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)

Mette N. Erichsen; Tri H. V. Huynh; Bjarke Abrahamsen; Jesper F. Bastlund; Christoffer Bundgaard; Olja Monrad; Anders Bekker-Jensen; Christina W. Nielsen; Karla Frydenvang; Anders A. Jensen; Lennart Bunch

doi:10.1021/jm1009154

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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Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure–Activity Relationship Study

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.6b01058 ◽

2016 ◽

Vol 59 (19) ◽

pp. 8757-8770 ◽

Cited By ~ 11

Author(s):

Stinne W. Hansen ◽

Mette N. Erichsen ◽

Bingru Fu ◽

Walden E. Bjørn-Yoshimoto ◽

Bjarke Abrahamsen ◽

...

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Structure Activity Relationship ◽

Amino Acid Transporter ◽

Activity Relationship ◽

Excitatory Amino Acid Transporter ◽

New Class ◽

Structure Activity ◽

Relationship Study ◽

Acid Transporter

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Identification and Structure–Activity Relationship Study of Imidazo[1,2-a]pyridine-3-amines as First Selective Inhibitors of Excitatory Amino Acid Transporter Subtype 3 (EAAT3)

ACS Chemical Neuroscience ◽

10.1021/acschemneuro.9b00447 ◽

2019 ◽

Vol 10 (10) ◽

pp. 4414-4429

Author(s):

Peng Wu ◽

Walden E. Bjørn-Yoshimoto ◽

Markus Staudt ◽

Anders A. Jensen ◽

Lennart Bunch

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Structure Activity Relationship ◽

Amino Acid Transporter ◽

Activity Relationship ◽

Selective Inhibitors ◽

Excitatory Amino Acid Transporter ◽

Structure Activity ◽

Relationship Study ◽

Subtype 3

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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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Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the Excitatory Amino Acid Transporters (EAATs): improving the potency of a micromolar screening Hit is not truism

SpringerPlus ◽

10.1186/2193-1801-2-112 ◽

2013 ◽

Vol 2 (1) ◽

pp. 112

Author(s):

Tri HV Huynh ◽

Charles S Demmer ◽

Bjarke Abrahamsen ◽

Emil Marcher ◽

Mikael Frykman ◽

...

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Amino Acid Transporters ◽

Excitatory Amino Acid Transporters ◽

Structure Activity ◽

Relationship Study ◽

Potential Inhibitors

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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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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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Three-dimensional quantitative structure–activity relationship analyses of substrates of the human proton-coupled amino acid transporter 1 (hPAT1)

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2011.08.058 ◽

2011 ◽

Vol 19 (21) ◽

pp. 6409-6418 ◽

Cited By ~ 7

Author(s):

Iris Thondorf ◽

Valerie Voigt ◽

Sarah Schäfer ◽

Sabine Gebauer ◽

Katja Zebisch ◽

...

Keyword(s):

Amino Acid ◽

Three Dimensional ◽

Quantitative Structure Activity Relationship ◽

Structure Activity Relationship ◽

Amino Acid Transporter ◽

Activity Relationship ◽

Quantitative Structure ◽

Structure Activity ◽

Acid Transporter

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Loratadine and Analogues: Discovery and Preliminary Structure–Activity Relationship of Inhibitors of the Amino Acid Transporter B0AT2

Journal of Medicinal Chemistry ◽

10.1021/jm501086v ◽

2014 ◽

Vol 57 (22) ◽

pp. 9473-9479 ◽

Cited By ~ 11

Author(s):

Serena Cuboni ◽

Christian Devigny ◽

Bastiaan Hoogeland ◽

Andrea Strasser ◽

Sebastian Pomplun ◽

...

Keyword(s):

Amino Acid ◽

Structure Activity Relationship ◽

Amino Acid Transporter ◽

Activity Relationship ◽

Structure Activity ◽

Acid Transporter ◽

Relationship Of

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Structure–activity relationship study of compounds binding to large amino acid transporter 1 (LAT1) based on pharmacophore modeling and in situ rat brain perfusion

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2012.11.014 ◽

2013 ◽

Vol 48 (3) ◽

pp. 523-531 ◽

Cited By ~ 26

Author(s):

Henna Ylikangas ◽

Lauri Peura ◽

Kalle Malmioja ◽

Jukka Leppänen ◽

Krista Laine ◽

...

Keyword(s):

Amino Acid ◽

Rat Brain ◽

Brain Perfusion ◽

Structure Activity Relationship ◽

Amino Acid Transporter ◽

Pharmacophore Modeling ◽

Activity Relationship ◽

Structure Activity ◽

Relationship Study

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Structure-activity relationship of a novel series of inhibitors for cancer type transporter L-type amino acid transporter 1 (LAT1)

Journal of Pharmacological Sciences ◽

10.1016/j.jphs.2017.01.006 ◽

2017 ◽

Vol 133 (2) ◽

pp. 96-102 ◽

Cited By ~ 31

Author(s):

Pornparn Kongpracha ◽

Shushi Nagamori ◽

Pattama Wiriyasermkul ◽

Yoko Tanaka ◽

Kazuko Kaneda ◽

...

Keyword(s):

Amino Acid ◽

Structure Activity Relationship ◽

Amino Acid Transporter ◽

Activity Relationship ◽

Cancer Type ◽

Structure Activity ◽

Acid Transporter ◽

Relationship Of

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