Publications by authors named "Azusa Takeda"
Article Synopsis
- Ras•GTP exists in two forms: an inactive state (state 1) and an active state (state 2), but understanding how it transitions between these states has been difficult due to a lack of structural data on state 1.
- Newly solved crystal structures of wild-type H-Ras show the characteristics of both state 1 and state 2, revealing the state 2 structure may act as a bridge during the transition between the two states.
- Analysis of the structural changes points to significant rearrangements in specific regions of the molecule, suggesting that interactions and movements of certain key residues and water molecules play critical roles in the transition, while biochemical studies indicate that state 1 may function as a stable reservoir in the GDP
Proc Natl Acad Sci U S A
May 2013
Article Synopsis
- * Researchers developed small-molecule inhibitors by screening for compounds that bind to a newly identified pocket in the M-Ras⋅GTP structure, with compounds like Kobe0065 showing promising results by inhibiting H-Ras binding and inducing cancer cell death.
- * The study validates a structure-based approach for drug development, with the Kobe0065 compounds potentially acting as a foundation for creating more effective Ras inhibitors in the future.
