Target Validation Information
Target ID T89529
Target Name mRNA of Protein tyrosine phosphatase-1B
Target Type
Successful
Drug Potency against Target USNIC ACID Drug Info IC50 = 16400 nM [1]
16-alphaH,17-isovaleryloxy-ent-kauran-19-oic acid Drug Info IC50 = 7100 nM [2]
EVANS BLUE Drug Info IC50 = 1300 nM [3]
TRYPAN BLUE Drug Info IC50 = 3900 nM [3]
Abyssinone-VI-4-O-methyl ether Drug Info IC50 = 14800 nM [4]
DYSIDINE Drug Info IC50 = 6700 nM [5]
Ohioensin G Drug Info IC50 = 5600 nM [6]
Mulberrofuran W Drug Info IC50 = 2700 nM [7]
PHELLIGRIDIN I Drug Info IC50 = 3000 nM [8]
Abyssinone-IV Drug Info IC50 = 16000 nM [4]
Abyssinoflavanone VI Drug Info IC50 = 18900 nM [9]
USIMINE A Drug Info IC50 = 15000 nM [1]
BURTTINONE Drug Info IC50 = 18900 nM [10]
CAULERPIN Drug Info IC50 = 3770 nM [11]
FORMYLCHROMONE Drug Info Ki = 4300 nM [12]
Oxalylaminobenzoic acid Drug Info Ki = 18 nM [12]
OLEANOLIC_ACID Drug Info IC50 = 4200 nM [13]
Isoxazolecarboxylic acid Drug Info Ki = 5700 nM [12]
Oleanonic acid Drug Info IC50 = 3500 nM [14]
ALBAFURAN A Drug Info IC50 = 9200 nM [7]
URSOLIC ACID Drug Info IC50 = 3600 nM [15]
NEORAUTENOL Drug Info IC50 = 7600 nM [15]
Abyssinin II Drug Info IC50 = 17300 nM [9]
Sigmoidin F Drug Info IC50 = 14200 nM [9]
Kuwanon L Drug Info IC50 = 16900 nM [16]
LICOAGROCHALCONE A Drug Info IC50 = 16900 nM [9]
Ohioensin F Drug Info Ki = 1500 nM [6]
24-hydroxyursolic acid Drug Info IC50 = 12800 nM [14]
Erysubin E Drug Info IC50 = 8800 nM [15]
Erybreadin D Drug Info IC50 = 6400 nM [15]
3,9-Dihydroxy-4-prenyl-[6aR,11aR]pterocarpan Drug Info IC50 = 19500 nM [15]
Isochroman mono-carboxylic acid Drug Info IC50 = 51.63 nM [12]
Kuwanon R Drug Info IC50 = 8200 nM [7]
Spathodic acid Drug Info IC50 = 18800 nM [14]
Kuwanon V Drug Info IC50 = 13800 nM [7]
5-deoxyabyssinin II Drug Info IC50 = 19200 nM [9]
Abyssinoflavanone VII Drug Info IC50 = 15700 nM [9]
SIGMOIDIN A Drug Info IC50 = 14400 nM [9]
3alpha,24-dihydroxyolean-12-en-27-oic acid Drug Info IC50 = 11700 nM [17]
3beta-acetoxyolean-12-en-27-oic acid Drug Info IC50 = 8500 nM [17]
3beta-hydroxyurs-12-en-27-oic acid Drug Info IC50 = 4900 nM [17]
3beta,6beta-dihydroxyolean-12-en-27-oic acid Drug Info IC50 = 12800 nM [17]
3-oxoolean-12-en-27-oic acid Drug Info IC50 = 6800 nM [17]
18beta-Glycyrrhetic acid Drug Info IC50 = 13800 nM [17]
Methyl3beta-hydroxyolean-12-en-27-oate Drug Info IC50 = 16000 nM [17]
ERYTHRIBYSSIN A Drug Info IC50 = 19300 nM [15]
Pomolic acid Drug Info IC50 = 3900 nM [14]
SIGMOIDIN B Drug Info IC50 = 19400 nM [9]
Augustic acid Drug Info IC50 = 4930 nM [18]
3-epi-masilinic acid Drug Info IC50 = 14330 nM [18]
Sanggenon C Drug Info IC50 = 2600 nM [16]
OHIOENSIN A Drug Info IC50 = 4300 nM [6]
ERTIPROTAFIB Drug Info IC50 = 1400 nM [19]
3beta-hydroxyolean-12-en-27-oic acid Drug Info IC50 = 5200 nM [17]
18alpha-Glycyrrhetic acid Drug Info IC50 = 15600 nM [17]
Mulberrofuran D Drug Info IC50 = 4300 nM [7]
Ohioensin C Drug Info IC50 = 7600 nM [6]
1,2,3,4,6-penta-O-galloyl-D-glucopyranose Drug Info IC50 = 4800 nM [20]
RK-682 Drug Info IC50 = 4400 nM [21]
3-(4,5-Bis-biphenyl-4-yl-1H-imidazol-2-yl)-phenol Drug Info IC50 = 8600 nM [22]
Kuwanon J Drug Info IC50 = 2700 nM [7]
Methyl 3beta-hydroxyolean-12-en-28-oate Drug Info IC50 = 14200 nM [17]
Rotungenic acid Drug Info IC50 = 10900 nM [14]
Abyssinin I Drug Info IC50 = 18200 nM [9]
4'-((2-butylbenzofuran-3-yl)methyl)biphenyl-4-ol Drug Info IC50 = 1190 nM [23]
4-(p-toluidino)-3-isopropylnaphthalene-1,2-dione Drug Info IC50 = 19590 nM [24]
1,2-NAPHTHOQUINONE Drug Info IC50 = 1640 nM [25]
LICOAGROCHACONE A Drug Info IC50 = 19100 nM [26]
Sanggenon G Drug Info IC50 = 1600 nM [16]
3-isopropyl-4-(phenylthio)naphthalene-1,2-dione Drug Info IC50 = 13660 nM [24]
MASLINIC ACID Drug Info IC50 = 5930 nM [18]
4'-(2-butylbenzofuran-3-yl)biphenyl-4-ol Drug Info IC50 = 740 nM [23]
Mulberrofuran C Drug Info IC50 = 4900 nM [16]
ERYBREADIN B Drug Info IC50 = 4200 nM [15]
UVAOL Drug Info IC50 = 15600 nM [14]
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid Drug Info IC50 = 8100 nM [14]
CHROMOTROPATE Drug Info IC50 = 9700 nM [3]
FOLITENOL Drug Info IC50 = 7800 nM [15]
Erybreadin C Drug Info IC50 = 7300 nM [15]
Action against Disease Model ISIS 113715 In cultured monkey hepatocytes, ISIS 113715 treatment dose-dependently reduced PTP-1B mRNA expression, with an IC 50 of less than 10 nM. [27] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Although heterozygous loss of PTP1B has no effect on t uMorigenesis,homozygous PTP1B deficiency dramatically delays or prevents the onset of MMTV-NeuNT-evoked breast t uMors. The effects of PTP1B deficiency correlate with defective extracellular signal-regulated kinase activation in preneoplastic mammary glands from compound mutant mice.In contrast,PTP1B deficiency has no effect on MMTV-polyoma middle T t uMorigenesis. Our data raise the possibility that PTP1B inhibitors may be chemopreventative for some forms of breast cancer. [27]
References
REF 1J Nat Prod. 2008 Apr;71(4):710-2. Epub 2008 Feb 21.Usimines A-C, bioactive usnic acid derivatives from the Antarctic lichen Stereocaulon alpinum.
REF 2Bioorg Med Chem Lett. 2006 Jun 1;16(11):3061-4. Epub 2006 Mar 20.Inhibition of protein tyrosine phosphatase 1B by diterpenoids isolated from Acanthopanax koreanum.
REF 3Bioorg Med Chem Lett. 2004 Apr 19;14(8):1923-6.Evans Blue and other dyes as protein tyrosine phosphatase inhibitors.
REF 4J Nat Prod. 2006 Nov;69(11):1572-6.Protein tyrosine phosphatase-1B inhibitory activity of isoprenylated flavonoids isolated from Erythrina mildbraedii.
REF 5Bioorg Med Chem Lett. 2009 Jan 15;19(2):390-2. Epub 2008 Nov 24.A novel sesquiterpene quinone from Hainan sponge Dysidea villosa.
REF 6Bioorg Med Chem Lett. 2008 Jan 15;18(2):772-5. Epub 2007 Nov 17.Ohioensins F and G: protein tyrosine phosphatase 1B inhibitory benzonaphthoxanthenones from the Antarctic moss Polytrichastrum alpinum.
REF 7Bioorg Med Chem Lett. 2009 Dec 1;19(23):6759-61. Epub 2009 Oct 7.Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis.
REF 8J Nat Prod. 2007 Feb;70(2):296-9. Epub 2007 Feb 6.Structures, biogenesis, and biological activities of pyrano[4,3-c]isochromen-4-one derivatives from the Fungus Phellinus igniarius.
REF 9J Nat Prod. 2007 Jun;70(6):1039-42. Epub 2007 May 10.Isoprenylated flavonoids from the stem bark of Erythrina abyssinica.
REF 10Bioorg Med Chem. 2008 Dec 15;16(24):10356-62. Epub 2008 Oct 10.Flavanones from the stem bark of Erythrina abyssinica.
REF 11Bioorg Med Chem Lett. 2006 Jun 1;16(11):2947-50. Epub 2006 Mar 24.Two novel aromatic valerenane-type sesquiterpenes from the Chinese green alga Caulerpa taxifolia.
REF 12Eur J Med Chem. 2010 Sep;45(9):3709-18. Epub 2010 May 15.Synthesis and evaluation of some novel dibenzo[b,d]furan carboxylic acids as potential anti-diabetic agents.
REF 13J Nat Prod. 2009 Sep;72(9):1620-6.Chemical Constituents of the Roots of Euphorbia micractina.
REF 14J Nat Prod. 2008 Oct;71(10):1775-8. Epub 2008 Sep 18.Triterpenoids from the leaves of Diospyros kaki (persimmon) and their inhibitory effects on protein tyrosine phosphatase 1B.
REF 15Bioorg Med Chem Lett. 2009 Dec 1;19(23):6745-9. Epub 2009 Oct 1.Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.
REF 16Bioorg Med Chem Lett. 2006 Mar 1;16(5):1426-9. Epub 2005 Dec 13.Protein tyrosine phosphatase 1B inhibitors from Morus root bark.
REF 17Bioorg Med Chem Lett. 2006 Jun 15;16(12):3273-6. Epub 2006 Mar 31.Protein tyrosine phosphatase 1B inhibitory activity of triterpenes isolated from Astilbe koreana.
REF 18Bioorg Med Chem Lett. 2009 Dec 1;19(23):6618-22. Epub 2009 Oct 8.Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.
REF 19Bioorg Med Chem Lett. 2007 Oct 1;17(19):5357-60. Epub 2007 Aug 15.2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.
REF 20J Nat Prod. 2010 Sep 24;73(9):1578-81.Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor.
REF 21Bioorg Med Chem Lett. 2010 Sep 15;20(18):5398-401. Epub 2010 Aug 1.Prenylflavonoids from Glycyrrhiza uralensis and their protein tyrosine phosphatase-1B inhibitory activities.
REF 22J Med Chem. 2002 May 23;45(11):2213-21.Molecular docking and high-throughput screening for novel inhibitors of protein tyrosine phosphatase-1B.
REF 23Bioorg Med Chem. 2009 Apr 1;17(7):2658-72. Epub 2009 Mar 5.Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors.
REF 24Bioorg Med Chem Lett. 2006 Apr 1;16(7):1905-8. Epub 2006 Jan 24.Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases.
REF 25Bioorg Med Chem Lett. 2002 Aug 5;12(15):1941-6.Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents.
REF 26Bioorg Med Chem Lett. 2009 Sep 1;19(17):5155-7. Epub 2009 Jul 24.Inhibitory effect of chalcones and their derivatives from Glycyrrhiza inflata on protein tyrosine phosphatase 1B.
REF 27Inhibition of protein tyrosine phosphatase-1B with antisense oligonucleotides improves insulin sensitivity and increases adiponectin concentrations in monkeys. Endocrinology. 2009 Apr;150(4):1670-9. doi: 10.1210/en.2008-0885. Epub 2009 Jan 22.

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