10 Questions
Which protein is the first element in the MAPK cascade and the first oncogenic protein discovered in human tumors?
Ras
What is the common mutation found in K-Ras that leads to its activation?
SNP in the codon for glycine in position 12
Which Ras isoform was identified in human neuroblastoma?
NRAS
What effect does the SNP in K-Ras have on the protein?
It becomes insensitive to the activity of GAP helper protein
Which type of tumors are highly associated with activating mutations in RAS?
Pancreatic and lung cancer
What was the initial approach to inhibiting Ras?
Inhibiting Ras by preventing its membrane association
Why were statins tested in relation to Ras inhibition?
They inhibit the HMG-CoA reductase, involved in the synthesis of prenyl substrates
Why did GTP analogues fail to show expected efficacy as inhibitors of Ras?
They didn't act as competitive inhibitors of GTP required for RAS activation
What was the main reason for considering Ras an undruggable target for a long time?
The protein has a relative smooth/flat surface, lacking a well-defined binding pocket
Why did inhibitors targeting enzymes involved in post-translational lipid modification fail?
The enzymes were not specific to Ras prenylation process
Explore the strategies for blocking oncogenic signals and targeting signaling proteins of the MAPK cascade in tumors. Learn about activating mutations in proteins of the MAPK cascade and their implications for tumor development.
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