Design, synthesis and pharmacological evaluation of novel endomorphin analogues with multiple structural modifications

Mallareddy, Jayapal Reddy; Borics, Attila; Keresztes, Attila; Tóth, Géza

doi:10.1016/s1734-1140(11)70450-9

Cited by 1 publication

(2 citation statements)

References 121 publications

(39 reference statements)

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“…Likewise FPhe shows significant impact on endomorphin (EM) peptides studies. EM have the longest half-lives compared to all endogenous opioid ligands, but in order to consider them as a potential therapeutic drugs it is important to increase their ability to enter the central nervous system and their resistance to enzymatic degradation [18,19]. Incorporation of 4FPhe and other un-natural amino acids into EM increased its affinities for µ-opioid receptor in receptor binding assay [18].…”

Section: Fluoro-phenylalanine (Fphe)mentioning

confidence: 99%

“…Depending on the protein and its applications, one of these methods has been used for incorporation of amino acid analogues to study structural and functional properties of protein. For instance, residue specific labeling was used to examine the conformational changes of proteins and for detection of protein-ligand interaction by 19 FNMR spectroscopy [8]. Incorporation of fluorinated aromatic amino acids into proteins increased its shelf life compared to the wild type which is one of the great benefits, especially in therapeutic proteins and vaccine studies [9].…”

Section: Introductionmentioning

confidence: 99%

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Fluorinated Aromatic Amino Acids and its Therapeutic Applications

Andra¹

2015

Biochem Anal Biochem

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Fluorinated amino acids play a significant role in peptides and protein studies. These are known to enhance the stability of proteins folds and serve as valuable analogues for investigation of enzyme kinetics, protein-protein and ligand-receptor interactions. Due to the unique properties of fluorine, fluorinated amino acids are used as a powerful tool to study biological process and to develop anti-cancer reagents and vaccines. Previous reviews cover synthesis and applications of fluorinated amino acids in broad range; this short review provides the importance of fluorinated aromatic amino acids and the impact of fluorine substitution in its aromatic rings that facilitate the study of structure, function and stability of therapeutic proteins and peptides which have great potential for future therapeutic applications.

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Section: Fluoro-phenylalanine (Fphe)mentioning

confidence: 99%