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Discovery of a transdermally deliverable pentapeptide for activating AdipoR1 to promote hair growth
EMBO Molecular Medicine ( IF 9.0 ) Pub Date : 2021-09-06 , DOI: 10.15252/emmm.202013790
Jungyoon Ohn 1, 2, 3, 4 , Kyung Wook Been 5 , Jin Yong Kim 2, 3, 4 , Eun Ju Kim 2, 3, 4 , Taeyong Park 5 , Hye-Jin Yoon 5 , Jeong Seok Ji 5 , Miki Okada-Iwabu 6 , Masato Iwabu 6 , Toshimasa Yamauchi 6 , Yeon Kyung Kim 2, 3, 4 , Chaok Seok 5 , Ohsang Kwon 2, 3, 4 , Kyu Han Kim 1, 2, 3, 4 , Hyung Ho Lee 5 , Jin Ho Chung 2, 3, 4
Affiliation  

Alopecia induced by aging or side effects of medications affects millions of people worldwide and impairs the quality of life; however, there is a limit to the current medications. Here, we identify a small transdermally deliverable 5-mer peptide (GLYYF; P5) that activates adiponectin receptor 1 (AdipoR1) and promotes hair growth. P5 sufficiently reproduces the biological effect of adiponectin protein via AMPK signaling pathway, increasing the expression of hair growth factors in the dermal papilla cells of human hair follicle. P5 accelerates hair growth ex vivo and induces anagen hair cycle in mice in vivo. Furthermore, we elucidate a key spot for the binding between AdipoR1 and adiponectin protein using docking simulation and mutagenesis studies. This study suggests that P5 could be used as a topical peptide drug for alleviating pathological conditions, which can be improved by adiponectin protein, such as alopecia.

中文翻译:

发现可透皮递送的五肽,用于激活 AdipoR1 以促进毛发生长

由衰老或药物副作用引起的脱发影响着全世界数百万人并损害生活质量;然而,目前的药物是有限制的。在这里,我们鉴定了一种可透皮递送的小 5 聚体肽(GLYYF;P5),它可以激活脂联素受体 1 (AdipoR1) 并促进毛发生长。P5通过AMPK信号通路充分再现脂联素蛋白的生物学效应,增加人毛囊真皮乳头细胞中毛发生长因子的表达。P5 可加速小鼠体外毛发生长,并在小鼠体内诱导毛发生长初期周期。此外,我们通过对接模拟和诱变研究阐明了 AdipoR1 和脂联素蛋白之间结合的关键点。这项研究表明,P5 可以作为一种局部肽药物,用于缓解脂联素蛋白可以改善的病理状况,例如脱发。
更新日期:2021-10-07
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