Stability against enzymatic hydrolysis of endomorphin-1 analogues containing β-proline
G Cardillo, L Gentilucci, A Tolomelli… - Organic & …, 2003 - pubs.rsc.org
The enantiomer of endomorphin-1 (Tyr-Pro-Trp-PheNH2) and the analogues containing (S)-
or (R)-β-proline have been synthesized, and their affinities towards μ-opioid receptors have …
or (R)-β-proline have been synthesized, and their affinities towards μ-opioid receptors have …
Endomorphin-1 analogues containing β-proline are μ-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance
G Cardillo, L Gentilucci, AR Qasem… - Journal of medicinal …, 2002 - ACS Publications
In this paper we describe the synthesis and affinity toward the μ-opioid receptor of some
tetrapeptides obtained from endomorphin-1, H-Tyr-Pro-Trp-Phe-NH2 (1), by substituting …
tetrapeptides obtained from endomorphin-1, H-Tyr-Pro-Trp-Phe-NH2 (1), by substituting …
Synthesis and binding activity of endomorphin-1 analogues containing β-amino acids
G Cardillo, L Gentilucci, P Melchiorre… - Bioorganic & medicinal …, 2000 - Elsevier
Endomorphin-1 (Tyr-Pro-Trp-PheNH2) has been proposed as the most potent endogenous
ligand of the μ-opioid receptors. In this paper, we describe the synthesis of some …
ligand of the μ-opioid receptors. In this paper, we describe the synthesis of some …
Stereochemical requirements for receptor recognition of the μ-opioid peptide endomorphin-1
MG Paterlini, F Avitabile, BG Ostrowski, DM Ferguson… - Biophysical journal, 2000 - cell.com
A series of diastereoisomers of endomorphin-1 (EM1, Tyr 1-Pro 2-Trp 3-Phe 4-NH 2) have
been synthesized and their potency measured using the guinea pig ileum assay.[d-Phe 4] …
been synthesized and their potency measured using the guinea pig ileum assay.[d-Phe 4] …
Biological activity of endomorphin and [Dmt1] endomorphin analogs with six-membered proline surrogates in position 2
R Perlikowska, K Gach, J Fichna, G Toth… - Bioorganic & medicinal …, 2009 - Elsevier
Endogenous μ-opioid receptor (MOR) selective peptides, endomorphin-1 (EM-1) and
endomorphin-2 (EM-2), unlike so called 'typical opioids', are characterized by the presence …
endomorphin-2 (EM-2), unlike so called 'typical opioids', are characterized by the presence …
The structure of an endomorphin analogue incorporating 1-aminocyclohexane-1-carboxlylic acid for proline is similar to the β-turn of Leu-enkephalin
M Doi, A Asano, E Komura, Y Ueda - Biochemical and biophysical research …, 2002 - Elsevier
Endomorphin (EM2, Tyr–Pro–Phe–Phe–NH2) can assume various conformations related to
cis/trans-rotamers of the amide linkage of Tyr–Pro. To control isomerization, restricted or …
cis/trans-rotamers of the amide linkage of Tyr–Pro. To control isomerization, restricted or …
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2
The opioid agonists endomorphins (Tyr–Pro–Trp–Phe–NH2; EM1 and Tyr–Pro–Phe–Phe–
NH2; EM2) and morphiceptin (Tyr–Pro–Phe–Pro–NH2) exhibit an extremely high selectivity …
NH2; EM2) and morphiceptin (Tyr–Pro–Phe–Pro–NH2) exhibit an extremely high selectivity …
cis-4-Amino-l-proline Residue As a Scaffold for the Synthesis of Cyclic and Linear Endomorphin-2 Analogues: Part 2
A Mollica, F Pinnen, A Stefanucci… - Journal of Medicinal …, 2012 - ACS Publications
Recently, we reported synthesis and activity of a constrained cyclic analogue of
endomorphin-2 (EM-2: Tyr-Pro-Phe-Phe-NH2) and related linear models containing the cis …
endomorphin-2 (EM-2: Tyr-Pro-Phe-Phe-NH2) and related linear models containing the cis …
Synthesis of stereoisomeric analogues of endomorphin-2, H-Tyr-Pro-Phe-Phe-NH2, and examination of their opioid receptor binding activities and solution …
Y Okada, A Fukumizu, M Takahashi, Y Shimizu… - Biochemical and …, 2000 - Elsevier
All sixteen stereoisomeric analogues of endomorphin-2 (H-Tyr-Pro-Phe-Phe-NH2) were
synthesized by Fmoc-strategy using solid phase methods. Although synthetic endomorphin …
synthesized by Fmoc-strategy using solid phase methods. Although synthetic endomorphin …
Preferred conformation of endomorphin-1 in aqueous and membrane-mimetic environments
S Fiori, C Renner, J Cramer, S Pegoraro… - Journal of molecular …, 1999 - Elsevier
The newly discovered endomorphin-1 (Tyr-Pro-Trp-Phe-NH2) and endomorphin-2 (Tyr-Pro-
Phe-Phe-NH2) are potent opioid peptides with the highest affinity and selectivity for the μ …
Phe-Phe-NH2) are potent opioid peptides with the highest affinity and selectivity for the μ …
相关搜索
- β proline enzymatic hydrolysis
- proline surrogates endomorphin analogs
- stereoisomeric analogues endomorphin 2
- β proline receptor agonists
- biological activity endomorphin analogs
- preferred conformation endomorphin 1
- β proline hydrolysis resistance
- morphiceptin analogues endomorphin 2
- proline surrogates endomorphin 2
- proline surrogates morphiceptin analogues