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. Author manuscript; available in PMC: 2014 Jan 30.

Published in final edited form as: J Mol Biochem. 2012 Jun 16;1(2):86–98.

Table 3.

Receptor binding, activation and cell growth inhibitory properties of methylated triptorelin derivatives.

Cell Type	HEK293_[SCL60]		WPE-1-NB26-3
	Binding IC₅₀, (nM)	Inositol phosphate EC₅₀, (nM)	Binding IC₅₀, (nM)	Inositol phosphate EC₅₀, (nM)
Peptide
D-Trp⁶ GnRH	0.5 ± 0.2	0.14 ± 0.01	0.9 ± 0.3	0.15 ± 0.01
6Me DL-Trp⁶ GnRH	2.3 ± 0.2	1.70 ± 0.4	2.7 ± 0.3	1.05 ± 0.05
5Me DL-Trp⁶ GnRH	97.7 ± 17.0	0.30 ± 0.03	0.7 ± 0.3	0.17 ± 0.01
4Me DL-Trp⁶ GnRH	0.6 ± 0.07	36.6 ± 5.10	138.5 ± 26.0	11.90 ±1.40

Cell Type	HEK293_[SCL60]		WPE-1-NB26-3
	Cell growth inhibition IC₅₀, (nM )		Cell growth inhibition IC₅₀, (nM)
Peptide
D-Trp⁶ GnRH	0.4 ± 0.06		0.17 ± 0.05
4Me DL-Trp⁶ GnRH	4.5 ± 0.6		0.8 ± 0.20
5Me DL-Trp⁶ GnRH	0.5 ± 0.06		0.1 ± 0.01
6Me DL-Trp⁶ GnRH	64.4 ± 4.0		10.1 ± 0.10