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.

Target	Cat No.	Target	Cat No.
WRN	S2207F-H01HF	DDX11 (ChR1)	S2503F-H04G
BLM	E2202T-H19H	DHX36	S2503F-H18HA
RECQ1	E2204T-H02H	DDX41	E2412F-H08H
RECQ4	E2204T-H01HU	DHX39	E2412T-H14G
RECQ5	E2204T-H04H	DDX21	E2501T-H18H
HELQ	S2307F-H01HMF	XPD	S2501F-H13H
DHX9	S2309T-H13HF	LGP2 (DHX58)	S2412F-H09H
POLQ	S2201T-H02H	DDX3X	E2501T-H17H
MDA5 (IFIH1)	E2403T-H04G	RIG-I (DDX58)	E2410T-H26HU
FANCJ	S2204F-H07FH	DDX48 (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.

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 K_d value shown in the “Ref. Cpd” row corresponds to a different known binder selected for each individual target. 

Compound	Kd,nM - Helicase Targets
	DHX9	RIG-I	DDX3X	LGP2	DHX41	DDX21	DDX39	DDX48	XPD	WRN
Ref. Cpd (per target)	20.1	201	7700	1700	655	6000	5780	25200	557	259

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