[NLE4, D-PHE7]-α-MSH

A superpotent melanotropin that “Irreversibly“ activates melanoma tyros inase

Mac E. Hadley, Zalfa A Abdel Malek, Mohamed M. Marwan, Kristie L. Kreutzfeld, Victor J Hruby

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27 Citations (Scopus)

Abstract

The superpotent and ultranrolongecL melanotropic properties of an -melanotropin analog, [Nle4, D-Phe]-MSH, were investigated in a Cloudman S91 (CCL 53.1) melanoma cell line. [Nle4, D-Phe]-MSH is 100-fold more effective than the native hormone, -melanocyte stimulating hormone (-MSH), in stimulating melanoma cell tyrosinase 1. activity. as determined from their minimum effective doses (10 M and 10 M, respectively). [Nle4, D-Phe7]-MSH also exhibits a more sustained effect than -MSH on tyrosinase after removal of the melanotropins from the incubation medium. When cells were exposed to -MSH (10 M) för 24 h, residual activity after removal of the hormone was minimally signifleant.7 In contrast, under the same experimental conditions [Nle4, D-Phe7]-MSH treatment induced tyrosinase activity 2-3 fold above basal level, and maintained remarkable stimulatory effects up to 72 h following melanotropin removal. When the exposure time to melanotropins was reduced to 4 h, -MSH failed to elicit significant tyrosinase activity, whereas [Nle4, D-Phe7]-MSH stimulated significant tyrosinase activity during the first 24 h subsequent to melanotropin removal. Interestingly, this stimulation by the analog increased at 48 h, reached a maximum at 72 h following removal of the melanotropin analog, and remained significantly stimulated för 6 consecutive days in the absence of the analog.

Original languageEnglish (US)
Pages (from-to)157-170
Number of pages14
JournalEndocrine Research
Volume11
Issue number4 --Mar
DOIs
StatePublished - 1985

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Melanocyte-Stimulating Hormones
Melanoma
Monophenol Monooxygenase
Hormones

ASJC Scopus subject areas

  • Endocrinology

Cite this

[NLE4, D-PHE7]-α-MSH : A superpotent melanotropin that “Irreversibly“ activates melanoma tyros inase. / Hadley, Mac E.; Malek, Zalfa A Abdel; Marwan, Mohamed M.; Kreutzfeld, Kristie L.; Hruby, Victor J.

In: Endocrine Research, Vol. 11, No. 4 --Mar, 1985, p. 157-170.

Research output: Contribution to journalArticle

Hadley, Mac E. ; Malek, Zalfa A Abdel ; Marwan, Mohamed M. ; Kreutzfeld, Kristie L. ; Hruby, Victor J. / [NLE4, D-PHE7]-α-MSH : A superpotent melanotropin that “Irreversibly“ activates melanoma tyros inase. In: Endocrine Research. 1985 ; Vol. 11, No. 4 --Mar. pp. 157-170.
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abstract = "The superpotent and ultranrolongecL melanotropic properties of an -melanotropin analog, [Nle4, D-Phe]-MSH, were investigated in a Cloudman S91 (CCL 53.1) melanoma cell line. [Nle4, D-Phe]-MSH is 100-fold more effective than the native hormone, -melanocyte stimulating hormone (-MSH), in stimulating melanoma cell tyrosinase 1. activity. as determined from their minimum effective doses (10 M and 10 M, respectively). [Nle4, D-Phe7]-MSH also exhibits a more sustained effect than -MSH on tyrosinase after removal of the melanotropins from the incubation medium. When cells were exposed to -MSH (10 M) f{\"o}r 24 h, residual activity after removal of the hormone was minimally signifleant.7 In contrast, under the same experimental conditions [Nle4, D-Phe7]-MSH treatment induced tyrosinase activity 2-3 fold above basal level, and maintained remarkable stimulatory effects up to 72 h following melanotropin removal. When the exposure time to melanotropins was reduced to 4 h, -MSH failed to elicit significant tyrosinase activity, whereas [Nle4, D-Phe7]-MSH stimulated significant tyrosinase activity during the first 24 h subsequent to melanotropin removal. Interestingly, this stimulation by the analog increased at 48 h, reached a maximum at 72 h following removal of the melanotropin analog, and remained significantly stimulated f{\"o}r 6 consecutive days in the absence of the analog.",
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AB - The superpotent and ultranrolongecL melanotropic properties of an -melanotropin analog, [Nle4, D-Phe]-MSH, were investigated in a Cloudman S91 (CCL 53.1) melanoma cell line. [Nle4, D-Phe]-MSH is 100-fold more effective than the native hormone, -melanocyte stimulating hormone (-MSH), in stimulating melanoma cell tyrosinase 1. activity. as determined from their minimum effective doses (10 M and 10 M, respectively). [Nle4, D-Phe7]-MSH also exhibits a more sustained effect than -MSH on tyrosinase after removal of the melanotropins from the incubation medium. When cells were exposed to -MSH (10 M) för 24 h, residual activity after removal of the hormone was minimally signifleant.7 In contrast, under the same experimental conditions [Nle4, D-Phe7]-MSH treatment induced tyrosinase activity 2-3 fold above basal level, and maintained remarkable stimulatory effects up to 72 h following melanotropin removal. When the exposure time to melanotropins was reduced to 4 h, -MSH failed to elicit significant tyrosinase activity, whereas [Nle4, D-Phe7]-MSH stimulated significant tyrosinase activity during the first 24 h subsequent to melanotropin removal. Interestingly, this stimulation by the analog increased at 48 h, reached a maximum at 72 h following removal of the melanotropin analog, and remained significantly stimulated för 6 consecutive days in the absence of the analog.

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