Biologically active monoiodinated alpha-MSH derivatives for receptor binding studies using human melanoma cells

Journal Article · Tue Jan 01 00:00:00 EST 1991 · Journal of Receptor Research; (United States)

DOI:https://doi.org/10.3109/10799899109066410· OSTI ID:5031600

Eberle, A N; Verin, V J; Solca, F; Siegrist, W; Kueenlin, C B; Bagutti, C; Stutz, S; Girard, J ^[1]

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1. Department of Research (ZLF), University Hospital, Basel (Switzerland)

Three different monoiodinated radioligands of alpha-MSH (alpha-melanocyte-stimulating hormone) were compared in a binding assay with human D10 melanoma cells: (Tyr(125I)2)-alpha-MSH, (Tyr(125I)2,NIe4)-alpha-MSH, and (Tyr(125I)2,NIe4,D-Phe7)-alpha-MSH. They were prepared either by the classical chloramine T method or by the Enzymobead method. A simple and rapid purification scheme was developed consisting of a primary separation on reversed-phase C18 silica cartridges immediately after the iodination, followed by HPLC purification before each binding experiment. Biological testing of the three radioligands showed that they all retained high melanotropic activity in the B16 melanin assay and the Anolis melanophore assay. However, in human D10 melanoma cells, (Tyr(125I)2,NIe4)-alpha-MSH led to a high degree of non-specific binding to the cells which could not be displaced by excess alpha-MSH and only partially by (NIe4)-alpha-MSH. The (Tyr(125I)2,NIe4,D-Phe7)-alpha-MSH tracer gave similar results but with a much lower proportion of non-specific binding. On the other hand, (Tyr(125I)2)-alpha-MSH proved to be an excellent radioligand whose non-specific binding to the D10 cells was not higher than 20% of the total binding.

• OSTI ID: 5031600
• Journal Information: Journal of Receptor Research; (United States), Vol. 11:1-4; ISSN 0197-5110
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
HORMONES
RECEPTORS
BIOCHEMICAL REACTION KINETICS
CHLORAMINES
FRACTIONATION
IODINE 125
LIGANDS
LIQUID COLUMN CHROMATOGRAPHY
MAN
MELANOMAS
PITUITARY GLAND
RADIOASSAY
TRACER TECHNIQUES
TUMOR CELLS
AMINES
ANIMAL CELLS
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
CHROMATOGRAPHY
DAYS LIVING RADIOISOTOPES
DISEASES
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
GLANDS
INTERMEDIATE MASS NUCLEI
INTERNAL CONVERSION RADIOISOTOPES
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
MAMMALS
MEMBRANE PROTEINS
NEOPLASMS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC CHLORINE COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANS
PRIMATES
PROTEINS
RADIOISOTOPES
REACTION KINETICS
SEPARATION PROCESSES
VERTEBRATES
550201* - Biochemistry- Tracer Techniques