Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor

Saara Laulumaa; Kathrine Voigt Hansen; Magdalena Masternak; Thomas Drapier; Pierre Francotte; Bernard Pirotte; Karla Frydenvang; Jette Sandholm Kastrup

doi:10.1021/acsmedchemlett.8b00369

Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor

ACS Medicinal Chemistry Letters ◽

10.1021/acsmedchemlett.8b00369 ◽

2018 ◽

Vol 10 (3) ◽

pp. 243-247

Author(s):

Saara Laulumaa ◽

Kathrine Voigt Hansen ◽

Magdalena Masternak ◽

Thomas Drapier ◽

Pierre Francotte ◽

...

Keyword(s):

Ligand Binding ◽

Crystal Structures ◽

Binding Domain ◽

Ligand Binding Domain ◽

Allosteric Modulators ◽

Positive Allosteric Modulators

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Thermodynamic Characterization of New Positive Allosteric Modulators Binding to the Glutamate Receptor A2 Ligand-Binding Domain: Combining Experimental and Computational Methods Unravels Differences in Driving Forces

Journal of Chemical Information and Modeling ◽

10.1021/ci500559b ◽

2014 ◽

Vol 54 (12) ◽

pp. 3404-3416 ◽

Cited By ~ 14

Author(s):

Ann-Beth Nørholm ◽

Pierre Francotte ◽

Eric Goffin ◽

Iuliana Botez ◽

Laurence Danober ◽

...

Keyword(s):

Ligand Binding ◽

Glutamate Receptor ◽

Computational Methods ◽

Driving Forces ◽

Binding Domain ◽

Ligand Binding Domain ◽

Allosteric Modulators ◽

Thermodynamic Characterization ◽

Positive Allosteric Modulators

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Exploring the Role of Positive Allosteric Modulators in Stabilizing the GluR2 Ligand-Binding Domain Dimer

Biophysical Journal ◽

10.1016/j.bpj.2009.12.3323 ◽

2010 ◽

Vol 98 (3) ◽

pp. 609a

Author(s):

Christopher P. Ptak ◽

Ahmed H. Ahmed ◽

Michael K. Fenwick ◽

Alexander S. Maltsev ◽

Robert E. Oswald

Keyword(s):

Ligand Binding ◽

Binding Domain ◽

Ligand Binding Domain ◽

Allosteric Modulators ◽

Positive Allosteric Modulators

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Faculty Opinions recommendation of X-ray crystal structures of the estrogen-related receptor-gamma ligand binding domain in three functional states reveal the molecular basis of small molecule regulation.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1047292.497229 ◽

2006 ◽

Author(s):

Paul Webb

Keyword(s):

Ligand Binding ◽

Crystal Structures ◽

Small Molecule ◽

Molecular Basis ◽

Binding Domain ◽

Ligand Binding Domain ◽

X Ray ◽

Functional States ◽

Estrogen Related Receptor

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Faculty Opinions recommendation of Apo and InsP₃-bound crystal structures of the ligand-binding domain of an InsP₃ receptor.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.13323991.14688104 ◽

2011 ◽

Author(s):

Stephen Shears

Keyword(s):

Ligand Binding ◽

Crystal Structures ◽

Binding Domain ◽

Ligand Binding Domain

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Comparison of crystal structures of human androgen receptor ligand-binding domain complexed with various agonists reveals molecular determinants responsible for binding affinity

Protein Science ◽

10.1110/ps.051905906 ◽

2006 ◽

Vol 15 (5) ◽

pp. 987-999 ◽

Cited By ~ 149

Author(s):

Karine Pereira de Jésus-Tran ◽

Pierre-Luc Côté ◽

Line Cantin ◽

Jonathan Blanchet ◽

Fernand Labrie ◽

...

Keyword(s):

Androgen Receptor ◽

Ligand Binding ◽

Crystal Structures ◽

Binding Affinity ◽

Binding Domain ◽

Ligand Binding Domain ◽

Receptor Ligand ◽

Molecular Determinants ◽

Human Androgen Receptor

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First High-Resolution Crystal Structures of the Glucocorticoid Receptor Ligand-Binding Domain–Peroxisome Proliferator-Activated γ Coactivator 1-α Complex with Endogenous and Synthetic Glucocorticoids

Molecular Pharmacology ◽

10.1124/mol.119.116806 ◽

2019 ◽

Vol 96 (4) ◽

pp. 408-417 ◽

Cited By ~ 7

Author(s):

Xu Liu ◽

Yashuo Wang ◽

Eric A. Ortlund

Keyword(s):

High Resolution ◽

Glucocorticoid Receptor ◽

Ligand Binding ◽

Crystal Structures ◽

Binding Domain ◽

Ligand Binding Domain ◽

Peroxisome Proliferator ◽

Receptor Ligand ◽

Synthetic Glucocorticoids

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Analysis of Crystal Structures of LXRβ in Relation to Plasticity of the Ligand-Binding Domain upon Ligand Binding

Chemical Biology & Drug Design ◽

10.1111/j.1747-0285.2007.00620.x ◽

2008 ◽

Vol 71 (2) ◽

pp. 140-154 ◽

Cited By ~ 7

Author(s):

Nagulapalli Malini ◽

Hariharan Rajesh ◽

Pooja Berwal ◽

Samiron Phukan ◽

Vittukudi Narayanaiyengar Balaji

Keyword(s):

Ligand Binding ◽

Crystal Structures ◽

Binding Domain ◽

Ligand Binding Domain

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Correlating AMPA Receptor Activation and Cleft Closure across Subunits: Crystal Structures of the GluR4 Ligand-Binding Domain in Complex with Full and Partial Agonists†

Biochemistry ◽

10.1021/bi8013196 ◽

2008 ◽

Vol 47 (52) ◽

pp. 13831-13841 ◽

Cited By ~ 16

Author(s):

Avinash Gill ◽

Amanda Birdsey-Benson ◽

Brian L. Jones ◽

Leslie P. Henderson ◽

Dean R. Madden

Keyword(s):

Ligand Binding ◽

Crystal Structures ◽

Ampa Receptor ◽

Receptor Activation ◽

Binding Domain ◽

Ligand Binding Domain ◽

Partial Agonists ◽

Cleft Closure

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Ligand recognition by A‐class Eph receptors: crystal structures of the EphA2 ligand‐binding domain and the EphA2/ephrin‐A1 complex

EMBO Reports ◽

10.1038/embor.2009.91 ◽

2009 ◽

Vol 10 (7) ◽

pp. 722-728 ◽

Cited By ~ 72

Author(s):

Juha P Himanen ◽

Yehuda Goldgur ◽

Hui Miao ◽

Eugene Myshkin ◽

Hong Guo ◽

...

Keyword(s):

Ligand Binding ◽

Crystal Structures ◽

Binding Domain ◽

Ligand Binding Domain ◽

Ligand Recognition ◽

Eph Receptors

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Vitamin D Nuclear Receptor Ligand-Binding Domain Crystal Structures

Vitamin D ◽

10.1016/b978-012252687-9/50018-8 ◽

2005 ◽

pp. 279-289 ◽

Cited By ~ 1

Author(s):

NATACHA ROCHEL ◽

DINO MORAS

Keyword(s):

Vitamin D ◽

Ligand Binding ◽

Crystal Structures ◽

Nuclear Receptor ◽

Binding Domain ◽

Ligand Binding Domain ◽

Receptor Ligand

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