| Tartalom: |
http://real.mtak.hu/41280/ |
| Archívum: |
MTA Könyvtár |
| Gyűjtemény: |
Status = Published
Type = Article
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| Cím: |
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs
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| Létrehozó: |
Adamska, Anna
Kluczyk, Alicja
Cerlesi, Maria Camilla
Calo, Girolamo
Janecka, Anna
Borics, Attila
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| Kiadó: |
Elsevier
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| Dátum: |
2016-02-26
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| Téma: |
QD Chemistry / kémia
QH301 Biology / biolĂłgia
QH3011 Biochemistry / biokémia
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| Tartalmi leírás: |
Morphiceptin (Tyr-Pro-Phe-Pro-NH2), a tetrapeptide amide, is a selective ligand of the l-opioid receptor
(MOR). This study reports the synthesis and biological evaluation of a series of novel morphiceptin analogs
modified in positions 2 or/and 4 by introduction of 4,4-difluoroproline (F2Pro) in L or D configuration.
Depending on the fluorinated amino acid configuration and its position in the sequence, new analogs
behaved as selective full MOR agonists showing high, moderate, or relatively low potency. The most
potent analog, Tyr-F2Pro-Phe-D-F2Pro-NH2, was also able to activate the j-opioid receptor (KOR),
although with low potency. Docking studies and the comparison of results with the high resolution crystallographic
structure of a MOR-agonist complex revealed possible structure–activity relationships of this
compound family.
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| Nyelv: |
angol
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| Típus: |
Article
PeerReviewed
info:eu-repo/semantics/article
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| Formátum: |
text
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| Azonosító: |
Adamska, Anna and Kluczyk, Alicja and Cerlesi, Maria Camilla and Calo, Girolamo and Janecka, Anna and Borics, Attila (2016) Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs. BIOORGANIC & MEDICINAL CHEMISTRY (24). pp. 1582-1588. ISSN 0968-0896
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