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Beilstein J. Org. Chem. 2018, 14, 2495–2509, doi:10.3762/bjoc.14.226
Graphical Abstract
Figure 1: Schematic structure of Dau-conjugated GnRH-III or its derivatives containing 4Lys with acetyl or bu...
Figure 2: Cellular uptake of Dau–GnRH-III conjugates and free daunorubicin (Dau) by A2058 cells. Cellular upt...
Figure 3: Short-term growth inhibitory effects of the conjugates and daunorubicin (Dau) on A2058 cells. The m...
Figure 4: Effects of conjugates and daunorubicin (Dau) on cell cycle progression of A2058 melanoma cells. The...
Figure 5: Effects of the conjugates and daunorubicin (Dau) on melanoma cell adhesion. The Delta CI (Delta Cel...
Figure 6: Chemotactic effects of Dau–GnRH-III conjugates on A2058 cell line. The ‘Chemotaxis index’ (Chtx. in...
Figure 7: Effects of GnRH-III(Dau=Aoa) (a–c), [4Lys(Ac)]-GnRH-III(Dau=Aoa) (d–f) and [4Lys(Bu)]-GnRH-III(Dau=...
Figure 8: Schematic representation of the proposed mechanisms of the effects of GnRH-III conjugates containin...
Beilstein J. Org. Chem. 2018, 14, 756–771, doi:10.3762/bjoc.14.64
Scheme 1: Syntheses of GnRH-III–[(4Lys(Bu)/4Ser, 6Aaa, 8Lys(Dau=Aoa)] bioconjugates. a) (1) 2% hydrazine in D...
Figure 1: Far-UV ECD spectra of GnRH-III and its drug conjugates in water (GnRH-III solid, K1 dash, K2 dot, 1...
Figure 2: Degradation of the GnRH-III bioconjugates by rat liver lysosomal homogenate. A) Cleavage sites prod...
Figure 3: Cytostatic effect of the GnRH-III bioconjugates at different concentrations on A) HT-29 and B) MCF-...
Figure 4: Cellular uptake of the GnRH-III bioconjugates at different concentrations on A) HT-29 and B) MCF-7 ...
Figure 5: Cellular uptake of bioconjugate K2 (40 µM) visualized by confocal laser scanning microscopy (CLSM) ...
Figure 6: Competitive inhibition of the GnRH-R on MCF-7 cells. Cellular uptake of the GnRH-III bioconjugate K2...