STM Platform » GPM Technology
Signum Bioscience’s patented compounds and methods revolve around a group of derivatives called prenyl peptides. Signum's GPM Technology Platform constitutes a new class of non-steroidal anti-inflammatories that have broad utility over multiple therapeutic areas by acting as G-protein modulators (GPMs). Initially anti-aging and anti-inflammatory compounds will have immediate impact in skin care products as topical cosmeceuticals (e.g. Arazine™) followed by pharmaceutical inflammatory skin applications. Furthermore, Signum’s goal is the development of anti-inflammatory pharmaceuticals.
GPMs: Mechanism of Action
G-proteins are important signal-transducing molecules in cells. Located near the end of each G-protein is a conserved cysteine residue modified with a prenyl tail (either 15 or 20 carbon side-chain). Analogous to a lock-and-key model, G-proteins insert their prenylated cysteine tail into a prenyl-binding pocket located within specific proteins which facilitates binding and proper signaling. Our GPM compounds are structural mimics of the G-protein tail and thus have the ability to modulate signaling pathways. For example, inflammatory signals activate G-protein-coupled receptors (GPCRs), initiating interactions with G-proteins (via the prenyl-cysteine tail) and downstream signaling, resulting in redness, swelling and irritation (see figure below). GPMs, through their unique mechanism of action successfully modulate inflammatory signaling by binding to the GPCR prenyl-binding pocket, normally used by G-proteins to activate inflammation signaling pathways. Several important signaling proteins, in addition to GPCRs, have recently been identified to possess prenyl-binding pockets or require a prenyl tail for binding representing other potential targets for GPMs (Marshall '93, Scheer and+ Gierschik '95, Dietrich et al. '03, Fogg et al. '01, Akgoz et al '02, Kloog + Cox '04).
Arazine™ and 2nd Generation GPMs Modulate G-Protein Inflammatory Signaling
GPM Compounds: Excellent Safety Profile
Arazine™, our proof-of-concept GPM compound is in essence a naturally occurring amino acid that is readily metabolized once it enters the body. GPM compounds have several properties that make it a safe therapeutic to treat various skin conditions and diseases. Our published results demonstrate that the anti-inflammatory effects of Arazine™ unlike corticosteroids, act only at the site of topical application. This along with several other factors contributes to its excellent safety profile. Studies show Arazine™:
- Ophthalmic study, Arazine™ applied for 4 weeks daily to the eye area. Performed by CRO Study under the
supervision of an Ophthalmologist
- Does not cause corneal corrosion when applied to the eye
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