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Chemical Compound Review:

SureCN10339587 2-[4-(4- fluorophenyl)carbonyl-1- piperidyl]...

Synonyms: E-2001, AC1L2W18, E 2001

This record was replaced with 129687.

Kaneko, T. et al., Rossi, B. et al., Bang, R. et al., Thomas, D.D. et al., Rajala, R.V. et al., et al.

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Disease relevance of 2-[4-(4-fluorobenzoyl)-1-piperidyl]-1-naphthalen-2-yl-ethanone

1. Pretreatment with E-2001 ameliorated the degeneration of pyramidal neurons in the hippocampal CA1 sector following transient ischemia in Mongolian gerbils [1].

High impact information on 2-[4-(4-fluorobenzoyl)-1-piperidyl]-1-naphthalen-2-yl-ethanone

A previous study by our laboratory identified an amino acid position, Leu(176), critical for CRP binding to FcgammaRI and work by others (Agrawal, A., Shrive, A. K., Greenhough, T. J., and Volanakis, J. E. (2001) J. Immunol. 166, 3998-4004) determined several residues important for C1q binding [2].
Previous studies (Golfman, L. S., Bakovic, M., and Vance, D. E. (2001) J. Biol. Chem. 276, 43688-43692) demonstrated that CT alpha mRNA accumulates during S phase in preparation for cellular mitosis [3].
Increased lipopolysaccharide (LPS)-stimulated TNFalpha expression in macrophages after chronic ethanol feeding is associated with a stabilization of TNFalpha mRNA (Kishore, R., McMullen, M. R., and Nagy, L. E. (2001) J. Biol. Chem. 276, 41930-41937) [4].
We have shown previously that expression of the murine CTP:phosphocholine cytidylyltransferase (CT) alpha gene is regulated during cell proliferation (Golfman, L. S., Bakovic, M., and Vance, D. E. (2001) J. Biol. Chem. 276, 43688-43692) [5].
The intestinal Ca(2+) transport protein CaT1 encoded by TRPV6 has been reported (Yue, L., Peng, J. B., Hediger, M. A., and Clapham, D. E. (2001) Nature 410, 705-709) to be all or a part of the Ca(2+) release-activated Ca(2+) channel (CRAC) [6].

Chemical compound and disease context of 2-[4-(4-fluorobenzoyl)-1-piperidyl]-1-naphthalen-2-yl-ethanone

Furthermore, E-2001 prevented the excessive accumulation of extracellular glutamate induced by a brief ischemia in gerbils [1].

Biological context of 2-[4-(4-fluorobenzoyl)-1-piperidyl]-1-naphthalen-2-yl-ethanone

Recently, we have shown that phosphoinositide 3-kinase (PI3K) in bovine rod outer segment (ROS) is activated in vitro by tyrosine phosphorylation of the C-terminal tail of the insulin receptor (Rajala, R. V. S., and Anderson, R. E. (2001) Invest. Ophthal. Vis. Sci. 42, 3110-3117) [7].
(Harada, T., Morooka, T., Ogawa, S., and Nishida, E. (2001) Nat. Cell Biol. 3, 453-459) have prompted us to propose a model for feedback down-regulation of the MAP kinase signal cascade by cdk5 inactivation of MEK1 [8].
Among them, phosphatidylinositol 3-kinase (PI 3-kinase) has been recently suggested to negatively regulate sperm motility (Luconi, M., Marra, F., Gandini, L., Lenzi, A., Filimberti, E., Forti, G. and Baldi, E. (2001). Hum. Reprod. 16, 1931-1937) [9].

Anatomical context of 2-[4-(4-fluorobenzoyl)-1-piperidyl]-1-naphthalen-2-yl-ethanone

2. E-2001 improved stroke symptoms induced by permanent unilateral carotid artery ligation in gerbils [1].
E2001 (2-(4-(p-fluorobenzoyl)-piperidin-1-yl)-2'-acetonaphthone hydrochloride, CAS 107025-80-9) is a novel anti-ischemic agent, which is reported to protect against delayed neuronal death in the CA1 subfield of the hippocampus [10].

Associations of 2-[4-(4-fluorobenzoyl)-1-piperidyl]-1-naphthalen-2-yl-ethanone with other chemical compounds

In a previous paper [Serrani, F., Rossi, B. and Berardi, E (2001) Nitrogen metabolite repression in Hansenula polymorpha: the nmrl-l mutation. Curr. Genet. 40, 243-250], we identified five loci (NMR1-NMR5) involved in NMR, and characterised one of them (NMR1), which likely identifies a regulatory factor [11].

Gene context of 2-[4-(4-fluorobenzoyl)-1-piperidyl]-1-naphthalen-2-yl-ethanone

We have previously described a general ribonucleotidase activity of the first nucleotide binding domain (NBD1) of human ABCR (Biswas, E. E. (2001) Biochemistry 40, 8181-8187) [12].
CRHSP-28 is a member of the tumor protein D52 protein family that was recently shown to regulate Ca(2+)-stimulated secretory activity in streptolysin-O-permeabilized acinar cells (Thomas, D. H., Taft, W. B., Kaspar, K. M., and Groblewski, G. E. (2001) J. Biol. Chem. 276, 28866-28872) [13].

Analytical, diagnostic and therapeutic context of 2-[4-(4-fluorobenzoyl)-1-piperidyl]-1-naphthalen-2-yl-ethanone

E-2001 also prolonged the survival time following intravenous injection of KCN into mice [1].

References

Anti-ischemic effect of the novel anti-ischemic agent 2-(4-(p-fluorobenzoyl)-piperidin-1-yl)-2'-acetonaphthone hydrochloride and possible mechanism of its action. Kaneko, T., Nakazawa, T., Ueno, M., Furuya, Y., Ikeda, M., Mihara, M., Abe, K., Tanaka, K., Uzuo, T., Fukuda, T. Arzneimittel-Forschung. (1989) [Pubmed]
Analysis of binding sites in human C-reactive protein for Fc{gamma}RI, Fc{gamma}RIIA, and C1q by site-directed mutagenesis. Bang, R., Marnell, L., Mold, C., Stein, M.P., Clos, K.T., Chivington-Buck, C., Clos, T.W. J. Biol. Chem. (2005) [Pubmed]
Activation of CTP:phosphocholine cytidylyltransferase alpha expression during the S phase of the cell cycle is mediated by the transcription factor Sp1. Banchio, C., Schang, L.M., Vance, D.E. J. Biol. Chem. (2003) [Pubmed]
Chronic ethanol exposure increases the binding of HuR to the TNFalpha 3'-untranslated region in macrophages. McMullen, M.R., Cocuzzi, E., Hatzoglou, M., Nagy, L.E. J. Biol. Chem. (2003) [Pubmed]
Oncogenic Ha-Ras transformation modulates the transcription of the CTP:phosphocholine cytidylyltransferase alpha gene via p42/44MAPK and transcription factor Sp3. Bakovic, M., Waite, K., Vance, D.E. J. Biol. Chem. (2003) [Pubmed]
Store depletion-activated CaT1 currents in rat basophilic leukemia mast cells are inhibited by 2-aminoethoxydiphenyl borate. Evidence for a regulatory component that controls activation of both CaT1 and CRAC (Ca(2+) release-activated Ca(2+) channel) channels. Schindl, R., Kahr, H., Graz, I., Groschner, K., Romanin, C. J. Biol. Chem. (2002) [Pubmed]
In vivo regulation of phosphoinositide 3-kinase in retina through light-induced tyrosine phosphorylation of the insulin receptor beta-subunit. Rajala, R.V., McClellan, M.E., Ash, J.D., Anderson, R.E. J. Biol. Chem. (2002) [Pubmed]
Phosphorylation of MEK1 by cdk5/p35 down-regulates the mitogen-activated protein kinase pathway. Sharma, P., Veeranna, n.u.l.l., Sharma, M., Amin, N.D., Sihag, R.K., Grant, P., Ahn, N., Kulkarni, A.B., Pant, H.C. J. Biol. Chem. (2002) [Pubmed]
Increased phosphorylation of AKAP by inhibition of phosphatidylinositol 3-kinase enhances human sperm motility through tail recruitment of protein kinase A. Luconi, M., Carloni, V., Marra, F., Ferruzzi, P., Forti, G., Baldi, E. J. Cell. Sci. (2004) [Pubmed]
Protective effect of the novel anti-ischemic agent 2-(4-(p-fluorobenzoyl)-piperidin-1-yl)-2'-acetonaphthone hydrochloride against ischemia-induced impairment of the passive avoidance response in gerbils. Ueno, M., Nakazawa, T., Mihara, M., Kaneko, T., Yamatsu, K. Arzneimittel-Forschung. (1990) [Pubmed]
Hansenula polymorpha NMR2 and NMR4, two new loci involved in nitrogen metabolite repression. Rossi, B., Manasse, S., Serrani, F., Berardi, E. FEMS Yeast Res. (2005) [Pubmed]
Biochemical defects in retina-specific human ATP binding cassette transporter nucleotide binding domain 1 mutants associated with macular degeneration. Suárez, T., Biswas, S.B., Biswas, E.E. J. Biol. Chem. (2002) [Pubmed]
Identification of annexin VI as a Ca2+-sensitive CRHSP-28-binding protein in pancreatic acinar cells. Thomas, D.D., Kaspar, K.M., Taft, W.B., Weng, N., Rodenkirch, L.A., Groblewski, G.E. J. Biol. Chem. (2002) [Pubmed]

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