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Gestodene Accelerates Cutaneous Wound Healing via PAR1-Selective Positive Allosteric Modulation
Hyejin Jeon1, Yunkyung Heo1, Yechan Lee1
1College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 85 Songdogwahak-ro, Yeonsu-gu, Incheon 21983, Republic of Korea.
International Journal of Molecular Sciences
|June 26, 2026
Summary
Gestodene, a PAR1-selective positive allosteric modulator, accelerates wound healing by enhancing cell proliferation and collagen deposition. This study highlights gestodene
Area of Science:
- Pharmacology
- Dermatology
- Cell Biology
Background:
- Protease-activated receptor 1 (PAR1) is crucial for cutaneous wound healing processes.
- Limited availability of PAR1-selective positive allosteric modulators (PAMs) hinders therapeutic development.
Purpose of the Study:
- To investigate the wound healing efficacy of gestodene, a selective PAR1 PAM.
- To elucidate the mechanism of gestodene's action in wound repair.
Main Methods:
- Characterized gestodene's effect on PAR1-activating peptide (PAR1-AP)-induced calcium signaling in human keratinocytes and dermal fibroblasts.
- Assessed gestodene's impact on PAR1-dependent cell proliferation, migration, and ERK1/2 activation.
- Evaluated gestodene's efficacy in a murine wound model following topical administration.
Main Results:
- Gestodene selectively potentiated PAR1 signaling without intrinsic agonist activity.
- Gestodene enhanced PAR1-dependent cell proliferation, migration, and expression of wound healing genes (MMPs, fibronectin, collagen).
- Topical gestodene accelerated wound closure and collagen deposition in mice, with effects reversed by PAR1 inhibition.
Conclusions:
- Gestodene accelerates cutaneous wound healing via PAR1-selective positive allosteric modulation.
- Gestodene shows potential as a drug repositioning candidate for wound repair therapies.
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