Sonenberg M, Guller S, Wu K Y, Corin R E, Allen D L
Memorial Sloan-Kettering Cancer Center, New York, NY 10021.
Mol Cell Endocrinol. 1994 Mar;99(2):193-9. doi: 10.1016/0303-7207(94)90008-6.
Chemically synthesized bovine growth hormone (bGH) bGH 96-133 and its human homologue, hGH 95-133, have similar in vitro biological activities. Unlike native GH, bGH 96-133 and hGH 95-133 were completely without adipogenic or anti-insulin activity at doses up to 10 microM. bGH 96-133 had insulin-like activity, with a 100% increase in glucose uptake at 10 microM. bGH was anti-mitogenic and bGH 96-133 and hGH 95-133 were mitogenic (EC50 approximately 180 nM and maximal response at 1-2 microM). Only bGH 96-133 and hGH 95-133 displaced [125I]hGH 95-133 binding from 3T3-F442A fibroblasts with a Kd between 60-120 nM. bGH, hGH, insulin and IGF-I were without effect on [125I]hGH 95-133 binding. bGH 96-133 and hGH 95-133 did not significantly inhibit [125I]hGH or [125I]IGF-I binding. These experiments indicate that GH containing peptides bGH 96-133 and hGH 95-133 have mitogenic and insulin-like activity without the adipogenic, anti-insulin or anti-mitogenic activity of bGH. These peptides have a specific binding site which appears to be distinct from the GH, insulin and IGF-I receptors.
化学合成的牛生长激素(bGH)bGH 96 - 133及其人源同源物hGH 95 - 133具有相似的体外生物学活性。与天然生长激素不同,bGH 96 - 133和hGH 95 - 133在高达10微摩尔的剂量下完全没有成脂或抗胰岛素活性。bGH 96 - 133具有胰岛素样活性,在10微摩尔时葡萄糖摄取增加100%。bGH具有抗有丝分裂作用,而bGH 96 - 133和hGH 95 - 133具有促有丝分裂作用(半数有效浓度约为180纳摩尔,在1 - 2微摩尔时达到最大反应)。只有bGH 96 - 133和hGH 95 - 133能以60 - 120纳摩尔之间的解离常数从3T3 - F442A成纤维细胞上取代[125I]hGH 95 - 133的结合。bGH、hGH、胰岛素和IGF - I对[125I]hGH 95 - 133的结合没有影响。bGH 96 - 133和hGH 95 - 133没有显著抑制[125I]hGH或[125I]IGF - I的结合。这些实验表明,含生长激素的肽bGH 96 - 133和hGH 95 - 133具有促有丝分裂和胰岛素样活性,而没有bGH的成脂、抗胰岛素或抗有丝分裂活性。这些肽具有一个特异性结合位点,该位点似乎与生长激素、胰岛素和IGF - I受体不同。