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Structure of the catalytic domain of human phosphodiesterase 5 with bound drug molecules

Nature, ISSN: 0028-0836, Vol: 425, Issue: 6953, Page: 98-102
2003
  • 252
    Citations
  • 0
    Usage
  • 149
    Captures
  • 4
    Mentions
  • 0
    Social Media
Metric Options:   Counts1 Year3 Year

Metrics Details

  • Citations
    252
  • Captures
    149
  • Mentions
    4
    • References
      3
      • Wikipedia
        3
    • News Mentions
      1
      • News
        1

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Article Description

Phosphodiesterases (PDEs) are a superfamily of enzymes that degrade the intracellular second messengers cyclic AMP and cyclic GMP. As essential regulators of cyclic nucleotide signalling with diverse physiological functions, PDEs are drug targets for the treatment of various diseases, including heart failure, depression, asthma, inflammation and erectile dysfunction. Of the 12 PDE gene families, cGMP-specific PDE5 carries out the principal cGMP-hydrolysing activity in human corpus cavernosum tissue. It is well known as the target of sildenafil citrate (Viagra) and other similar drugs for the treatment of erectile dysfunction. Despite the pressing need to develop selective PDE inhibitors as therapeutic drugs, only the cAMP-specific PDE4 structures are currently available. Here we present the three-dimensional structures of the catalytic domain (residues 537-860) of human PDE5 complexed with the three drug molecules sildenafil, tadalafil (Cialis) and vardenafil (Levitra). These structures will provide opportunities to design potent and selective PDE inhibitors with improved pharmacological profiles.

Bibliographic Details

Sung, Byung-Je; Hwang, Kwang Yeon; Jeon, Young Ho; Lee, J I; Heo, Yong-Seok; Kim, Jin Hwan; Moon, Jinho; Yoon, Jung Min; Hyun, Young-Lan; Kim, Eunmi; Eum, Sung Jin; Park, Sam-Yong; Lee, Jie-Oh; Lee, Tae Gyu; Ro, Seonggu; Cho, Joong Myung

Springer Science and Business Media LLC

Multidisciplinary

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