Lecture 13: ACTIVATION AND INHIBITION OF PROTEINS (PART 1) Flashcards
What is the first common step in activation and inhibition of proteins?
Chemical substance travels from its source
What happens after the chemical substance travels from its source?
Chemical substance interacts with the target protein- binding/reception
What is reception?
When the protein receives the substance
What happens after the chemical substance interacts with the target protein- binding/reception?
The binding event effects the protein to either activate or inhibit it
What happens after the binding event effects the protein to either activate or inhibit it?
Functional consequences that change the cellular response
How does the activation and inhibition relate to HIV protease?
Saquinavir binds to HIV and inhibits any further action
What are receptors?
A cellular protein (or assembly of proteins) that control chemical signalling between and within cells
How many individual receptor proteins are there?
About 1000
What do receptors control?
Many important physiological processes, including sight, smell and taste
What are receptors the cellular targets for?
Many drugs and some toxins
What do one third of drugs do?
Activate or inhibit receptors
How do enzymes and receptors compare in binding sites?
Enzymes typically have one active site and receptors can have several binding sites
How do enzymes and receptors compare in what they bind?
Enzymes bind substrates and receptors ind ligands
How do enzymes and receptors compare in what they do to what binds?
Enzymes change substrate to product and receptors release the ligand unchanged
How do enzymes and receptors compare in where they are found?
They can both be found membrane bound or free in the cytosol
What can be don’t with both enzymes and receptors?
They can be activated, inhibited or used as drug targets
What are the main classes of receptors?
Ligand-gated ion channels, G protein coupled receptor (GPCR) and receptor tyrosine kinase (RTK)
What is different between the three receptor classes?
Their structure which is important to their function
What is the same between the three receptor classes?
They have the same overall steps of activation and inhibition but the exact details differ