首页   按字顺浏览 期刊浏览 卷期浏览 Intemalisation of Isotope-Coupled Somatostatin Analogues
Intemalisation of Isotope-Coupled Somatostatin Analogues

 

作者: L.J. Hofland,   P.M. van Koetsveld,   M. Waaijers,   S.W.J. Lamberts,  

 

期刊: Digestion  (Karger Available online 1996)
卷期: Volume 57, issue 1  

页码: 2-6

 

ISSN:0012-2823

 

年代: 1996

 

DOI:10.1159/000201382

 

出版商: S. Karger AG

 

关键词: sst;Scintigraphy;Octreotide;Tumour;Pituitary;Mouse;Human

 

数据来源: Karger

 

摘要:

With the technique of in vivo somatostatin (SRIF) receptor (sst) scintigraphy a variety of human sst-positive tumours can be visualised 24-48 h after intravenous injection of the radiolabelled (SRIF) analogue [111In-DTPA-D-Phe1ctreotide. This rather long residence time of radioactivity on tumours suggests that the radioligand is internalised by the tumour cells; literature data for normal pituitary and pancreatic islet cells agree with this. Internalised SRIF has been found to be associated with cytoplasmic organelles, especially the Golgi apparatus, lysosomes and secretory granules. We have found that mouse AtT20 and primary cultures of human growth-hormone-secreting pituitary adenoma cells internalised a high amount of radio-iodinated [Tyr3]octreotide. Since octreotide binds with high affinity to the sst5 and ssts subtypes and because both sst subtypes are expressed in these cells, one or both subtypes may be involved in this process. We also found that unlabelled octreotide, SRIF-14 or SRIF-28 can increase the intemalisation of the radioligand. These observations, together with other studies on the manipulation of sst expression, may help to optimise the uptake of radioligand in in vivo sst scintigraphy in humans and improve the potential effect of radiotherapy with radiolabelled (subtype-specific) SRIF analogues.

 

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