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