Premium
Divergent Melanophore‐Dispersing and Tyrosinase‐Stimulating Activity of Synthetic Leucine 9 ‐α‐melanotropin
Author(s) -
Eberle Alex,
Schwyzer Robert
Publication year - 1979
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.19790620740
Subject(s) - chemistry , melanophore , melanocyte stimulating hormone , stimulation , tyrosinase , receptor , frog skin , in vitro , homogeneous , leucine , stereochemistry , potency , biochemistry , endocrinology , amino acid , chromatophore , organic chemistry , enzyme , medicine , physics , thermodynamics , fishery , biology , sodium
Leucine 9 ‐α‐melanotropin ([Leu 9 ]α‐MSH) was synthesized in homogeneous solution by a fragment condensation approach, and it was assayed for its melanophore‐dispersing and its tyrosinase‐stimulating activity with a reflectometric in vitro frog skin assay and with cultured mouse melanoma cells, respectively. In both assay systems, parallel log dose‐response curves were obtained for ([Leu 9 )]α‐MSH and α‐MSH; however, in the frog skin assay the activity of the title compound was 1 middot; 10 10 Units/mmol, i.e. 25% of the activity of α‐MSH, whereas its tyrosinasestimulating potency was only 1% compared to α‐MSH (EC 50 = 2.5 · 10 −7 M ). This indicates a major difference in the recognition/stimulation process of the receptors of the two cell types.