Jacob T. Bush
Highly Influential Citations5
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2-Oxoglutarate and iron dependent oxygenases are therapeutic targets for human diseases. Using a representative 2OG oxygenase panel, we compare the inhibitory activities of… Continue Reading
The four-component Ugi reaction is applied to synthesize biotin and rhodamine tagged compounds (V) of which a series of photoaffinity probes (VIII) for 2-OG oxygenase is derived.
The synthesis of small molecule based 1,3,5-trisubstituted benzenes for photo-mediated capture of human carbonic anhydrase II with visualisation by fluorescence is described.
YcfD from Escherichia coli is a homologue of the human ribosomal oxygenases NO66 and MINA53, which catalyse histidyl-hydroxylation of the 60S subunit and affect cellular proliferation (Ge et al., Nat… Continue Reading
Photoaffinity probes are increasingly being used for the study of biological interactions; however, the lack of structure–activity relationship studies has hindered their rational application. We… Continue Reading
We describe covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) and studies towards a strategy for photocapture of PHD2 substrates. Reversible active site… Continue Reading
The hypoxia-inducible factors (HIFs) are key transcription factors in determining cellular responses involving alterations in protein levels in response to limiting oxygen availability in animal… Continue Reading
The CDK family plays a crucial role in the control of the cell cycle. Dysregulation and mutation of the CDKs has been implicated in cancer and the CDKs have been investigated extensively as potential… Continue Reading