Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 beta-Endorphin: synthesis of analogs modified at the carboxyl terminus with increased activites.

Literature DB >> 226965

beta-Endorphin: synthesis of analogs modified at the carboxyl terminus with increased activites.

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

Abstract

Three analogs of human beta-endorphin (beta h-EP) have been synthesized: [Gly31]beta h-EP, [Gly31]beta h-endorphinamide, and [Gly31]beta h-endorphinylglycine. All are more active than beta 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 beta 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.

Entities: Chemical Disease Gene Species

Mesh：

Substances：

Year: 1979 PMID： 226965 PMCID： PMC383807 DOI： 10.1073/pnas.76.7.3276

Source DB: PubMed Journal: Proc Natl Acad Sci U S A ISSN： 0027-8424 Impact factor: 11.205

19 in total

1. beta-endorphin: synthesis and morphine-like activity of analogs with D-amino acid residues in positions 1, 2, 4, and 5.

Authors: D Yamashiro; L F Tseng; B A Doneen; H H Loh; C H Li
Journal: Int J Pept Protein Res Date: 1977

beta-Endorphin: synthesis of analogs modified at the carboxyl terminus with increased activites.

1. beta-endorphin: synthesis and morphine-like activity of analogs with D-amino acid residues in positions 1, 2, 4, and 5.

2. A synthetic enkephalin analogue with prolonged parenteral and oral analgesic activity.

3. beta-Endorphin: structure-activity relationships in the guinea pig ileum and opiate receptor binding assays.

4. beta-Endorphin: a pituitary peptide with potent morphine-like activity.

5. The purification of peptides by partition chromatography based on a hydrophobicity scale.

6. beta-Endorphin: complete primary structure is required for full analgesic activity.

7. [D-Thr2, Thz5]- and [D-Met2 ,Thz5]-enkephalinamides: potent analgesics by intravenous injection.

8. Preparation and properties of tritiated human beta-endorphin with high specific radioactivity.

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

10. The synthesis and opiate activity of human beta-endorphin analogs. Substituted at residue positions 27 and 31.

1. beta-Endorphin: characterization of binding sites specific for the human hormone in human glioblastoma SF126 cells.

2. C-terminal amidation of PACAP-38 and PACAP-27 is dispensable for biological activity at the PAC1 receptor.