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NanoBRET Tracer Development for Class I Bromodomain Target Engagement in Live Cells.

Molly S Sneddon1, Chun-Ju Tsou1, Xiang Fu2

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Summary

A new NanoBRET tracer, MS-1, enables live-cell assessment of bromodomain inhibitor engagement. This tool effectively targets BPTF and other class I bromodomains, aiding drug discovery for diseases like cancer.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Bromodomain proteins play roles in diseases like cancer and inflammation.
  • Non-BET bromodomains are understudied, and high-throughput assays for inhibitors are limited.
  • Existing inhibitors like BZ1 show non-selectivity across class I bromodomains.

Purpose of the Study:

  • To design a NanoBRET tracer for assessing live-cell target engagement of bromodomain inhibitors.
  • To evaluate the tracer's broad applicability across different class I bromodomains.
  • To demonstrate the tracer's utility in inhibitor development and target engagement studies.

Main Methods:

  • Development of a NanoBRET tracer (MS-1) based on a BZ1 analog.
  • Utilizing live-cell assays to measure target engagement.
  • Testing MS-1 against BPTF, PCAF, GCN5, and CECR2 bromodomains.
  • Determining IC50 values for various inhibitors.

Main Results:

  • MS-1 effectively binds BPTF, PCAF, GCN5, and CECR2 bromodomains in HEK293T cells.
  • Binding occurs at low to sub-micromolar concentrations.
  • The tracer demonstrated versatility for assessing inhibitor activity against multiple class I bromodomains.

Conclusions:

  • MS-1 is a broadly applicable NanoBRET tracer for class I bromodomains.
  • This tracer facilitates functional assessment of inhibitor activity in live cells.
  • MS-1 aids future target engagement studies and inhibitor development for epigenetic targets.