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Vyučující
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Brulíková Lucie, doc. RNDr. Ph.D.
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Obsah předmětu
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1. Introduction Basic terms, overview of important viral and cancer diseases, antimetabolites and their use in the treatment. Cell cycle, regulation of cell cycle, microtubules. Aims of chemotherapy. Survey of infectious and immune diseases treatment. Central dogma of molecular biology. Brief look at gene regulation. 2. Structure and function of nucleic acids RNA, DNA. Covalent interactions of nucleic acids with small molecules, reactions with nucleophiles, electrophiles. Reversible small molecule-nucleic acid interactions. 3. Nucleic acids biosynthesis and metabolism Nucleosides biosynthesis de novo. Biosynthesis and degradation of pyrimidine and purine nucleotides. Enzymes as a target for chemoterapeutics. Inhibitors of biosynthesis and catabolism of nucleic acids components. 4. Chemistry of nucleosides, nucleotides and oligonucleotides Syntheses of analog purine and pyrimidine bases. Glycosid bond formation. Bases modification. Aspects of chiral drugs synthesis. Hilbert-Johnson reaction. Circle building. Transformation of pyrimidine and purine bases. Transformation of sugar parts of drugs. Nucleotides synthesis. Oligonucleotides synthesis. 5. Viruses and antiviral drugs Virus infections. Virus structures and their life cycle. Virus distribution and survey of virus and immune infections. Vaccines. Viruses and cancer. 6. Inhibitors of viral life cycle phases Fuse and entry inhibitors. Uncoating inhibitors. Inhibitors of synthesis of viral nucleic acids (herpesvirus helikase-primase inhibitors, RNA-dependent-RNA polymerase inhibitors, DNA-dependent-RNA polymerase inhibitors). HBV and HCV inhibitors. Serin HCMV protease inhibitors. Cystein rhinovirus protease inhibitors. 7. Inhibitors of HIV virus Fuse and entry inhibitors, nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs). HIV integrase and protease inhibitors. Syntheses examples. Therapy of serious retroviral infections. Advances in therapy of AIDS and infectious hepatitis. 8. Acyclic nucleosides and nucleotides acyclic nucleosides as antiviral and antitumour drugs. Synthesis of examples. Acyclic nucleosidphosphonates and their synthesis. New cyclic phosphonates. 9. Antitumor and antileukemic chemotherapy 1 alkylating agent, mechanism of action of DNA alkylating drugs. Pt complexes. Hypoxia-selective antitumor agents. 10. Antitumor and antileukemic chemotherapy 2 Topoisomerase inhibitors, specific inhibitors of topoisomerase I and topoisomerase II. Angiogenesis inhibitors. Thymidine phosporylase inhibitors. Radiomimetics. Telomerase inhibitors. 11. Antitumor and antileukemic chemotherapy 3 Tubulin interactive antimitoic agents. Proteinkinases inhibitors. Protein prenylation inhibitors. Androgen and estrogen undesirable effects inhibitors.
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Studijní aktivity a metody výuky
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Přednášení
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Výstupy z učení
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Specialized course focusing on the summary of modern principles in drug development.
Define main concepts, explain principles, analyze problems, describe new trends in the development of drugs.
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Předpoklady
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nespecifikováno
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Hodnoticí metody a kritéria
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Písemná zkouška
Successful passing of written examination - obtaining of at least 60% of credit points.
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Doporučená literatura
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Blackburn, G.M. et al. Nucleic Acids in Chemistry and Biology.
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Holý, A. (2004). Principy bioorganické chemie ve vývoji antivirotik a cytostatik. UP Olomouc.
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Klener jr, P.; Klener, P. (2013). Principy systémové protinádorové léčby. Praha.
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Wenke, Hynie. (1985). Farmakologie pro lékaře I, II. Aviccenum, Praha.
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