DRUG AFFINITY Flashcards
HOW MUCH OF THE HUMAN GENOME IS DISEASE CAUSING
10%
IF A PROTEIN HAS A ‘POCKET’ IN WHICH A SMALL MOLECULE CAN FIT, WHAT CAN WE DO
TARGET THE PROTEIN WITH DRUGS
DEFINE DRUGS
SMALL MOLECULES THAT TARGET PROTEINS
WHAT TYPES OF TARGET PROTEINS ARE THERE
- RECEPTORS
- ION CHANNELS
- ENZYMES
- TRANSPORTERS
- OTHER TARGETS SUCH AS MICROTUBULES
WHAT CAN BE SAID ABOUT THE SPECIFICITY OF DRUGS
NO DRUG IS 100% SPECIFIC
HOW CAN RECEPTORS BE CLASSIFIED
- STRUCTURE
- PHARMACEUTICAL PROPERTIES
- SIGNALLING
WHAT IS AN AGONIST
BRING ABOUT CELL FUNCTION CHANGE (DIRECT/INDIRECT)
WHAT IS AN ANTAGONIST
BIND TO A RECEPTOR STOPPING ACTIVATION AND DISALLOWING OTHER AGONISTS TO BIND
WHAT IS AN INVERSE AGONIST
BIND TO RECEPTOR STOPPING ACTIVATION
WHAT EFFECTS CAN SMALL MOLECULES HAVE ON CHANNELS
- BLOCKERS
2. MODULATORS
IN TERMS OF ENZYMES AND TRANSPORTERS, HOW CAN THEY BE AFFECTED
- INHIBITORS CAN BIND TO PREVENT FUNCTION
- FALSE SUBTRATES CREATE ABNORMAL METABOLITES
- PRO DRUGS METABOLISED TO CREATE THE ACTUAL ACTIVE DRUG
WHAT ARE THE RECEPTOR FAMILIES
- LIGAND GATED ION CHANNELS (IONOTROPIC)
- GPCR (METABOTROPIC)
- KINASE LINKED
- NUCLEAR
WHAT MAIN TYPES OF LIGAND GATED ION CHANNELS ARE THERE
- CYS LOOP
- GLUTAMATE
- P2X
- CA RELEASE
HOW MANY TMSD DO GPCR HAVE
7
HOW MANY TMSD DO NUCLEAR RECEPTORS HAVE
NONE AS THEY ARE IN THE NUCLEUS AND NOT IN THE BILAYER
WHAT TYPE OF BINDING DOMAIN TO NUCLEAR RECEPTORS HAVE
DNA BINDING (ZINC FINGERS)
