Protein tyrosine phosphatase IB

AmpC P-Lactamase Phosphodiesterase 4 Protein Tyrosine Phosphatase IB... 

Protein tyrosine phosphatase IB (PTP1B) inhibitor. IC5o = 4.1 pM... 

Doman TN, McGovern SL, Witherbee BJ, Kasten TP, Kurumbail R, Stallings WC, Connolly DT, Shoichet BK. Molecular docking and high throughput screening for novel inhibitors of protein tyrosine phosphatase IB. J Med Chem 2002 45 2213-21. 

A machine-learning method was proposed by Klon et al. [104] as an alternative form of consensus scoring. The method proved unsuccessful for PKB, but showed promise for the phosphatase PTPIB (protein tyrosine phosphatase IB). In this approach, compounds were first docked into the receptor and scored using conventional means. The top scoring compounds were then assumed to be active and used to build a naive Bayes classification model, all compounds were subsequently re-scored and ranked using the model. The method is heavily dependent upon predicting accurate binding... 

The synthesis of benzo[Z>]furan derivatives has become a very active field because these molecules have been recently identified as having a variety of biological activities. For example, they can function as inhibitors of protein tyrosine phosphatase IB with antihyperglycemic properties <00JMC1293>, as well as potent and short-acting p-blockers in the treatment of various cardiovascular diseases . An inexpensive, reusable clay has been utilized to catalyze a facile cyclodehydration under microwave without solvent to form 3-substituted benzo[2>]furans from substituted a-phenoxy acetophenones 104. One of the important features of this procedure is that all the selected cyclodehydration reactions are complete in less than 10 minutes <00SL1273>. 

Trodusquemine (221) (isolated from the liver of the dogfish shark, Squalus acanthias) Sulfated aminosterol Trodusquemine (MSI-1436) (221) Diabetes Suppresses mammalian appetite through inhibition of protein tyrosine phosphatase IB (PTP-IB) Phase I (against type 2 diabetes and related symptoms) Genaera Corporation 974-978... 

Three prenylated flavanones (144-146) isolated from stem barks of Erythrina abyssinica (family Liguminosae) exhibited inhibitory activity against protein tyrosine phosphatase IB (PTPIB) in an dose-dependent manner with IC50 values of > 60, 18.9 1.9 and 15.7 0.4 /tM, respectively hence, the flavanone (143) bearing a 2,2-dimethylpyran moiety on B ring is less potent than the other two (144 and 145) in the series. The... 

Na MK, Jang JP, Njamen D, Mbafor JT, Fomum ZT, Kim BY, Oh WK, Ahn JS. (2006) Protein tyrosine phosphatase-IB inhibitory activity of isoprenylated flavonoids isolated from Erythrina mildbraedii. J Nat Prod 69 1572-1576. 

Johnson TO, ErmoUeff J, Jirousek MR. Protein tyrosine phosphatase IB inhibitors for diabetes. Nat Rev Drug Discern 2002 1 696-709. 

M.R. Groves, Z.J. Yao, P.P. Roller, T.R. Burke Jr, D. Barford, Structural basis for inhibition of the protein tyrosine phosphatase IB by phosphotyrosine peptide mimetics. Biochemistry 37 (1998) 17773-17783. 

Ahmad, E Li, P.-M. Meyerovitch, J. Goldstein, B.J. Osmotic loading of neutrahzing antibodies demonstrates a role of protein-tyrosine phosphatase IB in negative regulation of the insulin action pathway. J. Biol. Chem., 270, 20503-20508 (1995)... 

Tjernberg, A., et al., Mechanism of action of pyridazine analogues on protein tyrosine phosphatase IB (PTP1B). Bioorg Med Chem Lett, 2004, 14, 891-895. 

Classen-Houben, D., Sippl, W., Holtje, H.-D. Molecular Modeling on Ligand-Receptor Complexes of Protein-Tyrosine-Phosphatase IB. In EuroQSAR 2002 Designing Drugs and Crop Protectants Processes, Problems and Solutions, Ford, M., Livingstone, D., Dearden, J., Van de Waterbeemd, H. (eds), Black-well, Bournemouth, 2002. 

Liljebris et al. synthesized 2-[4-[(2amino)propyl]-2-(l(2)7/-tetrazol-5-yl)phenoxy]acetic acid 606, peptidomimetic inhibitors of protein tyrosine phosphatase IB <2002JME1785>. 

Salmeen, A., J.N. Andersen, M.P. Myers, T.C. Meng, J.A. Hinks, N.K. Tonks, and D. Barford. 2003. Redox regulation of protein tyrosine phosphatase IB involves a sulphenyl-amide intermediate. Nature. 423 769-73. 

Qiu, W., R.K. Avramoglu, N. Dube, T.M. Chong, M. Naples, A. C., K.G. Sidiropoulos, G.F. Lewis, J.S. Cohn, M.L. Tremblay, and K. Adeh 2004. Hepatic TRP-1B expression regulates the assembly and secretion of apolipoprotein B-containing lipoproteins. Evidence from protein tyrosine phosphatase-IB overexpression knockout and RNAi studies. Diabetes 53 3057-3066. 

Fig. 2. Mechanisms of VO(OPT)-enhanced neurogenesis after brain ischemia in the hippocampal dentate gyrus. VO(OPT) inhibits protein tyrosine phosphatase IB, thereby stimulating Akt and ERK signaling. The downstream targets of Akt and ERK include HIF-la, GSK-3/3, and CREB, which are involved in the proliferation, migration, and maturation of the neural progenitor cells.

Lee SR, Kwon KS, Kim SR, Rhee SG. 1998. Reversible inactivation of protein-tyrosine phosphatase IB in A431 cells stimulated with epidermal growth factor. J Biol Chem 273 15366-15372. 

B. P., and Tremblay, M. L. 2002. Attenuation of leptin action and regulation of obesity by protein tyrosine phosphatase IB. Dev. Cell 2 497-503. 

Sivaramakrishnan S, Keerthi K, Gates KS (2005) A chemical model for redox regulation of protein tyrosine phosphatase IB (PTP1B) Activity. J Am Chem Soc 127 10830-10831... 

Figure4.1 Protein tyrosine phosphatase IB (2hnq (a)) and CDC25B (lcwt (b)) employ the same catalytic mechanism for hydrolysis of phosphorylated substrates but share no sequence homology and exhibit very different folds. The similarity of their binding sites can, however, be detected on the level of the interaction properties exposed to a ligand.

D. Barfbrd, A. J. Flint, and N. K. Tonks. Crystal structure of human protein tyrosine phosphatase IB fsee comments). Science, 263 (5152), 1397-1404, 1994. 

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