QUESTIONS AND CORRECT ANSWERS
What is a drug? - correct answer a type of molecule that interacts with specific
molecular components of an organism to cause biochemical and physiologic changes
Basics of protein structure (4) - correct answer primary
Secondary
Tertiary
Quaternary
Primary structure - correct answer a protein's amino acid sequence
Secondary structure - correct answer amino acid interaction with nearby amino acids
mediated by hydrogen bonding, forming well-defined conformations (alpha-helix, beta
pleated sheet, beta barrel)
Tertiary structure - correct answer results from the interaction of amino acids more
distant from each other, resulting in hydrogen bonds, ionic bonds, disulfide bridges (through
covalent binding)
Quaternary structure - correct answer results from the interaction of separate
polypeptides
Types of bonds that occur between receptors and drugs - correct answer range from
weak (van der waals) to strong (covalent)
* ionic and hydrophobic interactions are essential for the initiation of the association of a
drug and a receptor
Four major classes of receptors (listed) - correct answer * ion channels
* membrane g protein-coupled receptors
, * enzyme-linked receptor
* nuclear receptor (aka steroid receptor)
Ion channels (ligand gated) - correct answer * located in the cell membrane (plasma
membrane or in the membranes of subcellular organelles such as the endoplasmic reticulum
and mitochondria)
* act as channels that when open allow ions and small molecules to pass into and out of the
cell
* drugs bind to the channels to change the confirmation of the channel - this either opens or
closes the channel
* contain multiple subunits, and for this reason they can interact with fairly diverse groups of
drugs
* example: gaba receptor
Membrane g protein-coupled receptors - correct answer * possess 7 alpha helical
transmembrane domains that pass through the plasma membrane
* these receptors interact with a heterotrimeric g protein, which then interacts with different
cellular signalling mechanisms that allow transduction of a signal from outside the cell to
inside the cell
* example: ne acting on an adrenergic receptor
Enzyme-linked receptor - correct answer * transmembrane receptor located in the
plasma membrane
* ligand binding domain for these receptors extends into the extracellular space while the
enzymatic portion is located in the cytoplasm
* activation of these receptors by a ligand activates the intracellular enzyme that transduces
the extracellular signal
* receptors have two potential places of interaction with drugs: the extracellular ligand
binding site and the intracellular enzymatic domain
* example: epidermal growth factor binding to the epidermal growth factor receptor