24697-70-9Relevant articles and documents
Live-Cell Protein Modification by Boronate-Assisted Hydroxamic Acid Catalysis
Adamson, Christopher,Kajino, Hidetoshi,Kanai, Motomu,Kawashima, Shigehiro A.,Yamatsugu, Kenzo
supporting information, p. 14976 - 14980 (2021/09/29)
Selective methods for introducing protein post-translational modifications (PTMs) within living cells have proven valuable for interrogating their biological function. In contrast to enzymatic methods, abiotic catalysis should offer access to diverse and new-to-nature PTMs. Herein, we report the boronate-assisted hydroxamic acid (BAHA) catalyst system, which comprises a protein ligand, a hydroxamic acid Lewis base, and a diol moiety. In concert with a boronic acid-bearing acyl donor, our catalyst leverages a local molarity effect to promote acyl transfer to a target lysine residue. Our catalyst system employs micromolar reagent concentrations and affords minimal off-target protein reactivity. Critically, BAHA is resistant to glutathione, a metabolite which has hampered many efforts toward abiotic chemistry within living cells. To showcase this methodology, we installed a variety of acyl groups inE. colidihydrofolate reductase expressed within human cells. Our results further establish the well-known boronic acid-diol complexation as abona fidebio-orthogonal reaction with applications in chemical biology and in-cell catalysis.
Substituted imidazo[4,5-c]quinoline macrocyclic compound as multi-target kinase inhibitor
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Paragraph 0119-0121, (2020/04/17)
The invention discloses a substituted imidazo[4,5-c]quinoline macrocyclic compound as a multi-target kinase inhibitor, and relates to a compound represented by a formula (I) or a pharmaceutically acceptable salt, a solvate, a polymorphic substance or an isomer thereof, and applications of the compound in preparation of a medicine for treating ALK-mediated diseases.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 2610; 2611, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.