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Can I read Synthesis and in Vitro Evaluation of a Library of Modified Endomorphin 1 Peptides on EtoBox?
Synthesis and in Vitro Evaluation of a Library of Modified Endomorphin 1 Peptides by Yasuko Koda; Mark Del Borgo; Susanne T. Wessling; Lawrence H. Lazarus; Yoshio Okada; Istvan Toth; Joanne T. Blanchfield is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Synthesis and in Vitro Evaluation of a Library of Modified Endomorphin 1 Peptides about?
Endomorphin 1 (Endo-1 = Tyr-Pro-Trp-Phe-NH 2 ), an endogenous opioid with high affinity and selectivity for l-opioid receptors, mediates acute and neuropathic pain in rodents. To overcome metabolic instability and poor membrane permeability, the N-and C-termini of Endo-1 were modified by lipoamino acids (Laa) and/or sugars, and 2 0 ,6 0 -dimethyltyrosine (Dmt) replacement of Tyr. Analogues were assessed for l-opioid receptor affinity, inhibition of cAMP accumulation, enzymatic stability, and permeability across Caco-2 cell monolayers. C-Terminus modification decreased receptor affinity, while N-terminus C8-Laa improved stability and permeability with slight change in receptor affinity. Dmt provided a promising lead compound: [C8Laa-Dmt[1]]-Endo-1 is nine times more stable (t 1/2 = 43.5 min), >8-fold more permeable in Caco-2 cell monolayers, and exhibits 140-fold greater l-opioid receptor affinity (K il = 0.08 nM).
Who reads Synthesis and in Vitro Evaluation of a Library of Modified Endomorphin 1 Peptides?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Yasuko Koda; Mark Del Borgo; Susanne T. Wessling; Lawrence H. Lazarus; Yoshio Okada; Istvan Toth; Joanne T. Blanchfield
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2008
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)