bind to AS, compete with substrate, prevent substrate binding
3 of 31
non competitive
binds allosteric site, conformational change - substrate can no longer bind
4 of 31
example of irreversible inhibitor
asprin - cox enzymes
5 of 31
example of reversible competitive
simvastatin
6 of 31
example of reversible non competitive
donepezil - alzeimhers
7 of 31
drugs can interact with receptors, they may
activate or inhibit the normal response
8 of 31
types of receptors (4)
Ion channels. GPCRs. Tyrosine kinase receptors . Nuclear receptors
9 of 31
Ion channels
fast transmission. Seconds time frame .
10 of 31
ligand binding to ion channels
may open channel, may block channel - prevent it opening
11 of 31
GPCRS operate in the
operate in the second time frame.
12 of 31
ligand binding
binding activates the G protein complex, which dissociates and activates membrane bound enzymes releasing 2nd messenger
13 of 31
GPCRS are the most common receptor for drug target
TRUE - 45% of drugs target GPCRs
14 of 31
Tyrosine kinase receptors
operates in the minute s- hour time frame . involved in the signal transduction of Growth factors and insulin.
15 of 31
ligand binding
causes activation from resting state --> cell division cycle - can be targeted by anticancer drugs
16 of 31
Nuclear receptors
found inside cells - so ligands need to be able to enter the cell. interact mainly with hormones and then involved in transcription. operates in the hours time frame.
17 of 31
ligand binding
hormone binds to receptor which activates a conformational change - DNA binding region now exposed - now transcription can occur
18 of 31
Structural protiens as targets
microtubules are involved in cell division- these are formed by the polymerization of TUBULIN- drugs can bind to tublin and prevent conversion into microtubules - preventing mitosis
19 of 31
Transport proteins as targets
drugs bind to TP and inhibit transport across CM - called re uptake inhibitors - example is anti depressants
20 of 31
Protein building block as targets
vancomycin targets building blocks of cell wall synthesis of bact
21 of 31
protein - protein interactions
most processes involve 2+ proteins - drugs can target this
22 of 31
Lipids as targets
interfere with lipids in CM , disrupt CM
23 of 31
Lipid drugs - tunneling molecules
insert self into CM of fungi/bact - disrupt CM - in particular loss of K+
24 of 31
Lipid drugs - ion carries
increase perm of CM to ions - not specific to any particular ions
25 of 31
Carbs as targets
only recently discovered as targets, still being researched - not fully understood yet. wehn we talk about carbs as targets we mean complex carbs on CM as recognition - not simple carbs
Comments
No comments have yet been made