Constrained Peptidomimetics for TRH: cis-Peptide Bond Analogs
作者： Yunsong Tong , Jacek Olczak , Janusz Zabrocki , Marvin C Gershengorn , Garland R Marshall
DOI: 10.1016/S0040-4020(00)00886-3
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摘要: Abstract Two constrained analogs of the tripeptide hormone thyroliberin (TRH) have been synthesized. In both, HisPro peptide bond has ‘locked’ into a cis -conformation. first analog, constraint used was identical to in an earlier trans -peptide analog that potent agonist for TRH endocrine receptor TRH-R 1 . The second built order take advantage tetrazole ring as constraint. Neither showed or antagonist behavior toward suggesting conformation may not play role affinity
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