Target Information
Target General Infomation | |||||
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Target ID |
T70977
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Former ID |
TTDC00162
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Target Name |
Glycogen synthase kinase-3 beta
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Gene Name |
GSK3B
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Synonyms |
GSK-3 beta; GSK3B
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Target Type |
Clinical Trial
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Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
Acute myeloid leukemia; Acute promyelocytic leukemia [ICD9: 205.0, 208.9; ICD10: C91-C95, C92.0, C92.4] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | |||||
Osteosarcoma [ICD9: 170; ICD10: C40-C41] | |||||
Parkinson's disease [ICD9: 332; ICD10: G20] | |||||
Function |
Constitutively active protein kinase that acts as a negative regulator in the hormonal control of glucose homeostasis, Wnt signaling and regulation of transcription factors and microtubules, by phosphorylating and inactivating glycogen synthase (GYS1 or GYS2), EIF2B, CTNNB1/beta-catenin, APC, AXIN1, DPYSL2/CRMP2, JUN, NFATC1/NFATC, MAPT/TAU and MACF1. Requires primed phosphorylation of the majority of its substrates. In skeletal muscle, contributes to insulin regulation of glycogen synthesis by phosphorylating and inhibiting GYS1 activity and hence glycogen synthesis. May also mediate the development of insulin resistance by regulating activation of transcription factors. Regulates protein synthesis by controlling the activity of initiation factor 2B (EIF2BE/EIF2B5) in the same manner as glycogen synthase. In Wnt signaling, GSK3B forms a multimeric complex with APC, AXIN1 and CTNNB1/beta-catenin and phosphorylates the N-terminus of CTNNB1 leading to its degradation mediated by ubiquitin/proteasomes. Phosphorylates JUN at sites proximal to its DNA-binding domain, thereby reducing its affinity for DNA. Phosphorylates NFATC1/NFATC on conserved serine residues promoting NFATC1/NFATC nuclear export, shutting off NFATC1/NFATC gene regulation, and thereby opposing the action of calcineurin. Phosphorylates MAPT/TAU on 'Thr-548', decreasing significantly MAPT/TAU ability to bind and stabilizemicrotubules. MAPT/TAU is the principal component of neurofibrillary tangles in Alzheimer disease. Plays an important role in ERBB2-dependent stabilization of microtubules at the cell cortex. Phosphorylates MACF1, inhibiting its binding to microtubules which is critical for its role in bulge stem cell migration and skin wound repair. Probably regulates NF-kappa-B (NFKB1) at the transcriptional level and is required for the NF-kappa-B-mediated anti-apoptotic response to TNF-alpha (TNF/TNFA). Negatively regulates replication in pancreatic beta-cells, resulting in apoptosis, loss of beta-cells and diabetes. Through phosphorylation of the anti-apoptotic protein MCL1, may control cell apoptosis in response to growth factors deprivation. Phosphorylates MUC1 in breast cancer cells, decreasing the interaction of MUC1 with CTNNB1/beta-catenin. Is necessary for the establishment of neuronal polarity and axon outgrowth. Phosphorylates MARK2, leading to inhibit its activity. Phosphorylates SIK1 at 'Thr-182', leading to sustain its activity. Phosphorylates ZC3HAV1 which enhances its antiviral activity. Phosphorylates SNAI1, leading to its BTRC-triggered ubiquitination and proteasomal degradation. Phosphorylates SFPQ at 'Thr-687' upon T-cell activation. Phosphorylates NR1D1 st 'Ser-55' and 'Ser-59' and stabilizes it by protecting it from proteasomal degradation. Regulates the circadian clock via phosphorylation of the major clock components including ARNTL/BMAL1, CLOCK and PER2. Phosphorylates CLOCK AT 'Ser-427' and targets it for proteasomal degradation. Phosphorylates ARNTL/BMAL1 at 'Ser-17' and 'Ser-21' and primes it for ubiquitination and proteasomal degradation. Phosphorylates OGT at 'Ser-3' or 'Ser-4' which positively regulates its activity.
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BioChemical Class |
Kinase
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Target Validation |
T70977
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UniProt ID | |||||
EC Number |
EC 2.7.11.1
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Sequence |
MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTK
VIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSG EKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHR DIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDV WSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHP WTKVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALF NFTTQELSSNPPLATILIPPHARIQAAASTPTNATAASDANTGDRGQTNNAASASASNST |
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Drugs and Mode of Action | |||||
Drug(s) | CI-1040 | Drug Info | Phase 2 | Discovery agent | [521505], [541019] |
LY2090314 | Drug Info | Phase 2 | Acute myeloid leukemia; Acute promyelocytic leukemia | [523195], [542874] | |
tideglusib | Drug Info | Phase 2 | Osteosarcoma | [531710] | |
Neu-120 | Drug Info | Phase 1/2 | Parkinson's disease | [522217] | |
AZD-1080 | Drug Info | Discontinued in Phase 1 | Alzheimer disease | [542763], [548027] | |
RO-320432 | Drug Info | Terminated | Discovery agent | [541291], [545975] | |
SAN-61 | Drug Info | Terminated | Alzheimer disease | [548877] | |
Inhibitor | (2'Z,3'E)-7-Azaindirubin-3'-oxime | Drug Info | [530564] | ||
(E)-N-(6-(prop-1-enyl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
12,13-DEHYDRO-8-O-ACETYLMANZAMINE A | Drug Info | [528991] | |||
12,13-DEHYDROMANZAMINE A | Drug Info | [528991] | |||
3-(6-(phenylamino)-9H-purin-8-yl)benzonitrile | Drug Info | [530921] | |||
3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione | Drug Info | [529153] | |||
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole | Drug Info | [527308] | |||
4-(5-bromo-1H-indol-3-yl)pyrimidin-2-amine | Drug Info | [529753] | |||
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol | Drug Info | [528490] | |||
6-deoxymanzamine X | Drug Info | [528991] | |||
6-hydroxymanzamine A | Drug Info | [528991] | |||
8-O-(4-bromobenzenesulfonyl)manzamine F | Drug Info | [528991] | |||
8-O-(4-chlorobenzenesulfonyl)manzamine F | Drug Info | [528991] | |||
8-O-(4-toluenesulfonyl)manzamine A | Drug Info | [528991] | |||
8-OH-MANZAMINE A | Drug Info | [528342] | |||
9-N-ETHYL-8-ETHOXY-MANZAMINE A | Drug Info | [528991] | |||
9-N-METHYL-8-METHOXY-MANZAMINE A | Drug Info | [528991] | |||
Adenosine-5'-Diphosphate | Drug Info | [551391] | |||
alsterpaullone 2-cyanoethyl | Drug Info | [529213] | |||
AR-A014418 | Drug Info | [529753] | |||
AS-601245 | Drug Info | [529039] | |||
AZAKENPAULLONE | Drug Info | [526916] | |||
BISINDOLYLMALEIMIDE IX | Drug Info | [525872] | |||
BX-795 | Drug Info | [527484] | |||
BX-912 | Drug Info | [527484] | |||
CHIR-98014 | Drug Info | [526553] | |||
CHIR-98023 | Drug Info | [529753] | |||
CHIR-99021 | Drug Info | [526553] | |||
CI-1040 | Drug Info | [525872] | |||
compound 2 | Drug Info | [531356] | |||
compound 52 | Drug Info | [529213] | |||
compound 5b | Drug Info | [532816] | |||
compound 89S | Drug Info | [529892] | |||
CP-70949 | Drug Info | [543539] | |||
CT-98024 | Drug Info | [530695] | |||
ELLAGIC ACID | Drug Info | [528129] | |||
GF-109203 | Drug Info | [525872] | |||
GSK-3beta inhibitor II | Drug Info | [526343] | |||
GSK-3beta inhibitor XI | Drug Info | [527088] | |||
I-5 | Drug Info | [551393] | |||
IM-12 | Drug Info | [531101] | |||
indirubin deriv. 8a | Drug Info | [526957] | |||
K00244 | Drug Info | [530144] | |||
KENPAULLONE | Drug Info | [526916] | |||
L-779450 | Drug Info | [527836] | |||
LEUCETTAMINE B | Drug Info | [530492] | |||
MANZAMINE A | Drug Info | [529574] | |||
Manzamine E | Drug Info | [528342] | |||
Manzamine Y | Drug Info | [528342] | |||
N,8-diphenyl-9H-purin-6-amine | Drug Info | [530921] | |||
N-(6-(2-chlorophenyl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-(3-hydroxyphenyl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-(4-aminophenyl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-(4-fluorophenyl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-(4-hydroxyphenyl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-(furan-3-yl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-(pyridin-3-yl)-1H-indazol-3-yl)butyramide | Drug Info | [530757] | |||
N-(6-(pyridin-4-yl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-(thiophen-3-yl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-(trifluoromethyl)-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-benzyl-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-bromo-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-chloro-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-chloro-5-p-tolyl-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-chloro-5-phenyl-1H-indazol-3-yl)butyramide | Drug Info | [530757] | |||
N-(6-phenethyl-1H-indazol-3-yl)butyramide | Drug Info | [530735] | |||
N-(6-phenyl-1H-indazol-3-yl)butyramide | Drug Info | [530757] | |||
N-(8-(3-cyanophenyl)-9H-purin-6-yl)pentanamide | Drug Info | [530921] | |||
Neo-kauluamine | Drug Info | [528342] | |||
NU-6102 | Drug Info | [527906] | |||
PAULLONE | Drug Info | [530695] | |||
PF-228 | Drug Info | [528764] | |||
Phosphoaminophosphonic Acid-Adenylate Ester | Drug Info | [551374] | |||
PYRAZOLOPYRIDAZINE 1 | Drug Info | [527192] | |||
PYRAZOLOPYRIDAZINE 2 | Drug Info | [527192] | |||
Quinoxaline1 | Drug Info | [529213] | |||
RGB-286147 | Drug Info | [529213] | |||
RO-320432 | Drug Info | [530695] | |||
SAN-61 | Drug Info | [548878] | |||
SB-415286 | Drug Info | [529753] | |||
STAUROSPORINONE | Drug Info | [525872] | |||
TDZD-8 | Drug Info | [532096] | |||
Thieno analogue of kenpaullone | Drug Info | [526916] | |||
tideglusib | Drug Info | [531710] | |||
TWS-119 | Drug Info | [527964] | |||
Modulator | AZD-1080 | Drug Info | |||
LY2090314 | Drug Info | [533221] | |||
Neu-120 | Drug Info | ||||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | ErbB signaling pathway | ||||
Chemokine signaling pathway | |||||
Cell cycle | |||||
PI3K-Akt signaling pathway | |||||
Wnt signaling pathway | |||||
Hedgehog signaling pathway | |||||
Axon guidance | |||||
Hippo signaling pathway | |||||
Focal adhesion | |||||
Signaling pathways regulating pluripotency of stem cells | |||||
T cell receptor signaling pathway | |||||
B cell receptor signaling pathway | |||||
Neurotrophin signaling pathway | |||||
Dopaminergic synapse | |||||
Insulin signaling pathway | |||||
Melanogenesis | |||||
Prolactin signaling pathway | |||||
Thyroid hormone signaling pathway | |||||
Non-alcoholic fatty liver disease (NAFLD) | |||||
Alzheimer' | |||||
s disease | |||||
Hepatitis C | |||||
Measles | |||||
Influenza A | |||||
HTLV-I infection | |||||
Epstein-Barr virus infection | |||||
Pathways in cancer | |||||
Colorectal cancer | |||||
Endometrial cancer | |||||
Prostate cancer | |||||
Basal cell carcinoma | |||||
PANTHER Pathway | Alzheimer disease-presenilin pathway | ||||
Angiogenesis | |||||
Cadherin signaling pathway | |||||
Hedgehog signaling pathway | |||||
Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
Insulin/IGF pathway-protein kinase B signaling cascade | |||||
Interleukin signaling pathway | |||||
PDGF signaling pathway | |||||
PI3 kinase pathway | |||||
Wnt signaling pathway | |||||
Ras Pathway | |||||
CCKR signaling map ST | |||||
Pathway Interaction Database | LPA receptor mediated events | ||||
Degradation of beta catenin | |||||
Reelin signaling pathway | |||||
Presenilin action in Notch and Wnt signaling | |||||
Integrin-linked kinase signaling | |||||
CDC42 signaling events | |||||
LKB1 signaling events | |||||
Canonical Wnt signaling pathway | |||||
Role of Calcineurin-dependent NFAT signaling in lymphocytes | |||||
Glucocorticoid receptor regulatory network | |||||
C-MYC pathway | |||||
Regulation of Androgen receptor activity | |||||
BMP receptor signaling | |||||
Hedgehog signaling events mediated by Gli proteins | |||||
Signaling events mediated by Stem cell factor receptor (c-Kit) | |||||
Validated transcriptional targets of deltaNp63 isoforms | |||||
Aurora A signaling | |||||
Insulin-mediated glucose transport | |||||
Class I PI3K signaling events mediated by Akt | |||||
p53 pathway | |||||
Trk receptor signaling mediated by PI3K and PLC-gamma | |||||
Reactome | Degradation of beta-catenin by the destruction complex | ||||
AKT phosphorylates targets in the cytosol | |||||
Regulation of HSF1-mediated heat shock response | |||||
CRMPs in Sema3A signaling | |||||
Disassembly of the destruction complex and recruitment of AXIN to the membrane | |||||
S33 mutants of beta-catenin aren' | |||||
t phosphorylated | |||||
S37 mutants of beta-catenin aren' | |||||
S45 mutants of beta-catenin aren' | |||||
T41 mutants of beta-catenin aren' | |||||
Degradation of GLI2 by the proteasome | |||||
Constitutive Signaling by AKT1 E17K in Cancer | |||||
WikiPathways | DNA Damage Response (only ATM dependent) | ||||
Senescence and Autophagy in Cancer | |||||
Notch Signaling Pathway | |||||
Glycogen Metabolism | |||||
Insulin Signaling | |||||
Wnt Signaling Pathway | |||||
Wnt Signaling Pathway and Pluripotency | |||||
IL-6 signaling pathway | |||||
Wnt Signaling Pathway Netpath | |||||
Copper homeostasis | |||||
Focal Adhesion | |||||
Induction (Part 1 of 3) | |||||
Cardiac Hypertrophic Response | |||||
Degradation of beta-catenin by the destruction complex | |||||
T-Cell Receptor and Co-stimulatory Signaling | |||||
Cardiac Progenitor Differentiation | |||||
BDNF signaling pathway | |||||
Corticotropin-releasing hormone | |||||
B Cell Receptor Signaling Pathway | |||||
IL17 signaling pathway | |||||
Neural Crest Differentiation | |||||
Alzheimers Disease | |||||
IL-7 Signaling Pathway | |||||
Regulation of Microtubule Cytoskeleton | |||||
TWEAK Signaling Pathway | |||||
Leptin signaling pathway | |||||
Semaphorin interactions | |||||
Cell Cycle | |||||
MicroRNAs in cardiomyocyte hypertrophy | |||||
Androgen receptor signaling pathway | |||||
IL-5 Signaling Pathway | |||||
References | |||||
Ref 521505 | ClinicalTrials.gov (NCT00033384) CI-1040 in Treating Patients With Advanced Breast, Colon, Pancreatic, or Non-Small Cell Lung Cancer. U.S. National Institutes of Health. | ||||
Ref 522217 | ClinicalTrials.gov (NCT00607451) Safety, Tolerability, PK and PD Study of Neu-120 in the Treatment of Levodopa-induced Dyskinesia. U.S. National Institutes of Health. | ||||
Ref 523195 | ClinicalTrials.gov (NCT01214603) A Study in Participants With Acute Leukemia. U.S. National Institutes of Health. | ||||
Ref 531710 | Evidence for irreversible inhibition of glycogen synthase kinase-3beta by tideglusib. J Biol Chem. 2012 Jan 6;287(2):893-904. | ||||
Ref 541019 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5676). | ||||
Ref 541291 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6034). | ||||
Ref 542763 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7819). | ||||
Ref 542874 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7958). | ||||
Ref 545975 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005586) | ||||
Ref 525872 | Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. | ||||
Ref 526343 | Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors. Bioorg Med Chem Lett. 2002 Jun 3;12(11):1525-8. | ||||
Ref 526553 | Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95. | ||||
Ref 526916 | Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. | ||||
Ref 526957 | Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J Med Chem. 2004 Feb 12;47(4):935-46. | ||||
Ref 527088 | Design, synthesis, and biological evaluation of novel 7-azaindolyl-heteroaryl-maleimides as potent and selective glycogen synthase kinase-3beta (GSK-3beta) inhibitors. Bioorg Med Chem. 2004 Jun 15;12(12):3167-85. | ||||
Ref 527192 | J Med Chem. 2004 Sep 9;47(19):4716-30.N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. | ||||
Ref 527308 | J Med Chem. 2004 Dec 2;47(25):6239-47.Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. | ||||
Ref 527484 | Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. Epub 2005 Mar 16. | ||||
Ref 527836 | Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. Epub 2005 Nov 2.The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. | ||||
Ref 527906 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. Epub 2005 Dec 1.Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. | ||||
Ref 527964 | Nat Chem Biol. 2005 Jul;1(2):74-84.Diversity-oriented synthesis: exploring the intersections between chemistry and biology. | ||||
Ref 528129 | J Med Chem. 2006 Apr 20;49(8):2363-6.Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. | ||||
Ref 528342 | J Nat Prod. 2006 Jul;69(7):1034-40.Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. | ||||
Ref 528490 | J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. | ||||
Ref 528764 | J Biol Chem. 2007 May 18;282(20):14845-52. Epub 2007 Mar 28.Cellular characterization of a novel focal adhesion kinase inhibitor. | ||||
Ref 528991 | J Nat Prod. 2007 Sep;70(9):1397-405. Epub 2007 Aug 21.Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease. | ||||
Ref 529039 | Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. | ||||
Ref 529153 | Bioorg Med Chem. 2008 Jan 15;16(2):636-43. Epub 2007 Oct 22.Novel GSK-3beta inhibitors from sequential virtual screening. | ||||
Ref 529213 | Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. Epub 2007 Dec 11.A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. | ||||
Ref 529574 | Bioorg Med Chem. 2008 Jul 15;16(14):6702-6. Epub 2008 Jun 5.2-N-Methyl modifications and SAR studies of manzamine A. | ||||
Ref 529753 | Eur J Med Chem. 2009 Jun;44(6):2361-71. Epub 2008 Sep 16.Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models. | ||||
Ref 529892 | First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem. 2009 Jan 22;52(2):293-307. | ||||
Ref 530144 | The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg Med Chem Lett. 2009 Jul 1;19(13):3586-92. | ||||
Ref 530492 | Eur J Med Chem. 2010 Feb;45(2):805-10. Epub 2009 Oct 12.Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors. | ||||
Ref 530564 | J Nat Prod. 2009 Dec;72(12):2199-202.Synthesis and antiproliferative activity of 7-azaindirubin-3'-oxime, a 7-aza isostere of the natural indirubin pharmacophore. | ||||
Ref 530695 | Bioorg Med Chem Lett. 2010 Mar 1;20(5):1693-6. Epub 2010 Jan 25.Discovery of potent and bioavailable GSK-3beta inhibitors. | ||||
Ref 530735 | Bioorg Med Chem Lett. 2010 Mar 15;20(6):1985-9. Epub 2010 Jan 25.Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2. | ||||
Ref 530757 | Bioorg Med Chem Lett. 2010 Apr 1;20(7):2344-9. Epub 2010 Feb 2.Design of potent and selective GSK3beta inhibitors with acceptable safety profile and pharmacokinetics. | ||||
Ref 530921 | Eur J Med Chem. 2010 Aug;45(8):3389-93. Epub 2010 Apr 28.Novel 8-arylated purines as inhibitors of glycogen synthase kinase. | ||||
Ref 531101 | Bioorg Med Chem. 2010 Sep 15;18(18):6785-95. Epub 2010 Jul 25.Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. | ||||
Ref 531356 | 6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3beta inhibitors. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1429-33. | ||||
Ref 531710 | Evidence for irreversible inhibition of glycogen synthase kinase-3beta by tideglusib. J Biol Chem. 2012 Jan 6;287(2):893-904. | ||||
Ref 532096 | Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3beta inhibitors through virtual screening. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7232-6. | ||||
Ref 532816 | Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization. ACS Med Chem Lett. 2012 Jan 24;3(4):278-83. | ||||
Ref 533221 | Activating the Wnt/beta-Catenin Pathway for the Treatment of Melanoma--Application of LY2090314, a Novel Selective Inhibitor of Glycogen Synthase Kinase-3. PLoS One. 2015 Apr 27;10(4):e0125028. | ||||
Ref 543539 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2030). | ||||
Ref 548878 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029796) |
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