Bulletin of the Korean Chemical Society

  • 제31권6호
  • /
  • Pages.1501-1505
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  • 2010
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  • 0253-2964(pISSN)
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  • 1229-5949(eISSN)
대한화학회 (Korean Chemical Society)
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Discovery of Novel TRPV1 Ligands through Rational Approach Based on Its Putative Endogenous Ligand, 12(S)-HPETE

  • Min, Kyung-Hoon (College of Pharmacy, Chung-Ang University) ;
  • Lee, Seul (College of Pharmacy, Chung-Ang University) ;
  • Kim, Hwa-Soon (Seoul Metropolitan Government Research Institute of Public Health and Environment) ;
  • Suh, Young-Ger (College of Pharmacy, Seoul National University)
  • 투고 : 2010.03.02
  • 심사 : 2010.03.31
  • 발행 : 2010.06.20
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초록

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.

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참고문헌

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피인용 문헌

  1. ChemInform Abstract: Discovery of Novel TRPV1 Ligands Through Rational Approach Based on Its Putative Endogenous Ligand, 12(S)-HPETE. vol.41, pp.45, 2010, https://doi.org/10.1002/chin.201045079