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A Photoreactive Small-Molecule Probe for 2-oxoglutarate Oxygenases

A Photoreactive Small-Molecule Probe for 2-oxoglutarate Oxygenases

Dante Rotili, Mikael Altun, Akane Kawamura, Alexander Wolf, Roman Fischer, Ivanhoe K H Leung, Mukram M Mackeen, Ya-Min Tian, Peter J Ratcliffe, Antonello Mai, Benedikt M Kessler, Christopher J Schofield

Chem Biol. 2011 May 27;18(5):642-654.

PMID: 21609845

Abstract:

2-oxoglutarate (2-OG)-dependent oxygenases have diverse roles in human biology. The inhibition of several 2-OG oxygenases is being targeted for therapeutic intervention, including for cancer, anemia, and ischemic diseases. We report a small-molecule probe for 2-OG oxygenases that employs a hydroxyquinoline template coupled to a photoactivable crosslinking group and an affinity-purification tag. Following studies with recombinant proteins, the probe was shown to crosslink to 2-OG oxygenases in human crude cell extracts, including to proteins at endogenous levels. This approach is useful for inhibitor profiling, as demonstrated by crosslinking to the histone demethylase FBXL11 (KDM2A) in HEK293T nuclear extracts. The results also suggest that small-molecule probes may be suitable for substrate identification studies.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR42416102	FBXL11 human			Price

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