Macrocyclic Peptides Targeting c-Myc for Cancer Therapy Resistance

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Solution Overview

Problem

Current therapies for prostate and breast cancers, such as androgen deprivation therapy, are initially effective but often lead to recurrence due to non-responsiveness, particularly with overexpression of the oncoprotein c-Myc, which contributes to cancer progression and resistance to hormonal therapies.

Innovation Solution

Administration of macrocyclic peptides, specifically cyclo[Phe-D-Pro-Phe-Trp] and cyclo[Phe-D-Pro-Phe-D-Trp], which induce cytotoxicity and lower c-Myc protein levels in cancer cells, thereby inhibiting cell proliferation and metastasis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If androgen deprivation therapy is used to treat prostate cancer, then initial effectiveness is achieved, but cancer recurrence occurs due to non-responsiveness and hormonal therapy resistance

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidduration of therapy response
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent introduces macrocyclic peptides as intermediary substances that mediate between the cancer cell and the therapeutic effect. These peptides specifically target c-Myc protein, acting as a mediator to disrupt the androgen receptor-c-Myc axis and induce cytotoxicity, thereby overcoming hormonal therapy resistance and extending the duration of therapeutic response.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the therapeutic parameter by targeting c-Myc protein levels rather than solely relying on androgen depletion. By reducing c-Myc protein expression through macrocyclic peptide treatment, the therapy achieves sustained effectiveness against cancer cells that have developed resistance to conventional androgen deprivation therapy.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If c-Myc protein levels are increased in cancer cells, then cancer progression and therapy resistance are enhanced, but reducing c-Myc levels inhibits cell proliferation and metastasis

Engineering Contradiction:
Improvecancer cell growth inhibitionVSAvoidc-Myc protein overexpression
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and specifically targets the harmful c-Myc protein from the cancer cell system. Macrocyclic peptides are designed to bind to and reduce c-Myc protein levels, effectively removing this harmful factor that drives cancer progression and therapy resistance, thereby achieving sustained cancer cell growth inhibition.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent converts the harmful effect of c-Myc overexpression into a beneficial therapeutic target. By designing macrocyclic peptides that specifically reduce c-Myc levels, the therapy transforms the previously harmful protein overexpression into a controlled parameter, achieving cancer cell death and metastasis inhibition through c-Myc depletion.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentUS11510964B2Macrocyclic peptides to decrease c-Myc protein levels and reduce cancer cell growth
Publication Date: 2022.11.29 UNIV OF FLORIDA RESEARCH FOUNDATION INC
  • US11510964B2 patent drawing
  • US11510964B2 patent drawing
  • US11510964B2 patent drawing

AI summary

The present technology provides methods end medicaments useful for treating prostate cancer and breast cancer. Such methods include administering at least one of cyclo[Phe-D-Pro-Phe-Trp] and cyclo[Phe-D-Pro-Phe-D-Trp] to a subject suffering from prostate cancer or breast cancer.