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Biophysical approac...
Biophysical approach reveals a novel allosteric ligand binding site of SMYD3 histone methyltransferase
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- Talibov, Vladimir O., 1991- (author)
- Uppsala universitet,Institutionen för kemi - BMC
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- Faibini, Edoardo (author)
- Department of Pharmacy and Biotechnology, University of Bologna
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- FitzGerald, Edward A. (author)
- Uppsala universitet,Institutionen för kemi - BMC
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- Mihalic, Filip (author)
- Uppsala universitet,Institutionen för kemi - BMC
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- Talu, Martin J. (author)
- Department of Biology and Biological Engineering, Chalmers University of Technology
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- Rachman, Moira M. (author)
- Institute of Biomedicine, University of Barcelona
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- Bartolini, Manuela (author)
- Department of Pharmacy and Biotechnology, University of Bologna
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- Del Rio, Alberto (author)
- Department of Pharmacy and Biotechnology, University of Bologna
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- Barril, Xavier (author)
- Institute of Biomedicine, University of Barcelona
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- Dobritzsch, Doreen (author)
- Uppsala universitet,Institutionen för kemi - BMC
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- Danielson, U. Helena (author)
- Uppsala universitet,Institutionen för kemi - BMC
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(creator_code:org_t)
- English.
- Related links:
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https://urn.kb.se/re...
Abstract
Subject headings
Close
- 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
- vet (subject category)
- ovr (subject category)
To the university's database
- By the author/editor
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Talibov, Vladimi ...
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Faibini, Edoardo
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FitzGerald, Edwa ...
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Mihalic, Filip
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Talu, Martin J.
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Rachman, Moira M ...
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show more...
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Bartolini, Manue ...
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Del Rio, Alberto
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Barril, Xavier
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Dobritzsch, Dore ...
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Danielson, U. He ...
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show less...
- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Biological Scien ...
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and Biochemistry and ...
- By the university
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Uppsala University