Thyrotropin releasing hormone analogs: A building block approach to the construction of tetracyclic peptidomimetics

Wenhua Chu, Jeffrey H. Perlman, Marvin C. Gershengorn, Kevin D. Moeller

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

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 tripepride 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.

Original languageEnglish
Pages (from-to)3093-3096
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number21
DOIs
StatePublished - Nov 1998

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