Please enable JavaScript.
Coggle requires JavaScript to display documents.
drug targets - Coggle Diagram
drug targets
examples
-
dactinomycin
intercalating agent that binds to DNA bases to stabilize it and prevent uncoiling so no transcription
bleomycin
intercalating agent that uses ferrous ions to create radicals which causes destabilization and chain cutting and also ihibits the enzymes responsible for fixing this cutting
-
-
-
-
salbutamol + formoterol
anti asthmatics that bind to the B2 adrenreceptor to cause smooth muscle relaxation (salbutamol has t-butyl group, formoterol has lower lipophillicity because hydrophobic side chain)
benzodiazepines
allosteric modulators that binds to GABA receptor and keeps it open so there's continual neuronal firing of relaxation
aliskerin
renin inhibitor that stabilizes the trsnsition state of angiotension-renin interactions by mimicking the transition state through a hydroxyl group
-
raloxifene
antagonist that blocks the conf change of estrogen receptor after binding to it and doesn't let the coactivator bind causing transcription to stop
-
-
taxol
structural protein upregulates tubulin synthesis which makes more microtubule which causes less cell division so anticancer
wrenchnolol
amphiphillic drug mimicking the tf-coactivator interaction through its hydrophobic jaws and polar handle
-
-
other
-
-
structural proteins: taxol accelerates tubulin making which makes cell division harder and anticancer!
protein-protein interactions: wrenchnolol mimics coactivator-transcription factor interaction to prevent it and anticancer!
DNA/RNA
-
-
-
can target rRNA and prevent translation: chloramphenicol prevents peptide chain transfer --> can cause aplastic anaemia
enzymes
-
irreversible inhibition: strong covalent bond irreversibly bound to active site (often time-dependent)
-
-
if you dont want side effects of strong electrophile, use mild electrophile and selective binders
ibuprofen and aspirin inhibit COX2 enzyme which inhibits synthesis of prostaglandins responsible for pain perception
measurements:
- IC50: I conc required to reduce enzyme to 50% activity
- ki: eqv constant for I binding --> low=potent
- EC50: I conc required to reduce effect by 50%
receptors
agonists: bind to receptor reversibly and mimic ligand effect (takes size, shape and flexibility into account) ex-glucocorticoid receptors
anti-asthmatics: salbutamol agonist that binds to adrenoreceptor subtype (more sensitive bc t-butyl), formoterol also binds because lower lipophillcity
-
desensitization--> combat with phosphorylation, endocytosis or reduced receptor synthesis
-
-
antagonists: block messenger from binding to receptor irreversibly through allosteric binding or umbrella effect but no effect
-
-