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Chemical Compound Review

Tyrphostin 23     2-[(3,4-dihydroxyphenyl) methylidene]propan...

Synonyms: Tyrphostin A23, Lopac-T-7165, Tocris-0493, AG-18, CHEMBL76904, ...
 
 
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High impact information on Tyrphostin A23

 

Biological context of Tyrphostin A23

 

Anatomical context of Tyrphostin A23

 

Associations of Tyrphostin A23 with other chemical compounds

 

Gene context of Tyrphostin A23

  • The stimulatory action of ET-1[1-31] on TK activity was annulled by tyrphostin-23, while that on MAPK activity was reduced by calphostin-C and abolished by either tyrphostin-23 and PD-98059 [17].
  • IKK activity was stimulated by both TNF-alpha and TPA, and these effects were inhibited by Ro 31-8220 or tyrphostin 23 [18].
  • Cell surface expression of hTfR increases upon treatment with tyrphostin A23, which inhibits the interaction between the YTRF endocytosis signal in the hTfR cytosolic tail and the mu2-subunit of the AP2 complex [8].
  • In contrast, the ZG proliferogenic effect of 10(-8) M ADM was abolished by either the tyrosine kinase (TK) inhibitor tyrphostin-23 (10(-5) M) or the mitogen-activated protein kinase (MAPK) antagonists PD-98059 and U0216 (10(-4) M) [19].
  • We recently reported that tyrphostin 23 (3,4-dihydroxybenzylidene malononitrile) is unstable in solution and that some of the degradation products are better inhibitors of the tyrosine kinase activity of Src and the EGF-receptor kinase than the parent compound itself (Ramdas et al., Cancer Res. 54, 867-868, 1994) [20].
 

Analytical, diagnostic and therapeutic context of Tyrphostin A23

  • In combination with Northern blot analysis of cholesterol side-chain cleavage cytochrome P450 (P450scc) message, it is shown that a novel protein kinase inhibitor, tyrphostin AG18, arrests the FSH-induced accumulation of P450scc mRNA [21].
  • The constriction induced by 1 microM ET-1 measured 0.14 mN in the presence and 0.13 mN following pre-incubation with the tyrosine kinase inhibitor Tyrphostin A23 (100 microM) [22].
  • P3 was purified from oxidized tyrphostin 23 by solvent extraction, silica-gel flash chromatography, and reverse-phase high-pressure liquid chromatography [20].
  • Both Ro31-8220, an inhibitor of protein kinase C (PKC), and tyrphostin-23, an inhibitor of tyrosine kinase (TK), evoked a partial reversal of ANG-II effect, and when added together to the perfusion medium abolished it [23].

References

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  2. The degree of inhibition of protein tyrosine kinase activity by tyrphostin 23 and 25 is related to their instability. Ramdas, L., McMurray, J.S., Budde, R.J. Cancer Res. (1994) [Pubmed]
  3. Heat-shock treatment-mediated increase in transduction by recombinant adeno-associated virus 2 vectors is independent of the cellular heat-shock protein 90. Zhong, L., Qing, K., Si, Y., Chen, L., Tan, M., Srivastava, A. J. Biol. Chem. (2004) [Pubmed]
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  6. Biological activity of substrate-bound basic fibroblast growth factor (FGF2): recruitment of FGF receptor-1 in endothelial cell adhesion contacts. Tanghetti, E., Ria, R., Dell'Era, P., Urbinati, C., Rusnati, M., Ennas, M.G., Presta, M. Oncogene (2002) [Pubmed]
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  8. Trafficking of the human transferrin receptor in plant cells: effects of tyrphostin A23 and brefeldin A. Ortiz-Zapater, E., Soriano-Ortega, E., Marcote, M.J., Ortiz-Masi??, D., Aniento, F. Plant J. (2006) [Pubmed]
  9. Phagocytosis of gram-negative bacteria by a unique CD14-dependent mechanism. Schiff, D.E., Kline, L., Soldau, K., Lee, J.D., Pugin, J., Tobias, P.S., Ulevitch, R.J. J. Leukoc. Biol. (1997) [Pubmed]
  10. Adrenomedullin stimulates DNA synthesis of rat adrenal zona glomerulosa cells through activation of the mitogen-activated protein kinase-dependent cascade. Semplicini, A., Ceolotto, G., Baritono, E., Malendowicz, L.K., Andreis, P.G., Sartori, M., Rossi, G.P., Nussdorfer, G.G. J. Hypertens. (2001) [Pubmed]
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  12. The high affinity Fc gamma receptor (CD64) induces phagocytosis in the absence of its cytoplasmic domain: the gamma subunit of Fc gamma RIIIA imparts phagocytic function to Fc gamma RI. Indik, Z.K., Hunter, S., Huang, M.M., Pan, X.Q., Chien, P., Kelly, C., Levinson, A.I., Kimberly, R.P., Schreiber, A.D. Exp. Hematol. (1994) [Pubmed]
  13. Oxytocin and lysophosphatidic acid induce stress fiber formation in human myometrial cells via a pathway involving Rho-kinase. Gogarten, W., Emala, C.W., Lindeman, K.S., Hirshman, C.A. Biol. Reprod. (2001) [Pubmed]
  14. Growth factors mediate intracellular signaling in vascular smooth muscle cells through protein kinase C-linked pathways. Touyz, R.M., Schiffrin, E.L. Hypertension (1997) [Pubmed]
  15. Protein kinase calpha but not p44/42 mitogen-activated protein kinase, p38, or c-Jun NH(2)-terminal kinase is required for intercellular adhesion molecule-1 expression mediated by interleukin-1beta: involvement of sequential activation of tyrosine kinase, nuclear factor-kappaB-inducing kinase, and IkappaB kinase 2. Chen, C.C., Chen, J.J., Chou, C.Y. Mol. Pharmacol. (2000) [Pubmed]
  16. Induction of c-jun protooncogene expression by hydrogen peroxide through hydroxyl radical generation and p60SRC tyrosine kinase activation. Lee, S.F., Huang, Y.T., Wu, W.S., Lin, J.K. Free Radic. Biol. Med. (1996) [Pubmed]
  17. Endothelin-1[1-31], acting as an ETA-receptor selective agonist, stimulates proliferation of cultured rat zona glomerulosa cells. Mazzocchi, G., Rossi, G.P., Malendowicz, L.K., Champion, H.C., Nussdorfer, G.G. FEBS Lett. (2000) [Pubmed]
  18. Tumor necrosis factor alpha-induced activation of downstream NF-kappaB site of the promoter mediates epithelial ICAM-1 expression and monocyte adhesion. Involvement of PKCalpha, tyrosine kinase, and IKK2, but not MAPKs, pathway. Chen, C., Chou, C., Sun, Y., Huang, W. Cell. Signal. (2001) [Pubmed]
  19. Adrenomedullin enhances cell proliferation and deoxyribonucleic acid synthesis in rat adrenal zona glomerulosa: receptor subtype involved and signaling mechanism. Andreis, P.G., Markowska, A., Champion, H.C., Mazzocchi, G., Malendowicz, L.K., Nussdorfer, G.G. Endocrinology (2000) [Pubmed]
  20. A tyrphostin-derived inhibitor of protein tyrosine kinases: isolation and characterization. Ramdas, L., Obeyesekere, N.U., McMurray, J.S., Gallick, G.E., Seifert, W.E., Budde, R.J. Arch. Biochem. Biophys. (1995) [Pubmed]
  21. Tyrosine kinase inhibitor AG18 arrests follicle-stimulating hormone-induced granulosa cell differentiation: use of reverse transcriptase-polymerase chain reaction assay for multiple messenger ribonucleic acids. Orly, J., Rei, Z., Greenberg, N.M., Richards, J.S. Endocrinology (1994) [Pubmed]
  22. ET(A) receptors are the primary mediators of myofilament calcium sensitization induced by ET-1 in rat pulmonary artery smooth muscle: a tyrosine kinase independent pathway. Evans, A.M., Cobban, H.J., Nixon, G.F. Br. J. Pharmacol. (1999) [Pubmed]
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