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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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beta-Endorphin: synthesis and analgesic activity of several analogs modified in positions 2 and 5.

The solid-phase syntheses of [Sar2]-, [Ala2]-, [D-Leu2]-, [D-Lys2]-beta-endorphins and [Pro5]-, [Leu5]-, [D-Leu5]-, [D-Ala2, D-Leu5]-beta-endorphins are described. The synthetic peptides were purified by chromatography on carboxymethylcellulose and partition chromatography on Sephadex G-50. They were characterized by partition chromatography on agarose, thin-layer chromatography, paper electrophoresis, and amino acid analyses of acid and enzymic hydrolysates. Bioassay of the synthetic analogs for analgesic activity by the tail-flick method showed the D-Leu2 analog to be 48% as potent as betah-endorphin while the Ala2, D-Lys2, Leu5, and [D-Ala2, D-Leu5] analogs were 8 to 17% as active. The Sar2, D-Leu5, and Pro5 analogs were less than 1% as potent.[1]

References

  1. beta-Endorphin: synthesis and analgesic activity of several analogs modified in positions 2 and 5. Yamashiro, D., Li, C.H., Tseng, L.F., Loh, H.H. Int. J. Pept. Protein Res. (1978) [Pubmed]
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