Dugga 1

Question 1

What do agonists do?

Answer 1

mimic the natual ligand

Question 2

What do antagonists do?

Answer 2

Bind to the receptor but do not activate it

Question 3

Do antagonists bind to regions of the receptor that are not involved in binding the natural ligand?

Answer 3

Yes

Question 4

What do partial agonists do?

Answer 4

They induce a weaker effect than a full agonist

Question 5

What is an inverse agonist?

Answer 5

Acts as an antagonist and also eliminate any resting activity

Question 6

What is desensitisation?

Answer 6

When an agonist is bound to its receptor for a long time

Question 7

What is sensitisation?

Answer 7

When an antagonist is bound to a receptor for a long time, the cells synthesise more receptors to counter the effect

Question 8

What is tolerance?

Answer 8

When an increased dose is required over time to achieve same effect

Question 9

What is dependence?

Answer 9

The body’s ability do adapt to the presence of a drug

Question 10

What is pharmacodynamics?

Answer 10

How drugs interact with their targets to produce a pharmacological effect

“What the drug does to the body”

Question 11

What is pharmacokinteics?

Answer 11

The study of factors that affect the ability of the drug to reach its
target in the body

“What the body does to the drug”

Question 12

What is affinity?

Answer 12

A measure of how strongly a drug binds to a receptor

Question 13

What is efficacy?

Answer 13

A measure of the effect of the binding of a drug on the cell

Question 14

What is potency?

Answer 14

How effective a drug is in producing a cellular effect

Question 15

What sorts of molecules do transport proteins transport?

Answer 15

Polar molecules

Question 16

What can drugs that target viral structural proteins do?

Answer 16

Prevent viruses from entering the cell and inhibit the uncoating

Question 17

What is tubulin?

Answer 17

A structural protein crucial to cell division and mobility

Question 18

What do vinca alkaloids do to tubulin?

Answer 18

Bind and inhibit the polymerisation process

Question 19

What does paclitaxel do to tubulin?

Answer 19

Bind and accelerate polymerisation by stabilising resulting microtubules

Question 20

How does a drug targeting lipids work?

Answer 20

Disrupting the lipid structure of cell membranes

Question 21

What do tunelling molecules and ion carriers do to the plasma membrane and to the cell?

Answer 21

They result in uncontrolled movement of ions across the cell membrane leading to cell death

Question 22

What is valinomycin?

Answer 22

A cyclic structure with alternating ester and amide bonds and acts as a ion carrier

Question 23

What is the definition of a drug target?

Answer 23

A macromolecule that has a binding site where the drug binds

Question 24

How do drugs bind their target?

Answer 24

Intermolecular bonds

Question 25

Where do hydrogen bonds occur?

Answer 25

Between an electron rich heteroatom and an electron deficient hydrogen

Question 26

What are hydrophobic interactions?

Answer 26

The displacement of ordered layer of water molecules that surround hydrophobic regions. This increases entropy.

Question 27

What needs to happen to polar groups before intermolecular interactions can take place?

Answer 27

They have to be desolvated

Question 28

What is the primary structure?

Answer 28

The order in which amino acids are linked together

Question 29

What is the secondary structure?

Answer 29

Regions of ordered structure within the protein such as alpha helices, beta pleated sheets and beta turns

Question 30

What is the tertiary structure

Answer 30

The overall three dimensional shape, how the alpha and beta regions are ordered and linked by interactions

Question 31

What is he quarternary structure?

Answer 31

Proteins containing two or more subunits, how the subunits are arranged

Question 32

How are the structures determined?

Answer 32

To maximise the favourable intramolecular and intermolecular bonds and minimise unfavourable interactions

Question 33

Where are the polar residues typically favoured?

Answer 33

On the outside of the protein because this allows for interactions with water

Question 34

What is proteomics?

Answer 34

The study of the structure and function of novel proteins discovered through genomics

Question 35

What are common drug targets?

Answer 35

Transport proteins, enzymes and receptors

Question 36

What do transport proteins do?

Answer 36

Transport essential polar molecules across the hydrophobic cell membrane

Question 37

What is tubulin?

Answer 37

A structural protein crucial to cell division and mobility

Question 38

How does a substrate bind to an active site?

Answer 38

With intermolecular bonds

Question 39

When a substrate binds in an enzyme, the shape of the active site may change to maximise binding interactions and in this process what may happen to the bonds in the substrate?

Answer 39

It may weaken crucial bonds

Question 40

The amino acid histine is often present in the active site, what does it do?

Answer 40

It acts as an acid/base catalyst

Question 41

The amino acid histine is often present in the active site to act as an acid/base catalyst, which other amino acids may be present?

Answer 41

Glutamic acid, aspartic acid, tyrosine

Question 42

Which amino acids act as nucleophiles in the reacton mechanism of some enzymes?

Answer 42

Serine and cysteine. In some enzymes lysine

Question 43

What are cofactors?

Answer 43

Metal ions or small organic molecules. They can be viewed as the body's chemical reagents.

Question 44

What is a prothetic group?

Answer 44

A cofactor bound covalently to an enzyme

Question 45

What is an allosteric inhibitor?

Answer 45

Binds to a different binding site and alters the shape of the enzyme so that the active site nolonger works. Often involved in feedback control of biosynthetic pathways

Question 46

What is an isozyme?

Answer 46

A variation of the same enzyme. Catalyse same reaction but differ in primary structure, substrate specificity and tissue distribution

Question 47

What does the Michaelis Menten equation relate?

Answer 47

The rate of an enzyme catalysed reaction to the substrate concentration

Question 48

What is the Michaelis contant equal to?

Answer 48

The substrate concentration at which the rate of enzyme catalysed reaction is half of its max value

Question 49

What does G protein coupled receptors activate?

Answer 49

G proteins

Question 50

How many transmembrane section does a G protein coupled receptor have?

Answer 50

7

Question 51

Where is the C and N terminals located in a G protein coupled receptor?

Answer 51

The C terminal is within the cell and the N terminal outside the cell

Question 52

Receptor types have subtypes. Is it possible for a drug to target only one subtype of the receptor?

Answer 52

Yes

Question 53

Intracellular receptors are located within the cell and are important in controlling...

Answer 53

transcription

Question 54

How does a chemical messenger for an intracellular receptor pass through the cell membrane?

Answer 54

It must be sufficiently hydrophobic

Question 55

What does a G protein consist of?

Answer 55

3 protein subunits of which the alpha one is bound to the G protein

Question 56

What happens to the G protein coupled receptor when a ligand binds?

Answer 56

GDP is exchanged for GTP which the G protein fractions into an alpha subunit and a beta gamma subunit

Question 57

What does the alpha s subunit bind to?

Answer 57

Adenylate cyclase catalysing the formation of cAMP from ATP

Question 58

What does the alpha i subunit do?

Answer 58

Inhibits adenylate cyclase

Question 59

What does cAMP do?

Answer 59

Acts as a secondary messenger and activates PKA

Question 60

What does PKA do?

Answer 60

It catalyses the phosphorylation of serine and threonine residues in other enzymes

Question 61

What are tyrosine kinases?

Answer 61

Enzymes that phosphorylate the phenol group of tyrosine. Phosphorylation is a conformational change that affects the activity of the substrate enzyme

Question 62

What do intracellular receptors do?

Answer 62

Regulate gene transcription