In vitro and in vivo effect of parathyroid hormone analogue (1-14) containing -amino-iso-butyric acid residue (Aib)1,3.

Yonsei Medical Journal
Yumie RheeSung-Kil Lim

Abstract

Firstly, parathyroid hormone (1-14) [PTH (1-14)] analogue containing various -amino-iso-butyric acid residue (Aib) was synthesized by exchanging the 1st and 3rd Ala residues of alpha carbon of PTH (1-14). This analogue revealed to have the quite tight and stable -helical structure using the nuclear magnetic resonance (NMR) analysis. The biological activities of these analogues were examined using a cAMP- generating assay in LLC-PK1 cell lines stably transfected with the wild- type human PTH1 receptor. Only the PTH analogue substituted with methyl moiety without acetylation showed significant cAMP generating action with 15.0 +/- 3.414 of EC50. Then, we used an ovariectomized rat model system to compare the in vivo effects of parathyroid hormone analogue with that of PTH (1-84). Daily subcutaneous administration of the unacetylated Aib1,3PTH (1-14) for 5 weeks in 30 nM/kg subcutaneously with positive control group receiving PTH (1-84) with 8 nM/ kg were performed. However, there was no significant change in spinal or femoral bone mineral density assessed by dual x-ray absorptiometry (DXA) in the Aib1,3PTH (1-14) group where definite increase of these parameters shown in the PTH (1-84) group (p < 0.001). Assessment of bone strengt...Continue Reading

References

Dec 16, 1983·Biochemical and Biophysical Research Communications·M RanceK Wüthrich
Mar 1, 1997·Journal of Bone and Mineral Research : the Official Journal of the American Society for Bone and Mineral Research·R Armamento-VillarealR Civitelli
Oct 3, 1998·Acta Crystallographica. Section D, Biological Crystallography·A T BrüngerG L Warren
Jan 10, 2001·Journal of Bone and Mineral Research : the Official Journal of the American Society for Bone and Mineral Research·D B BurrJ M Hock
Sep 8, 2001·Journal of Bone and Mineral Research : the Official Journal of the American Society for Bone and Mineral Research·J M AlexanderM Rosenblatt
Jul 1, 2004·Yonsei Medical Journal·Eun Jin LeeSung Kil Lim

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Citations

Mar 22, 2013·The Journal of Pharmacology and Experimental Therapeutics·Meghan E CuppWilliam J Thomsen

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Methods Mentioned

BETA
X-ray
acetylation
NMR

Software Mentioned

SPSS
NMR
sparky
CNS
XWIN

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