Structure-Guided WRN Helicase Inhibitors for MSI-H Tumors

Q15, a novel spirocyclic WRN inhibitor, demonstrated complete tumor regression at 40 mg/kg in preclinical models. This dataset, shared by Qibang Sui on figshare in June 2026, contains structural data for rationally designed Werner syndrome RecQ helicase inhibitors. It supports research into synthetic lethal therapies for microsatellite instability-high cancers.

Use Cases

• Comparing in vitro activity and cellular selectivity of novel WRN inhibitors based on structural design.
• Analyzing oral pharmacokinetic properties and antitumor efficacy of candidate compounds like Q15 and HRO761.
• Studying the relationship between solvent-exposed region targeting and inhibitor potency for structure-based drug design.
• Evaluating preliminary safety profiles of spirocyclic compounds and benzo-fused heterocyclic analogs.

Strengths

• Dataset includes specific, potent candidate compounds like Q15 and HRO761 with reported in vivo results.
• Structural design is guided by the WRN-HRO761 complex, providing a rational basis for the data.
• Data is shared under a CC-BY-NC-4.0 license, allowing for non-commercial reuse with attribution.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• Data may reflect the specific experimental and temporal bias inherent to the single research project.

Provenance

Source

figshare

Collection Method

Likely contains results from rational drug design and in vitro/in vivo testing.

Freshness

Last updated 2026-06-03 18:37:19; freshness should be verified.