Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00191

Target Information
NamemRNA of Protein-tyrosine phosphatase, non-receptor type 1    
Type of targetClinical trial target    
SynonymsPTP-1B    
PTP1B    
Protein tyrosine phosphatase 1B    
Protein tyrosine phosphatase-1B    
Protein-tyrosine phosphatase 1B    
Tyrosine phosphatase 1B    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[2][3][1]
Obesity
[ICD9: 278   ICD10: E66]
[4][1][5]
Drug(s)ISIS 113715Phase IIDiabetes[6][7]
ISIS-PTP1BRxPhase IIDiabetes
ISIS-PTP1BrxPhase IType 2 diabetes
BioChemical ClassHydrolases acting on ester bonds    
EC NumberEC 3.1.3.48
PathwayAdherens junction
Insulin signaling pathway
UniProt IDP18031
PDB Structure1A5Y; 1AAX; 1BZC; 1BZH; 1BZJ; 1C83; 1C84; 1C85.    
SequenceMEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLH QEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLK CAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWP DFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKD PSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLE PPPEHIPPPPRPPKRILEPHNGKCREFFPNHQWVKEETQEDKDCPIKEEKGSPLNAAPYG IESMSQDTEVRSRVVGGSLRGAQAASPAKGEPSLPEKDEDHALSYWKPFLVNMCVATVLT AGAYLCYRFLFNSNT
Related US Patent6,365,592
6,448,429
6,465,444
6,472,545
6,486,141
6,486,142
6,498,151
6,583,126
6,627,767
6,642,381
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,2,5-THIADIAZOLIDIN-3-ONE-1,1-DIOXIDE[8]
1-Iodyl-3-nitro-benzene[9]
1-Iodyl-4-nitro-benzene[9]
1-METHYL-3-PHENYL-1H-PYRAZOL-5-YLSULFAMIC ACID[10]
2- (Oxalyl-Amino)-Benzoic Acid[11]
2-Methyl-2,4-Pentanediol[11]
3- (Oxalyl-Amino)-Naphthalene-2-Carboxylic Acid[11]
3-Iodyl-benzoic acid[9]
4-Iodyl-benzoic acid[9]
6- (Oxalyl-Amino)-1h-Indole-5-Carboxylic Acid[11]
Acetate Ion[11]
B-Octylglucoside[11]
Compound 15[11]
Compound 19[11]
Compound 9[11]
Cysteine Sulfenic Acid[10]
Cysteinesulfonic Acid[11]
Double Oxidized Cysteine[11]
Hydrogen peroxide[9]
ISOTHIAZOLIDINONE ANALOG[8]
Iodyl-benzene[9]
KR61639[12]
Novo Nordisk a/S Compound[11]
PARA- (BENZOYL)-PHENYLALANINE[8]
PNU177836[11]
Selective inhibitors of PTP1B[13]
Sp7343-Sp7964[11]
[[4- (Aminomethyl)Phenyl]Amino]Oxo-Acetic Acid,[11]
AntisenseISIS 107772[14]
ISIS 107773[14]
ISIS 107774[14]
ISIS 107775[14]
ISIS 107776[14]
ISIS 107791[14]
ISIS 107792[14]
ISIS 113715[6][7]
ISIS 113715[15]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Protein tyrosine phosphatase 1B: a new target for the treatment of obesity and associated co-morbidities. J Intern Med. 2002 Jun;251(6):467-75. To Reference
Ref 2Cellular effects of small molecule PTP1B inhibitors on insulin signaling. Biochemistry. 2003 Nov 11;42(44):12792-804. To Reference
Ref 3Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action. Biochemistry. 2001 May 15;40(19):5642-54. To Reference
Ref 4Increased insulin sensitivity and obesity resistance in mice lacking the protein tyrosine phosphatase-1B gene. Science. 1999 Mar 5;283(5407):1544-8. To Reference
Ref 5Structure-based design of selective and potent inhibitors of protein-tyrosine phosphatase beta. J Biol Chem. 2004 Jun 4;279(23):24226-35. Epub 2004 Mar 15. To Reference
Ref 6ISIS. Product Development Pipeline. 2009. To Reference
Ref 7Lack of pharmacokinetic interaction for ISIS 113715, a 2'-0-methoxyethyl modified antisense oligonucleotide targeting protein tyrosine phosphatase 1B messenger RNA, with oral antidiabetic compounds metformin, glipizide or rosiglitazone. Clin Pharmacokinet. 2006;45(8):789-801. To Reference
Ref 8Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 9Bioorg Med Chem Lett. 1999 Feb 8;9(3):353-6.Periodinates: a new class of protein tyrosine phosphatase inhibitors. To Reference
Ref 10Nucleic Acids Res. 2011 January; 39(Database issue): D1035¨CD1041. DrugBank 3.0: a comprehensive resource for ¡®Omics¡¯ research on drugs To Reference
Ref 11Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 12Discovery of a novel protein tyrosine phosphatase-1B inhibitor, KR61639: potential development as an antihyperglycemic agent. Eur J Pharmacol. 2004 Feb 6;485(1-3):333-9. To Reference
Ref 13Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21. To Reference
Ref 14US Patent 6261840 To Reference
Ref 15US Patent 7563884 To Reference



 

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