drug target - 4py019, Lecture notes of Pharmacy

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Body adapts to environmental

changes

HOMEOSTASIS

:

systems

exist to be able to keep

physiological

parameters

in

healthy

limits

. And if body habitually

exceeds these limits ,

a state of disease resulti

·

Pharmacy

attempts

to correct disease

using drugs

understanding

of how

drugs

interact

with homeostasis mechanisms

CELLULAR E MOLECULAR PERSPECTIVE

:

poumanismwhimessagearrivefrom where

ligand binding results

in cell event De

proteins

is wall me aa

all are proteins

containing

site for binding

either ligands/substrates

ON CHANNES

:

ligand

binding opens

channel allowing

enter/exit

of

ions

osynthetic

:

drug

to

drug target

enzymes: makes

things

or

breaks them

down

DRUGS

:

Are not naturally occuring

< binds to

a

target

protein by stopping

natural

ligand/substrate

binding

to restore homeostasis Caveats-some

drugs

do not

fit

this

models We

do not know how

they target

POTENCY

:

Drug

lines being

bound to

target

large DG-negative

energy

will

stay

bound even when substrates are

present If

a

drug

stops

this ; the

enzyme

can't

process

the substrate /the

enzyme

stops working

=

enzyme

inhibitor

If

a

drug

stops transporter

:

transport

inhibitor

·

measured

in terms of concentration (1Cso)

• concentration of drug

needed to reduce

target activity

to 50 % normal value Lower Iso

= more potent drug: required

low

amounts

of drug

ION CHANNELS VERSUS RECEPTORS

:

naturally occuring ligands making

channels a receptors

work - agonists

drugs

which stop

naturally

occuring ligands from binding

antagonists

blockers

drugs

which

have a

stronger s

, natural effect of agonists

measured

with

Elso-agonists

SELECTIVITY

:

drugs on-target

effects

will restore

healthy

homeostasis

same

drugs

will bind to other

targets

but if

it binds less

potently

with

higher

= selective

Similar

1250 drugs

against

other targets

= non-selective

off-target

effecti

• Ideal

drug=highly

potent

& Selective

ENZYME INHIBITION

:

Inhibiting

ACE blood

pressure

Ag

enzyme Receptor

Antigiotensinogen

in

,

Angiotensin

1

Angiotensin

ATAR

I

vasoconstrictions

((az]

= -

↑ [P] =

PL

RECEPTOR AGONISTS /ANTAGONISTS

:

TRANSPORT INHIBITORS

:

nerve cells release neurotransmitter molecules to

convey signals

to

other cells

• Turned

off

Signals by

neurotransmitter back

to nerve cell that

release them requiring transporter. blocking

=

Reuptake

inhibitor elong