Teacher
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BOTTA Lorenzo
(syllabus)
General Section Definition of drug. Pharmacokinetics: absorption, distribution, metabolism and elimination. Physico-chemical properties of the drug that influence each of these phases. Bioavailability and bioequivalence concepts. Cell membrane properties. Fatty acids: classification, properties and biological role. Pharmacodynamics. Receptor: definition and characteristics. Classification of receptors. Receptor site and its specificity. Allosteric and accessory sites. Ligand-receptor interaction: role of the chemical bond in the receptor interaction. Ionotropic receptors: structure and characteristics. Drug targets: Proteins, Enzymes, Receptors and Nucleic Acids: structure and function. Receptors and signal transduction. Receptor activation mechanisms: ionotropic; voltage-dependent and ligand-dependent; receptor activated by phosphorylation. G protein coupled receptors: structure and activation of the G protein cycle. Role of the α portion of the G protein. Effectors of the α portion and effects mediated by Gs, Gi, Gq. Structure and functional groups of the main endogenous ligands of ionotropic and metabotropics receptors: Gaba, Glycine, Aspartate, Glutamate, Acetylcholine, Adrenaline, Noradrenaline, Serotonin, Dopamine, Histamine. Protein kinase receptor. Transmembrane single strand GTPase receptor. The pharmacophore and the molecular outline of a drug. Concept of affinity and intrinsic activity. Definition of agonist, partial agonist, inverse agonist, antagonist. Cellular excitability. Mechanism of propagation of the impulse. Chemical synapses: structure, role of vesicles, mechanisms of synthesis and storage of the mediator, release of the mediator. The postsynaptic receptors. Mechanism of presynaptic reuptake of the mediator. Characteristics of the receptor site of the main neurotransmitters: Serotonin, Dopamine, Histamine, Acetylcholine, Noradrenaline. Drug-receptor interactions. Electronic interactions. Bonds involved in the drug-receptor complex: covalent bond, ionic bond, hydrogen bond, charge transfer complexes, Van der Waals forces and other interactions. Steric interactions: steric effects in the drug-receptor complex. Computational Chemistry: Molecular Modelling (conformational analysis, identification of the 3D pharmacophore), Docking, Virtual Screening, Homology Modelling, Pseudoreceptors, De novo drug design. Formulation and delivery of drugs: principles and use of specific carriers (liposomes, micelles, antibodies, lignin).
Special Part Antibacterial agents: inhibitors of cell metabolism (Antimetabolites), inhibitors of plasma membrane synthesis, inhibitors of protein synthesis, inhibitors of nucleic acid transcription and replication. Antiviral agents: nucleic acids structure and properties, drugs against DNA and RNA viruses, antisense oligonucleotides, broad spectrum drugs, vaccines Antitumor agents: drugs that act on nucleic acids (intercalants, topoisomerase poisons, alkylating and metalizing agents, chain terminator), antisense therapy, drugs that act on enzymes (adrenergic antagonists, antimetabolites), drugs acting on structural proteins, antibodies and antibody-drug conjugates.
(reference books)
"An Introduction to Medicinal Chemistry", Patrick L. Graham, Oxford University Press
"Chimica farmaceutica" of Alberto Gasco, Fulvio Gualtieri, Carlo Melchiorre
"Medicinal Natural Products: A Biosynthetic Approach" di Paul M. Dewick
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