Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.
Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.
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促甲状腺激素释放激素类似物:构建四环肽模拟物的构建方法。
DOI:
10.1016/s0960-894x(98)00567-8
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发表时间:
1998
期刊:
影响因子:
--
通讯作者:
Moeller,KD
中科院分区:
文献类型:
--
作者:
Chu,W;Perlman,JH;Gershengorn,MC;Moeller,KD
A building block based approach was used to synthesize a pair of tetracyclic peptidomimetics that constrain all but one of the rotational degrees of freedom of the hypothalamic tripeptide hormone thyroliberin. One of the analogs bound to the thyroliberin endocrine receptor (TRH-R) with an affinity greater than that of an analog without constraints. The tetracyclic peptidomimetics were found to be partial agonists for the TRH-R receptor.