Drug Targets: Nucleic Acids

Question 1

Drugs acting on DNA

Answer 1

1
2
3
4
5
6
7....

Question 2

Drugs acting on DNA
INTERCALATING AGENTS
Mechanism of action
What do they contain?

Answer 2

Planar aromatic or heteroaromatic ring systems

Question 3

Drugs acting on DNA
INTERCALATING AGENTS
Structure

Answer 3

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Question 4

Drugs acting on DNA
INTERCALATING AGENTS
What does proflavine target?

Answer 4

…

Question 5

Drugs acting on DNA
INTERCALATING AGENTS
Proflavine helical structure

Answer 5

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Question 6

Drugs acting on DNA
INTERCALATING AGENTS
Anticancer drug example
Doxorubicin 
Alternative name

Answer 6

Adriamycin

Question 7

Drugs acting on DNA
INTERCALATING AGENTS
Anticancer drug example
Doxorubicin (Adriamycin)
Structure

Answer 7

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Question 8

Drugs acting on DNA
INTERCALATING AGENTS
Anticancer drug example
Doxorubicin
Where is the extra binding?

Answer 8

…

Question 9

Drugs acting on DNA
INTERCALATING AGENTS
Anticancer drug example
Bleomycins
Structure

Answer 9

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Question 10

Drugs acting on DNA
INTERCALATING AGENTS
Anticancer drug example
Bleomycins
What do they intercalate with?

Answer 10

….

Question 11

Drugs acting on DNA
INTERCALATING AGENTS
Anticancer drug example
Etoposide
Structure

Answer 11

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Question 12

Drugs acting on DNA
INTERCALATING AGENTS
Anticancer drug example
Teniposide structure

Answer 12

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Question 13

Drugs acting on DNA
INTERCALATING AGENTS
Anticancer drug example
Camptothecin structure

Answer 13

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Question 14

Drugs acting on DNA
Non-INTERCALATING AGENTS
Topoisomerase poisons
Nalidixic acid structure

Answer 14

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Question 15

Drugs acting on DNA
NON-INTERCALATING AGENTS
How are fluoroquinolones bound to DNA and enzymes?

Answer 15

Hydrogen and ….

Question 16

Drugs acting on DNA

Alkylating agents contain what groups?

Answer 16

Highly electroPHILIC groups

Question 17

Drugs acting on DNA
ALKYLATING AGENTS
What do they prevent?

Answer 17

Replication and transcription

Question 18

Drugs acting on DNA
ALKYLATING AGENTS
Toxic side effect example

Answer 18

Alkylating of proteins

Question 19

Drugs acting on DNA
ALKYLATING AGENTS
Crosslinking
Intrastrand

Answer 19

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Question 20

Drugs acting on DNA
ALKYLATING AGENTS
Interstrand

Answer 20

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Question 21

Drugs acting on DNA
ALKYLATING AGENTS example
Chlormethine alternative name

Answer 21

Nitrogen mustard

Question 22

Drugs acting on DNA
ALKYLATING AGENTS
Chlormethine structure

Answer 22

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Question 23

Drugs acting on DNA
ALKYLATING AGENTS
Chlormethine mechanism of action

Answer 23

….

Question 24

Drugs acting on DNA
ALKYLATING AGENTS
Nitrosoureas 2 examples

Answer 24

1 loumustine

2

Question 25

Drugs acting on DNA ALKYLATING AGENTS Busulfan structure

Answer 25

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Question 26

Drugs acting on DNA ALKYLATING AGENTS Cisplatin mechanism of action structure

Answer 26

...

Question 27

Drugs acting on DNA ALKYLATING AGENTS Decarbazine How is it activated?

Answer 27

The prodrug is activated by demethylation in liver

Question 28

Drugs acting on DNA ALKYLATING AGENTS Dacarbazine What does it form when decomposed?

Answer 28

A methyldiazonium ion

Question 29

Drugs acting on DNA ALKYLATING AGENTS Dacarbazine What does it alkylate?

Answer 29

Guanine groups

Question 30

Drugs acting on DNA ALKYLATING AGENTS Dacarbazine mechanism of action

Answer 30

See slide

Question 31

Drugs acting on DNA | Chain terminator example

Answer 31

Aciclovar

Question 32

Drugs acting on DNA | Chain terminators

Answer 32

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