Binding and cAMP Studies of Melanotropin Peptides with the Cloned Human Peripheral Melanocortin Receptor, hMC1R

C. Haskellluevano, H. Miwa, C. Dickinson, Victor J Hruby, T. Yamada, I. Gantz

Research output: Contribution to journalArticle

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Abstract

Binding and stimulation of cAMP by the melanotropin peptides α-MSH (α-melanocyte-stimulating hormone) and its superpotent analogues [Nle4, DPhe7] α-MSH (MT-I) and [formula] α-MSH4-10-NH2 (MT-II) were undertaken to examine their respective properties on the human peripheral melanocyte melanocortin receptor, hMC1R. α-MSH was found to possess a binding IC50 value of 6.5 ± 0.9 × 10-9 M and cAMP EC50 value of 2.0 ± 0.6 × 10-9 M. MT-I possesses a binding IC50 value of 1.2 ± 0.3 × 10-9 M and a cAMP EC50 of 0.5 ± 0.03 × 10-9 M. MT-II possesses a binding IC50 of 0.57 ± 0.08 × 10-9 M and cAMP EC50 value of 0.20 ± 0.05 × 10-9 M.

Original languageEnglish (US)
Pages (from-to)1137-1142
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume204
Issue number3
DOIs
StatePublished - Nov 14 1994

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Melanocortin Receptors
Melanocyte-Stimulating Hormones
Inhibitory Concentration 50
Peptides
Receptor, Melanocortin, Type 1

ASJC Scopus subject areas

  • Molecular Biology
  • Biophysics
  • Biochemistry

Cite this

Binding and cAMP Studies of Melanotropin Peptides with the Cloned Human Peripheral Melanocortin Receptor, hMC1R. / Haskellluevano, C.; Miwa, H.; Dickinson, C.; Hruby, Victor J; Yamada, T.; Gantz, I.

In: Biochemical and Biophysical Research Communications, Vol. 204, No. 3, 14.11.1994, p. 1137-1142.

Research output: Contribution to journalArticle

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AU - Yamada, T.

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AB - Binding and stimulation of cAMP by the melanotropin peptides α-MSH (α-melanocyte-stimulating hormone) and its superpotent analogues [Nle4, DPhe7] α-MSH (MT-I) and [formula] α-MSH4-10-NH2 (MT-II) were undertaken to examine their respective properties on the human peripheral melanocyte melanocortin receptor, hMC1R. α-MSH was found to possess a binding IC50 value of 6.5 ± 0.9 × 10-9 M and cAMP EC50 value of 2.0 ± 0.6 × 10-9 M. MT-I possesses a binding IC50 value of 1.2 ± 0.3 × 10-9 M and a cAMP EC50 of 0.5 ± 0.03 × 10-9 M. MT-II possesses a binding IC50 of 0.57 ± 0.08 × 10-9 M and cAMP EC50 value of 0.20 ± 0.05 × 10-9 M.

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