first lecture Flashcards
drug discovery is a
long process
2 step process of drug discovery
molecule identification –> patient
ways lead compound is found
novel molecule that possesses traits/interesting biological activity that could be biologically useful
novel molecule is designed in order to modify a target molecules (enzyme/receptor) activity
what is a lead compound
compound that has biological activity that is likely to be therapeutically useful
may need to be modified first
how do lead compounds turn into medicine
- identified
- developed through a long and expensive process
1796 jenner
inoculated boy with cowpocks
lead to immunity against smallpocks
1700 withering
extracted digitalis from foxglove for cardiac problems
1864 pasteur
identified that microorganisms caused disease.
made vaccines using attenuated rabies
for rabies vaccines
attenuated meaning
reduced in force
aka weaker
1900s quinine
derived from cinchona tree bark
used to treat malaria
1900s aspirin
extracted from willow tree bark
treats fever
7 diff ways drugs come from
- nature
- animal
- microbial
- endogeous lead compound
- minerals
- synthesis
- serendipity
drugs from nature eg
morphine (analgesic)
neem
rose
tobacco
lovastatin (hypolipidemic)
drugs from animal sources eg
insulin - cows pancreas
pepsin - cow stomach
drugs from microbial sources
penicillin (antibiotic)
drugs from endogenous lead compounds eg
occur naturally in the body
histamine
adrenaline
salbutanol
ranitidine
drugs from minerals eg
FeSO4 - anemia
MgSO4 - purgative
NaHCO3 - antacid
drugs from syntheis eg
azo dyes + their antibac properties
phenazopyridine + urinary antiseptic
drugs from serendipity eg
sildenafil - <3 and <3!
Synthetic drugs can form from
scanning chemical libraries
these allow us to find lead compounds
made by chem synthesis to immitate a natural product
2 diff drug types
small molecules
biologics
based on the size//weight of the active principle
small molecules
MW < 900Da
biologics
MW > 900
grown + purified from large scale cell cultures of bacteria, yeast, plant or animal cells
small molecule examples
fatty acids
glucose
amino acids
cholesterol
secondary metabolites (lipids)
either synthesised in nature or extracted from plants
biologics examples
vaccines, growth factors, immune modulators, monoclonal antibodies, products derived from human blood/plasma
whats different about biological therapeutics
they are regulated, tested and controlled differently than other medicines
(practive of treating disease from living organisms)