FIGURE

Fig. 2.

ID

ZDB-FIG-221226-122

Publication

Do et al., 2022 - Hypoxia deactivates epigenetic feedbacks via enzyme-derived clicking proteolysis-targeting chimeras

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Fig. 2.

A) Chemical structure of GSH-responsive CRBN ligand (J266); GSH- and NTR-responsive CRBN ligand (JW4); cleaved J266; CBT-linked BRD4-targeting ligand (JQ1-CBT); click-induced BRD4 degrader (J252). (B) LC-MS spectra of NTR uncaging JW4 (10 μM) to form J266 at different time points in NTR (40 μg/ml) dissolved in phosphate-buffered saline (PBS; 10 mM) (pH 7.4). (C) Selectivity of JW4 toward a broad range of biological and chemical agents with or without NADH. (D) Time-dependent LC-MS spectra of click J252 formation under reducing reagent [tris(2-carboxyethyl)phosphine (TCEP)] that cleave the J266 to induce cleaved J266 before the click reaction with JQ1-CBT in buffer solution. (E) Ratio of peak areas of click J252 and cleaved J266 to J266 over multiple time points in (D).

Expression Data

Expression Detail

Antibody Labeling

Phenotype Data

Phenotype Detail

Acknowledgments

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