Gianluca SBARDELLA | CHEMISTRY OF MOLECULAR TARGETS AND DRUG DESIGN
Gianluca SBARDELLA CHEMISTRY OF MOLECULAR TARGETS AND DRUG DESIGN
cod. 0760200063
CHEMISTRY OF MOLECULAR TARGETS AND DRUG DESIGN
| 0760200063 | |
| DIPARTIMENTO DI FARMACIA | |
| EQF7 | |
| PHARMACEUTICAL CHEMISTRY AND TECHNOLOGY | |
| 2023/2024 |
| YEAR OF DIDACTIC SYSTEM 2020 | |
| AUTUMN SEMESTER |
| SSD | CFU | HOURS | ACTIVITY | |
|---|---|---|---|---|
| CHIM/08 | 6 | 48 | LESSONS |
| Objectives | |
|---|---|
| THE COURSE AIMS TO PROVIDE AN ADVANCED KNOWLEDGE OF THE MOLECULAR STRUCTURE OF MAJOR MACROMOLECULAR DRUG TARGETS AS WELL AS OF THE MECHANISM OF MOLECULAR RECOGNITION. RECEPTOR THEORIES AND MODELS WILL BE DISCUSSED TOGETHER WITH MAJOR CLASSES OF CELLULAR TARGETS AND THEIR INTERACTIONS WITH DIFFERENT LIGANDS. THE MAIN BIOCHEMICAL AND BIOPHYSICAL TECHNIQUES AND METHODS USED TO STUDY AND CHARACTERIZE DRUG TARGETS AND THEIR BINDING INTERACTIONS WITH VARIOUS LIGANDS WILL ALSO BE DISCUSSED AS WELL AS THE RELATIONSHIP BETWEEN STRUCTURAL PROPERTIES AND THE EFFECT ON BIOLOGICAL ACTIVITY AND/OR SELECTIVITY. THE STUDENT WILL LEARN HOW TO APPLY SUCH PRINCIPLES TO DESIGN AND SYNTHESIZE BIOLOGICALLY ACTIVE MOLECULES. KNOWLEDGE AND UNDERSTANDING BY THE END OF THE COURSE THE STUDENT WILL KNOW: - RECEPTOR THEORIES AND MODELS, THE MAJOR CLASSES OF CELLULAR TARGETS AND THEIR INTERACTIONS WITH DIFFERENT LIGANDS, THE MOLECULAR BASES THAT REGULATE SUCH INTERACTIONS AND THE MECHANISMS THROUGH WHICH SMALL MOLECULES ACTIVATE OR BLOCK THEIR MOLECULAR TARGETS; - THE MAIN BIOCHEMICAL AND BIOPHYSICAL TECHNIQUES AND METHODS USED TO STUDY AND CHARACTERIZE DRUG TARGETS AND THEIR BINDING INTERACTIONS WITH VARIOUS LIGANDS; - THE RELATIONSHIP BETWEEN STRUCTURAL PROPERTIES AND THE EFFECT ON BIOLOGICAL ACTIVITY AND/OR SELECTIVITY. APPLYING KNOWLEDGE AND UNDERSTANDING BY THE END OF THE COURSE THE STUDENT WILL BE ABLE TO: - APPLY RECEPTOR THEORIES AND MODELS TO DESCRIBE THE INTERACTIONS OF DRUGS WITH THEIR MOLECULAR TARGETS, INCLUDING KINETIC AND THERMODYNAMICAL ASPECTS; - KNOW THE KIND OF MODULATION OF THE TARGET ACTIVITY OR OF THE TARGET-MEDIATED SIGNALING; - KNOW THE METHODOLOGIES TO STUDY MOLECULAR TARGETS AND THEIR INTERACTIONS WITH LIGANDS, AS WELL AS THEIR TECHNOLOGICAL PRINCIPLES; - APPLY THE ACQUIRED KNOWLEDGE TO ANALYZE STRUCTURE-ACTIVITY RELATIONSHIPS OF MOST COMMON CLASSES OF DRUGS; - TO DEVISE AND SUSTAIN CRITICAL ARGUMENTS IN THE FIELD OF MEDICINAL CHEMISTRY, PROVING TO BE ABLE TO HAVE A PROFESSIONAL APPROACH TO DISCIPLINE. MAKING JUDGMENTS: THE STUDENT WILL BE ABLE TO: - PUT IN THE RIGHT CONTEXT THE QUESTIONS SHE/HE WILL BE ASKED DURING THE EXAMINATION (BOTH WRITTEN AND ORAL) AND SELECT THE MOST APPROPRIATE AND SPECIFIC ANSWER, AVOIDING UNNECESSARY AND NOT REQUESTED GENERAL DISSERTATIONS; - PROPERLY LINK TOGETHER THE KNOWLEDGE DERIVING FROM DIFFERENT DISCIPLINES ON A CERTAIN TOPIC AND INTEGRATE THEM TO HAVE A BETTER UNDERSTANDING; - INTERACT WITH THE THEMES SUGGESTED BY THE TEACHER AND, EVEN WITH THE HELP OF THE RECOMMENDED TEXTS AND TEACHING MATERIALS, BE ABLE TO MAKE INDEPENDENT JUDGMENTS COMMUNICATION SKILLS: THE STUDENT WILL BE ABLE TO EXPLAIN AND DEVELOP CONCEPTS WITH CLARITY, SYNTHESIS AND LANGUAGE SKILLS. |
| Prerequisites | |
|---|---|
| IT IS REQUIRED TO KNOW THE BASICS OF ORGANIC CHEMISTRY (I AND II), INTRODUCTIVE MEDICINAL CHEMISTRY, MEDICINAL CHEMISTRY I, PHYSICAL METHODS IN ORGANIC CHEMISTRY, APPLIED BIOCHEMISTRY. |
| Contents | |
|---|---|
| INTRODUCTION: THE RECEPTOR AND THE BINDING INTERATIONS (2 H) RECEPTOR THEORIES AND MODELS: THE OCCUPATIONAL THEORY (CLARKE, ARIENS, STEPHENSON), THE SPARE RECEPTORS THEORY (FURCHGOTT AND SCHILD), THE RATE THEORY (PATON), THE INDUCED FIT THEORY, THE TWO-STAGE MODEL, THE CO-OPERATIVE RECEPTOR MODEL, THE MOBILE RECEPTOR MODEL (6 H) STRUCTURE AND CLASSIFICATION OF RECEPTORS: MEMBRANE RECEPTORS, METABOTROPIC RECEPTORS AND IONOTROPIC RECEPTORS, NUCLEAR RECEPTORS (2 H) BIOCHEMICAL AND BIOPHYSICAL METHODS TO STUDY DRUG TARGETS (6 H) AMINOACIDS RECEPTORS: GLYCINE, GABA, GLUTAMATE (4 H) CATECHOLAMINE RECEPTORS: ADRENERGIC, DOPAMINERGIC (3 H) CHOLINERGIC RECEPTORS: MUSCARINIC, NICOTINIC. THE CHOLINESTERASES (2 H) SEROTONIN RECEPTORS (2 H) HISTAMINE RECEPTORS (2 H) PEPTIDE RECEPTORS: OPIOIDS, INSULINE, GROWTH FACTORS, ANGIOTENSIN AND ACE (3 H) THE ENDOCANNABINOID SYSTEM: CANNABINOID RECEPTORS AND VANYLLOID RECEPTORS (2 H) THE GLUCOSIDE RECEPTORS (2 H) THE STEROID RECEPTORS (3 H) ION CHANNELS (3 H) CYCLOOXYGENASES, KINASES (2 H) EPIGENETIC TARGETS (WRITERS, ERASERS, READERS) (2 H) |
| Teaching Methods | |
|---|---|
| THE COURSE WILL INCLUDE LECTURES AND IN-CLASS DISCUSSIONS OF PRIMARY LITERATURE FOR A TOTAL OF 48 HOURS (6 CFU = 6 ECTS). |
| Verification of learning | |
|---|---|
| THE FINAL ORAL EXAMINATION WILL CONSIST OF IN-DEPTH QUESTIONS AND DISCUSSION OF THE TOPICS COVERED DURING THE COURSE. TO PASS THE EXAMINATION, THE STUDENT SHOULD OBTAIN A SCORE OF AT LEAST 18/30. |
| Texts | |
|---|---|
| CHIMICA FARMACEUTICA, A CURA DI ALBERTO GASCO, FULVIO GUALTIERI, CARLO MELCHIORRE, ZANICHELLI. G.L. PATRICK, CHIMICA FARMACEUTICA, A CURA DI GABRIELE COSTANTINO, EDISES. G.L. PATRICK, INTRODUZIONE ALLA CHIMICA FARMACEUTICA, EDISES, II EDIZIONE. D.A. WILLIAMS, T.L. LEMKE, FOYE’S PRINCIPI DI CHIMICA FARMACEUTICA, PICCIN. T. NOGRADY, D. WEAVER, MEDICINAL CHEMISTRY – A MOLECULAR AND BIOCHEMICAL APPROACH, 3RD ED., OXFORD UNIVERSITY PRESS. MONOGRAFIE DELLA COLLANA "CHIMICA DEI RECETTORI", EDITORE C. MELCHIORRE, CLUEB (BOLOGNA). C. WERMUTH, LE APPLICAZIONI DELLA CHIMICA FARMACEUTICA, EDISES. P. KROGSGAARD-LARSEN, T. LILJEFORS, U. MADSEN ED., TEXTBOOK OF DRUG DESIGN AND DISCOVERY, TAYLOR & FRANCIS. GOODMAN & GILMAN'S THE PHARMACOLOGICAL BASIS OF THERAPEUTICS, TWELFTH EDITION, MCGRAW-HILL MEDICAL PUBLISHING DIVISION (2011). WILSON AND GISVOLD'S TEXTBOOK OF ORGANIC MEDICINAL AND PHARMACEUTICAL CHEMISTRY-LIPPINCOTT WILLIAMS & WILKINS KLEEMANN, ENGEL, KUTSCHER, REICHERT, PHARMACEUTICAL SUBSTANCES, 5TH ED., THIEME VERLAG. BURGER’S MEDICINAL CHEMISTRY, DRUG DISCOVERY AND DEVELOPMENT. 7TH EDITION. WILEY. JOURNAL OF MEDICINAL CHEMISTRY, HTTP://PUBS.ACS.ORG/JOURNAL/JMCMAR CHEMMEDCHEM, HTTP://ONLINELIBRARY.WILEY.COM/JOURNAL/10.1002/(ISSN)1860-7187 NATURE REVIEWS DRUG DISCOVERY, HTTP://WWW.NATURE.COM/NRD/INDEX.HTML ACS CHEMICAL BIOLOGY, HTTP://HTTP://PUBS.ACS.ORG/JOURNAL/ACBCCT NATURE CHEMICAL BIOLOGY, HTTP://WWW.NATURE.COM/NCHEMBIO/INDEX.HTML CELL CHEMICAL BIOLOGY, HTTP://WWW.CELL.COM/CELL-CHEMICAL-BIOLOGY/HOME |
| More Information | |
|---|---|
| THE COURSE WILL BE TAUGHT IN ITALIAN. ATTENDANCE IS HIGLY RECOMMENDED. FOR MORE INFORMATION, PLEASE CONTACT PROF. GIANLUCA SBARDELLA (GSBARDELLA@UNISA.IT) OR VISIT THE WEBSITE HTTP://DOCENTI.UNISA.IT/005059 |
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