TY - JOUR
T1 - Thyrotropin releasing hormone analogs
T2 - A building block approach to the construction of tetracyclic peptidomimetics
AU - Chu, Wenhua
AU - Perlman, Jeffrey H.
AU - Gershengorn, Marvin C.
AU - Moeller, Kevin D.
N1 - Funding Information:
observation that suggests that it is possible to develop antagonists for TRH-R. Efforts to develop TRH-R antagonists and to explore methods of restoring full agonist behaviour to a fully restricted TRH analog are underway. Acknowledgements: We thank the National Institutes of HeaLth (RO1 GM5324001A1) for their generous financial support. In addition, we thank the Washington University High Resolution NMR Facility, partially supported by NIH grants RR02004, RR05018, and RR07155, and the Washington University Mass Spectrometry Resource Center, partially supported by NIH RR00954, for their assistance.
PY - 1998/11
Y1 - 1998/11
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0032212497&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(98)00567-8
DO - 10.1016/S0960-894X(98)00567-8
M3 - Article
C2 - 9873682
AN - SCOPUS:0032212497
SN - 0960-894X
VL - 8
SP - 3093
EP - 3096
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 21
ER -