Gamma scintigraphy of111In-labelled branched chain polypeptides (BCP) with a poly(L-lysine) backbone in mice with mammary carcinoma: Effect of charge on biodistribution and tumour imaging potential

Malcolm V. Pimm, Alan C. Perkins, Sandra J. Gribben, G. Mező, D. Gaál, F. Hudecz

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Radiolabelled synthetic branched chain polypeptides (BCP) represent a new and novel range of materials with potential as radiopharmaceuticals. Preliminary imaging studies have been under-taken with111In-labelled BCP in mice with subcutaneously transplanted mammary carcinoma. Four polypeptides each with a poly(L-lysine) backbone and side chains of DL-alanine residues were studied. These were AK, which is polycationic, EAK which is amphoteric, having additional glutamic acid residues at the end of the side chains, and AcEAK (anionic) and SucEAK (highly polyanionic) where the terminal glutamic acid amino groups were acetylated or succinylated respectively. Radiolabelling was achieved by previous conjugation with DTPA. Serial images up to 48 hours showed marked retention of111In-labelled polycationic AK and polyanionic SucEAK in the liver and spleen, with renal uptake also being visible in the case of AK.111In-labelled EAK and AcEAK showed longer blood survival with some liver uptake, but tumour uptake was also visualized by 24 hours with both of these polypeptides. These studies demonstrate the feasibility of using111In-labelled synthetic branched chain polypeptides as radiopharmaceuticals for gamma scintigraphy and the visualization of tumours by modification of the side chain structure. These materials warrant further study.

Original languageEnglish
Pages (from-to)247-251
Number of pages5
JournalAnnals of Nuclear Medicine
Volume9
Issue number4
DOIs
Publication statusPublished - Dec 1995

Fingerprint

Radionuclide Imaging
Lysine
Breast Neoplasms
Peptides
Radiopharmaceuticals
Neoplasms
Glutamic Acid
Pentetic Acid
Liver
Feasibility Studies
Alanine
Spleen
Kidney

Keywords

  • mammary carcinoma
  • polypeptides
  • radiopharmaceuticals
  • scintigraphy

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

Cite this

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title = "Gamma scintigraphy of111In-labelled branched chain polypeptides (BCP) with a poly(L-lysine) backbone in mice with mammary carcinoma: Effect of charge on biodistribution and tumour imaging potential",
abstract = "Radiolabelled synthetic branched chain polypeptides (BCP) represent a new and novel range of materials with potential as radiopharmaceuticals. Preliminary imaging studies have been under-taken with111In-labelled BCP in mice with subcutaneously transplanted mammary carcinoma. Four polypeptides each with a poly(L-lysine) backbone and side chains of DL-alanine residues were studied. These were AK, which is polycationic, EAK which is amphoteric, having additional glutamic acid residues at the end of the side chains, and AcEAK (anionic) and SucEAK (highly polyanionic) where the terminal glutamic acid amino groups were acetylated or succinylated respectively. Radiolabelling was achieved by previous conjugation with DTPA. Serial images up to 48 hours showed marked retention of111In-labelled polycationic AK and polyanionic SucEAK in the liver and spleen, with renal uptake also being visible in the case of AK.111In-labelled EAK and AcEAK showed longer blood survival with some liver uptake, but tumour uptake was also visualized by 24 hours with both of these polypeptides. These studies demonstrate the feasibility of using111In-labelled synthetic branched chain polypeptides as radiopharmaceuticals for gamma scintigraphy and the visualization of tumours by modification of the side chain structure. These materials warrant further study.",
keywords = "mammary carcinoma, polypeptides, radiopharmaceuticals, scintigraphy",
author = "Pimm, {Malcolm V.} and Perkins, {Alan C.} and Gribben, {Sandra J.} and G. Mező and D. Ga{\'a}l and F. Hudecz",
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T1 - Gamma scintigraphy of111In-labelled branched chain polypeptides (BCP) with a poly(L-lysine) backbone in mice with mammary carcinoma

T2 - Effect of charge on biodistribution and tumour imaging potential

AU - Pimm, Malcolm V.

AU - Perkins, Alan C.

AU - Gribben, Sandra J.

AU - Mező, G.

AU - Gaál, D.

AU - Hudecz, F.

PY - 1995/12

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N2 - Radiolabelled synthetic branched chain polypeptides (BCP) represent a new and novel range of materials with potential as radiopharmaceuticals. Preliminary imaging studies have been under-taken with111In-labelled BCP in mice with subcutaneously transplanted mammary carcinoma. Four polypeptides each with a poly(L-lysine) backbone and side chains of DL-alanine residues were studied. These were AK, which is polycationic, EAK which is amphoteric, having additional glutamic acid residues at the end of the side chains, and AcEAK (anionic) and SucEAK (highly polyanionic) where the terminal glutamic acid amino groups were acetylated or succinylated respectively. Radiolabelling was achieved by previous conjugation with DTPA. Serial images up to 48 hours showed marked retention of111In-labelled polycationic AK and polyanionic SucEAK in the liver and spleen, with renal uptake also being visible in the case of AK.111In-labelled EAK and AcEAK showed longer blood survival with some liver uptake, but tumour uptake was also visualized by 24 hours with both of these polypeptides. These studies demonstrate the feasibility of using111In-labelled synthetic branched chain polypeptides as radiopharmaceuticals for gamma scintigraphy and the visualization of tumours by modification of the side chain structure. These materials warrant further study.

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