KRAS Cycle
Name the two states of KRAS
What is GDP-KRAS (off state) and GTP-KRAS (on state)?
What is Switch I/II?
What is the name of the molecule primarily used to show that KRAS is druggable
What is BI-2852?
True or False:
GTP-KRAS main function is to inhibit cell growth within the cell
FALSE
Name two types of methodology approaches used within this study
Answers Vary
Within Figure Two,
What is the major difference between the protein structure A & B?
Answers Vary:
-size of the pocket region
-Molecule shape
What is the ROLE of GTP-KRAS within step 2 of the KRAS cycle?
GTP-KRAS speeds up the Gaunine exchange factor (SOS) by binding to allosteric pocket
or
Allosteric Activator
Why was KRAS considered Undruggable?
What is lack of druggable pockets within the KRAS molecular structure
Within Panel F of Figure 5 What effect did concentration have on BI-2852 inhibition?
Higher concentration of BI-2852 led to greater inhibition of GDP-KRAS conversion to GTP-KRAS
What is the name of the protein in step 4 of the KRAS cycle which Deactivates GTP-KRAS?
GAP ( GTPase activating protein)
This technique allows you to map 3d images of protein structures and small molecules
What is X-Ray crystallography?
True or False:
Figure 6 showcases Panels A-G
False:
Figure 6 showcases panels A-F
What are the overall products of the Deactivation of GTP-KRAS to GDP-KRAS in step 4
What is Phosphorous, Water and GDP-KRAS?
This Fragment-Based screening through Saturation Transfer Difference NMR and Microscale Thermophoresis yielded how many fragments?
Answers will be considered correct within the ~500 range
What is 1,800 Fragments?
Within Panel C of figure 3, what experiment was conducted to yield the enthalpy of reaction for compound 18?
What is Isothermal Titration Calorimetry (ITC)?