DCAI, an Inactive Ras, is bound to a GDP and activated by SOS (son of sevenless, among others), which converts it to the active GTP form. DCAI is a known binder to Ras, which inhibits SOS nucleotide exchange, inhibiting Ras activation.
DCAI, an inactive Ras, is bound to a GDP and activated by SOS (son of sevenless, among others) which converts it to the active GTP form.
Journal of medicinal chemistry, 58(5), 2265-2274 (2015-02-20)
Constitutively active mutant KRas displays a reduced rate of GTP hydrolysis via both intrinsic and GTPase-activating protein-catalyzed mechanisms, resulting in the perpetual activation of Ras pathways. We describe a fragment screening campaign using X-ray crystallography that led to the discovery
Cyclic peptides have great potential as therapeutic agents and research tools. However, their applications against intracellular targets have been limited, because cyclic peptides are generally impermeable to the cell membrane. It was previously shown that fusion of cyclic peptides with
Proceedings of the National Academy of Sciences of the United States of America, 109(14), 5299-5304 (2012-03-21)
The Ras gene is frequently mutated in cancer, and mutant Ras drives tumorigenesis. Although Ras is a central oncogene, small molecules that bind to Ras in a well-defined manner and exert inhibitory effects have not been uncovered to date. Through
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