Design and Evaluation of Novel Radiolabelled VIP Derivatives for Tumour Targeting

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Figure 1.
In vitro stability testing of the seven ¹¹¹In-labelled VIP derivatives in fresh human serum (1.5 μM peptide/1 ml serum) at selected time points. Values are expressed as the percentage of intact radioligand [Dip: diphenylalanine; DOTA: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; M(O): oxidised form of methionine; Met: methionine; VIP: vasoactive intestinal peptide].
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Figure 2.
Cell uptake studies of different ¹¹¹In-labelled VIP analogues on VPAC₁ and VPAC₂ receptor-positive cells after 30 and 60 min incubation: ¹¹¹In-VIP-DOTA and ¹¹¹In-DOTA-VIP-A7 had a much higher cell uptake in comparison with ¹¹¹In-DOTA-VIP-M(O) and ¹¹¹In-VIP-A6-DOTA, with an impaired receptor affinity. For the blocking studies 10 μM native VIP was used. Values are expressed as means±standard deviation (n=5). [DOTA: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; M(O): oxidised form of methionine; VIP: vasoactive intestinal peptide].