A direct high-throughput protein quantification strategy facilitates discovery and characterization of a celastrol-derived BRD4 degrader
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Abstract
We describe a generalizable time-resolved Förster resonance energy transfer (TR-FRET)-based platform to profile the cellular action of heterobifunctional degraders (or proteolysis-targeting chimeras [PROTACs]) that is capable of both accurately quantifying protein levels in whole-cell lysates in less than 1 h and measuring small-molecule target engagement to endogenous proteins, here specifically for human bromodomain-containing protein 4 (BRD4). The detection mix consists of a single primary antibody targeting the protein of interest, a luminescent donor-labeled anti-species nanobody, and a fluorescent acceptor ligand. Importantly, our strategy can readily be applied to other targets of interest and will greatly facilitate the cell-based profiling of small-molecule inhibitors and PROTACs in a high-throughput format with unmodified cell lines. We furthermore validate our platform in the characterization of celastrol, a p-quinone methide-containing pentacyclic triterpenoid, as a broad cysteine-targeting E3 ubiquitin ligase warhead for potent and efficient targeted protein degradation.
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Payne et al. applied TR-FRET to profile PROTAC-induced degradation of BRD4.
“Recently, Payne et al. applied time-resolved fluorescence resonance energy (TR-FRET) to profile PROTAC-induced degradation of BRD4.165”
From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [165]
By combining a fluorescent JQ1-based tracer with a primary BRD4 antibody and a labeled nano-secondary antibody, the authors monitored BRD4 levels.
“By combining a fluorescent JQ1-based tracer with a primary BRD4 antibody and a labeled nano-secondary antibody, the authors were able to monitor BRD4 levels.”
From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [165]
The assay was miniaturized to a 96-well plate format, enabling scalable profiling of molecules in unmodified biological systems.
“The assay was miniaturized to a 96-well plate format, enabling the scalable profiling of molecules in unmodified biological systems.”
From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [165]
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- Authors
- Payne, N. C., Maksoud, S., Tannous, B. A., & Mazitschek, R.
- Affiliations
- Harvard University (US)
- Broad Institute (US)
- Corresponding author
- Mazitschek, Ralph
- Venue
- Cell Chemical Biology
- Publisher
- Elsevier BV
- Published
- 2022-08
- Volume
- 29
- Issue
- 8
- Pages
- 1333-1340.e5
- ISSN
- 2451-9448 (ISSN-L)
- 2451-9456
- PMC
- PMC9391279
- OpenAlex
- W4281661759
- Cited by
- 44
- References
- 36
- Citations by year
- 2026: 7 · 2025: 12 · 2024: 12 · 2023: 8 · 2022: 5
- FWCI
- 3.10
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- www.elsevier.com/tdm/userlicense/1.0/ (tdm)
- www.elsevier.com/legal/tdmrep-license (tdm)
- www.elsevier.com/open-access/userlicense/1.0/ (vor, 382 d)
- doi.org/10.15223/policy-017 (stm-asf)
- doi.org/10.15223/policy-037 (stm-asf)
- doi.org/10.15223/policy-012 (stm-asf)
- doi.org/10.15223/policy-029 (stm-asf)
- doi.org/10.15223/policy-004 (stm-asf)
- Locations
- Cell chemical biology (publishedVersion)
- bioRxiv (Cold Spring Harbor Laboratory) (acceptedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- NIH (1R01NS064983)
- National Science Foundation (DGE1745303, 1830941)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biophysics › Advanced Fluorescence Microscopy Techniques
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Keywords
- PROTACs, heterobifunctional degraders, BRD4, celastrol, protein quantification, target engagement, nanobodies, E3 ubiquitin ligase, targeted protein degradation, p-quinone methides, high-throughput screening, bromodomain proteins
- MeSH terms
- Bromodomain Containing Proteins, Humans, Nuclear Proteins, Transcription Factors, Cell Cycle Proteins, Ubiquitin-Protein Ligases, Pentacyclic Triterpenes, Proteolysis
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