6012-49-3Relevant academic research and scientific papers
Proximity Histidine Labeling by Umpolung Strategy Using Singlet Oxygen
Nakane, Keita,Sato, Shinichi,Niwa, Tatsuya,Tsushima, Michihiko,Tomoshige, Shusuke,Taguchi, Hideki,Ishikawa, Minoru,Nakamura, Hiroyuki
supporting information, p. 7726 - 7731 (2021/05/29)
While electrophilic reagents for histidine labeling have been developed, we report an umpolung strategy for histidine functionalization. A nucleophilic small molecule, 1-methyl-4-arylurazole, selectively labeled histidine under singlet oxygen (1O2) generation conditions. Rapid histidine labeling can be applied for instant protein labeling. Utilizing the short diffusion distance of 1O2 and a technique to localize the 1O2 generator, a photocatalyst in close proximity to the ligand-binding site, we demonstrated antibody Fc-selective labeling on magnetic beads functionalized with a ruthenium photocatalyst and Fc ligand, ApA. Three histidine residues located around the ApA binding site were identified as labeling sites by liquid chromatography-mass spectrometry analysis. This result suggests that 1O2-mediated histidine labeling can be applied to a proximity labeling reaction on the nanometer scale.
TARGETED DRUG DELIVERY THROUGH AFFINITY BASED LINKERS
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Paragraph 00285, (2015/12/08)
The current invention discloses targeted drug delivery conjugates comprising a targeting moiety linked to a drug via a molecule having an affinity for the targeting moiety. Typically, the conjugate comprises a targeting ligand and a molecule of interest, e.g., a therapeutic agent. The targeting ligand and the molecule of interest are linked to each other via an affinity ligand. The affinity ligand is further covalently or non-covalently linked to a drug or therapeutic agent. The drug can be modified to make it more soluble and so that it cleaves from the linking molecule at the target site.
