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WorksheetsDrug Discovery & Development
Total questions: 20
Worksheet time: 8mins
The first step in rational drug design is to ________
identify the target molecule
characterize the shape of the target molecule
find a lead
test the drug molecule
In rational drug design, you cannot design a new drug until _______
you have tested a similar drug on animals
you have tested a similar drug on people
you have characterized the structure of the target molecule
you have received clearance to do so from the FDA
The target molecules can be the following EXCEPT
receptors
enzymes
free oxygen
transcription factors
Which of these statements best describes a lead compound?
A compound that contains the element lead
A molecule that shows some activity or property of interest and serves as the starting point for the development of a drug
A compound from the research laboratory that is chosen to go forward for preclinical and clinical trials
The first compound of a structural class of compounds to reach the market.
Identify the kind of interactions that are typically involved in binding a drug to the binding site of a protein.
predominantly van der Waals interactions
predominantly hydrophobic interactions
predominantly hydrogen bonds
a combination of all of the above
Which of the following statements best describes an induced fit?
the process by which a binding site alters shape such that it is ready to accept a drug
the process by which a drug adopts the correct binding conformation before entering a binding site
the process by which binding of a drug to a binding site alters the shape of the binding site
the process by which a binding site alters the shape of the drug into the binding conformation before binding
Which of the following descriptions most accurately describes binding sites and binding regions?
a binding site is part of a binding region
a binding region is part of a binding site
a binding region is the same as a binding site
a binding region is on a drug whereas a binding site is on a macromolecular target
Which of the following statements best describes pharmacokinetics?
the study of how drugs reach their target in the body and how the levels of a drug in the blood are affected by absorption, distribution, metabolism and excretion
the study of how drugs can be designed using molecular modelling based on drug's pharmacophore.
the study of how a drug interacts with its target binding site at the molecular level to produce a particular pharmacological effect.
the study of which functional groups are important to a drug's activity, and the identification of a pharmacophore.
What is meant by ADME in pharmacokinetics?
Affinity, dosage, marketing, efficacy
Absorption, distribution, metabolism, excretion
Agonism, dependence, mobility, efficiency
Antagonism, deficiency, mean, efflux
Which of the following is one of the rules in Lipinski's rule of five?
A molecular weight equal to 500
No more than five hydrogen bond acceptor groups
No more than 10 hydrogen bond donor groups
A calculated logP value less than +5
Which of the following statements is false regarding the blood brain barrier?
The walls of the capillaries supplying the brain have
tight fitting cells making it difficult for polar drugs
to leave the capillaries
The capillaries in the brain have a fatty coating making it more difficult for drugs to enter the brain
The walls of the capillaries supplying the brain are made up of several layers of cells, which act as a barrier to the release of drugs
Hydrophobic drugs pass through the blood brain barrier more easily than hydrophilic drugs
In identifying a new drug to be taken orally to treat stroke, the perfect molecule will :
be rapidly metabolized
be well absorbed
bind irreversibly to the target protein
reach its site of action after oral administration
In order for a new drug to be considered successful, safety tests must show that the drug meets all of the following criteria EXCEPT?
Must be on the list of FDA approved disease states
Must be absorbed through the bloodstream
Must distribute to the site of action
Demonstrate to be non-toxic
Which of the following is NOT a part of the Investigational New Drug (IND) Review?
Review of preclinical trial results
Identification of side effect profile
Authorization to ship across the state lines
Determination of safety in human use
How many volunteers are in Phase III trials?
100-300
300-500
500-700
300-3000
Which phase of a clinical drug trial is ongoing?
I
II
III
IV
How many volunteers are in Phase II of a clinical trial?
50-75
75-200
100-300
300-500
Which phase of testing is followed with presenting to the FDA for approval?
I
II
III
IV
How long does a drug patent last?
5 years
10 years
20 years
Patent does not expire
Bioassays
are the main methods used in high throughput screening
measure a functional response in a biological tissue
measure the binding affinity of an agonist
require the use of radiolabelled ligands
