GMS6504 Exam 2 Questions With Correct
Answers
What 4 factors determine whether a drug is good or bad? - answer1. Lipinski's Rule of 5
2. Chemical Reactivity: Good or bad
3. Functional Groups
4. Drug Targets
Name atleast 3 Lipinski's Rules (Basic) - answer1. Molecular mass greater than 500 Da
...
What 4 factors determine whether a drug is good or bad? - answer✔1. Lipinski's Rule of 5
2. Chemical Reactivity: Good or bad
3. Functional Groups
4. Drug Targets
Name atleast 3 Lipinski's Rules (Basic) - answer✔1. Molecular mass greater than 500 Da
2. High Lipophilicity, LogP greater than 5
3. More than 5H bond donors (FH,NH,OH)
4. More than 10H bond acceptors (O,F,N)
When we have high values of Lipinski's Rules of 5. what does this tell us? - answer✔We can
determine whether we have poor absorption and permeation or not
Name atleast 3 Lipinski's Rules (Improved) - answer✔1. Molecular Mass from 160-500 Da
2. Molar Refractivity from 40 to 130
3. Number of atoms from 20 to 70 H bond donors and acceptors.
What is Partition Coefficient? - answer✔Its the ratio of equilibrium concentration of a
dissolved substance in a 2 phase system. Typically, it contains ocantol and water.
Why do we use LogP for partition coefficient? - answer✔We measure with Log10 so that we
have a more managable range for lipophilicity.
How can we determine if the chemical reactivity is good or bad? - answer✔1. Is there
nonselective or selective modification of proteins/nucleic acids?
2. Is it labile in biological systems?
What most common functional groups are found labile in biological systems? - answer✔1.
Esters
2. Disulfide Bonds
Name 2 most common chemically reactive functional groups - answer✔1. Epoxides
2. Micheal Acceptor
Give an example of using a pro-drug approach. - answer✔In a situation where normal
physiology will not allow the drug to pass through the BBB or membrane. Thus, we use a pro-
drug to alter the properties of the molecule to allow passage.
What functional group is the most commonly used for pro-drugs? - answer✔Esters
What makes an easily "druaggable" target? - answer✔1. Enzymes: Kinases, Phosphates
2. Cell surface receptors: GPCR's, RTK
What makes a hard "undruaggable" target? - answer✔1. Transcription factors
2. Protein-Protein interaction
What is synthetic lethality? - answer✔Loss of function of both genes leads to cell death,
whereas a inactivation in only one of these genes does not.
2 advantages of synthetic lethality - answer✔1. It can be used against a majority of cancer
mutations
2. Identify and target the lethal gene partner
What makes kinases good drug targets? - answer✔1. ATP competitive kinase inhibitors are
easy to design
2. They are involved in many pathways
What makes kinases bad drug targets? - answer✔1. If you affect one, you may affect many
2. Inhibition of one kinase may not work since many do the same job
What does the P loop do? - answer✔The P loop is the phosphate binding loop, this helps ATP
binding. Typically, its a glycine motif with amino acid residues.
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