Pharmaceutical Biochemistry
Objectives
Understand basic concepts in pharmacology. Criteria for ADME (Absorption; Distribution; Metabolism; Elimination) of a drug. To know drug biotransformation systems (Phase I and Phase II). To establish redox mediated processes by cytochromes P450 (CYPs) and its relationship with the structure of the enzyme. Familiarization with computational methods and Nuclear Magnetic Resonance for the analysis of drug/receptor interactions and in drug design. To evaluate the importance of inhibition/induction processes in CYP in drug-drug interactions.
General characterization
Code
10718
Credits
6.0
Responsible teacher
José Ricardo Ramos Franco Tavares
Hours
Weekly - 4
Total - 61
Teaching language
Português
Prerequisites
General knowledge of physiology, chemistry, biochemistry and molecular biology
Bibliography
Human Drug Metabolism: An Introduction, Michael Coleman, 3rd Edition (2020), Wiley-Blackwell, ISBN: 978-0-470-74217-4 (Chapters of interest: 1 to 5 and Appendixes)
Drug Metabolism in Drug Design and Development, Donglu Zhang, Mingshe Zhu, W. Griffith Humphreys, eds., 1st Edition (2007), John Wiley & Sons, ISBN: 978-0-471-73313-3
Handbook of Chemoinformatics, ed. Johnann Gasteiger, Wiley-VCH, 2003.
Autodock tutorials http://autodock.scripps.edu/faqs-help/tutorial
High-Resolution NMR Techniques in Organic Chemistry Book, Timothy D.W.Claridge, 3rd Edition (2016), Elsevier Science, eBook ISBN: 9780080999937
Teaching method
Theoretical/Practical classes are presentation of the themes by the Professor., intersepersed with analysis and group discussion, in classroom, of scientific articles. Practical classes are learning and practice of computational methods for the analysis of the drug-protein interaction, as well as presentation of group seminars, followed by discussion in classroom.
Evaluation method
Theoretical evaluation (40% of the final grade) with two components:
1) 10% - Scientific article discussion and analysis during the theoretical classes by Prof. Ricardo Franco.
2) 30% - Final test about all the theoretical-practical contents of the semester, taught by Prof. Ricardo Franco
The grade in this component must be equal or above 9.5 in order to be accounted for calculating the final grade of this course.
Seminar evaluation (30% of the final grade): For this grade both the quality of the presentation of the Seminar and its PDF version will be taken into account.
Drug Design evaluation (30% of the final grade) with two components:
1) 10% - average of two evaluations after each block (Docking and NMR interactions).
2) 20% - Multiple choice final test, about all the contents of the semester on this part.
There is no threshold grade on test. The absence to the test, gives a grade of zero.
The recourse exam (70% of final grade), can be used by students that had an average classification in the tests below 9,5; or by students that want to improve their final grade (in the latter case, the student must register and pay the due fee). This exam will include only the theoretical-practical part taught by Prof. Ricardo Franco (60% final grade) and the drug design part (40% final grade) evaluations. The drug design evaluation will focus equally on both themes approached during druig design sessions.
Subject matter
1. Introduction and definitions in Pharmaceutical Biochemistry and Drug Development
2. Introduction to Drug Design: Computational and Nuclear Magnetic Resonance (NMR) methods
3. Pharmacokinetics and drug biotransformation systems (Phase I and Phase II).
4. Drug netabolism: cytochrome P450 (CYP)-mediated oxidation and reduction
5. Structure-function relationships in CYP
6. Induction and Inhibition in CYP systems