biophysics --- Biomolecules --- Systems biology --- Tumors --- Cancer research --- Proteolytic enzymes --- Peptide hydrolases --- Proteases --- Hydrolases --- Physiological effect. --- Peptide Hydrolases --- Neoplasms. --- Benign Neoplasms --- Malignancy --- Malignant Neoplasms --- Neoplasia --- Neoplasm --- Neoplasms, Benign --- Cancer --- Benign Neoplasm --- Cancers --- Malignancies --- Malignant Neoplasm --- Neoplasias --- Neoplasm, Benign --- Neoplasm, Malignant --- Neoplasms, Malignant --- Tumor --- Medical Oncology --- Esteroproteases --- Peptidases --- Proteinases --- Proteolytic Enzymes --- Gene Products, pol --- Enzims --- Cèl·lules --- Càncer --- Carcinoma --- Carcinosi --- Càncer d'ossos --- Càncer de cap --- Càncer de coll --- Càncer de bufeta --- Càncer de fetge --- Càncer de laringe --- Càncer de mama --- Càncer de pàncrees --- Càncer de pell --- Càncer de pròstata --- Càncer de pulmó --- Càncer de ronyó --- Càncer de tiroide --- Càncer d'ovari --- Càncer gastrointestinal --- Càncer ginecològic --- Càncer en els adolescents --- Càncer en els infants --- Medicaments antineoplàstics --- Melanoma --- Leucèmia --- Sarcoma --- Carcinògens --- Cèl·lules canceroses --- Cirurgia oncològica --- Infermeria oncològica --- Malalts de càncer --- Metàstasi --- Oncologia --- Biologia --- Fisiologia --- Reproducció --- Astròcits --- Blastoderma --- Cèl·lules eucariotes --- Cèl·lules epitelials --- Cèl·lules germinals --- Cèl·lules hepàtiques --- Cèl·lules i teixits vegetals --- Cèl·lules mare --- Cèl·lules musculars --- Cèl·lules sanguínies --- Citoplasma --- Cromatina --- Fecundació --- Fibroblasts --- Histologia --- Irritabilitat --- Mort cel·lular --- Neurones --- Neurones motores --- Patologia cel·lular --- Protoplasts --- Protozous --- Ou (Biologia) --- Ultraestructura (Biologia) --- Citologia --- Clonatge --- Embriologia --- Protoplasma --- Regeneració (Biologia) --- Biocatalitzadors --- Ferments --- Catalitzadors --- Proteïnes --- Coenzims --- Enzims al·lostèrics --- Enzims microbians --- Fibrinolítics --- Hidrolases --- Iduronat-2-sulfatasa --- Inducció enzimàtica --- Isoenzims --- Malt --- Metal·loenzims --- Oxidoreductases --- Transferases --- Biocatàlisi --- Fermentació