d) We discussed a research paper in class that optimized potency and specificity

Question

d) We discussed a research paper in class that optimized potency and specificity of several inhibitors targeting K-RAS, our fa K-RAS mutant G12C to increase specificity of the inhibitor they he deelPe bs How did the researchers take advantage of the lung cancer r covalent e) The figure below shows one of their typical western blot assays for "labeling", o cation, of K-RAS G12C. Recall that labeling leads to a shift of the band for K-RAS protein up in the gel. DMSO lacks any inhibitors, and a-tubulin serves as a control for ARS853 4 AM a 1 2 4 6 8 1 2 4 6 8(h), 10 HM KRAS (T202/Y204) Which inhibitor (ARS853 or 4_AM) has the highest krae? Explain your logic with 1 sentence. [4 pts] ) AM he cause Can What consequence does K-RAS labeling have on downstream phosphorylation of ERK1 and ERK2 the MAP kinases? Based on the figure above, which inhibitor is better? (4 pts

Explanation / Answer

The rate constant, Kinact is directly proportional to the strength of the bond formation, which implies that higher the Kinact, higher is the binding.

The picture of the gel clearly shows higher binding of the inhibitor 4_AM as evidenced by an upward shift in the band size within 1hours of the incubation and the binding persisted throughout the study period i.e., up to 8 hours against the inhibitor, ARS853, in which the binding is observed only after 4 hours that too partial. Therefore, it may be concluded that the inhibitor, 4_AM has higher Kinact than ARS853.

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