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Honours Directed 3 Notes

Pharmacology Notes > Drug Development (BIOL10822) Notes

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Drugs: From Molecules to Man - Lecture 11 (5/03/2018)

*HD3* G Protein-Coupled Receptors
This lecture includes:

Methods for determining receptor structure, such as X ray crystallography and homology modelling.
The concept of a superfamily.
The classification of GPCRs.
The structures of Family A, B, C receptors.

Protein Structures

Knowing things about the 3D shape of a drug target is a big advantage in drug design.

However, proteins are complex molecules and we do not currently have the ability to predict the 3D protein structure from the primary sequence and so we must use experimental methods to work out its shape.

Methods for determining the Molecular Structure

There are three main techniques for determining the structures of biological molecules.

These methods include:

X-ray crystallography.
NMR (Nuclear Magnetic Resonance).
Molecular Modelling.

Determining Molecular Structures using X-ray Crystallography

The principle of X-ray crystallography is very simple: make a crystal of the molecule you are interested in, shine x-rays through it and look at the diffraction pattern.

This diffraction pattern will depend on the arrangement of atoms in the crystal and thus you should be able to translate it into a working structural model of the molecule.

X ray crystallography is a very powerful technique and can give us a lot of information about proteins.

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