4.5 Article

2-Oxoglutarate analogue inhibitors of prolyl hydroxylase domain 2

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 21, Pages 6192-6195

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.09.005

Keywords

Hypoxia; Inhibition; Mass spectrometry; 2-Oxoglutarate; Prolyl hydroxylase domain 2

Funding

  1. Newton-Abraham Fund
  2. Rhodes Trust
  3. Commonwealth Scholarship Scheme
  4. Biotechnology and Biological Sciences Research Council
  5. Wellcome Trust

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Analogues of the 2-oxoglutarate cosubstrate of the human oxygen sensing enzyme prolyl hydroxylase domain 2 (PHD2) with variations in the potential iron-chelating group were screened as inhibitors and for binding (using non-denaturing electrospray ionization mass spectrometry) to PHD2. (c) 2009 Elsevier Ltd. All rights reserved.

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