• Title/Summary/Keyword: 12(S)-HPETE

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Discovery of Novel TRPV1 Ligands through Rational Approach Based on Its Putative Endogenous Ligand, 12(S)-HPETE

  • Min, Kyung-Hoon;Lee, Seul;Kim, Hwa-Soon;Suh, Young-Ger
    • Bulletin of the Korean Chemical Society
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    • v.31 no.6
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    • pp.1501-1505
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    • 2010
  • We report design and synthesis of the novel TRPV1 ligands through a rational approach. Simplified analogues of 12(S)-HPETE showing TRPV1 agonistic effect are disclosed. Biological evaluation revealed that substitution of functional groups without any change in conformation converted agonist into antagonist. Our work provided key information with regard to TRPV1 agonist/antagonist switching.

Design. Synthesis and Biological Activities of Novel Vanilloid Receptor (VR) Agonists and Antagonists

  • Suh, Young-Ger;Lee, Bo-Young;Kim, Jin-Kwan;Min, Kyung-Hoon;Park, Ok-Hui;Lee, Young-Sil;Oh, Uh-Taek;Park, Young-Ho;Joo, Yung-Hyup;Choi, Jin-Kyu;Jeong, Yeon-Su;Koh, Hyun-Ju
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.355.1-355.1
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    • 2002
  • Recently. we have reported that several lipoxygenases products directly activate the capsaicin-activated channel as intracellular messengers in neuron. In particular, 12-(S)-hydroperoxyeicosatetraenoic acid turned out to be the most potent endogenous VR activator. This finding prompted us to search for a novel non-vaniloid VR agonists and antagonists. We have designed and synthesized a series of non-vanilloid VR binding ligands based on the structural simllarity between 12-HPETE and capsaicin, the natural VR agonist. Our recent studies on the development of selective vanilloid receptor agonists and antagonists will be presented.

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