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Biophysical approach reveals a novel allosteric ligand binding site of SMYD3 histone methyltransferase

Talibov, Vladimir O., 1991- (author)
Uppsala universitet,Institutionen för kemi - BMC
Faibini, Edoardo (author)
Department of Pharmacy and Biotechnology, University of Bologna
FitzGerald, Edward A. (author)
Uppsala universitet,Institutionen för kemi - BMC
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Mihalic, Filip (author)
Uppsala universitet,Institutionen för kemi - BMC
Talu, Martin J. (author)
Department of Biology and Biological Engineering, Chalmers University of Technology
Rachman, Moira M. (author)
Institute of Biomedicine, University of Barcelona
Bartolini, Manuela (author)
Department of Pharmacy and Biotechnology, University of Bologna
Del Rio, Alberto (author)
Department of Pharmacy and Biotechnology, University of Bologna
Barril, Xavier (author)
Institute of Biomedicine, University of Barcelona
Dobritzsch, Doreen (author)
Uppsala universitet,Institutionen för kemi - BMC
Danielson, U. Helena (author)
Uppsala universitet,Institutionen för kemi - BMC
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 (creator_code:org_t)
English.
  • Other publication (other academic/artistic)
Abstract Subject headings
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  • SET-and MYND-domain containing protein 3 (SMYD3) is a lysine methyltransferase that plays a role in epigenetic regulation. The protein was shown to have cancerogenic activities and is considered to be a perspective drug target. Here, we propose a Surface Plasmon Resonance-based (SPR) biophysical platform to aid SMYD3 drug discovery. The SPR screening assay was validated with a small subset of drug-like compounds, and resulted in an assay hit. The hit compound-SMYD3 complex structure was solved, and a new allosteric ligand binding site of the protein was revealed. The interaction was found localized within the previously reported SMYD3-heat shock protein 90 (HSP90) recognition site, thereby rendering the hit compound as a perspective candidate for a development of a protein-protein interface inhibitor.

Subject headings

NATURVETENSKAP  -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
NATURAL SCIENCES  -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)

Keyword

Biokemi
Biochemistry
Medicinal Chemistry
Läkemedelskemi
Biokemi
Biochemistry

Publication and Content Type

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ovr (subject category)

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