β-Endorphin: Synthesis of analogs modified at the carboxyl terminus with increased activities

C. H. Li; D. Yamashiro; L. F. Tseng; W. C. Chang; P. Ferrara

doi:10.1073/pnas.76.7.3276

β-Endorphin: Synthesis of analogs modified at the carboxyl terminus with increased activities

C. H. Li, D. Yamashiro, L. F. Tseng, W. C. Chang, P. Ferrara

Research output: Contribution to journal › Article › peer-review

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Abstract

Three analogs of human β-endorphin (β(h)-EP) have been synthesized: [Gly ³¹]β(h)-EP, [Gly ³¹]β(h)-endorphinamide, and [Gly ³¹]β(h)-endorphinylglycine. All are more active than β(h)-EP in both the guinea pig ileum bioassay and the opiate receptor binding assay. The last two analogs are about twice as active as β(h)-EP in an assay for analgesia. Modification at position 31 and extension at the COOH terminus may afford a route toward analogs with even greater biological activity.

Original language	English
Pages (from-to)	3276-3278
Number of pages	3
Journal	Proceedings of the National Academy of Sciences of the United States of America
Volume	76
Issue number	7
DOIs	https://doi.org/10.1073/pnas.76.7.3276
Publication status	Published - Dec 1 1979
Externally published	Yes

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title = "β-Endorphin: Synthesis of analogs modified at the carboxyl terminus with increased activities",

abstract = "Three analogs of human β-endorphin (β(h)-EP) have been synthesized: [Gly 31]β(h)-EP, [Gly 31]β(h)-endorphinamide, and [Gly 31]β(h)-endorphinylglycine. All are more active than β(h)-EP in both the guinea pig ileum bioassay and the opiate receptor binding assay. The last two analogs are about twice as active as β(h)-EP in an assay for analgesia. Modification at position 31 and extension at the COOH terminus may afford a route toward analogs with even greater biological activity.",

author = "Li, {C. H.} and D. Yamashiro and Tseng, {L. F.} and Chang, {W. C.} and P. Ferrara",

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doi = "10.1073/pnas.76.7.3276",

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T1 - β-Endorphin

T2 - Synthesis of analogs modified at the carboxyl terminus with increased activities

AU - Li, C. H.

AU - Yamashiro, D.

AU - Tseng, L. F.

AU - Chang, W. C.

AU - Ferrara, P.

PY - 1979/12/1

Y1 - 1979/12/1

N2 - Three analogs of human β-endorphin (β(h)-EP) have been synthesized: [Gly 31]β(h)-EP, [Gly 31]β(h)-endorphinamide, and [Gly 31]β(h)-endorphinylglycine. All are more active than β(h)-EP in both the guinea pig ileum bioassay and the opiate receptor binding assay. The last two analogs are about twice as active as β(h)-EP in an assay for analgesia. Modification at position 31 and extension at the COOH terminus may afford a route toward analogs with even greater biological activity.

AB - Three analogs of human β-endorphin (β(h)-EP) have been synthesized: [Gly 31]β(h)-EP, [Gly 31]β(h)-endorphinamide, and [Gly 31]β(h)-endorphinylglycine. All are more active than β(h)-EP in both the guinea pig ileum bioassay and the opiate receptor binding assay. The last two analogs are about twice as active as β(h)-EP in an assay for analgesia. Modification at position 31 and extension at the COOH terminus may afford a route toward analogs with even greater biological activity.

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β-Endorphin: Synthesis of analogs modified at the carboxyl terminus with increased activities

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