Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea.

@article{Yoganathan2004InhibitionOT,
  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.},
  author={K. Yoganathan and C. Rossant and R. Glover and Shugeng Cao and J. Vittal and S. Ng and Y. Huang and A. D. Buss and M. Butler},
  journal={Journal of natural products},
  year={2004},
  volume={67 10},
  pages={
          1681-4
        }
}
An extract from the fungus Emericella aurantiobrunnea was found to compete with macrophage inflammatory protein (MIP)-1alpha 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 microM, 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… Expand
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