GMS6551- FUNDAMENTALS OF PHARMACOLOGY:
DISCOVERY AND NOMENCLATURE
what do you do first when finding/developing a drug? - Correct Answer choose a disease:
-pharma made of companies
-tend to target diseases that have a large market
-government incentives to target orphan diseases (affects fewer than 200,000 people nationwide)
drug target - Correct Answer molecule the drug will interact with such as an enzyme, receptor, other
protein, DNA, RNA, etc.
selectivity - Correct Answer -target determines side effects
-easier to target non-human protein
-target mutated cancer protein
assay development - Correct Answer -in vitro
-in vivo
-ex vivo
examples of in vitro - Correct Answer test tube and cell culture
examples of in vivo - Correct Answer living animals
examples of ex vivo - Correct Answer tissue
what are some advantages of in vitro? - Correct Answer -fast - hundreds/thousands per day
-in expensive
-less red tape
-clean systems
what are some disadvantages of in vitro? - Correct Answer a test tube or cell is NOT an animal
, what are advantages to in vivo? - Correct Answer results more likely to translate to humans
what are disadvantages to in vivo? - Correct Answer -more expensive
-may cause suffering to animals
-regulations
-complex systems
lead compound - Correct Answer -first compound found that has the activity we want
how can we find a lead compound? - Correct Answer -natural products such as plants, algae,
bacteria, fungi
-chemical banks - thousands or millions
-rational drug design- utilize side effect and alter natural ligand
computer-aided drug design/molecular docking - Correct Answer -crystal structures of many proteins
known
-program calculates chemical attraction
what are some advantages to computer-aided drug design/molecular docking? - Correct Answer fast
and cheap/free
what are some disadvantages to computer-aided drug design/molecular docking? - Correct Answer
skips a lot of details such as conformations and cell membrane
T/F: the larger release of gibbs free energy is going to predict stronger binding - Correct Answer True
structure activity relationships (SAR) - Correct Answer -optimize lead compound and functionalize
-test new compounds
-choose best compound
-functionalize new compound
-makes better drug and eliminates unneeded functionalization - reduced off-target effects
DISCOVERY AND NOMENCLATURE
what do you do first when finding/developing a drug? - Correct Answer choose a disease:
-pharma made of companies
-tend to target diseases that have a large market
-government incentives to target orphan diseases (affects fewer than 200,000 people nationwide)
drug target - Correct Answer molecule the drug will interact with such as an enzyme, receptor, other
protein, DNA, RNA, etc.
selectivity - Correct Answer -target determines side effects
-easier to target non-human protein
-target mutated cancer protein
assay development - Correct Answer -in vitro
-in vivo
-ex vivo
examples of in vitro - Correct Answer test tube and cell culture
examples of in vivo - Correct Answer living animals
examples of ex vivo - Correct Answer tissue
what are some advantages of in vitro? - Correct Answer -fast - hundreds/thousands per day
-in expensive
-less red tape
-clean systems
what are some disadvantages of in vitro? - Correct Answer a test tube or cell is NOT an animal
, what are advantages to in vivo? - Correct Answer results more likely to translate to humans
what are disadvantages to in vivo? - Correct Answer -more expensive
-may cause suffering to animals
-regulations
-complex systems
lead compound - Correct Answer -first compound found that has the activity we want
how can we find a lead compound? - Correct Answer -natural products such as plants, algae,
bacteria, fungi
-chemical banks - thousands or millions
-rational drug design- utilize side effect and alter natural ligand
computer-aided drug design/molecular docking - Correct Answer -crystal structures of many proteins
known
-program calculates chemical attraction
what are some advantages to computer-aided drug design/molecular docking? - Correct Answer fast
and cheap/free
what are some disadvantages to computer-aided drug design/molecular docking? - Correct Answer
skips a lot of details such as conformations and cell membrane
T/F: the larger release of gibbs free energy is going to predict stronger binding - Correct Answer True
structure activity relationships (SAR) - Correct Answer -optimize lead compound and functionalize
-test new compounds
-choose best compound
-functionalize new compound
-makes better drug and eliminates unneeded functionalization - reduced off-target effects
