THYROTROPIN-RELEASING-HORMONE ANALOGS - A BUILDING-BLOCK APPROACH TO THE CONSTRUCTION OF TETRACYCLIC PEPTIDOMIMETICS

Authors
CHU WH PERLMAN JH GERSHENGORN MC MOELLER KD
Citation
Wh. Chu et al., THYROTROPIN-RELEASING-HORMONE ANALOGS - A BUILDING-BLOCK APPROACH TO THE CONSTRUCTION OF TETRACYCLIC PEPTIDOMIMETICS, Bioorganic & medicinal chemistry letters, 8(21), 1998, pp. 3093-3096
Citations number
27
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
21
Year of publication
1998
Pages
3093 - 3096
Database
ISI
SICI code
0960-894X(1998)8:21<3093:TA-ABA>2.0.ZU;2-5
Abstract
A building block based approach was used to synthesize a pair of tetra cyclic peptidomimetics that constrain all but one of the rotational de grees 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. (C) 1998 Elsevier Science Ltd. All rights reserve d.