Course ID: | PHRM 8600. 3 hours. |
Course Title: | Drug Targets in Signal Transduction Pathways |
Course Description: | Cellular mechanisms of signal transduction by multiple pathways,
with specific emphasis on sites for therapeutic intervention and
manipulation. Function, regulation, and structure of the
components of the pathway including current or potential
strategies to pharmacologically manipulate components of the
pathway. |
Oasis Title: | SIGNAL TRANSDUCTION |
Prerequisite: | Permission of department |
Semester Course Offered: | Offered fall semester every year. |
Grading System: | A-F (Traditional) |
|
Course Objectives: | In this course, students will learn the cellular mechanisms of
signal transduction by multiple pathways, with specific emphasis
on sites for therapeutic intervention and manipulation. For
each signaling pathway, the current knowledge of the function,
regulation, and structure of the components of the pathway will
be discussed, and the relevance of the pathway to physiology and
pathology will be explored. Drugs that impinge on these
signaling pathways that are currently in clinical use will be
presented, as well as potential therapeutic targets that are the
focus of current research and drug development. In each of the
lecture sections outlined below (except the introductory
section), two relevant papers from the primary scientific
literature will be presented and discussed by the students: one
of historical significance, and one report of a recent finding
with significant potential for therapeutic use.
Grading: 30% Paper presentation/discussion; 30% Mid-term; 40%
Final exam
Exam format: Tests will be short answer/discussion format, and
will include interpretation of data. The final will be
cumulative. |
Topical Outline: | Section I: Principles of Cell Signaling and Drug Targeting
1. General Introduction
2-3. Structure-guided drug design
4-5. Library screening
6-7. Drug delivery
8. Receptor concepts
9 . Signal cascade concepts
Section II: G-protein signaling pathways
10. Structures: GPCRs, Heterotrimeric G-proteins, RGS
proteins
11. G-protein regulation, deactivation
12. Effectors and second messengers
13. Lipid signaling pathways
14. Monomeric G-proteins: Structure, function, diversity
15. Paper presentation/discussion
Section III: Ligand-gated channel pathways
16. Structure and gating of ligand-gated channels
17. Regulation by G-proteins (cross-talk)
18 Sensory channels (TRP channels)
19. Neuronal signaling
20. Paper presentation/discussion
Mid-term Exam
Section IV: Signaling Regulation of Transcription and
Translation
21. Nuclear transactivators and repressors
22. Chromatin remodeling
23. Nuclear receptors
24. Regulation of translation
25. Paper presentation/discussion
Section V: Cellular and physiologic responses to signaling
26. Insulin signaling
27. Apoptosis--intrensic
28. Apoptosis--extrensic
29. Cytokine responses
30. Long-term potentiation in memory
31. Sensory systems
32. Paper presentation/discussion
Section VI: Recent advances in signaling and Drug Design
33. Macromolecular complex assembly, anchoring to
cytoskeleton
34. Mathematical models of signaling complexes
35. Live cell imaging
36. Highthroughtput screening technology
36. Paper presentation/discussion
Final Exam |
Honor Code Reference: | Students will be held to the highest standard of academic
integrity, as described in "A Culture of Honesty"
(www.uga.edu/ovpi). All work submitted in the form of
examinations and presentations are expected to be produced by
individual students. |