2. Academic Validation
  3. Hyaluronic acid-FGF2-derived peptide bioconjugates for suppression of FGFR2 and AR simultaneously as an acne antagonist

Hyaluronic acid-FGF2-derived peptide bioconjugates for suppression of FGFR2 and AR simultaneously as an acne antagonist

  • J Nanobiotechnology. 2023 Feb 17;21(1):55. doi: 10.1186/s12951-023-01812-7.
Zijian Su # 1,  Yibo Zhang # 1,  Jieqiong Cao # 1 2,  Yuanmeng Sun 1,  Yuling Cai 1,  Bihui Zhang 1,  Liu He 1,  Zilei Zhang 1,  Junye Xie 1,  Qilin Meng 1,  Lin Luo 1,  Fu Li 1,  Jingsheng Li 1,  Jinting Zhang 1,  Xiaojia Chen 3,  An Hong 4
Affiliations

Affiliations

  • 1 Department of Cell Biology, College of Life Science and Technology, Jinan University; National Engineering Research Center of Genetic Medicine; Guangdong Provincial Key Laboratory of Bioengineering Medicine; Guangdong Provincial Biotechnology Drug & Engineering Technology Research Center, Jinan University, Guangzhou, 510632, Guangdong, China.
  • 2 The First Affiliated Hospital of Jinan University, Guangzhou, 510630, China.
  • 3 Department of Cell Biology, College of Life Science and Technology, Jinan University; National Engineering Research Center of Genetic Medicine; Guangdong Provincial Key Laboratory of Bioengineering Medicine; Guangdong Provincial Biotechnology Drug & Engineering Technology Research Center, Jinan University, Guangzhou, 510632, Guangdong, China. tchenxj@jnu.edu.cn.
  • 4 Department of Cell Biology, College of Life Science and Technology, Jinan University; National Engineering Research Center of Genetic Medicine; Guangdong Provincial Key Laboratory of Bioengineering Medicine; Guangdong Provincial Biotechnology Drug & Engineering Technology Research Center, Jinan University, Guangzhou, 510632, Guangdong, China. tha@jnu.edu.cn.
  • # Contributed equally.
PMID: 36803994 DOI: 10.1186/s12951-023-01812-7
Abstract

Acne is a chronic skin condition that has serious consequences for mental and social well-being because it frequently occurs on the face. Several acne treatment approaches have commonly been used but have been hampered by side effects or weak activity. Thus, the investigation of the safety and efficacy of anti-acne compounds is of considerable medical importance. Herein, an endogenous peptide (P5) derived from fibroblast growth factors 2 (FGF2) was conjugated to the polysaccharide hyaluronic acid (HA) to generate the bioconjugate nanoparticle HA-P5, which suppresses Fibroblast Growth Factor receptors (FGFRs) to significantly rehabilitate acne lesions and reduce sebum accumulation in vivo and in vitro. Moreover, our results show that HA-P5 inhibits both Fibroblast Growth Factor receptor 2 (FGFR2) and Androgen Receptor (AR) signalling in SZ95 cells, reverses the acne-prone transcriptome, and decreases sebum secretion. Furthermore, the cosuppression mechanism revealed that HA-P5 blocks FGFR2 activation, as well as the YTH N6-methyladenosine RNA binding protein F3 (YTHDF3) downstream molecules, including an N6-methyladenosine (m6A) reader that facilitates AR translation. More importantly, a significant difference between HA-P5 and the commercial FGFR Inhibitor AZD4547 is that HA-P5 does not trigger the overexpression of aldo-keto reductase family 1 member C3 (AKR1C3), which blocks acne treatment by catalyzing the synthesis of testosterone. Overall, we demonstrate that a polysaccharide-conjugated and naturally derived oligopeptide HA-P5 can alleviate acne and act as an optimal FGFR2 Inhibitor and reveal that YTHDF3 plays a crucial role in signalling between FGFR2 and AR.

Keywords

AR; Acne therapy; FGFR; HA polysaccharide; Oligopeptides; Signalling crosstalk.

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Inhibitors & Agonists
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-13330
    99.85%, FGFR抑制剂
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