Analogues of dealanylalahopcin are inhibitors of human HIF prolyl hydroxylases.

Abstract

Analogues of the naturally occurring cyclic hydroxamate dealanylalahopcin, which is an inhibitor of procollagen prolyl-4-hydroxylase, were synthesised and shown to be inhibitors of the human hypoxia-inducible factor prolyl hydroxylases.

• Authors: Imre Schlemminger, David R Mole, Luke A McNeill, Anupma Dhanda, Kirsty S Hewitson, Ya-Min Tian, Peter J Ratcliffe, Christopher W Pugh, Christopher J Schofield
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 13 Issue 8 Pg. 1451-4 (Apr 17 2003) ISSN: 0960-894X [Print] England
• PMID: 12668010 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Aminobutyrates
• Enzyme Inhibitors
• HIF1A protein, human
• Hypoxia-Inducible Factor 1, alpha Subunit
• Isoenzymes
• Transcription Factors
• Tumor Suppressor Proteins
• dealanylalahopcin
• Iron
• Procollagen-Proline Dioxygenase

Topics

• Aminobutyrates (chemical synthesis, chemistry, metabolism, pharmacology)
• Animals
• Autoradiography
• Binding Sites
• Enzyme Inhibitors (chemistry, pharmacology)
• Humans
• Hypoxia-Inducible Factor 1, alpha Subunit
• Iron (metabolism)
• Isoenzymes (antagonists & inhibitors, metabolism)
• Procollagen-Proline Dioxygenase (antagonists & inhibitors, metabolism)
• Transcription Factors (metabolism)
• Tumor Suppressor Proteins (analysis, metabolism)