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A Semi-Quantitative Drug Affinity Responsive Target Stability DARTS assay for studying Rapamycin/mTOR interaction

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D-DARTS: an alternative method for NaV1.5 affinity molecules identification based on dual-drug affinity responsive

Zirui Lü¹, Xiandong Dai¹, Huixia Li¹

¹State Key Laboratory of Chemistry for NBC Hazards Protection, Beijing 102205, China.

Bioorganic & Medicinal Chemistry

|October 14, 2025

Summary

Dual-DARTS (D-DARTS) is a novel method for identifying protein binders by assessing dual stability against chemical and enzymatic degradation. This technique successfully identified ligands for the NaV1.5 channel, including the bullet ant peptide poneratoxin.

Keywords:

D-DARTS NaV1.5 channel Proteinase K VDAC1, target identification dual-drug affinity responsive target stability

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NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode

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Published on: June 4, 2021

Area of Science:

Biochemistry
Molecular Biology
Pharmacology

Background:

Drug affinity responsive target stability (DARTS) is a label-free method for detecting target engagement.
DARTS application to multi-transmembrane channel proteins is limited due to their instability and protease resistance.

Purpose of the Study:

To develop a novel strategy, Dual-DARTS (D-DARTS), for evaluating target protein stability against chemical denaturation and enzymatic degradation.
To identify affinity ligands for the NaV1.5 channel and assess the general utility of D-DARTS for multi-transmembrane proteins.

Main Methods:

Developed Dual-DARTS (D-DARTS) using controlled proteolysis in an SDS-containing denaturing buffer.
Applied D-DARTS to identify NaV1.5 channel binders and the mitochondrial protein VDAC1.
Validated findings using electrophysiological assays and molecular docking.

Main Results:

Successfully identified inhibitors and agonists for the NaV1.5 channel using D-DARTS.
Discovered poneratoxin as a high-affinity NaV1.5 binder, with binding site predictions.
Demonstrated D-DARTS applicability to VDAC1, confirming its broad utility.

Conclusions:

D-DARTS enables target engagement assessment for challenging multi-transmembrane proteins.
This method offers a simple, cost-effective alternative to electrophysiology for screening channel protein binders.
D-DARTS is a promising strategy for target identification and active molecule screening across various transmembrane proteins.