Analogues of dealanylalahopcin are inhibitors of human HIF prolyl hydroxylases.
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.
Schlemminger
Imre
I
Oxford Centre for Molecular Sciences, Dyson Perrins Laboratory, South Parks Road, UK.
Mole
David R
DR
McNeill
Luke A
LA
Dhanda
Anupma
A
Hewitson
Kirsty S
KS
Tian
Ya-Min
YM
Ratcliffe
Peter J
PJ
Pugh
Christopher W
CW
Schofield
Christopher J
CJ
D000613:Aminobutyrates / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001345:Autoradiography; D001665:Binding Sites; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D051795:Hypoxia-Inducible Factor 1, alpha Subunit; D007501:Iron / Q000378:metabolism; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D011393:Procollagen-Proline Dioxygenase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014157:Transcription Factors / Q000378:metabolism*; D025521:Tumor Suppressor Proteins / Q000032:analysis / Q000378:metabolism
D000613:Aminobutyrates; D004791:Enzyme Inhibitors; C497442:HIF1A protein, human; D051795:Hypoxia-Inducible Factor 1, alpha Subunit; D007527:Isoenzymes; D014157:Transcription Factors; D025521:Tumor Suppressor Proteins; C045372:dealanylalahopcin; D007501:Iron; D011393:Procollagen-Proline Dioxygenase