Description
Demethylasterriquinone B1 (DMAQ B1) is a natural insulin mimic that activates insulin receptor tyrosine kinase (IRTK; EC
50 = 6 μM). It less potently activates IGF1R and EGFR (EC
50s = 100 μM for both). DMAQ B1 induces glucose uptake in adipocytes and skeletal muscle cells without activating proliferation. DMAQ B1 binds GAPDH
in vitro.
Biological Activity
Selective insulin receptor (IR) activator/mimetic (EC 50 values are 3-6 μ M for IRTK and 100 μ M for IGF1R and EGFR). Increases IR β subunit tyrosine phosphorylation and downstream activation of PI 3-kinase and Akt, but not ERK. Induces glucose uptake in adipocytes and skeletal muscle in vitro , without enhancing vascular proliferation. Binds GAPDH.
References
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10.1210/rp.56.1.107[2] HENRY J TSAI Shan Y C. A novel hydroxyfuroic acid compound as an insulin receptor activator. Structure and activity relationship of a prenylindole moiety to insulin receptor activation.[J]. Journal of Biomedical Science, 2009: 68. DOI:
10.1186/1423-0127-16-68[3] MICHAEL A. WEBER MDA. A novel insulin mimetic without a proliferative effect on vascular smooth muscle cells[J]. Journal of Vascular Surgery, 2000, 32 6: Pages 1118-1126. DOI:
10.1067/mva.2000.111280[4] NICHOLAS J. G. WEBSTER PROF. Michael C P Prof Kaapjoo Park. Signaling Effects of Demethylasterriquinone B1, a Selective Insulin Receptor Modulator[J]. ChemBioChem, 2003, 4 5: 379-385. DOI:
10.1002/cbic.200200468[5] HYUNSOO KIM. Glyceraldehyde 3-Phosphate Dehydrogenase Is a Cellular Target of the Insulin Mimic Demethylasterriquinone B1[J]. Journal of Medicinal Chemistry, 2007, 50 15: 3423-3426. DOI:
10.1021/jm070437i
