Synthesis and biological evaluation of a polyglutamic acid-dopamine conjugate: a new antiangiogenic agent

Fante, C., Eldar-Boock, A., Satchi-Fainaro, R., Osborn, H. M. I. ORCID: https://orcid.org/0000-0002-0683-0457 and Greco, F. (2011) Synthesis and biological evaluation of a polyglutamic acid-dopamine conjugate: a new antiangiogenic agent. Journal of Medicinal Chemistry, 54 (14). pp. 5255-5259. ISSN 0022-2623 doi: 10.1021/jm200382r

Abstract/Summary

Dopamine has previously been shown to inhibit angiogenesis in vitro and in vivo, but its clinical applications in this context are severely limited by its short half-life. Here we report the synthesis of a polyglutamic acid-dopamine conjugate and show that conjugation significantly extends (from 1 to 24 h) dopamine’s antiangiogenic activity in vitro and in vivo. These findings form the basis for the development of a new class of agents for the treatment of angiogenesis-dependent diseases.