Synthesis and in vitro bioactivity of human growth hormone-releasing factor analogs substituted with a single D-amino acid.
Synthesis and in vitro bioactivity of human growth hormone-releasing factor analogs substituted with a single D-amino acid.
复制标题
单一 D-氨基酸取代的人生长激素释放因子类似物的合成和体外生物活性。
DOI：
10.1016/0006-291x(87)90400-1
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发表时间：
1987
影响因子：
3.1
通讯作者：
Ling,N
中科院分区：
文献类型：
--
作者：
Sato,K;Hotta,M;Kageyama,J;Chiang,TC;Hu,HY;Dong,MH;Ling,N
Fifty-four analogs of human growth hormone-releasing factor (hGRF) substituted with a single D-amino acid were synthesized by solid phase methodology. Their capacity to release growth hormone was tested on rat anterior pituitary cells in monolayer culture. Among the series of 28 analogs, which had the amino acid at each position of hGRF (1–29)NH2, except glycine at position 15, substituted by the corresponding D-isomer, [D-Ala2]-, [D-Asp3]-, [D-Asn8]-, [D-Tyr10]-, [D-Asp25]-, [D-Met27]-, [D-Ser28]-, and [D-Arg29]hGRF(1–29)NH2were as potent as hGRF(1–29)NH2, while [D-Ile5]-, [D-Phe6]-, [D-Thr9]-, and [D-Val29]hGRF(1–29)NH2showed quite low potencies. Effects of substitution with other D-amino acids in positions 2,3,8,9,10 and 11 were also studied. In most cases, the resulting analogs showed decreased potency, but still retained high intrinsic activity. Only [D-Arg2]hGRF(1–29)NH2showed very low intrinsic activity and some antagonistic property.
