Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.
作者信息
Chu W, Perlman J H, Gershengorn M C, Moeller K D
机构信息
Department of Chemistry, Washington University, St. Louis, MO 63130, USA.
出版信息
Bioorg Med Chem Lett. 1998 Nov 3;8(21):3093-6. doi: 10.1016/S0960-894X(98)00567-8.
PMID:9873682
Abstract
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.
摘要
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