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Inositol phosphatase, inhibitors

Several 9-(phosphonoalkyl)- and 9-(difluoroalkyl)-guanine derivatives (12, X = H or F) have been studied as potential inhibitors of guanylate kinase. The most pronounced effect was observed with n - 5 Phenoxymethylene bisphosphonates (13, where R R and R represent a variety of substituents) were prepared and found to act as inositol phosphatase inhibitors and antimanic agents some inhibited the enzyme with IC50 < 50 pmol 4-(Phosphonomethylphenoxy)-l-carbamoylazetidine-2-ones (14) inhibited human leukocyte elastase for 14 (R R = OEt = 1.2 x 10 moL s (ref. 38). [Pg.769]

The preparation of inositol and structurally related phosphates continues to be explored. Examples include the synthesis of the enantiomers D- and L-myo-inositol 1,3,4,6-tetrakisphosphate (45) and (46) regioisomers of myo-inositol 1,3,4,5-tetrakisphosphate. Both D- and L-isomers are Ins (1,4,5)P3 5-phosphatase inhibitors, but not of Ins (1,4,5)P3 3-kinase (Figure 8). °... [Pg.305]

New IP3 5-phosphatase inhibitors have been prepared L- nyo-inositol 1,4,5-trisphosphorothioate and myo-inositol 1,3,5-trisphosphorothioate, which inhibited IP3 metabolism with concomitant elevation of the heparin-sensitive IP3-induced release of 45Ca2+ in T cells (Ward et al, 1994) and L-c/zira-inositol 1,4,6-triphosphate and the corresponding trisphosphoro-thioate compound L-c/n>o-I(l,4,6)PS3, which potentially and selectively inhibited inositol polyphosphate metabolism without affecting Ca + stores in electrically permeabilized neuroblastoma cells (Hansbro et al., 1994). These novel 5-phosphatase inhibitors may provide a starting point for development of cell-permeable analogues for further studies of the functions of IP3 and IP4 in the regulation of [Ca " ] in smooth muscle. [Pg.272]

From the evidence accumulated so far, it seems likely that the cAMP signal transduction pathway will be a major effector of a stimulatory signal to the pars tuberalis, which can be regulated by melatonin [115]. The effect of aluminum as AlF41 has been studied on inositol phosphate accumulation, calcium mobilization, and cyclic AMP production in ovine pars tuberalis cells [116]. In the presence of 10 mmol L-1 LiCl, AlF41 stimulated the net accumulation of inositol phosphates over a 40-min incubation. Lithium is a known inhibitor of phosphatases in the inositol phosphate-recycling pathway. The results show the existence of a lithium-sensitive phosphoinositide signaling. [Pg.174]

Huang, L.C., Heimark, D., Linko, J., Nolan, R., and Larner, J. A model phosphatase 2C->phosphatase 1 activation cascade via dual control of inhibitor-1 (INH-1) and DARPP-32 dephosphorylation by two inositol glycan putative insulin mediators from beef liver. Biochem. Biophys. Res. Commun., 1999, 255, 150-156. [Pg.116]

Figure 50. PTEN. The tumor suppressor gene and gene product protein PTEN (phosphatase tensin homolog deleted on chromosome ten, human 10q23.3) (Table VIII), is the natural inhibitor of oncogenes PI3K/Akt (phosphatidyl inositol kinase 3 protein kinase 3 phosphatidylinositol 3 phosphate Jacob Furth s AK mouse strain thymic lymphoma retroviral oncogene phosphoinosite-dependent kinase). The PTEN protein inactivates PIP3 by dephosphorylation PDKl (phosphoinositol-dependent kinase) is not recruited to the plasma membrane to activate Akt by phosphorylation. Sarah M. Planchon et al. The nuclear affairs of PTEN. J Cell Sci 2008 121 249-253. doi 10.1242/jcs.022459... Figure 50. PTEN. The tumor suppressor gene and gene product protein PTEN (phosphatase tensin homolog deleted on chromosome ten, human 10q23.3) (Table VIII), is the natural inhibitor of oncogenes PI3K/Akt (phosphatidyl inositol kinase 3 protein kinase 3 phosphatidylinositol 3 phosphate Jacob Furth s AK mouse strain thymic lymphoma retroviral oncogene phosphoinosite-dependent kinase). The PTEN protein inactivates PIP3 by dephosphorylation PDKl (phosphoinositol-dependent kinase) is not recruited to the plasma membrane to activate Akt by phosphorylation. Sarah M. Planchon et al. The nuclear affairs of PTEN. J Cell Sci 2008 121 249-253. doi 10.1242/jcs.022459...
The deoxygenated inositol analogue 98 (R = P03 ) is a known potent inhibitor of wyo-inositol 1-phosphatase (see Vol. 25, p. 218, ref. 131). A set of analogues with less polar groups than phosphate have been prepared 98 R = P(0)(0")(0 Pr), P(0)(0")(Me), P(0)(Me>2, SO3", SO2NH2 and SOzNHAc. The deoxygenated inositol derivatives 99 and 100 have been synthesized in chiral form as mechanism-based inhibitors and probes for wyo-inositol mono-phosphatase. ... [Pg.246]


See other pages where Inositol phosphatase, inhibitors is mentioned: [Pg.6]    [Pg.218]    [Pg.79]    [Pg.568]    [Pg.896]    [Pg.142]    [Pg.394]    [Pg.143]    [Pg.568]    [Pg.241]    [Pg.661]    [Pg.769]    [Pg.31]    [Pg.112]    [Pg.195]    [Pg.196]    [Pg.215]    [Pg.14]    [Pg.238]   
See also in sourсe #XX -- [ Pg.769 ]




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Inositol phosphatases

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