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Helicases

Helicases are essential enzymes that unwind DNA and RNA duplexes, playing critical roles in processes such as DNA replication, repair, recombination, and transcription. Given their pivotal role in maintaining genomic stability, helicases have emerged as promising therapeutic targets for a range of diseases, including cancer, viral infections, and genetic disorders. Targeting helicases can disrupt these vital processes in pathogens or cancer cells, offering a new approach to treatment. 

Services

Protein Products: High-quality in-house production of helicases.

ICE Bioscience Helicase Panel
TargetCat No.TargetCat No.
WRNS2207F-H01HFDDX11 (ChR1)S2503F-H04G
BLME2202T-H19HDHX36S2503F-H18HA
RECQ1E2204T-H02HDDX41E2412F-H08H
RECQ4E2204T-H01HUDHX39E2412T-H14G
RECQ5E2204T-H04HDDX21E2501T-H18H
HELQS2307F-H01HMFXPDS2501F-H13H
DHX9S2309T-H13HFLGP2 (DHX58)S2412F-H09H
POLQS2201T-H02HDDX3XE2501T-H17H
MDA5 (IFIH1)E2403T-H04GRIG-I (DDX58)E2410T-H26HU
FANCJS2204F-H07FHDDX48 (eIF4A3)E2412F-H15H

Biochemical Assays: ADP-Glo and Fluorescence Intensity (FI) Unwinding assays to assess helicase activity. All targets have been assembled into a standardized ATPase panel for side-by-side comparison of compound selectivity, as shown in the IC₅₀ data figure below.

helicasepanel.jpg

Biophysical Assays: SPR and Spectral Shift(Sps) assays for detailed kinetic studies of helicase interactions. SpS has been performed on a subset of helicases as below. Note: Each Kd value shown in the “Ref. Cpd” row corresponds to a different known binder selected for each individual target. 

SpS Binding Data - Helicase Panel
CompoundKd,nM - Helicase Targets
DHX9RIG-IDDX3XLGP2DHX41DDX21DDX39DDX48XPDWRN
Ref. Cpd (per target)20.1201770017006556000578025200557259

Protein Degradation Assays: Specialized assays for analyzing helicase degradation.

Cell Based Assays: Robust cell-based assays to evaluate the cellular effects of helicase modulation.

CDX and Resistance Models: Development and use of CDX models and resistance models for in vivo studies on helicase-targeting compounds.


Here, we highlight WRN helicase as an example to showcase our capabilities and service offerings.

WRN helicase, a member of the RecQ family, is crucial for DNA replication, repair, recombination, and telomere maintenance. Mutations in WRN lead to Werner syndrome, associated with premature aging and cancer predisposition. Targeting WRN in cancer therapy, particularly in tumors with microsatellite instability (MSI), has shown promising therapeutic potential.


APPLICATION NOTE: Comprehensive WRN Target Capabilities: Proteins, Assays, and In Vivo Resistance Model



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