Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0U9ZS)
Name
Protein-tyrosine phosphatase 1B (PTPN1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Protein-tyrosine phosphatase 1B; Tyrosine-protein phosphatase non-receptor type 1; PTP-1B; PTPase 1
Family Hydrolase (HDase)  >>  Ester bond hydrolase (EC 3.1)
Organism
Homo sapiens (Human)
Gene Name PTPN1 Gene ID
5770
UniProt ID PTN1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T16347 (click to find more therapeutic target data of this DBT)
INTEDE ID DME0495 (click to find more drug-metabolizing enzyme data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLH
QEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLK
CAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWP
DFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKD
PSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLE
PPPEHIPPPPRPPKRILEPHNGKCREFFPNHQWVKEETQEDKDCPIKEEKGSPLNAAPYG
IESMSQDTEVRSRVVGGSLRGAQAASPAKGEPSLPEKDEDHALSYWKPFLVNMCVATVLT
AGAYLCYRFLFNSNT
Function
Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion. May also regulate the hepatocyte growth factor receptor signaling pathway through dephosphorylation of MET. Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Allura red AC dye Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Colorant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 33000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PTN1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 410000 nM (tested by experiment) [1]
                   Tested Species Saccharomyces cerevisiae (Yeast)
                   UniProt ID PTP1_YEAST
          DIG Name: Carminic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Colorant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 26000 nM (estimated based on the structural similarity with CHEMBL1366408 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID PTN1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 15000 nM (estimated based on the structural similarity with CHEMBL1366408 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Saccharomyces cerevisiae (Yeast)
                   UniProt ID PTP1_YEAST
          DIG Name: FD&C red no. 4 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1200 nM (estimated based on the structural similarity with CHEMBL1200712 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.863387978
                   Tested Species Saccharomyces cerevisiae (Yeast)
                   UniProt ID PTP1_YEAST
          DIG Name: Gentisic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antioxidant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 > 100000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PTN1_HUMAN
          DIG Name: Glycyrrhizin Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 > 100000 nM (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PTN1_HUMAN
References
1 Evans Blue and other dyes as protein tyrosine phosphatase inhibitors. Bioorg Med Chem Lett. 2004 Apr 19; 14(8):1923-6.
2 Click to a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides: novel construction of PTP1B inhibitors on a sugar scaffold. Eur J Med Chem. 2011 Sep; 46(9):4212-8.
3 Protein tyrosine phosphatase 1B inhibitory activity of triterpenes isolated from Astilbe koreana. Bioorg Med Chem Lett. 2006 Jun 15; 16(12):3273-6.

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