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Chemical Compound Review

Rp-Cpt-camps     (1S,6R,8R,9R)-8-[6-amino-8- (4...

Synonyms: CHEMBL230552, SureCN7521869, KST-1A8082, AR-1A5498, LS-174912, ...
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Disease relevance of AIDS212162


High impact information on AIDS212162

  • RESULTS: Glucagon (10-100 nmol/L) and 8-CPT-cAMP (10 or 50 micromol/L) stimulated in rat hepatocytes the expression of MKP-1 messenger RNA and protein, which became maximal within 30 minutes and declined to nearly basal levels after 60 minutes [6].
  • Within 2 h, 8-CPT-cAMP altered expression of 152 genes that contain evolutionarily conserved cAMP-response elements within 5 kb of transcriptional start sites, including the circadian clock gene Per1 [1].
  • By contrast, gene expression was unaltered in Kin- S49 cells (that lack PKA) incubated with 8-CPT-cAMP [1].
  • We describe a cAMP derivative, 8-p-chlorophenylthioadenosine 3',5'-cyclic monophosphate (8-CPT-cAMP), which inhibits cAMP-induced chemotaxis at low concentrations but induces chemotaxis at supersaturating concentrations [7].
  • We report here that the membrane-permeant cAMP analogs, 8-(4-chlorophenylthio)-cAMP and 8-bromo-cAMP, can replace NGF in promoting long-term survival and neurite outgrowth in cultures of rat neonatal sympathetic and embryonic sensory neurons [8].

Biological context of AIDS212162


Anatomical context of AIDS212162

  • In agreement with the other data obtained, 8-(4-chlorophenylthio)-cAMP and RII alpha were found to sensitize cells to ricin, indicating an increased transport of ricin to the cytosol [13].
  • In these experiments, luciferase reporter activity in COS-1 cells expressing RIIalpha2Cbeta12 holoenzyme was half-maximal at 12-fold lower concentrations of 8-(4-chlorophenylthio)-cAMP and 5-fold lower concentrations of forskolin than in COS-1 cells expressing RIIalpha2Calpha2 holoenzyme [14].
  • Measurements by a stopped-flow light-scattering method revealed that the osmotic water permeability (Pf) of LLC-PK1 cells transfected with WT was 69.6 +/- 6.5 microm/s (24.8 +/- 2.2 microm/s for mock-transfected), and stimulation by 500 microM 8-(4-chlorophenylthio)-cAMP increased the Pf by 85 +/- 12% [15].
  • However, not only endosome-to-Golgi transport, but also retrograde ricin transport to the endoplasmic reticulum (ER), measured as sulfation and N-glycosylation of another modified ricin (ricin sulf-2), seemed to be increased in cells expressing RII alpha in the presence of a cAMP analog, 8-(4-chlorophenylthio)-cAMP [13].
  • After stimulation of plasma membrane Cl- conductance by 8-(4-chlorophenylthio)-cAMP (CPT-cAMP), trans-Golgi pH was 6.42 +/- 0.07 (n = 22, control), 6.47 +/- 0.07 (n = 20, CFTR), and 6.35 +/- 0 [16].

Associations of AIDS212162 with other chemical compounds


Gene context of AIDS212162


Analytical, diagnostic and therapeutic context of AIDS212162


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  2. Epidermal growth factor induction of cellular proliferation and protooncogene expression in growth-arrested rat H4IIE hepatoma cells: role of cyclic adenosine monophosphate. Squinto, S.P., Block, A.L., Doucet, J.P. Mol. Endocrinol. (1989) [Pubmed]
  3. Transfected D2 dopamine receptors mediate the potentiation of arachidonic acid release in Chinese hamster ovary cells. Kanterman, R.Y., Mahan, L.C., Briley, E.M., Monsma, F.J., Sibley, D.R., Axelrod, J., Felder, C.C. Mol. Pharmacol. (1991) [Pubmed]
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  7. Selective induction of gene expression and second-messenger accumulation in Dictyostelium discoideum by the partial chemotactic antagonist 8-p-chlorophenylthioadenosine 3',5'-cyclic monophosphate. Peters, D.J., Bominaar, A.A., Snaar-Jagalska, B.E., Brandt, R., Van Haastert, P.J., Ceccarelli, A., Williams, J.G., Schaap, P. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
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  9. Insulin inhibition of hepatic cAMP-dependent protein kinase: decreased affinity of protein kinase for cAMP and possible differential regulation of intrachain sites 1 and 2. Gabbay, R.A., Lardy, H.A. Proc. Natl. Acad. Sci. U.S.A. (1987) [Pubmed]
  10. Phosphorylation of the inositol 1,4,5-trisphosphate receptor. Cyclic GMP-dependent protein kinase mediates cAMP and cGMP dependent phosphorylation in the intact rat aorta. Komalavilas, P., Lincoln, T.M. J. Biol. Chem. (1996) [Pubmed]
  11. The pro-apoptotic protein Bim is a convergence point for cAMP/protein kinase A- and glucocorticoid-promoted apoptosis of lymphoid cells. Zhang, L., Insel, P.A. J. Biol. Chem. (2004) [Pubmed]
  12. Differential sensitivity of HTC and Fu5-5 cells for induction of tyrosine aminotransferase by 3',5'-cyclic adenosine monophosphate. Wasner, G., Simons, S.S. Mol. Endocrinol. (1987) [Pubmed]
  13. Endosome-to-Golgi transport is regulated by protein kinase A type II alpha. Birkeli, K.A., Llorente, A., Torgersen, M.L., Keryer, G., Taskén, K., Sandvig, K. J. Biol. Chem. (2003) [Pubmed]
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  15. Phosphorylation of serine 256 is required for cAMP-dependent regulatory exocytosis of the aquaporin-2 water channel. Fushimi, K., Sasaki, S., Marumo, F. J. Biol. Chem. (1997) [Pubmed]
  16. Evidence against defective trans-Golgi acidification in cystic fibrosis. Seksek, O., Biwersi, J., Verkman, A.S. J. Biol. Chem. (1996) [Pubmed]
  17. Modulation of high voltage-activated calcium channels by somatostatin in acutely isolated rat amygdaloid neurons. Viana, F., Hille, B. J. Neurosci. (1996) [Pubmed]
  18. Molecular cloning and characterization of a murine LPS-inducible cDNA. Lee, C.G., Demarquoy, J., Jackson, M.J., O'Brien, W.E. J. Immunol. (1994) [Pubmed]
  19. Regulation of Ras.GTP loading and Ras-Raf association in neonatal rat ventricular myocytes by G protein-coupled receptor agonists and phorbol ester. Activation of the extracellular signal-regulated kinase cascade by phorbol ester is mediated by Ras. Chiloeches, A., Paterson, H.F., Marais, R., Clerk, A., Marshall, C.J., Sugden, P.H. J. Biol. Chem. (1999) [Pubmed]
  20. Transmodulation of epidermal growth factor receptor function by cyclic AMP-dependent protein kinase. Barbier, A.J., Poppleton, H.M., Yigzaw, Y., Mullenix, J.B., Wiepz, G.J., Bertics, P.J., Patel, T.B. J. Biol. Chem. (1999) [Pubmed]
  21. cAMP potentiates H(2)O(2)-induced ERK1/2 phosphorylation without the requirement for MEK1/2 phosphorylation. Lee, K., Esselman, W.J. Cell. Signal. (2001) [Pubmed]
  22. Effects of 8-cpt-cAMP on the epithelial sodium channel expressed in Xenopus oocytes. Chraïbi, A., Schnizler, M., Clauss, W., Horisberger, J.D. J. Membr. Biol. (2001) [Pubmed]
  23. Mitogen-activated protein kinase activation and regulation of cyclooxygenase 2 expression by platelet-activating factor and hCG in human endometrial adenocarcinoma cell line HEC-1B. Munir, I., Fukunaga, K., Miyazaki, K., Okamura, H., Miyamoto, E. J. Reprod. Fertil. (1999) [Pubmed]
  24. Cellular mechanisms associated with spontaneous and ciliary neurotrophic factor-cAMP-induced survival and axonal regeneration of adult retinal ganglion cells. Park, K., Luo, J.M., Hisheh, S., Harvey, A.R., Cui, Q. J. Neurosci. (2004) [Pubmed]
  25. Expression and regulation of normal and polymorphic epithelial sodium channel by human lymphocytes. Bubien, J.K., Watson, B., Khan, M.A., Langloh, A.L., Fuller, C.M., Berdiev, B., Tousson, A., Benos, D.J. J. Biol. Chem. (2001) [Pubmed]
  26. Mutant AF-2 domain of PML-RARalpha in retinoic acid-resistant NB4 cells: differentiation induced by RA is triggered directly through PML-RARalpha and its down-regulation in acute promyelocytic leukemia. Kitamura, K., Kiyoi, H., Yoshida, H., Saito, H., Ohno, R., Naoe, T. Leukemia (1997) [Pubmed]
  27. Inhibition of hormone-sensitive lipase gene expression by cAMP and phorbol esters in 3T3-F442A and BFC-1 adipocytes. Plée-Gautier, E., Grober, J., Duplus, E., Langin, D., Forest, C. Biochem. J. (1996) [Pubmed]
  28. Multihormonal regulation of insulin-like growth factor-binding protein-1 in rat H4IIE hepatoma cells: the dominant role of insulin. Unterman, T.G., Oehler, D.T., Murphy, L.J., Lacson, R.G. Endocrinology (1991) [Pubmed]
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