Publications by authors named "Herodion Hartono"

Article Synopsis
  • Insulin-like peptide 5 (INSL5) primarily targets the RXFP4 receptor found in the colorectum and has potential for treating gastrointestinal issues like constipation.
  • While INSL5 can bind to the RXFP3 receptor, it does not activate it, highlighting the specificity of the INSL5/RXFP4 pathway for therapeutic applications.
  • The study developed an engineered INSL5 analogue (A13:B7-24-GG) that features a simpler structure, resulting in easier synthesis and improved potency and selectivity compared to native INSL5, making it a strong candidate for constipation treatment.
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Human insulin-like peptide 5 (INSL5) is a gut hormone produced by colonic L-cells, and its biological functions are mediated by Relaxin Family Peptide Receptor 4 (RXFP4). Our preliminary data indicated that RXFP4 agonists are potential drug leads for the treatment of constipation. More recently, we designed and developed a novel RXFP4 antagonist, A13-nR that was shown to block agonist-induced activity in cells and animal models.

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Clioquinol (5-chloro-7-iodo-8-hydroxyquinoline) is an antimicrobial agent whose actions as a zinc or copper ionophore and an iron chelator revived the interest in similar compounds for the treatment of fungal and bacterial infections, neurodegeneration and cancer. Recently, we reported zinc ionophores, including clioquinol, cause vasorelaxation in isolated arteries through mechanisms that involve sensory nerves, endothelium and vascular smooth muscle. Here, we report that clioquinol also uniquely acts as a competitive alpha-1 (α) adrenoceptor antagonist.

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