Membranes and receptors - 8 Flashcards
Define a ligand
A molecule (or e.g. ion) that binds specifically to a receptor.
Define affinity
Is a ligand’s ability to bind to its receptor. The higher a ligand’s affinity for its receptor the stronger the binding in the receptor-ligand complex.
Define efficacy
The ability of a ligand to cause a (measurable) response. This is goverened by intrinsic efficacy PLUS cell/tissue-dependent factors.
Define agonist
A ligand that binds to a receptor and activates it.
Define potency
a
Define partial agonist
a
Define intrinsic efficacy
How good an agonist is at generating the active state of a receptor.
Define antagonist
A ligand that binds to a receptor and stops it from being activated by its agonist.
Define functional antagonism
a
Define reversible competitive antagonism
a
Define non-competitive antagonism
a
How do drugs exert effects?
Binding to targets - these are mainly proteins, with the exception being some antimicrobial drugs and anti-tumour drugs which bind DNA.
What percentage of the drugs on the market target GPCRs?
~30% (~50 targets)
What is a biologic?
any pharmaceutical drug product manufactured in, extracted from, or semisynthesized from biological sources. Different from chemically synthesized pharmaceuticals, they include vaccines, blood, or blood components, allergenics, somatic cells, gene therapies, tissues, recombinant therapeutic protein, and living cells used in cell therapy
What factor is critical in determining a drugs action?
The concentration of drug molecules around their receptor target.