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Novel side-chain glucosylated and adamantylated [Asp2/Glu2]enkephalin analogues: synthesis and in vitro growth inhibition of human tumor cells


Horvat, Štefica; Kralj, Marijeta; Perc, Milica; Jerić, Ivanka; Varga-Defterdarović, Lidija; Jakas, Andreja; Roščić, Maja; Šuman, Lidija; Gredičak, Matija
Novel side-chain glucosylated and adamantylated [Asp2/Glu2]enkephalin analogues: synthesis and in vitro growth inhibition of human tumor cells // Chemical Biology and Drug Design, 73 (2009), 2; 253-257 doi:10.1111/j.1747-0285.2008.00763.x (međunarodna recenzija, članak, znanstveni)


Naslov
Novel side-chain glucosylated and adamantylated [Asp2/Glu2]enkephalin analogues: synthesis and in vitro growth inhibition of human tumor cells

Autori
Horvat, Štefica ; Kralj, Marijeta ; Perc, Milica ; Jerić, Ivanka ; Varga-Defterdarović, Lidija ; Jakas, Andreja ; Roščić, Maja ; Šuman, Lidija ; Gredičak, Matija

Izvornik
Chemical Biology and Drug Design (1747-0277) 73 (2009), 2; 253-257

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Leu-enkephalin; Met-enkephalin; Opioid peptides; In vitro antiproliferative activity; Peptide synthesis; Analogues

Sažetak
A series of new backbone-modified Leu- and Met-enkephalin analogues (13-20 a and b) were synthesized. Backbone manipulations involved the replacement of the Gly2 residue in Tyr-Gly-Gly-Phe-Leu/Met with side-chain glucosylated or adamantylated D/L-aspartic or -glutamic acids. The in vitro antiproliferative activity of these compounds was evaluated for several cell lines and the results were compared with the effect of Met-enkephalin, the native opioid growth factor (OGF). The tested compounds modestly inhibited the growth of the tumor cells (20 – 50% inhibition at millimolar concentrations). Among the tested compounds, Tyr-D-Glu(AdNH)-Gly-Phe-Met (20b) showed significant antiproliferative activity, somewhat more pronounced on MCF-7 (breast carcinoma) and MOLT-4 (lymphoblastic leukemia) cells.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti



POVEZANOST RADA


Projekt / tema
098-0982464-2514 - Uloga različitih mehanizama odgovora stanica na terapiju oštećenjem DNA (Marijeta Kralj, )
098-0982933-2936 - Kemijske preobrazbe prirodnih spojeva (Lidija Varga-Defterdarović, )

Ustanove
Institut "Ruđer Bošković", Zagreb

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


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