Theme 4 Lecture 13 Extra Reading Flashcards
Perm and tox/enzymes in vitro not real
Cell based vs biochemical assay?
Cell based assays mimic natural conditions(gives data on cell permeability and toxicity)
Biochemcial based assays are better for high throughput screening(use enzymes but not linked to real world)
HMTS/HDMS
Express
Therap
What is histone methylation?
Controlled by HMTS and HDMS
Methylation leads to increase or decrease and regulates gene expression+linked to human diseases
Thus makes its target for therapeutic inhibitors
In
Sel,pot,kin
What are HMT biochemical assays
Run in-vitro tests which are ideal for identifying inhibitors, assessing selectivity, potency, and kinetics
Perm and tox
What are the limitations of biochemical assays for HMT/HDM?
They use synthetic systems with purified enzymes, dont give informtion on permeabiity and toxicity.
Bio
tar
opposite of other one
What are the advantages of cell-based assays for HMT/HDM?
Biologically relevant cell based environment
Info on target functionality
Tox and perm
anti
time
What challenges do cell-based assays face?
Time and compplex for HMT/HDM
Rely on specific antibodies
Cellular phenotypes underlying certain epigenetic modifications might require incubation
periods in the range of days to weeks, a time frame not compatible with most high-throughput
cellular assays.
bio
chem
tar
Define a primary active compound.
Shows significant biological activity and begins link with chemical structure and target
pur,ide,cons,sec,spe,sel,drug
What constitutes a validated hit in drug discovery?
A validated hit has confirmed purity and identity, consistent activity in secondary assays, and meets criteria for specificity, selectivity, and druggability.
What is a purified enzyme?
Cleaned from other substaces, working with just the enzyme and nothing else.
What is HMT/HDM
Histone Methyl transferase/Histone Demethylase
