forgot password?
register here
Research articles
  search articles
  reviews guidelines
  articles index
My Pages
my alerts
  my messages
  my reviews
  my favorites
Members: 1973
Articles: 1'802'609
Articles rated: 2555

20 November 2017
  » pubmed » pmid12955149

  Article overview

Structure of the catalytic domain of human phosphodiesterase 5 with bound drug molecules
Byung-Je Sung ; Kwang Yeon Hwang ; Young Ho Jeon ; J I Lee ; Yong-Seok Heo ; Jin Hwan Kim ; Jinho Moon ; Jung Min Yoon ; Young-Lan Hyun ; Eunmi Kim ; Sung Jin Eum ; Sam-Yong Park ; Jie-Oh Lee ; Tae Gyu Lee ; Seonggu Ro ; Joong Myung Cho ;
Rating Members: 4/5 (1 reader)
Date 4 Sep 2003
Journal Nature, 425 (6953), 98-102
AbstractPhosphodiesterases (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.
Source PubMed, pmid12955149 doi: 10.1038/nature01914
Services Forum | Review | Favorites   
Visitor rating: did you like this article? no 1   2   3   4   5   yes

1 review found:
(To access fulltext of a review, click on titles below.)
1. review 16090070    * Rate this comment.
Review title: The head of the World Best Cure
Reviewer: reviewer1919
Date: 09 September 2016 at 20:16 GMT.
Comment: I aim and engage on essential regulators of cyclic nucleotide signalling with diverse physiological functions, PDEs are drug targets for the [...]

browser CCBot/2.0 (
» my Online CV
» Free

News, job offers and information for researchers and scientists:
myScience Austria
myScience Germany
myScience UK
myScience France
myScience Switzerland - International (over 7000 science jobs).
home  |  contact  |  terms of use  |  sitemap
Copyright © 2005-2017 - Scimetrica