Glyphosine

A glycine-phosphonic acid compound, negatively charged at neutral pH, with immunomodulatory and anti-diabetic properties. Shown to enhance CD4⁺ T cell response to B-chain of insulin (amino acids 9-23) even at 10 nM levels (EC₅₀ = 70.6 nM). Occupies a pocket 9 of I-A^g7 (the class II molecules of the diabetes-prone NOD mice) and alters TCR/peptide-MHC affinity. Stimulates IL-10 secretion in splenocyes in non-obese diabetic (NOD) mice. Daily administration of glyphosine is shown to delay the onset of diabetes in NOD mice. Acts as a competitive inhibitor of phoshoenolpyruvate carboxylase in plants.

A plant growth regulator that also enhances anti-B:9-23 (aa 9 to 23 of insulin B chain) TCR-dependent T cell activation (EC₅₀ = 70.6 nM; EC_max = 500 nM) by modulating murine class II MHC I-A^g7-mediated B:9-23 presentation on APCs, without affecting the activation of anti-chromogranin T cells by chromogranin- I-A^g7 complex. Reported to augment B:9-23 in stimulating IL-10 production from splenocytes of diabetic NOD mice and PBMCs of type 1 diabetic individuals with HLA-DQ8, and effectively prevent the onset of diabetes in NOD mice (80 mg/kg via daily i.p.). Computer structural docking analysis indicates pocket 9 of the I-A^g7 binding groove as the glyphosine targeting site.

Packaged under inert gas

Toxicity: Corrosive (L)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 year at -20°C.

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Michels, A.W., et al. 2011. J. Immunol.187, 5921.
Stadinski, B.D., et al. 2010. Proc. Natl. Acad. Sci. USA107, 10978.
Podesta, F.E., et al. 1987. Plant Cell Physiol.28, 375.

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