- 2-Oxoglutarate analogue inhibitors of prolyl hydroxylase domain 2
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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.
- Mecinovic, Jasmin,Loenarz, Christoph,Chowdhury, Rasheduzzaman,Schofield, Christopher J.
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- Inhibitors of the FEZ-1 metallo-β-lactamase
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Metallo-β-lactamases (MBLs) catalyze the hydrolysis of β-lactams including penicillins, cephalosporins and carbapenems. Starting from benzohydroxamic acid (1) structure-activity studies led to the identification of selective inhibitors of the FEZ-1 MBL, e.g., 2,5-substituted benzophenone hydroxamic acid 17 has a Ki of 6.1 ± 0.7 μM against the FEZ-1 MBL but does not significantly inhibit the IMP-1, BcII, CphA or L1 MBLs.
- Lienard, Benoit M.R.,Horsfall, Louise E.,Galleni, Moreno,Frere, Jean-Marie,Schofield, Christopher J.
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p. 964 - 968
(2008/12/23)
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- CARBOXY AND SUBSTITUTED CARBOXY ALKANOYL AND CYCLOALKANOYL PEPTIDES
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Peptides of the formula STR1 wherein X is various amino or imino acids or esters are useful as hypotensive agents.
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