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Drug Design > Quiz 3 flash cards > Flashcards

Quiz 3 flash cards

1
Q

What ways can a drug be transported into a cell?

A

Diffusion
Facillitated diffusion
Active transport

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2
Q

What charactoristics make dissolution the late limiting step of drug metabolism?

A 
Solubility of drug
Size of particle
Surface area
Crystalline and salt drug formation
Rate of disintegration
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3
Q

What are the charactoristic of pH-partiition for drug absorption?

A

Biological membranes act like lipid barriers
Un-ionized forms of drug is better absorbed
Most are absorbed by passive diffusion
rate and amount of drug absorption are related to oil-water partition coefficent
Weak acids and neutral drugs not usually absorbed in the stomach
Basic drugs are normally absorbed in the stomach

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4
Q

What are the hallmarks of cancer?

A 
Sustained proliferative signaling
Evading growth suppressors
Activating invasion/metasis
Enable replicative immortality
Induce angiogenesis
Resisting cell death
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5
Q

What is the molecular target for Mustard agents?

A

DNA

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6
Q

What is the MOA of Mustard agents?

A

Alkylate and crosslink the DNA

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7
Q

What type of cancer are Mustard agents used for?

A

Multiple

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8
Q

What is the molecular target of Mytomycin C?

A

DNA

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9
Q

What is the MOA for Mytomycin C?

A

Alkylate and cross link DNA

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10
Q

What type of cancer does Mytomycin C treat?

A

Stomach and Intestinal Cancer

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11
Q

What is the molecular target for Platinum Drugs

A

DNA

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12
Q

What is the MOA of Platinum drugs?

A

Alkylate and cross link DNA

Can alkylate the protein in the protein-DNA crosslink

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13
Q

What is the molecular target for Anthracyclins?

A

Topo 2a

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14
Q

What is the MOA for Anthracyclin?

A

Stabilizes transient cleavage complex with DNA

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15
Q

What cancers are treated with Anthracyclin?

A

Breast, endometiral, acute leukemia, cervical, stomach, lymphoma

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16
Q

What is the molecular target for Etoposide?

A

Topo 2A

17
Q

What is the mechanism of action for Etoposide?

A

Stabilizes transient cleavage complex with DNA

18
Q

What cancers are treated with Etoposide?

A

Lung and Testicular

19
Q

What are the molecular target of ICRF-193?

A

Topo 2A and chelate iron preventing ROS production

20
Q

What is the MOA of ICRF-193?

A

Stabilized closed clamp complex with DNA

21
Q

What is the molecular target of Imatinib?

A

BRC-ABL

22
Q

What is the MOA of Imatinib?

A

Competitive BCR-ABL inhibitor- makes ABL inactive

23
Q

What cancers can be treated by Imatinib?

A

Mainly leukemia ALL,CEL,CML

24
Q

What is the molecular target for Dasatinib?

A

BCR-ABL

25
Q

What is MOA of Dasatinib?

A

Binds to active ABL

26
Q

What cancers can be treated by Dasatinib?

A

Imatinib resistant Leukemia and Philadelpha chromosome positive

27
Q

What is the clinical significance of statins?

A

Lower LDL and sometime increase HDL cholesterol

28
Q

How do statins work?

A

They mimic the transition state Mevaidyl-CoA

29
Q

Which statins are natural products?

A

Compacitin and Simvastatin

30
Q

Which statins are SYnthetic products?

A

Fluvastatin, atorvastatin, rosuvastatin, cerivastatin

31
Q

What charactorist to all statins have in common?

A

They have HMG-like functional groups

Drug Design (2 decks)

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