Publications by authors named "Kailesh Gopalbhai"
Background: The Ras-dependent ERK1/2 MAP kinase signaling pathway plays a central role in cell proliferation control and is frequently activated in human colorectal cancer. Small-molecule inhibitors of MEK1/MEK2 are therefore viewed as attractive drug candidates for the targeted therapy of this malignancy. However, the exact contribution of MEK1 and MEK2 to the pathogenesis of colorectal cancer remains to be established.
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- The study investigates the inactivation mechanisms of MEK1 and MEK2, focusing on the role of phosphorylation, specifically at Ser(212), a conserved site among MAPKK family members.
- Mutating Ser(212) to alanine increased MEK1 activity, while mimicking phosphorylation with aspartate blocked activation in both MEK1 and a constitutively active mutant.
- This phosphorylation at Ser(212) does not affect other activation sites and is also functionally significant in yeast MAPKKs, indicating a conserved negative regulatory mechanism across species.