Analogs of MTII, lactam derivatives of alpha-melanotropin, modified at the N-terminus, and their selectivity at human melanocortin receptors 3, 4, and 5.

Bednarek MA, Macneil T, Kalyani RN, Tang R, Van der Ploeg LH, Weinberg DH

Biochemical and biophysical research communications1 Jul 1999Cited by 60 (Europe PMC)

PMID10405347DOI10.1006/bbrc.1999.0981PepBankPUB-10405347

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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study5

No result from this study comes from a test of the peptide.

Studies that did not test the peptide alone5

In this study, Melanotan II was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Melanotan II.

01LabNot a test of Melanotan II aloneIn vitro (cells)Activity measurement
The analog [Pro(4)]MTII had affinity and agonist potency at the human MC-4 receptor similar to MTII.
In plain wordsIn lab tests, a changed MTII analog worked about as well as MTII at one melanocortin receptor.
Peptide
Melanotan II
Outcome
No significant change[Pro4]MTII affinity and potency at hMC-4R
Study
n: not reported in source
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
Replacement of Nle(4) with Pro resulted in [Pro(4)]MTII with affinity to and agonist potency at hMC-4R similar to MTII
1 context sentence(design, population, supporting numbers)
Summary · context
In search for selective agonists at human melanocortin-4 receptor, proline-substituted analogs of MTII, a potent nonselective agonist at melanocortin receptors, were prepared by solid-phase syntheses and evaluated for their ability to bind and activate human MC-3, MC-4, and MC-5 receptors.
In this study, Melanotan II was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan II.
Report a problemFND-1040534701
02LabNot a test of Melanotan II aloneIn vitro (cells)Activity measurement
The analog [Pro(4)]MTII had about 400-fold lower potency than MTII at the human MC-5 receptor.
In plain wordsIn lab tests, a changed MTII analog was much less potent than MTII at another melanocortin receptor.
Peptide
Melanotan II
Outcome
Decrease[Pro4]MTII potency at hMC-5R
Study
n: not reported in source
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
but with about 400-fold lower potency at hMC-5R and about 20-fold lower potency at hMC-3R.
1 context sentence(design, population, supporting numbers)
Summary · context
In search for selective agonists at human melanocortin-4 receptor, proline-substituted analogs of MTII, a potent nonselective agonist at melanocortin receptors, were prepared by solid-phase syntheses and evaluated for their ability to bind and activate human MC-3, MC-4, and MC-5 receptors.
In this study, Melanotan II was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan II.
Report a problemFND-1040534702
03LabNot a test of Melanotan II aloneIn vitro (cells)Activity measurement
The analog [Pro(4)]MTII had about 20-fold lower potency than MTII at the human MC-3 receptor.
In plain wordsIn lab tests, a changed MTII analog was less potent than MTII at a third melanocortin receptor.
Peptide
Melanotan II
Outcome
Decrease[Pro4]MTII potency at hMC-3R
Study
n: not reported in source
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
and about 20-fold lower potency at hMC-3R.
1 context sentence(design, population, supporting numbers)
Summary · context
In search for selective agonists at human melanocortin-4 receptor, proline-substituted analogs of MTII, a potent nonselective agonist at melanocortin receptors, were prepared by solid-phase syntheses and evaluated for their ability to bind and activate human MC-3, MC-4, and MC-5 receptors.
In this study, Melanotan II was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan II.
Report a problemFND-1040534703
04LabNot a test of Melanotan II aloneIn vitro (cells)Activity measurement
MTII analogs with modified N-termini had agonist potency at hMC-4R similar to MTII.
In plain wordsIn lab tests, MTII analogs with a changed start of the chain worked as well as MTII at one receptor.
Peptide
Melanotan II
Outcome
No significant changeN-terminal MTII analogs at hMC-4R
Study
n: not reported in source
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
The similar agonist potency of these peptides to that of MTII at hMC-4R but significantly lower activity of these compounds at hMC-5R demonstrated that the N-terminal fragment of MTII has virtually no effect on the binding affinity and activation at hMC-4R, but it is essential for full potency at hMC-5R.
1 context sentence(design, population, supporting numbers)
Summary · context
In search for selective agonists at human melanocortin-4 receptor, proline-substituted analogs of MTII, a potent nonselective agonist at melanocortin receptors, were prepared by solid-phase syntheses and evaluated for their ability to bind and activate human MC-3, MC-4, and MC-5 receptors.
In this study, Melanotan II was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan II.
Report a problemFND-1040534704
05LabNot a test of Melanotan II aloneIn vitro (cells)Activity measurement
MTII analogs with modified N-termini had significantly lower activity than MTII at hMC-5R, so the N-terminal fragment is essential for full potency there.
In plain wordsIn lab tests, MTII analogs with a changed start of the chain were less active than MTII at another receptor.
Peptide
Melanotan II
Outcome
DecreaseN-terminal MTII analogs at hMC-5R
Study
n: not reported in source
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
The similar agonist potency of these peptides to that of MTII at hMC-4R but significantly lower activity of these compounds at hMC-5R demonstrated that the N-terminal fragment of MTII has virtually no effect on the binding affinity and activation at hMC-4R, but it is essential for full potency at hMC-5R.
1 context sentence(design, population, supporting numbers)
Summary · context
In search for selective agonists at human melanocortin-4 receptor, proline-substituted analogs of MTII, a potent nonselective agonist at melanocortin receptors, were prepared by solid-phase syntheses and evaluated for their ability to bind and activate human MC-3, MC-4, and MC-5 receptors.
In this study, Melanotan II was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan II.
Report a problemFND-1040534705

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
10 Oct 2026, 09:43 UTC
Study results updated
Version 1
9 Oct 2026, 03:04 UTC
First added · source update from Europe PMC

Subjects

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