Synthesis and biological evaluation of several dephosphonated analogues of CMP-Neu5Ac as inhibitors of GM3-synthase
Articolo
Data di Pubblicazione:
2015
Citazione:
Synthesis and biological evaluation of several dephosphonated analogues of CMP-Neu5Ac as inhibitors of GM3-synthase / P. Rota, F. Cirillo, M. Piccoli, A. Gregorio, G. Tettamanti, P. Allevi, L. Anastasia. - In: CHEMISTRY-A EUROPEAN JOURNAL. - ISSN 0947-6539. - 21:41(2015 Oct 05), pp. 14614-14629. [10.1002/chem.201501770]
Abstract:
Previous studies demonstrated that reducing the GM3 content in myoblasts increased the cell resistance to hypoxic stress, suggesting that a pharmacological inhibition of the GM3 synthesis could be instrumental for the development of new treatments for ischemic diseases. Herein, the synthesis of several dephosphonated CMP-Neu5Ac congeners and their anti-GM3-synthase activity is reported. Biological activity testes revealed that some inhibitors almost completely blocked the GM3-synthase activity in vitro and reduced the GM3 content in living embryonic kidney 293A cells, eventually activating the epidermal growth factor receptor (EGFR) signaling cascade.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
glycosides; inhibitors; sialic acids; sphingolipids
Elenco autori:
P. Rota, F. Cirillo, M. Piccoli, A. Gregorio, G. Tettamanti, P. Allevi, L. Anastasia
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