receptor basics Flashcards
Targets for drugs?
enzymes, channels and transporters
4 RECEPTOR families
ionotropic, metabotropic, kinase linked and nuclear
cys loop structure and examples
pentameric, e.g. GABAa, nAChr and 5HT3
ionotropic glutamate receptor structure and exmple
tetremer four large subunits and eg. NMDA
P2X type strucutre and example
trimeric and P2XR
GPCR structure
7 TM domain and 3rd loop interacts with Heterotrimeric Proteins
different targets for Gprotiens
adenylyl cyclase, PLC, ion channels, RhoA
Nucleur receptors, what ligands activate?
steroid hormones, ligands, vitamin A +D
Biopharmaceuticals definition
Complex, high molecular weight proteins and peptides that are produced in living systems. Recombinant DNA techniques allow a specific gene that will encode for a molecule that closely resembles the human active agent to be selected.
Biopharmaceuticals examples
gene therapy, oligonucleotides and engineered antibodies
Biopharmaceuticals features
bigger, unique, complex mechanisms, high affinity, long half life
3 different ways to deliver gene therapy drugs
liposomes - virus free and cheap, but low efficiency
DNA cassetts - virus free yet expression temporary
Retrovrus - efficient permeant but unstable and need to divide cells