The molecular chaperone TRAP1 regulates energy metabolism, and its activity is relevant in cancer and degenerative diseases. Here, Sanchez-Martin et al. identify highly selective allosteric inhibitors of TRAP1. These compounds revert biochemical and pro-neoplastic effects of TRAP1 and could both enlighten its mode of action and disclose novel therapeutic strategies.

Sanchez-Martin, C., Moroni, E., Ferraro, M., Laquatra, C., Cannino, G., Masgras, I., et al. (2020). Rational Design of Allosteric and Selective Inhibitors of the Molecular Chaperone TRAP1. CELL REPORTS, 31(3), 107531 [10.1016/j.celrep.2020.107531].

Rational Design of Allosteric and Selective Inhibitors of the Molecular Chaperone TRAP1

Carlos Sanchez-Martin;
2020-01-01

Abstract

The molecular chaperone TRAP1 regulates energy metabolism, and its activity is relevant in cancer and degenerative diseases. Here, Sanchez-Martin et al. identify highly selective allosteric inhibitors of TRAP1. These compounds revert biochemical and pro-neoplastic effects of TRAP1 and could both enlighten its mode of action and disclose novel therapeutic strategies.
2020
Pubblicato
Rilevanza internazionale
Articolo
Esperti anonimi
Settore BIOS-07/A - Biochimica
English
allosteric ligands; anticancer compound; cancer cell; chaperone inhibitors; HSP90; mitochondria; neurofibroma;
mitochondrial biology; molecular dynamics; TRAP; zebrafish; Allosteric Regulation; animals; Antineoplastic Agents;
Drug Design; female; HSP90 Heat-Shock Proteins; humans; Male; Mice; Molecular Chaperones; Zebrafish;
Molecular Dynamics Simulation; Nerve Sheath Neoplasms; Recombinant Proteins; Small Molecule Libraries
allosteric ligands; anticancer compound; cancer cells; chaperone inhibitors; HSP90; mitochondria; mitochondrial biology; molecular dynamics; neurofibroma; TRAP1; zebrafish
https://www.cell.com/cell-reports/fulltext/S2211-1247(20)30431-9?_returnURL=https://linkinghub.elsevier.com/retrieve/pii/S2211124720304319?showall=true
Sanchez-Martin, C., Moroni, E., Ferraro, M., Laquatra, C., Cannino, G., Masgras, I., et al. (2020). Rational Design of Allosteric and Selective Inhibitors of the Molecular Chaperone TRAP1. CELL REPORTS, 31(3), 107531 [10.1016/j.celrep.2020.107531].
Sanchez-Martin, C; Moroni, E; Ferraro, M; Laquatra, C; Cannino, G; Masgras, I; Negro, A; Quadrelli, P; Rasola, A; Colombo, G
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/408831
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