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Neuropharmacology

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M2_E25 Pharmaco-planning2018_2019

Biology Master, ENS
Year : M2
Semester : S1
Course code : E25
ECTS : 3
Coordinator : Lætitia MONY, Biology Department, ENS
Hours : 20h (07/01/19 to 11/01/19)

Keywords :
Pharmacology, Neuronal Receptors and Transporters, Structure-function relationship, Allosteric regulation, Molecular mechanisms

Prerequisites for the course :
-  Basic knowledge in chemistry and protein biochemistry : pH and pKa, amino acid properties, protein structure, protein/ligand interactions (H-bonds, hydrophobic interactions…)
-  Basic knowledge in pharmacology : what is an agonist/antagonist, notions of competitive and non-competitive inhibition

Course objectives and description :
This module is about neurotransmitter receptors and transporters, which are key actors of neuronal communication. The recent boom in membrane protein structures sheds a new light on our understanding of the function and the regulation mechanisms of these proteins. It also provides an unprecedented structural and conceptual framework to discover and develop new molecules of pharmacological interest. This module will tackle the molecular and structural organization, as well as the operating mechanisms of the main classes of neurotransmitter receptors and transporters. We will present their activation principles, as well as their interactions with ligands. Emphasis will be put on the allosteric mechanisms and subsequent conformational dynamics. We will also show how malfunction of these proteins can be at the origin of pathologies, making them targets of therapeutic interest. Finally, using concrete cases, this module will introduce students to the development process of new molecules of neurological and psychiatric interest.
07/01/19 to 11/01/19

Assessment / evaluation :
-  Paper analysis and oral presentation
-  Written exam (to be confirmed)

Course material (hand-outs, online presentation available, …) :
Ppt presentations of the speakers (online availability to be confirmed)

Suggested readings in relationship with the module content (textbook chapters, reviews, articles) :
Websites :
http://employees.csbsju.edu/hjakubowski/classes/ch331/protstructure/olprotein-aminoacid.html
http://www.wiley.com/legacy/college/boyer/0470003790/reviews/pH/ph_non-covalent.htm
http://www.ncbi.nlm.nih.gov/books/bv.fcgi?rid=mcb.section.285
https://www.ncbi.nlm.nih.gov/books/NBK21121/box/A5836/
http://www.pdg.cnb.uam.es/cursos/Barcelona2002/pages/Farmac/Comput_Lab/Guia_Glaxo/

Books :
Protein structure and non-covalent interactions :
-  Proteins : Structures and molecular properties, Thomas E. Creighton Second edition (1992) W.H.Freeman & Co Ltd

Ion channels :
-  Ion Channels of Excitable Membranes, Bertil Hille 3rd edition (2001) Sinauer Associates Inc.
-  Ion channels and Disease, Frances Ashcroft (2000), Academic Press