Abstract:
:Novel Leu-enkephalin (Leu-Enk) (1) analogs possessing various types of alpha-substituted serine instead of its glycine residue in the position 2 were synthesized via an efficient O,N-migration method. The binding characteristics of the synthetic analogs using Chinese hamster ovary (CHO) cells expressed cloned rat mu-, delta-, and kappa-receptors revealed that [(1R,2S)-Ahh2]Enk (7) was the most potent agonist of delta-opioid receptors among all the synthetic analogs tested, and was 10 times more potent than the native Leu-Enk.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Horikawa M,Shigeri Y,Yumoto N,Yoshikawa S,Nakajima T,Ohfune Ydoi
10.1016/s0960-894x(98)00349-7subject
Has Abstractpub_date
1998-08-04 00:00:00pages
2027-32issue
15eissn
0960-894Xissn
1464-3405pii
S0960894X98003497journal_volume
8pub_type
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