GMS6504 Exam 2 Questions And Answers
In terms of Lipinski's rules, which of the following functional groups serves as a hydrogen bond
donor? ANS -NH2
Will a hydrophobic molecule have a high or low logP? ANS high
Which is the best explanation as to why CNS drugs tend to have smaller polar surface areas than
drugs that target things outside of the CNS? ANS It helps the drug cross the blood brain barrier
Which functional group is most often utilized when making pro-drugs? ANS Esters
Which of the following protein domains would you expect to find in an "easily druggable" target but
NOT in an "undruggable" target? ANS ATP-binding domain
Would using a drug against cells in which it causes synthetic lethality tend to increase or decrease its
therapeutic index? ANS Increase
Inhibition of which enzyme is expected to cause synthetic lethality in cells harboring a BRCA2
mutation? ANS PARP
Kinases place which functional group on proteins? ANS Phosphates
Which of the following could be the sequence of the catalytic site of a kinase? ANS GIGSAG
What amino acid most commonly serves as the gatekeeper residue in a kinase? ANS Methionine
Type 1 kinase inhibitors specifically target ______. ANS active kinases
, Which would be expected to have the greatest selectivity towards the target enzyme? ANS
Allosteric kinase inhibitor
Which resistance mechanism would reduce the apparent affinity of Herceptin to the HER2 receptor?
ANS Epitope masking
Where would you go to download the crystal structure of a protein you want to use for molecular
docking? ANS PDB
What is the purpose of the "spheres" that we made in the docking process? ANS they tell the
computer where we want molecules to dock to.
What is the purpose of the "grid" that we made in the docking process? ANS It defines the
electrostatic environment to use for energy calculations.
Would you expect to achieve more accurate docking using rigid ligands or flexible ligands? ANS
Flexible
How is a grid score calculated? ANS It is the sum of the electrostatic score and the Van Der
Waals score.
Which grid score would predict the best binding to a protein? ANS -50
Which type of immune cells are most directly responsible for the killing of cancer cells during
immunotherapy? ANS Cytotoxic T Lymphocytes
Which type of antibody has a greater proportion of human sequence? ANS Humanized
Rituximab targets _________. ANS CD20
Gemtuzumab targets _________. ANS CD33
In terms of Lipinski's rules, which of the following functional groups serves as a hydrogen bond
donor? ANS -NH2
Will a hydrophobic molecule have a high or low logP? ANS high
Which is the best explanation as to why CNS drugs tend to have smaller polar surface areas than
drugs that target things outside of the CNS? ANS It helps the drug cross the blood brain barrier
Which functional group is most often utilized when making pro-drugs? ANS Esters
Which of the following protein domains would you expect to find in an "easily druggable" target but
NOT in an "undruggable" target? ANS ATP-binding domain
Would using a drug against cells in which it causes synthetic lethality tend to increase or decrease its
therapeutic index? ANS Increase
Inhibition of which enzyme is expected to cause synthetic lethality in cells harboring a BRCA2
mutation? ANS PARP
Kinases place which functional group on proteins? ANS Phosphates
Which of the following could be the sequence of the catalytic site of a kinase? ANS GIGSAG
What amino acid most commonly serves as the gatekeeper residue in a kinase? ANS Methionine
Type 1 kinase inhibitors specifically target ______. ANS active kinases
, Which would be expected to have the greatest selectivity towards the target enzyme? ANS
Allosteric kinase inhibitor
Which resistance mechanism would reduce the apparent affinity of Herceptin to the HER2 receptor?
ANS Epitope masking
Where would you go to download the crystal structure of a protein you want to use for molecular
docking? ANS PDB
What is the purpose of the "spheres" that we made in the docking process? ANS they tell the
computer where we want molecules to dock to.
What is the purpose of the "grid" that we made in the docking process? ANS It defines the
electrostatic environment to use for energy calculations.
Would you expect to achieve more accurate docking using rigid ligands or flexible ligands? ANS
Flexible
How is a grid score calculated? ANS It is the sum of the electrostatic score and the Van Der
Waals score.
Which grid score would predict the best binding to a protein? ANS -50
Which type of immune cells are most directly responsible for the killing of cancer cells during
immunotherapy? ANS Cytotoxic T Lymphocytes
Which type of antibody has a greater proportion of human sequence? ANS Humanized
Rituximab targets _________. ANS CD20
Gemtuzumab targets _________. ANS CD33
