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PDBsum entry 4lys

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Protein binding/inhibitor PDB id
4lys
Contents
Protein chain
124 a.a.
Ligands
2SJ
Metals
_NA ×2
Waters ×121

References listed in PDB file
Key reference
Title 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading.
Authors X.Lucas, D.Wohlwend, M.Hügle, K.Schmidtkunz, S.Gerhardt, R.Schüle, M.Jung, O.Einsle, S.Günther.
Ref. Angew Chem Int Ed Engl, 2013, 52, 14055-14059. [DOI no: 10.1002/anie.201307652]
PubMed id 24272870
Abstract
Bromodomains are acetyllysine epigenetic mark reader proteins. Small molecules inhibiting them have potential as anti-inflammatory, antiviral, and anticancer agents. A 4-acyl pyrrole derivative (see yellow structure in recognition pocket) has been identified that potently inhibits specific bromodomains and exhibits antiproliferative activity against leukemia cell lines.
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