7p6v

From Proteopedia

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH compound 3ag

Structural highlights

Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 1.17Å
Ligands:	5Z4
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Publication Abstract from PubMed

We present a one-step Ugi reaction protocol for the expedient synthesis of photoaffinity probes for live-cell MS-based proteomics. The reaction couples an amine affinity function with commonly used photoreactive groups, and a variety of handle functionalities. Using this technology, a series of pan-BET (BET: bromodomain and extra-terminal domain) selective bromodomain photoaffinity probes were obtained by parallel synthesis. Studies on the effects of photoreactive group, linker length and irradiation wavelength on photocrosslinking efficiency provide valuable insights into photoaffinity probe design. Optimal probes were progressed to MS-based proteomics to capture the BET family of proteins from live cells and reveal their potential on- and off-target profiles.

One-Step Synthesis of Photoaffinity Probes for Live-Cell MS-Based Proteomics.,Fallon DJ, Lehmann S, Chung CW, Phillipou A, Eberl C, Fantom KGM, Zappacosta F, Patel VK, Bantscheff M, Schofield CJ, Tomkinson NCO, Bush JT Chemistry. 2021 Jul 30. doi: 10.1002/chem.202102036. PMID:34328642^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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Citations

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References

↑ Fallon DJ, Lehmann S, Chung CW, Phillipou A, Eberl C, Fantom KGM, Zappacosta F, Patel VK, Bantscheff M, Schofield CJ, Tomkinson NCO, Bush JT. One-Step Synthesis of Photoaffinity Probes for Live-Cell MS-Based Proteomics. Chemistry. 2021 Jul 30. doi: 10.1002/chem.202102036. PMID:34328642 doi:http://dx.doi.org/10.1002/chem.202102036

1 Structural highlights
2 Publication Abstract from PubMed
3 See Also
4 References

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PDB ID 7p6v

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Categories: Large Structures | Chung C

7p6v

From Proteopedia

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH compound 3ag

Structural highlights

Publication Abstract from PubMed

See Also

References

Contents

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