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CH 456 Medicinal Chemistry > Chapter 10: Miscellaneous Drug Targets > Flashcards

Chapter 10: Miscellaneous Drug Targets Flashcards

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1
Q

How can transport proteins act as drug targets?

A

The binding site for the molecule being transported has a drug bind it and therefore prevent transport

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2
Q

What are two examples of drugs that bind to transport proteins and what is their effect on the body?

A

Cocaine and tricyclic antidepressants

bind to transport proteins and prevent neurotransmitters (e.g., noradrenaline, dopamine) from re-entering nerve cells

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3
Q

_______ acts centrally to inhibit the reuptake of serotonin, noradrenaline and, to a lesser extent, dopamine. The increase in serotonin results in?

A

Sibutramine,

Increase in serotonin = dulls appetite

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4
Q

What 6 antidepressant drugs act on transport proteins to block the uptake of serotonin?

A 
Fluoxetine (prozac)
Citalopram
EScitalopram
Sertraline
Paroxetine 
Fluvoxamine
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5
Q

Enfuvirtide (HIV fusion inhibitor) can be used to prevent _______ assembly or viral entry into a cell

A

Capsid (outer protein shell of virus)

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6
Q

What are the two drugs that inhibit tubulin polymerization

A

colchicine – used in the treatment of gout

Vinca alkaloids derived from periwinkle plant – anticancer agents
ie, vincristine, vinblastine, vindesine and vinorelbine

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7
Q

What drug and its analog inhibit tubulin depolymerization?

A

paclitaxel (Taxol) and the semi-synthetic analogue, docetaxel, are important anticancer agents

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8
Q

How can drugs take advantage of the transport across the cell membrane

A

Polar molecules cross the hydrophobic cell membrane, therefore . drugs can be designed to take advantage of this transport system in order to gain access to cells or to block the transport protein.

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9
Q

____ is structural protein crucial to cell division and cell mobility and is the target for several anticancer drugs.

A

Tubulin

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10
Q

How do the Vinca alkaloids work to effect tubulin?

A

The Vinca alkaloids bind to tubulin and inhibit the polymerization process.

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11
Q

How does taxol work to effect tubulin?

A

bind to tubulin and accelerate polymerization by stabilizing the resulting microtubules

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12
Q

What is the one biosynthetic building block as a drug target?

A

Vancomycin

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13
Q

What does vancomycin inhibit?

A

inhibits proper cell wall synthesis in Gram-positive bacteria

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14
Q

How does vancomycin work?

A

large hydrophilic molecule is able to form hydrogen bond interactions with the terminal D-alanyl-D-alanine moieties of the NAM/NAG-peptides

Crystal structure of a short peptide L-Lys-D-Ala-D-Ala

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15
Q

What is the one biosynthetic process (chain terminator) as a drug target?

A

Puromycin

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16
Q

What effect does puromycin have?

A

terminates polypeptide elongation during protein translation

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17
Q

True or False: Puromycin enters the B site of the ribosome and assists aminoacyl-tRNA molecules to bind

A

False, enters the A site of the ribosome and prevent aminoacyl-tRNA molecules from binding

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18
Q

How does the transfer of the peptide chain to puromycin work?

A

NH2 group attacks Carbon group, NH becomes bound to peptide group and double bond O

leaving OH group on aminoacyl-tRNA

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19
Q

What are the two examples of antibodies that can inhibit protein-protein interactions?

A

daclizumab

abciximab

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20
Q

_____ is a human monoclonal antibody that was developed as a immunosuppressant in kidney transplants (discontinued) to treat adults with relapsing forms of MS

A

daclizumab

21
Q

What is the effect(s) of abciximab?

A

inhibits blood clotting following angioplasty by preventing platelets from sticking together and causing thrombus (blood clot) formation within the coronary artery

22
Q

Describe the interaction between MDM2-p53

A

Normally: MDM2 binds to p53, MDM2 ubiquitinates p53 resulting in p53 leaving nucleus. P53 degradation is mediated by MDM2 in the cytosol

23
Q

What 5 things cause p53 to activate?

A 
DNA damage
Telomere damage 
Oncogene 
Ribonucleotide depletion 
Oxidative stressor hypoxia
24
Q

What are the 6 hallmarks of tumors that enable them to survive?

A 
Resisting cell death 
Evading growth suppressors
Sustaining proliferative signalling 
Activating invasion and metastasis 
Enabling replicative immortality
Inducing angiogenesis

RESAEI

25
Q

True or False: Overexpression of MDM2 promotes the development of the malignant phenotype

A

True

MDM2 functions as E3 ligase (assists in transfer of ubiquitin), moves p53 to cytosol to be degraded by proteolytic enzymes,

MDM2 inhibits transcriptional activity of p53

26
Q

True or False: Inhibition of MDM2 allows for restoration of p53 tumour suppressor function

A

True

27
Q

_____ are a series of cis-imidazoline analogues that are a important negative regulator of the p53 tumour suppressor

A

Nutulins

28
Q

How do nutulins work?

A

mimic 3 amino acids (amino acid finger) present on p53 (Leu-26, Trp-23, Phe-19) and prevent the interaction mdm2 and p53

29
Q

True or False: Nutlin binds in the same cleft as the native p53 helix.

A

True

30
Q

____ as drug targets generally act by disrupting cell membrane structure

A

Lipids

31
Q

____ is used topically against athlete’s foot and systemically against life-threatening fungal diseases

A

Amphotericin B

32
Q

How does amphroectin B work?

A

interacts with the lipids and sterols (ergosterol) of fungal cell membranes to build ‘tunnels’ through the membrane

33
Q

How does Gramicidin work against the lipid membrane?

A

thought to coil into a helix such that the outside of the helix is hydrophobic and interacts with the membrane lipids

the inside of the helix contains hydrophilic groups

this allows the leaking of ions from the cell leading to cell death

34
Q

Gramicidin D is a heterogenous mixture of three antibiotic compounds, , gramicidins A, B and C, making up ______, ______, and ______, respectively

A

80%, 6%, 14%

peptide antibiotics with 15 alternating l- and d-amino acids

35
Q

______ allow molecules to leach out from the cell and cause cell death

A

Nanotubes

36
Q

True or False: cyclic peptides which will self-assemble in the cell membranes of bacteria to form tubules

A

True

37
Q

How do nanotubes work?

A

6 to 8 alternating d- and l-amino acids such that the amide groups are perpendicular to the plane of the cyclic structure, with the side chains pointing outwards in the same plane

38
Q

Why is valinomycin known as a natural neutral ionophore?

A

does not have a residual charge

39
Q

____ is a dodecadepsipeptide made of 12 alternating amino acids and esters to form a macrocyclic molecule

A

Valinomycin

40
Q

True or False: Valinomycin is obtained from the cells of several Streptomyces strains

A

True

41
Q

A ____ ion sits in the _____ centre of valinomycin

A

Potassium, hydrophillic

42
Q

How does valinomycin disrupt the cell?

A

Valinomycin kills bacteria by facilitating the transport of K+ ions across the cell membrane, thereby disrupting the normal distribution of ions in the bacterium

43
Q

True or False: the K+–valinomycin complex is highly soluble in the nonpolar interior of the membrane

A

True

44
Q

________ and ______ act on the plasma membrane and result in the uncontrolled movement of ions across the cell membrane leading to cell death.

A

‘Tunnelling’ molecules, ion carriers

45
Q

________ are being designed which will self-assemble to form nanotubes in the cell membranes of bacteria.

A

Cyclic peptides

46
Q

How can carbohydrates as drug targets be used to fight against cancers?

A

antibodies in the treatment of cancer by producing antibodies which will target carbohydrate-containing antigens that are overexpressed on the surface of cancer cells

can be used by themselves to mark cancer cells for destruction or as a means of delivering anticancer drugs to cancer cells

47
Q

the interior of cyclodextrins is relatively _______ and can accommodate drug-sized molecules

A

hydrophobic

have been extensively studied as a means of drug delivery for hydrophobic drugs

48
Q

sugammadex, a cyclodextrin that acts as a _______ for rocuronium, a neuromuscular blocker used in modern anaesthesia

A

‘scavenger’

CH 456 Medicinal Chemistry (7 decks)

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