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|Title:||Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea|
|Source:||Yoganathan, K., Rossant, C., Glover, R.P., Cao, S., Vittal, J.J., Ng, S., Huang, Y., Buss, A.D., Butler, M.S. (2004-10). Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea. Journal of Natural Products 67 (10) : 1681-1684. ScholarBank@NUS Repository. https://doi.org/10.1021/np049844c|
|Abstract:||An extract from the fungus Emericella aurantiobrunnea was found to compete with macrophage inflammatory protein (MIP)-1α for binding to human CCR5 in a scintillation proximity assay (SPA). Bioassay-guided fractionation led to the isolation of variecolin (1) and variecolol (2), which had IC50 values of 9 and 32 μM, respectively. An X-ray crystal structure of variecolin (1) was obtained for the first time. Also isolated were four new inactive analogues, emericolin A (3), B (4), C (5), and D (6), and the relative stereochemistry of these compounds was determined by NMR methods using ROESY spectra and 1H/1H coupling constants.|
|Source Title:||Journal of Natural Products|
|Appears in Collections:||Staff Publications|
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