Abstract
The synthetic peptide octarphin (TPLVTLFK, fragment 12–19 of β-endorphin), a selective agonist of nonopioid β-endorphin receptor, was prepared with specific activity 28 Ci/mmol. The binding of [3H]octarphin to T and B lymphocytes isolated from the blood of donors was studied. It was found that [3H]octarphin binds both to T and B cells with high affinity: K d = 3.0 ± 0.2 and 3.2 ± 0.3 nM, respectively. The specific binding of [3H]octarphin to T and B lymphocytes was competitively inhibited by unlabeled β-endorphin (K i = 1.9 ± 0.2 and 2.2 ± 0.3 nM, respectively) and was not inhibited by unlabeled naloxone, [Met5]enkephalin, [Leu5]enkephalin, α-endorphin, and γ-endorphin. Thus, T and B lymphocytes of human blood possess a nonopioid β-endorphin receptor whose binding is provided by the fragment 12–19 (the octarphin sequence).
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Abbreviations
- Con A:
-
concanavalin A
- HSCIE:
-
high-temperature solid-state catalytic isotope exchange
- [IC]50 :
-
concentration of inhibitor that causes 50% inhibition
- K d :
-
equilibrium dissociation constant
- K i :
-
equilibrium inhibition constant
- SEM:
-
the variation coefficient of the standard error of estimated mean
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Published in Russian in Biokhimiya, 2013, Vol. 78, No. 3, pp. 407–412.
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Nekrasova, Y.N., Zolotarev, Y.A. & Navolotskaya, E.V. Interaction of synthetic peptide octarphin with human blood lymphocytes. Biochemistry Moscow 78, 309–313 (2013). https://doi.org/10.1134/S0006297913030140
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DOI: https://doi.org/10.1134/S0006297913030140