Synthesis and biological evaluation of a novel pyroglutamyl-modified TRH analogue
2002; Elsevier BV; Volume: 57; Issue: 6 Linguagem: Inglês
10.1016/s0014-827x(02)01232-6
ISSN1879-0569
AutoresLuigi Brunetti, Ivana Cacciatore, Antonio Di Stefano, Silvestro Duprè, Andrea De Giorgi, Grazia Luisi, Barbara Michelotto, Giustino Orlando, Francesco Pinnen, Lucia Recinella, Piera Sozio, Alessandra Spirito,
Tópico(s)Metabolism, Diabetes, and Cancer
ResumoThe TRH analogue 3, incorporating the (S)-isothiazolidine-1,1-dioxide-3-carboxylic acid (1) moiety in place of the native l-pyroglutamic acid (pGlu) residue, has been synthesized and fully characterized by 1H and 13C NMR. The effects of replacing pGlu with its sulphonamido counterpart on biological activity have been investigated. This peptide, which is significantly stabilized towards hydrolysis by pyroglutamyl peptidase type I (PP I, EC 3.4.19.3), has shown to maintain in vitro prolactin-releasing activity.
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