Discovery of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1

Anders A. Jensen; Mette N. Erichsen; Christina W. Nielsen; Tine B. Stensbøl; Jan Kehler; Lennart Bunch

doi:10.1021/jm8013458

Discovery of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1

Journal of Medicinal Chemistry ◽

10.1021/jm8013458 ◽

2009 ◽

Vol 52 (4) ◽

pp. 912-915 ◽

Cited By ~ 62

Author(s):

Anders A. Jensen ◽

Mette N. Erichsen ◽

Christina W. Nielsen ◽

Tine B. Stensbøl ◽

Jan Kehler ◽

...

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Selective Inhibitor ◽

Excitatory Amino Acid Transporter ◽

Acid Transporter

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Faculty Opinions recommendation of Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain.

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

10.3410/f.717971390.793470624 ◽

2013 ◽

Author(s):

Robert Vandenberg

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Selective Inhibitor ◽

Allosteric Modulation ◽

Excitatory Amino Acid Transporter ◽

Acid Transporter ◽

Subtype Selective ◽

Sustained Inhibition

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Chemo-Enzymatic Synthesis of (2S,4R)-2-Amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic Acid: A Novel Selective Inhibitor of Human Excitatory Amino Acid Transporter Subtype 2

Journal of Medicinal Chemistry ◽

10.1021/jm800091e ◽

2008 ◽

Vol 51 (14) ◽

pp. 4085-4092 ◽

Cited By ~ 13

Author(s):

Emanuelle Sagot ◽

Anders A. Jensen ◽

Darryl S. Pickering ◽

Xiaosui Pu ◽

Michelle Umberti ◽

...

Keyword(s):

Amino Acid ◽

Enzymatic Synthesis ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Selective Inhibitor ◽

Excitatory Amino Acid Transporter ◽

Acid Transporter ◽

Pentanedioic Acid

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Structure−Activity Relationship Study of First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101)

Journal of Medicinal Chemistry ◽

10.1021/jm1009154 ◽

2010 ◽

Vol 53 (19) ◽

pp. 7180-7191 ◽

Cited By ~ 82

Author(s):

Mette N. Erichsen ◽

Tri H. V. Huynh ◽

Bjarke Abrahamsen ◽

Jesper F. Bastlund ◽

Christoffer Bundgaard ◽

...

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Structure Activity Relationship ◽

Amino Acid Transporter ◽

Selective Inhibitor ◽

Activity Relationship ◽

Excitatory Amino Acid Transporter ◽

Structure Activity ◽

Relationship Study ◽

Acid Transporter

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Allosteric Modulation of an Excitatory Amino Acid Transporter: The Subtype-Selective Inhibitor UCPH-101 Exerts Sustained Inhibition of EAAT1 through an Intramonomeric Site in the Trimerization Domain

Journal of Neuroscience ◽

10.1523/jneurosci.3396-12.2013 ◽

2013 ◽

Vol 33 (3) ◽

pp. 1068-1087 ◽

Cited By ~ 34

Author(s):

B. Abrahamsen ◽

N. Schneider ◽

M. N. Erichsen ◽

T. H. V. Huynh ◽

C. Fahlke ◽

...

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Selective Inhibitor ◽

Allosteric Modulation ◽

Excitatory Amino Acid Transporter ◽

Acid Transporter ◽

Subtype Selective ◽

Sustained Inhibition

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A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2

European Journal of Pharmacology ◽

10.1016/s0014-2999(00)00625-7 ◽

2000 ◽

Vol 406 (1) ◽

pp. 41-44 ◽

Cited By ~ 14

Author(s):

Hans Bräuner-Osborne ◽

Mette B Hermit ◽

Birgitte Nielsen ◽

Povl Krogsgaard-Larsen ◽

Tommy N Johansen

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Selective Inhibitor ◽

Excitatory Amino Acid Transporter ◽

Structural Class ◽

Acid Transporter ◽

Subtype Selective

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Excitatory amino acid transporter 3 and the glutamate/cystine antiporter system Xc- cooperatively protect neuronal HT22 cells from oxidative glutamate toxicity

Aktuelle Neurologie ◽

10.1055/s-2004-833373 ◽

2004 ◽

Vol 31 (S 1) ◽

Author(s):

M Klein ◽

A Methner ◽

J Lewerenz

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Glutamate Toxicity ◽

Excitatory Amino Acid Transporter ◽

Ht22 Cells ◽

Acid Transporter

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The importance of the excitatory amino acid transporter 3 (EAAT3)

Neurochemistry International ◽

10.1016/j.neuint.2016.05.007 ◽

2016 ◽

Vol 98 ◽

pp. 4-18 ◽

Cited By ~ 30

Author(s):

Walden E. Bjørn-Yoshimoto ◽

Suzanne M. Underhill

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Excitatory Amino Acid Transporter ◽

Acid Transporter

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Excitatory Amino Acid Transporter

Encyclopedia of Biophysics ◽

10.1007/978-3-642-16712-6_100291 ◽

2013 ◽

pp. 715-715

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Excitatory Amino Acid Transporter ◽

Acid Transporter

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Association study of the excitatory amino acid transporter 2 (EAAT2) and glycine transporter 1 (GlyT1) gene polymorphism with schizophrenia in a Polish population

Neuropsychiatric Disease and Treatment ◽

10.2147/ndt.s194924 ◽

2019 ◽

Vol Volume 15 ◽

pp. 989-1000 ◽

Cited By ~ 1

Author(s):

Wojciech Merk ◽

Krzysztof Kucia ◽

Tomasz Mędrala ◽

Małgorzata Kowalczyk ◽

Aleksander Owczarek ◽

...

Keyword(s):

Amino Acid ◽

Gene Polymorphism ◽

Association Study ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Polish Population ◽

Excitatory Amino Acid Transporter ◽

Glycine Transporter 1 ◽

Glycine Transporter ◽

Acid Transporter

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Synthesis and Biological Evaluation of Novel Neuroprotective Pyridazine Derivatives as Excitatory Amino Acid Transporter 2 (EAAT2) Activators

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.7b00383 ◽

2017 ◽

Vol 60 (12) ◽

pp. 5216-5221 ◽

Cited By ~ 5

Author(s):

Alessia Chelini ◽

Simone Brogi ◽

Marco Paolino ◽

Angela Di Capua ◽

Andrea Cappelli ◽

...

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Biological Evaluation ◽

Excitatory Amino Acid Transporter ◽

Acid Transporter ◽

Pyridazine Derivatives ◽

Synthesis And Biological Evaluation

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