A distinctive approach
Activen’s miniproteins™ have the potential to take active ingredients to the next level and offer a unique value proposition.
With their short amino acid chain (for proteins), and their 3D structure, miniproteins exhibit relatively good skin penetration abilities. Strikingly, some miniproteins actually show better skin penetration features than linear peptides that could be find among active ingredients; this can be attributed to their intrinsic physico-chemical properties (hydrodynamic radius, exposed surface…).
A SUSTAINABLE APPROACH
MiniproteinsTM are not extracted from living organisms, thus protecting potentially rare species; no genetically modified organism is used. The manufacturing method Activen use for its miniproteins (namely solid-phase peptide synthesis) is not yet green chemistry, but it is done in Switzerland, in a controlled and safe manner. Plus, miniproteins are highly active, so the quantity needed to meet the market demand is very low, a few hundred grams per year - the overall ecological imprinting of chemically synthetizing so tiny amounts of material is probably much lower than the mere shipment of tons of natural extracts around the world. And finally, although miniproteins are chemically synthesized, they are still natural products that end in the environment as simple amino acids – which are as safe as water for humans and ecosystems.
Our MiniproteinsTM are designed to bind specific receptors that are expressed by target cell population. Thanks to their relatively large interaction surface, they activate or inhibit the aimed receptor with high efficacy.
EXCELLENT TOXICOLOGY PROFILE
Thanks to their unique interaction surface structure, miniproteins have little to no off-target toxicity. In addition, as chains of amino acids, miniproteins are generally broken down over time to yield individual natural amino acids that are completely non-toxic to the human body.
NEW WAY TO EXPLORE
Our discovery approach is unbiased versus conventional methodologies. Activen uses the new generation of sequencing: RNA sequencing (RNA-Seq). The analysis of gene expression in its entirety gives us priceless information on gene regulation and cell interaction.
Activen search for novel active ingredients begins by the selection of a relevant signaling pathway, and associated cellular receptor, that we aim to impact. Then, Activen relies on high throughput techniques to screen our proprietary miniprotein librairies and identify binders of the target receptor (for example EGFR). Typically, Activen has built a bank of bacteriophages expressing each miniprotein at their surface and is now able to use the phage display technique to identify potential binders. After binding characterization, Activen is committed to dig deeper its understanding of the miniprotein mechanism of action: for that, we compare the transcriptomes of cells exposed to the candidate miniprotein to the one of cells exposed to endogenous ligand (for example EGF). New Generation Sequencing allows Activen to analyze the impact of the miniprotein on the cell in a non-biased and exhaustive way and generates priceless data for the downstream clinical testing.
Cosmetics industry has heavily relied on natural compounds that are extracted from the environment. Thanks to immense efforts carried out to isolate and characterize these extracts, scientists have identified almost 200.000 different compounds, leaving less and less room for breakthrough discoveries. Plus, focusing on small (generally <500 Dalton) molecules intrinsically limit the diversity of the chemical space. On the contrary, miniproteins are bigger (> 500 Dalton) and composed of amino acids; the number of possible chains of 20 amino acids is already above a mind-boggling 1026! In addition, miniproteins have been mostly overlooked in research, and today we have only explored a meager 0.1% of its whole universe that continues to grow with the sequencing of new species.