Study summary · research use only
Human growth hormone-releasing factor (hGRF)1-29-albumin bioconjugates activate the GRF receptor on the anterior pituitary in rats: identification of CJC-1295 as a long-lasting GRF analog
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
In this rat study, the authors synthesized three maleimido derivatives of human growth hormone-releasing factor hGRF(1-29) and bioconjugated them to human serum albumin to extend plasma half-life. The conjugates showed enhanced in vitro stability against dipeptidylpeptidase-IV and stimulated GH secretion in cultured rat pituitary cells; given subcutaneously to Sprague Dawley rats, they produced acute plasma GH secretion. The best compound, CJC-1295, showed a 4-fold increase in GH area under the curve over 2 hours versus hGRF(1-29) and was detected in plasma beyond 72 h, with Western blot indicating association with serum albumin. The authors identify CJC-1295 as a stable, active hGRF(1-29) analog with extended half-life.
Abstract
In vivo bioconjugation to the free thiol on Cys34 of serum albumin by a strategically placed reactive group on a bioactive peptide is a useful tool to extend plasma half-life. Three maleimido derivates of human GH-releasing factor (hGRF)(1-29) were synthesized and bioconjugated to human serum albumin ex vivo. All three human serum albumin conjugates showed enhanced in vitro stability against dipeptidylpeptidase-IV and were bioactive in a GH secretion assay in cultured rat anterior pituitary cells. When the maleimido derivatives were individually administered sc to normal male Sprague Dawley rats, an acute secretion of GH was measured in plasma. The best compound, CJC-1295, showed a 4-fold increase in GH area under the curve over a 2-h period compared with hGRF(1-29). CJC-1295, a tetrasubstituted form of hGRF(1-29) with an added N epsilon-3-maleimidopropionamide derivative of lysine at the C terminus, was selected for further pharmacokinetic evaluation, where it was found to be present in plasma beyond 72 h. A Western blot analysis of the plasma of a rat injected with CJC-1295 showed the presence of a CJC-1295 immunoreactive species on the band corresponding to serum albumin, appearing after 15 min and remaining in circulation beyond 24 h. These results led to the identification of CJC-1295 as a stable and active hGRF(1-29) analog with an extended plasma half-life.
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