Venom peptide discovery platform for fibroblast and macrophage targeted drug delivery

Overview

This solution offers a discovery platform for identifying venom-derived peptides capable of selectively targeting activated fibroblasts and macrophages, two cell types central to fibrotic and inflammatory diseases. The platform draws on an extensive venom library spanning approximately 170 species and a curated peptide library of around 20,000 fractions. By combining proprietary fractionation methods with cell-based internalisation assays, the platform enables the systematic identification of peptides that bind specific cell surface proteins and lipids, opening new avenues for targeted therapeutics. Active peptides are sequenced and assessed for stability, with structure-activity relationship (SAR) studies performed to tune drug-like properties such as plasma half-life and cell-type selectivity.

Technical specifications

Key features:

• Targeted-Venom Discovery Array (T-VDA) platform producing 384-well screening plates with a historical 1-7% hit rate across drug discovery targets
• Proprietary assay for detecting unlabelled, cell-penetrant, and cell-type specific venom peptides
• Two-dimensional HPLC fractionation of venoms with standardised quality checks and replica plating
• Subtractive HPLC analysis of cell lysates to identify selective peptides, with intact mass and double-digest peptide mapping mass spectrometry for hit identification
• SAR workflow to determine active sites, minimum effective sequences, and tune plasma half-life
• In-vitro stability profiling including synthetic gastric and intestinal fluids and plasma half-life assessment
• Selectivity screening against non-target cell types such as CaCo2, smooth muscle, and non-activated fibroblasts

Technology readiness level

The platform has been validated over 13 years of screening campaigns across multiple drug discovery targets, with only one target (an orphan GPCR) failing to yield hits. The team has published collaborative work demonstrating discovery of novel scorpion venom ligands targeting Kv1.3, a channel predominantly expressed on macrophages. Current readiness supports near-term execution of a defined multi-phase discovery project, including array design, venom collection, fractionation, screening, selectivity validation, and SAR optimisation, with an estimated total timeline of approximately 25-28 weeks to deliver characterised, selectivity-confirmed peptide hits ready for further drug development.