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Journal articles
A New Potent Inhibitor of Glycogen Phosphorylase Reveals the Basicity of the Catalytic Site
Michael Mamais
1
Alessandra Degli esposti
2
Virginia Kouloumoundra
1
Thomas Gustavsson
3, 4
Filippo Monti
5
Alessandro Venturini
2
Evangelia D. Chrysina
6
Dimitra Markovitsi
3, 4
Thanasis Gimisis
1
4
DICO - Biomolécules Excitées
IRAMIS - Institut Rayonnement Matière de Saclay, LIDyl - Laboratoire Interactions, Dynamiques et Lasers (ex SPAM)
5
Gulliver
Michael Mamais 1
Author
Alessandra Degli esposti 2
Author
Virginia Kouloumoundra 1
Author
Thomas Gustavsson 3, 4
Author
Filippo Monti 5
Author
Alessandro Venturini 2
Author
Evangelia D. Chrysina 6
Author
Dimitra Markovitsi 3, 4
Author
Thanasis Gimisis 1
Author
1
NKUA - National and Kapodistrian University of Athens (Athens 157 72 - Greece)
2
ISOF-CNR - Istituto per la Sintesi Organica e la Fotoreattività (Via P. Gobetti, 101 - 40129 Bologna - Italy)
- CNR - Consiglio Nazionale delle Ricerche (Piazzale Aldo Moro, 7, 00185 Roma RM - Italy)
3
LIDyl - Laboratoire Interactions, Dynamiques et Lasers (ex SPAM) (LIDYL, CEA, CNRS, Université Paris-Saclay, CEA Saclay 91190 Gif sur Yvette - France)
- Université Paris-Saclay (Espace Technologique, Bat. Discovery - RD 128 - 2e ét., 91190 Saint-Aubin - France)
- CEA - Commissariat à l'énergie atomique et aux énergies alternatives : DRF/IRAMIS (Centre de Saclay Centre de Grenoble Centre de Cadarache etc - France)
- CNRS - Centre National de la Recherche Scientifique : UMR9222 (France)
4
DICO - Biomolécules Excitées (France)
- IRAMIS - Institut Rayonnement Matière de Saclay (91191 Gif-sur-Yvette, France - France)
- CEA - Commissariat à l'énergie atomique et aux énergies alternatives : DRF/IRAMIS (Centre de Saclay Centre de Grenoble Centre de Cadarache etc - France)
- Université Paris-Saclay (Espace Technologique, Bat. Discovery - RD 128 - 2e ét., 91190 Saint-Aubin - France)
- LIDyl - Laboratoire Interactions, Dynamiques et Lasers (ex SPAM) (LIDYL, CEA, CNRS, Université Paris-Saclay, CEA Saclay 91190 Gif sur Yvette - France)
- Université Paris-Saclay (Espace Technologique, Bat. Discovery - RD 128 - 2e ét., 91190 Saint-Aubin - France)
- CEA - Commissariat à l'énergie atomique et aux énergies alternatives : DRF/IRAMIS (Centre de Saclay Centre de Grenoble Centre de Cadarache etc - France)
- CNRS - Centre National de la Recherche Scientifique : UMR9222 (France)
5
Gulliver (ESPCI Paris
10, rue Vauquelin
75231 Paris cedex 05 - France)
- ESPCI Paris - Ecole Superieure de Physique et de Chimie Industrielles de la Ville de Paris (10 rue Vauquelin, 75231 Paris cedex 05 - France)
- PSL - Université Paris sciences et lettres (60 rue Mazarine 75006 Paris - France)
- CNRS - Centre National de la Recherche Scientifique : UMR7083 (France)
Abstract : The design and synthesis of a glucose-based acridone derivative (GLAC), a potent inhibitor of glycogen phosphorylase (GP) are described. GLAC is the first inhibitor of glycogen phosphorylase, the electronic absorption properties of which are clearly distinguishable from those of the enzyme. This allows probing subtle interactions in the catalytic site. The GLAC absorption spectra, associated with X-ray crystallography and quantum chemistry calculations, reveal that part of the catalytic site of GP behaves as a highly basic environment in which GLAC exists as a bis-anion. This is explained by water-bridged hydrogen-bonding interactions with specific catalytic site residues.
Document type :
Journal articles
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https://hal-cea.archives-ouvertes.fr/cea-01571665
Contributor : Caroline Lebe <>
Submitted on : Thursday, August 3, 2017 - 11:48:15 AM
Last modification on : Thursday, November 26, 2020 - 3:50:03 PM
Contributor : Caroline Lebe <>
Submitted on : Thursday, August 3, 2017 - 11:48:15 AM
Last modification on : Thursday, November 26, 2020 - 3:50:03 PM
Identifiers
- HAL Id : cea-01571665, version 1
- DOI : 10.1002/chem.201701591
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Citation
Michael Mamais, Alessandra Degli esposti, Virginia Kouloumoundra, Thomas Gustavsson, Filippo Monti, et al.. A New Potent Inhibitor of Glycogen Phosphorylase Reveals the Basicity of the Catalytic Site . Chemistry - A European Journal, Wiley-VCH Verlag, 2017, 23 (37), pp.8800-8805 ⟨10.1002/chem.201701591⟩. ⟨cea-01571665⟩
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