(Q36128825)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

title

Small-Molecule Inhibitors of GSK-3: Structural Insights and Their Application to Alzheimer's Disease Models (English)

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

0 references

2

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

author name string

Thomas Kramer

series ordinal

1

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

Fabio Lo Monte

series ordinal

3

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

publication date

22 July 2012

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

International journal of Alzheimer's disease

11 February 2020

published in

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

volume

2012

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

page(s)

381029

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

Creative Commons Attribution 3.0 Unported

11 February 2020

copyright license

start time

1 January 2012

1 reference

April 2022 Public Data File from Crossref

copyright status

copyrighted

1 reference

April 2022 Public Data File from Crossref

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2 October 2017

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Substrate competitive GSK-3 inhibitors - strategy and implications

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The marine natural-derived inhibitors of glycogen synthase kinase-3beta phenylmethylene hydantoins: In vitro and in vivo activities and pharmacophore modeling

2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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Efficacy of small-molecule glycogen synthase kinase-3 inhibitors in the postnatal rat model of tau hyperphosphorylation

2 October 2017

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Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3beta

2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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Current advances on different kinases involved in tau phosphorylation, and implications in Alzheimer's disease and tauopathies

2 October 2017

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Inhibition of glycogen synthase kinase-3 by lithium correlates with reduced tauopathy and degeneration in vivo

2 October 2017

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Structure-aided optimization of kinase inhibitors derived from alsterpaullone.

2 October 2017

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The development of potent and selective bisarylmaleimide GSK3 inhibitors.

2 October 2017

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Glycogen synthase kinase 3: a drug target for CNS therapies

2 October 2017

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GSK3 inhibitors: development and therapeutic potential

2 October 2017

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Design, synthesis, and biological evaluation of novel 7-azaindolyl-heteroaryl-maleimides as potent and selective glycogen synthase kinase-3beta (GSK-3beta) inhibitors

2 October 2017

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3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.

2 October 2017

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Novel GSK-3 inhibitors with improved cellular activity

2 October 2017

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Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.

2 October 2017

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Synthesis and biological evaluation of novel macrocyclic bis-7-azaindolylmaleimides as potent and highly selective glycogen synthase kinase-3 beta (GSK-3 beta) inhibitors

2 October 2017

1 reference

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Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor

2 October 2017

1 reference

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GSK-3-selective inhibitors derived from Tyrian purple indirubins

2 October 2017

1 reference

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Structural characterization of the GSK-3beta active site using selective and non-selective ATP-mimetic inhibitors

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Triple-transgenic model of Alzheimer's disease with plaques and tangles: intracellular Abeta and synaptic dysfunction

2 October 2017

1 reference

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GSK-3alpha regulates production of Alzheimer's disease amyloid-beta peptides

2 October 2017

1 reference

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Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation

2 October 2017

1 reference

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Glycogen synthase kinase 3: an emerging therapeutic target

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

The structure of phosphorylated GSK-3beta complexed with a peptide, FRATtide, that inhibits beta-catenin phosphorylation

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

GSK3 takes centre stage more than 20 years after its discovery

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Enhanced neurofibrillary degeneration in transgenic mice expressing mutant tau and APP.

2 October 2017

1 reference

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The effect of 1,3-diaryl-[1H]-pyrazole-4-acetamides on glucose utilization in ob/ob mice

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Structure of GSK3beta reveals a primed phosphorylation mechanism

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Decreased nuclear beta-catenin, tau hyperphosphorylation and neurodegeneration in GSK-3beta conditional transgenic mice

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Lithium inhibits glycogen synthase kinase-3 by competition for magnesium.

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Studies on new acidic azoles as glucose-lowering agents in obese, diabetic db/db mice

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Protein kinases — structure and function

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

A new alkaloid AM-2282 OF Streptomyces origin. Taxonomy, fermentation, isolation and preliminary characterization

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds

2 October 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Discovery of novel GSK-3β inhibitors with potent in vitro and in vivo activities and excellent brain permeability using combined ligand- and structure-based virtual screening

2 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode

2 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death

2 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Neurofibrillary tangles, amyotrophy and progressive motor disturbance in mice expressing mutant (P301L) tau protein

2 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Spectroscopic studies of GSK3{beta} phosphorylation of the neuronal tau protein and its interaction with the N-terminal domain of apolipoprotein E.

2 July 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

An English translation of Alzheimer's 1907 paper, "Uber eine eigenartige Erkankung der Hirnrinde".

21 January 2018

1 reference

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A novel GSK-3beta inhibitor reduces Alzheimer's pathology and rescues neuronal loss in vivo.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Glycogen synthase kinase-3beta phosphorylates protein tau and rescues the axonopathy in the central nervous system of human four-repeat tau transgenic mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Lithium inhibits caspase 3 activation and dephosphorylation of PKB and GSK3 induced by K+ deprivation in cerebellar granule cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Structure-based design leads to the identification of lithium mimetics that block mania-like effects in rodents. possible new GSK-3beta therapies for bipolar disorders

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Absolute Configuration of Staurosporine By X-Ray Analysis

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Synthesis and kinase inhibitory activity of novel substituted indigoids.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Intracellular Targets of Paullones. Identification following affinity purification on immobilized inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Efficacy of a novel, orally active GSK-3 inhibitor 6-Methyl-N-[3-[[3-(1-methylethoxy)propyl]carbamoyl]-1H-pyrazol-4-yl]pyridine-3-carboxamide in tau transgenic mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

A novel glycogen synthase kinase-3 inhibitor 2-methyl-5-(3-{4-[(S )-methylsulfinyl]phenyl}-1-benzofuran-5-yl)-1,3,4-oxadiazole decreases tau phosphorylation and ameliorates cognitive deficits in a transgenic model of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Propentofylline attenuates tau hyperphosphorylation in Alzheimer's Swedish mutant model Tg2576.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Structural features underlying selective inhibition of GSK3β by dibromocantharelline: implications for rational drug design

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Structural basis for the GSK-3beta binding affinity and selectivity against CDK-2 of 1-(4-aminofurazan-3yl)-5-dialkylaminomethyl-1H-[1,2,3] triazole-4-carboxylic acid derivatives

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Characterization of a double (amyloid precursor protein-tau) transgenic: tau phosphorylation and aggregation

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Accelerated amyloid deposition, neurofibrillary degeneration and neuronal loss in double mutant APP/tau transgenic mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Stress-induced hyperphosphorylation of tau in the mouse brain

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Lithium inhibits stress-induced changes in tau phosphorylation in the mouse hippocampus

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Developmental expression and localization of glycogen synthase kinase-3beta in rat brain

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Distribution of tau protein kinase I/glycogen synthase kinase-3beta, phosphatases 2A and 2B, and phosphorylated tau in the developing rat brain.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Tau and GSK3beta dephosphorylations are required for regulating Pin1 phosphorylation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

Effects of a glycogen synthase kinase-3 inhibitor, lithium, in adenomatous polyposis coli mutant mice.

21 January 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3408674

Selective loss of glycogen synthase kinase-3α in birds reveals distinct roles for GSK-3 isozymes in tau phosphorylation

23 September 2018

1 reference

https://api.crossref.org/works/10.1155%2F2012%2F381029

5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3)

21 January 2018

1 reference

12 December 2020

An organometallic inhibitor for glycogen synthase kinase 3

1 reference

12 December 2020

Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core

1 reference

12 December 2020

Transgenic zebrafish as a novel animal model to study tauopathies and other neurodegenerative disorders in vivo

1 reference

12 December 2020

New potent antihyperglycemic agents in db/db mice: synthesis and structure-activity relationship studies of (4-substituted benzyl) (trifluoromethyl)pyrazoles and -pyrazolones

1 reference

12 December 2020

The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity

1 reference

12 December 2020

Identifiers

DOI

10.1155/2012/381029

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json

11 February 2020

PubMed publication ID

22888461

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22888461%20AND%20SRC:MED&resulttype=core&format=json