Peptide Melanogenesis and Adipogenesis Regulation via MITF Phosphorylation

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Solution Overview

Problem

Current treatments for hypomelanosis and obesity lack effective and safe therapeutic options, with existing medications often causing significant side effects and limited efficacy.

Innovation Solution

A peptide with specific amino acid sequences (SEQ ID NO: 1 and SEQ ID NO: 2) that increases melanogenesis and inhibits adipogenesis, achieved through phosphorylation of MITF and CREB for melanin production and reduction of perilipin and PPARγ expression, respectively.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing medications for hypomelanosis and obesity are used, then therapeutic efficacy is limited, but side effects are significant

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention changes the chemical parameter from conventional small-molecule drugs to a specific peptide sequence (SEQ ID NO: 1), which alters the mechanism of action to achieve both high efficacy and safety. The peptide modifies cellular signaling pathways (cAMP, ERK1/2, MITF) differently than traditional drugs, resulting in potent melanogenesis promotion without the severe side effects of existing medications.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The peptide functions as a composite biological agent that interacts with multiple targets simultaneously (tyrosinase, Trp-1, Trp-2, MITF, cAMP pathway), creating a multi-faceted therapeutic effect that addresses both efficacy and safety requirements through coordinated molecular interactions.

Inventive Principle:
Principle #40Composite materials

2Reliability

If melanin production is increased to treat hypomelanosis, then pigmentation improves, but risk of abnormal pigmentation increases

Engineering Contradiction:
Improvepigmentation improvementVSAvoidabnormal pigmentation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The peptide activates a regulated feedback mechanism through the cAMP-MITF-tyrosinase pathway, where MITF acts as a transcription factor that controls tyrosinase expression in a controlled manner. This feedback regulation ensures melanin production increases appropriately without causing uncontrolled hyperpigmentation, as the pathway responds proportionally to cellular needs.

Inventive Principle:
Principle #23Feedback

Solution Approach 2:

The invention changes the regulatory parameter from uncontrolled melanin stimulation to a precisely regulated pathway activation through cAMP and MITF, which naturally controls the rate and extent of melanin production. This parameter change ensures therapeutic effect while preventing abnormal pigmentation through biological feedback mechanisms.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If conventional anti-obesity drugs are used, then weight loss effect is achieved, but severe side effects occur

Engineering Contradiction:
Improveweight loss effectVSAvoidsevere side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention extracts and utilizes the beneficial adipogenesis-inhibiting effect while eliminating the harmful side effects by using a peptide that specifically targets the adipogenic pathway (PPARγ, C/EBPα) without affecting cardiovascular, neurological, or digestive systems. The peptide isolates the therapeutic action to fat metabolism only.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention changes the therapeutic parameter from systemic appetite suppression or fat absorption inhibition to specific adipogenesis pathway modulation through peptide signaling, which selectively affects fat cell development without disrupting other physiological systems, thereby achieving weight loss without severe side effects.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3144316B1Peptide having efficacy for remedying hypopigmentation and inhibiting adipogenesis, and use of same
Publication Date: 2019.06.05 CAREGEN
  • EP3144316B1 patent drawingFigure 1a
  • EP3144316B1 patent drawingFigure 1b
  • EP3144316B1 patent drawingFigure 2a

AI summary

A peptide formed from the amino acid sequence of SEQ ID NO: 1 or SEQ ID NO: 2, according to the present invention, shows a melanogenesis increment activity and an adipogenesis inhibitory activity. A peptide of the present invention, by increasing phosphorylation of MITF, which is a transcription factor for increasing a tyrosinase expression, and CREB for increasing an MITF expression, consequently increases a tyrosinase expression and ultimately increases melanin synthesis. A peptide of the present invention, by reducing the amount of fat accumulated inside a cell and reducing expressions of perilipin and PPARγ, which contribute to adipogenic mechanism, ultimately inhibits adipogenesis. The present invention provides a composition for remedying or treating melanin hypopigmentation, the composition comprising the peptide, and provides pharmaceutical composition for treating or preventing obesity.