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

C. Haskellluevano; H. Miwa; C. Dickinson; V. J. Hruby; T. Yamada; I. Gantz

doi:10.1006/bbrc.1994.2581

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

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

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48 Scopus citations

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-MSH_4-10-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 language	English (US)
Pages (from-to)	1137-1142
Number of pages	6
Journal	Biochemical and Biophysical Research Communications
Volume	204
Issue number	3
DOIs	https://doi.org/10.1006/bbrc.1994.2581
State	Published - Nov 14 1994
Externally published	Yes

ASJC Scopus subject areas

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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

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.",

author = "C. Haskellluevano and H. Miwa and C. Dickinson and Hruby, {V. J.} and T. Yamada and I. Gantz",

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doi = "10.1006/bbrc.1994.2581",

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T1 - Binding and cAMP Studies of Melanotropin Peptides with the Cloned Human Peripheral Melanocortin Receptor, hMC1R

AU - Haskellluevano, C.

AU - Miwa, H.

AU - Dickinson, C.

AU - Hruby, V. J.

AU - Yamada, T.

AU - Gantz, I.

PY - 1994/11/14

Y1 - 1994/11/14

N2 - 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.

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

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