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GMS6504 Exam 2 Questions And Accurate Answers
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GMS6504 Exam 2 Questions And Accurate AnswersWhat 4 factors determine wether a drug is good or bad? - Ans 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) - Ans 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 find out if 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
Adavantages of function groups being labile in biological systems and how it affects
chemical reactivity? - Answer Can be incorporated in the design of a pro-drug approach
because they are known to break down.
DISadavantages of function groups being labile in biological systems and how it affects
chemical reactivity? - Answer Prone to breakdown in vivo.
Name 2 most common chemically reactive functional groups - Answer 1. Epoxides
2. Micheal Acceptor
Give one example of when we would use a pro-drug approach. When 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? Esters
What makes for an easily "druaggable" target? 1. Enzymes: Kinases, Phosphates
2. Cell surface receptors: GPCR's, RTK
What is a hard "undruaggable" target? - Answer 1. Transcription factors
2. Protein-Protein interaction
2 ways to address undruggable targets? - Answer 1. Synthetic Lethality
2. Genome Editing
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