TY - JOUR T1 - Design and Evaluation of Novel Radiolabelled VIP Derivatives for Tumour Targeting JF - Anticancer Research JO - Anticancer Res SP - 1537 LP - 1546 VL - 33 IS - 4 AU - CHRISTINE RANGGER AU - ANNA HELBOK AU - MELTEM OCAK AU - THORSTEN RADOLF AU - FRITZ ANDREAE AU - IRENE J. VIRGOLINI AU - ELISABETH VON GUGGENBERG AU - CLEMENS DECRISTOFORO Y1 - 2013/04/01 UR - http://ar.iiarjournals.org/content/33/4/1537.abstract N2 - Background: Vasoactive intestinal peptide (VIP) receptors are overexpressed in a broad variety of tumours. For the detection of these tumours, novel chemically modified and shortened VIP derivatives were designed. Materials and Methods: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-derivatised VIP analogues were radiolabelled with 111In and in vitro and in vivo behaviour was evaluated using stability and internalisation assays, as well as an initial biodistribution study. Results: Radiolabelling of the VIP analogues resulted in high radiochemical yields, without need for further purification steps. Stability of the VIP derivatives was variable and cell uptake studies in VIP receptor-positive cell lines revealed that only a limited number of derivatives were internalised. In the tumour mouse model, no specific tumour targeting was shown. Conclusion: Since the tested VIP derivatives exhibited impaired in vitro and in vivo characteristics alternative modifications to increase their stability while retaining receptor affinity should be considered to enable the use of synthetic VIP analogues for tumour targeting. ER -