Molecular & Cellular Drug Targets

Question 1

Why be concerned about drug targets ?

Answer 1

• interactions with other drugs new modalities for using drugs (most important)
• new indications for drugs
• new concerns regarding risk/benefit

Question 2

Are drug targets large or small

Answer 2

Drug targets are large molecules – macromolecules

Question 3

Are drugs generally larger or smaller than their targets

Answer 3

Drugs are generally much smaller than their targets

Question 4

How do drugs interact with their targets

Answer 4

Drugs interact with their targets by binding to binding sites

Question 5

are binding sites usually hydrophobic or hydrophilic

Answer 5

Binding sites are typically hydrophobic pockets on the surface of macromolecules

Question 6

what kind of bonds are typically involved in intermolecular bonds

Answer 6

Binding interactions typically involve intermolecular bonds

Question 7

what is a binding group

Answer 7

Functional groups on the drug are involved in binding interactions and are called binding groups (drug)

Question 8

What is a binding site

Answer 8

Specific regions within the binding site that are involved in binding interactions are called binding regions (target)

Question 9

T/F the binding group is associated with the drug

Answer 9

true

Question 10

t/f binding regions are with the target

Answer 10

true

Question 11

what are the 4 major drug targets

Answer 11

Four major drug targets
A. Receptors 
B. Ion channels 
C. Enzymes
D. Transporters

Question 12

What are the 3 ways that drugs work

Answer 12

1. Some drugs antagonize, block or inhibit
   endogenous proteins
2. Some drugs activate endogenous proteins
3. A few drugs have unconventional mechanisms of action

Question 13

What is an an antagonist

Answer 13

A drug is said to “antagonize” or “block” the receptor and is referred to as a receptor antagonist

Question 14

What is a receptor drug target

Answer 14

A macromolecular component of the organism that binds the drug and initiates the drug’s effect

Question 15

receptor drug targets are what kind of macromolecule

Answer 15

Most receptors are proteins

Question 16

Where are the 2 possible locations of receptor drug targets

Answer 16

cell surface receptor and nuclear receptor

Question 17

describe what a cell surface receptor looks like

Answer 17

CELL SURFACE RECEPTOR:
o embedded in the cell membrane
o functions to receive chemical information from the
extracellular compartment and to transmit that
information to the intracellular compartment

Question 18

describe what a nuclear receptor looks like

Answer 18

NUCLEAR RECEPTOR:
o exists in the intracellular compartment
o upon activation binds to regulator regions in the DNA
and modulates gene expression

Question 19

Some drugs bind to cell surface receptors, yet do not activate the receptors to trigger a response. What is this called

Answer 19

antagonist

Question 20

When cell surface receptors bind the drug molecule, the endogenous chemical cannot bind to the receptor and cannot trigger a response. What is this called

Answer 20

antagonist

Question 21

Some drugs bind to cell surface receptors and trigger a response
• Drugs in this group are called __________

Answer 21

Some drugs bind to cell surface receptors and trigger a response
• Drugs in this group are called receptor agonists

Question 22

receptor agonist will always produce a _____response

Answer 22

functional

Question 23

Some drugs bind to nuclear receptors, yet do not activate the receptors to translocate to the nucleus, bind DNA and alter gene expression. This is known as

Answer 23

receptor agonist

Question 24

T/F Receptor Antagonists: block endogenous mediators

Answer 24

True

Question 25

Where are ion channels found

Answer 25

Ion channels are proteins found in a cell’s membrane

Question 26

what is an ion channel

Answer 26

Ion channels create tiny openings in the membrane only to allow specific ions to pass through

Question 27

What is the function of an ion channel

Answer 27

on channels allow ions to transverse the cell membrane down an electrochemical gradient

Question 28

how do drugs effect ion channels

Answer 28

Some drugs bind to ion channels and physically block the pore or cause an allosteric change that closes the pore

Question 29

T/F there are ion channel openers and closers

Answer 29

true

Question 30

T/F there are ion channel blockers and modulators

Answer 30

true

Question 31

What is the function of an enzyme

Answer 31

•Enzymes catalyze the biosynthesis of products from substrates

Question 32

What are the 3 was that drugs interact with enzymes

Answer 32

• Inhibitor of enzyme reaction
• False substrate to enzyme
• Pro-drug (substrate)

Question 33

if she gives something that ends in -ase . What answer should you look for

Answer 33

enzyme!!

Question 34

is antagonist and agonist related to only receptors

Answer 34

yes

Question 35

transporters are made of what kind of macromolecules

Answer 35

protein

Question 36

how do transporters work

Answer 36

•Transporters bind to and shuttle membrane impermeable solutes across the cell membrane

Question 37

how do drugs interact with transporters

Answer 37

Some drugs bind to transporters and cause allosteric changes that prevent proper functioning of the transporters

Question 38

How many types of receptors are there what what are their names

Answer 38

1. Ionotropic receptors
2. Metabotropic receptors
3. Nuclear receptors
4. Receptors linked to enzymes:

Question 39

(Ligand-gated ion channels are also known as

Answer 39

Ionotropic receptors- associated with ion channel

Question 40

What happens to a channel when a liand binds to to an ionotropic receptor

Answer 40

on channels open or close upon binding of a ligand to the receptor on the ion channel

Question 41

What is a metabotrobic receptor also known as ? How does it function

Answer 41

G- protein-coupled receptors. Drugs bind to transmembrane receptor protein that stimulates a GTP-binding signal transducer protein (G- protein) that modulate enzyme activity or ion channel function.

Question 42

GPCR are associated with ____messengers

Answer 42

second

Question 43

which type of cells can enter cell

Answer 43

lipid

Question 44

t/f steroid hormones can enter cell

Answer 44

true, bx it is lipid soluble

Question 45

inotropic receptors are located on

Answer 45

ion channels

Question 46

metabotropic receptors are located on

Answer 46

attached with G protein receptors

Question 47

describe the physical structure of what an receptor linked to enzymes looks like

Answer 47

there is an extra cellular component that ligand binds to , then there is an intracellular component that has enzyme activity

Question 48

T/F There are Different receptors for different messengers

Answer 48

True, this is known as specificity

Question 49

T/F there is usually one kind of receptor on a cell

Answer 49

False, Each cell has a range of receptors in the cell membrane making it responsive to different chemical messengers. But each individual ligand binds to its own receptor

Question 50

would a drug like a laxative have any affect on the targets that we discussed

Answer 50

no! this is because it Is just targeting the physical properties , not any of the stuff she already talked about