1What are the three compistitions of a chemical probe?
Protein targeting lignad, linker, read our or pull down
2Describe 3 ways probes can modulate protein function?
target binding site of receptors and block signal
target active site and impact enzyme finction
allosterically bind and inhibit active or binding site function
3what is important to consider when making a drug? (3)hat is
safe
selective enough to limit side effects
may have undefined mehcanism
4What is important to consider when making probes? (4)
needs to address specific biological question
needs to be selective
defined mechanism
access cannot be restricted
5Explain the advantages of a cleavable linker in chemical probe? (4)
controlled release
target specificity
target amplification
delayed drug release
6Explain the advantages of a NON cleavable linker in chemical probe?
extended life
stability
selectivity
easier to synthesis
7What are the dis/advantages of immobilised chemical probes? (1)/(2)
easily synthesised
widely emplyed
can impact interactions
8Define Foreward Chemical Genetics
compound that alters property of system of interest then identify the modulated dene product which is respnsible.
9Advantages of forward chemical genetics
compounds are exposed to more biologically relevant contexts
10Challenges of forward chemical genetics
dont know the target
target discovery may be dificult
lot of subsequent effort needed to discover moelcular targets and understand their selectivity and mechanism
11Define reverse chemical genetics
start with known target seek to investigate its function using perturbation experriments.
12What advantage does chemical genetics have over traditional genetics?
identifies target protein and characterises the protein-compound interaction
expose test system to compound, analyses phenotype and compart controls