Targeting TMPRSS2-ERG Fusion-Driven Prostate Cancer using Novel HBS-α-Helicomimics
Start here
Stapled alpha-helicomimics designed to mimic the ERG recognition helix block ERG-DNA binding and suppress TMPRSS2-ERG fusion-driven prostate cancer, which occurs in roughly 50% of prostate cancers. The lead compound, stabilized by an N-terminal hydrogen-bond-surrogate macrocycle plus D363E and S366E mutations and dual NLS-TAT tags, inhibited ERG binding to ETS motifs, cut proliferation, migration and invasion in ERG-positive PCa cells, and suppressed tumor growth with reduced Ki-67 in a murine xenograft model without overt toxicity.
Excerpted from biorxiv.org
Coverage timeline
Follow the coverage to see the different angles.
- biorxiv.orgPickTargeting TMPRSS2-ERG Fusion-Driven Prostate Cancer using Novel HBS-α-Helicomimics
Stapled alpha-helicomimics designed to mimic the ERG recognition helix block ERG-DNA binding and suppress TMPRSS2-ERG fusion-driven prostate cancer, which occurs in roughly 50% of prostate cancers. The lead compound, stabilized by an N-terminal hydrogen-bond-surrogate macrocycle plus D363E and S366E mutations and dual NLS-TAT tags, inhibited ERG binding to ETS motifs, cut proliferation, migration and invasion in ERG-positive PCa cells, and suppressed tumor growth with reduced Ki-67 in a murine xenograft model without overt toxicity.
Heat trend for this story
Heat now 7·Peak in the comparable set 8 (Oct 16 17:00)·Change over 24h in the comparable set –
The trend compares only the participants observed in full throughout, so its set can be smaller than the heat figure itself. Move the pointer or click the chart for an hour's heat; the left and right arrow keys work too.