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Literature summary for 3.1.3.48 extracted from

  • Hellmuth, K.; Grosskopf, S.; Lum, C.T.; Wuertele, M.; Roeder, N.; von Kries, J.P.; Rosario, M.; Rademann, J.; Birchmeier, W.
    Specific inhibitors of the protein tyrosine phosphatase Shp2 identified by high-throughput docking (2008), Proc. Natl. Acad. Sci. USA, 105, 7275-7280.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Protein Variants

Protein Variants Comment Organism
E76K leukemia-associated Shp2 mutant Homo sapiens
R362K the Shp2 mutant shows a strongly decreased affinity for the inhibitor phenylhydrazonopyrazolone sulfonate 1 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
orthovanadate
-
Homo sapiens
phenylhydrazonopyrazolone sulfonate 1 potent, active site-directed small molecule inhibitor which is specific for Shp2 over the closely related tyrosine phosphatases Shp1 and PTP1B Homo sapiens
phenylhydrazonopyrazolone sulfonate 4 the most potent inhibitor of Shp2 which shows a specificity profile similar to phenylhydrazonopyrazolone sulfonate 1 Homo sapiens
suramin
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl phosphate + H2O
-
Homo sapiens 4-nitrophenol + phosphate
-
?

Synonyms

Synonyms Comment Organism
protein tyrosine phosphatase
-
Homo sapiens
PTP1B
-
Homo sapiens
PTPN11
-
Homo sapiens
SHP1
-
Homo sapiens
SHP2
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0007
-
orthovanadate Ki value for inhibition of wild type Shp2 Homo sapiens
0.00073
-
phenylhydrazonopyrazolone sulfonate 1 Ki value for inhibition of wild type Shp2 Homo sapiens
0.0053
-
suramin Ki value for inhibition of wild type PTP1B Homo sapiens
0.0057
-
suramin Ki value for inhibition of wild type Shp2 Homo sapiens
0.0058
-
phenylhydrazonopyrazolone sulfonate 1 Ki value for inhibition of mutant Shp2 R362K Homo sapiens
0.0058
-
phenylhydrazonopyrazolone sulfonate 1 Ki value for inhibition of wild type PTP1B Homo sapiens
0.0107
-
phenylhydrazonopyrazolone sulfonate 1 Ki value for inhibition of wild type Shp1 Homo sapiens