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Drugs: From molecules to man > 1: Proteins as drug targets > Flashcards

1: Proteins as drug targets Flashcards

1
Q

which 4 drugs dont target proteins

A

antacids
osmotic diuretics
DNA modifying drugs
Membrane lipid targeting drugs

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2
Q

what is the main extracellular target protein

A

enzymes

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3
Q

main intracellular target proteins

A

nuclear hormone receptors
and
enzymes

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4
Q

what is binding domain

A

usually a acavity lined with amino acids that make up the protein
small part of the protein, so must ensure the binding energy that comes from the drug binding to it, has a conformational effect on the receptor

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5
Q

what are families and superfamilies based on

A

AA sequence similarity

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6
Q

what superfamily is the Estrogen like family part of

A

Nuclear hormone receptor superfamily

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7
Q

name the 4 subunits of estrogen receptors

A

androgen receptors
progesterone receptors
glucocorticoid receptors
mineralcorticoid receptors

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8
Q

general mechanism of NHR superfamily

A

bind lipohillic agonist
then regulate transcripstion of DNA
which causes changes in protein mexpression

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9
Q

what is an advantage of having multiple proteins that are tissue specific

A

the individual types ar especialised for each tissue

and if a disorder affects one protein, there’s only some functions that are affected instead of everything going to poo

also they can compensate for each other

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10
Q

where are corticosteroids produced

A

adrenal cortex

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11
Q

what are the natural steroids that bind to glucocorticoid (and mineralcorticoid undesireably)

A

hydrocortisone
corticosterone

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12
Q

what are 4 key receptors

A

Ligand-gated ion channel

Receptor tyrosine kinase

G protein-coupled receptors

nuclear hormone receptor

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13
Q

example of receptor tyronsine kinase

A

insulin receptor

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14
Q

what do RTKs bind

A

big molecules
peptide hormones
growth factors
cytokines

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15
Q

how do RTKs operate

A

recognise specfic AAs in target proteins
and phosphroyalte tyrosine residues in these target protein

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16
Q

G protein coupled receptor example

A

B2 adrenoceptor

17
Q

what is the characteristic structure of the GPCR

A

3 transmembrane domains

18
Q

whats name of enzyme that turns ATP into cyclic AMP

A

adenylate cyclase

19
Q

which G protein stimulates and which inhibits adenylate cyclase

A

Gs stimulates
Gi inhibits

20
Q

what pathway does Gq associate with

A

PIP2 pathway

21
Q

when PIP2 is cleaved, what does this yield

A

DAG (Activates membrane targets)
and IP3 (intracellular soluble message, binds to Ca2+ stores -> which then can activate protein kinase C)

22
Q

example of ligand gated ion channels

A

nicotinic Ach recpetor

23
Q

what allows the LGIC to have so much diversity

A

multisubunit
so they can have many combinations

24
Q

3 types of structures in LGIC

A

cys-loop receptors
iGlutamate receptors
P2X receptors

25
Q

how many muscarinic acetylchloine receptors are there

A

5

26
Q

what does the BetaGamma complex in G protein activate and inhibit

A

activates:
cardiac potassium channels
B-adrenoceptor kinase

inhibits:
calcium channels

27
Q

3 main g proteins

A

Gi
Gs
and
Gq

28
Q

3 subunits of Gi and the alpha subunits present

A

Gi - alpha i = inhibits adenylyl cyclase (AC)
Gt - alpha t (transducin) = activation of PDE-6 (vision)
Gg - alpha gust (gustducin) = activation of PDE-6 (taste)

29
Q

2 subunits of Gs and the alpha subunits present

A

Gs - alpha s - activates AC
Golf - alpha olf - activates AC (olfaction)

30
Q

whats the function of Gq subunit

A

phospholipase C activation

31
Q

key players in adenylyl cyclase pathway

A

Gs or Gi
Adenylyl cyclase duh
ATP->cAMP
CNG/HCN channels
protein kinase A

32
Q

key players in phospholipase C

A

Gq
phospholipase C
cleaves PIP2

DAG
IP3
Ca2+
protein kinase C

33
Q

what 2 binding domains do NHRs have

A

DNA binding domain
and
ligand binding domain

34
Q

what type of NHR is involved in transrepression

A

NHR monomer

35
Q

what is an orphan receptor

A

Don’t know the function of some GPCRs and NHRs nor do we know their natural ligand

Drugs: From molecules to man (1 decks)

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