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ID: ALA1130656

Journal: Bioorg Med Chem Lett

Title: Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.

Authors: Chu W, Perlman JH, Gershengorn MC, Moeller KD.

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.

CiteXplore: 9873682

DOI: 10.1016/s0960-894x(98)00567-8