Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. (Q39736371)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24900455%20AND%20SRC:MED&resulttype=core&format=json

20 March 2020

title

Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia (English)

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20 March 2020

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15

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20 March 2020

author name string

Amy B Dounay

1

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20 March 2020

Marie Anderson

2

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20 March 2020

Bruce M Bechle

3

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20 March 2020

Brian M Campbell

4

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20 March 2020

Michelle M Claffey

5

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20 March 2020

Artem Evdokimov

6

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20 March 2020

Edelweiss Evrard

7

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20 March 2020

Kari R Fonseca

8

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20 March 2020

Xinmin Gan

9

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20 March 2020

Somraj Ghosh

10

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20 March 2020

Matthew M Hayward

11

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20 March 2020

Weldon Horner

12

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20 March 2020

Ji-Young Kim

13

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20 March 2020

Laura A McAllister

14

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20 March 2020

Vanessa Paradis

16

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20 March 2020

Vinod D Parikh

17

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20 March 2020

Matthew R Reese

18

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20 March 2020

SuoBao Rong

19

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20 March 2020

Michelle A Salafia

20

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20 March 2020

Katherine Schuyten

21

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20 March 2020

Christine A Strick

22

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20 March 2020

Jamison B Tuttle

23

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20 March 2020

James Valentine

24

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20 March 2020

Hong Wang

25

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20 March 2020

Laura E Zawadzke

26

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20 March 2020

Patrick R Verhoest

27

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20 March 2020

publication date

25 January 2012

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ACS Medicinal Chemistry Letters

20 March 2020

published in

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20 March 2020

volume

3

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20 March 2020

issue

3

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20 March 2020

page(s)

187-192

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Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties

20 March 2020

cites work

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

The resurgence of covalent drugs

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Crystal Structure-Based Selective Targeting of the Pyridoxal 5′-Phosphate Dependent Enzyme Kynurenine Aminotransferase II for Cognitive Enhancement

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Elevated levels of kynurenic acid in the cerebrospinal fluid of patients with bipolar disorder

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Reduction of endogenous kynurenic acid formation enhances extracellular glutamate, hippocampal plasticity, and cognitive behavior

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Kynurenic acid is a potent endogenous aryl hydrocarbon receptor ligand that synergistically induces interleukin-6 in the presence of inflammatory signaling

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Structure, expression, and function of kynurenine aminotransferases in human and rodent brains

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

The astrocyte-derived alpha7 nicotinic receptor antagonist kynurenic acid controls extracellular glutamate levels in the prefrontal cortex

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Physicochemical drug properties associated with in vivo toxicological outcomes: a review

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Pharmacological manipulation of kynurenic acid: potential in the treatment of psychiatric disorders

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Crystal structure of human kynurenine aminotransferase II, a drug target for the treatment of schizophrenia

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

The kynurenic acid hypothesis of schizophrenia

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Ligand efficiency: a useful metric for lead selection

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

The brain metabolite kynurenic acid inhibits alpha7 nicotinic receptor activity and increases non-alpha7 nicotinic receptor expression: physiopathological implications

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Fast Calculation of Molecular Polar Surface Area as a Sum of Fragment-Based Contributions and Its Application to the Prediction of Drug Transport Properties

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

On the relationship between the two branches of the kynurenine pathway in the rat brain in vivo

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Specific inhibition of kynurenate synthesis enhances extracellular dopamine levels in the rodent striatum.

25 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

A glycine site associated with N-methyl-D-aspartic acid receptors: characterization and identification of a new class of antagonists

17 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Increased cortical kynurenate content in schizophrenia

17 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Biochemical and structural investigations on kynurenine aminotransferase II: an example of conformation-driven species-specific inhibition?

17 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Sequence variants in kynurenine aminotransferase II (KAT II) orthologs determine different potencies of the inhibitor S-ESBA.

20 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Elevated levels of kynurenic acid in the cerebrospinal fluid of male patients with schizophrenia

20 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Kynurenic acid levels are elevated in the cerebrospinal fluid of patients with schizophrenia

20 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4025856

Modulators of the Kynurenine Pathway of Tryptophan Metabolism: Synthesis and Preliminary Biological Evaluation of (S)-4-(Ethylsulfonyl)benzoylalanine, a Potent and Selective Kynurenine Aminotransferase II (KAT II) Inhibitor

20 August 2018

1 reference

12 December 2020

The influence of lead discovery strategies on the properties of drug candidates

1 reference

12 December 2020

Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists

1 reference

12 December 2020

A general strategy for the synthesis of cyclic N-aryl hydroxamic acids via partial nitro group reduction

1 reference

12 December 2020

Identifiers

DOI

10.1021/ML200204M

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20 March 2020

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20 March 2020

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