Molecular & Cellular Drug Targets Flashcards
Why be concerned about drug targets ?
- interactions with other drugs new modalities for using drugs (most important)
- new indications for drugs
- new concerns regarding risk/benefit
Are drug targets large or small
Drug targets are large molecules – macromolecules
Are drugs generally larger or smaller than their targets
Drugs are generally much smaller than their targets
How do drugs interact with their targets
Drugs interact with their targets by binding to binding sites
are binding sites usually hydrophobic or hydrophilic
Binding sites are typically hydrophobic pockets on the surface of macromolecules
what kind of bonds are typically involved in intermolecular bonds
Binding interactions typically involve intermolecular bonds
what is a binding group
Functional groups on the drug are involved in binding interactions and are called binding groups (drug)
What is a binding site
Specific regions within the binding site that are involved in binding interactions are called binding regions (target)
T/F the binding group is associated with the drug
true
t/f binding regions are with the target
true
what are the 4 major drug targets
Four major drug targets A. Receptors B. Ion channels C. Enzymes D. Transporters
What are the 3 ways that drugs work
- Some drugs antagonize, block or inhibit
endogenous proteins - Some drugs activate endogenous proteins
- A few drugs have unconventional mechanisms of action
What is an an antagonist
A drug is said to “antagonize” or “block” the receptor and is referred to as a receptor antagonist
What is a receptor drug target
A macromolecular component of the organism that binds the drug and initiates the drug’s effect
receptor drug targets are what kind of macromolecule
Most receptors are proteins
Where are the 2 possible locations of receptor drug targets
cell surface receptor and nuclear receptor
describe what a cell surface receptor looks like
CELL SURFACE RECEPTOR:
o embedded in the cell membrane
o functions to receive chemical information from the
extracellular compartment and to transmit that
information to the intracellular compartment
describe what a nuclear receptor looks like
NUCLEAR RECEPTOR:
o exists in the intracellular compartment
o upon activation binds to regulator regions in the DNA
and modulates gene expression
Some drugs bind to cell surface receptors, yet do not activate the receptors to trigger a response. What is this called
antagonist
When cell surface receptors bind the drug molecule, the endogenous chemical cannot bind to the receptor and cannot trigger a response. What is this called
antagonist