The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Cicaprost     2-[(2E)-2-[(3aS,4R,5R,6aR)-5- hydroxy-4...

Synonyms: Cicaprostum, AC1NSJVZ, SureCN61349, CHEMBL160629, ZK-96480, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Cicaprost

  • Treatment with pertussis toxin reversed the inhibitory effects of cicaprost on CRE occupancy, cyclin E-cdk2 activity, and S phase entry, suggesting the involvement of Gi signaling in cicaprost action [1].
  • In rats whose SMT2A tumors were surgically removed 10 days after tumor implantation, there was a strong decrease of lung metastases by cicaprost given from day 20 to day 36 [2].
  • Antiatherosclerotic effects of oral cicaprost in experimental hypercholesterolemia in rabbits [3].
  • Cicaprost also inhibited ET-1 induction of c-fos mRNA expression, an additional marker of hypertrophy in ARCM (n = 5, P < 0.005) [4].
  • In Cop rats bearing spontaneously metastasizing R 3327 MAT Lu prostate carcinomas, cicaprost (1.0 mg/kg p.o. daily) inhibited the number of lung metastases by about 80%, whereas the lower doses (0.1 and 0.5 mg/kg) exhibited borderline efficacy [5].

High impact information on Cicaprost

  • Depletion of PDE6delta using short interfering RNA abolished cicaprost-induced IP internalization in human aortic smooth muscle cells [6].
  • Levels of the closely related Cdk2 inhibitor, p21(Cip1), are unaffected by cicaprost [7].
  • Moreover, we show that cicaprost blocks the induction of Skp2 mRNA and that ectopic expression of a Skp2 cDNA overrides the effect of cicaprost on p27(Kip1) levels and S phase entry [7].
  • First, we show that cicaprost prevents the late G(1) phase down-regulation of p27(Kip1) and that the inhibitory effect of cicaprost on cyclin E-Cdk2 activity and S phase entry is eliminated by deleting p27(Kip1) [7].
  • Conversely, signaling by TP alpha S329A was insensitive to cicaprost stimulation whereas it was fully desensitized by NO/PKG signaling [8].

Chemical compound and disease context of Cicaprost

  • Rodent model of systemic mammary tumor disease by surgical removal of the spontaneously metastasizing SMT2A mammary carcinoma: inhibitory effect of the stable prostacyclin analogue cicaprost on occult metastasis [2].
  • The inhibitory effect of ILP and c-PGI(2) on AVP-stimulated L(p) is partially reversed by the protein kinase C inhibitor staurosporine and abolished by pertussis toxin; no effect was obtained with CCP [9].
  • In contrast, neither glibenclamide (10 microM), a blocker of ATP-sensitive K+ channels, nor fluoxetine hydrochloride (100 microM), a blocker of G-protein-gated inward rectifier K+ channels, nor pertussis toxin (PTX; 1 microg/ml), which irreversibly inhibits Gi/Go, reduced relaxation to cicaprost [10].
  • Effects of cicaprost and fosinopril on the progression of rat diabetic nephropathy [11].

Biological context of Cicaprost

  • Consistent with previous studies, cicaprost abrogated U46619-mediated platelet aggregation and mobilization of intracellular calcium ([Ca(2+)](i)) [12].
  • Whole cell phosphorylation assays demonstrated that the mIP undergoes cicaprost-induced PKA phosphorylation. mIP(S357A), a site-directed mutant of mIP, efficiently coupled to G alpha(s) but failed to couple to G alpha(i) or to efficiently couple to G alpha(q):PLC [13].
  • OBJECTIVE: We investigated the role of the inward rectifier potassium (KIR) channel and the cyclic AMP-dependent pathway in mediating vasorelaxation induced by the prostacyclin analogue cicaprost [10].
  • Serum-induced proliferation, as assessed by [(3)H]thymidine incorporation (30 h) or cell number (48 h), was significantly inhibited with a 10-fold difference in potency, ranking in effectiveness UT-15 > iloprost > cicaprost > beraprost [14].
  • Cicaprost was used as the test agonist because of its high stability, selectivity and potency (IC50 = 3.8 nM) [15].

Anatomical context of Cicaprost


Associations of Cicaprost with other chemical compounds

  • Moreover, the prostacyclin mimetic, cicaprost, and the cAMP analogue, dibutyryl cAMP, inhibited GM-CSF release from these cells [19].
  • In functional studies, PGI2 and its analogs, iloprost and cicaprost, were able to stimulate LHRH release from the GT1-1 cells with elevated potencies (EC50 = 0.6-4.3 nM); PGE1 was only slightly less active (EC50 = 28.5 nM), whereas PGE2, considered the major PG involved in LHRH secretion, was poorly effective (EC50 = 921 nM) [20].
  • METHODS: Small vessel myography was used to assess responses to cicaprost in segments of rat tail artery contracted with phenylephrine [10].
  • In the same samples, the LPS-stimulated production of TNF was markedly attenuated by rolipram or cicaprost [21].
  • The selective adenosine A1-receptor antagonist, DPCPX, used at a sufficiently high concentration (5 microM) to block adenosine A2-receptors, did not affect cicaprost inhibition.(ABSTRACT TRUNCATED AT 250 WORDS)[15]

Gene context of Cicaprost


Analytical, diagnostic and therapeutic context of Cicaprost

  • 2. We have investigated the pharmacological effects of cicaprost, a synthetic PGI2 analogue which is metabolically stable and bioavailable after oral administration, in eight healthy male volunteers [24].
  • Cicaprost also induced a significant elevation in RPF and a significant decrease in filtration fraction [25].
  • Plasma and urine levels of cicaprost were measured with a sensitive radioimmunoassay on the last treatment day [26].
  • Longer studies with dose titration are probably needed to demonstrate the beneficial effects, if any, of cicaprost in patients with Raynaud's secondary to SSc, and these are being planned [27].
  • Thus, cicaprost is an orally available PGI2-mimetic, for which effects on platelet aggregation and vascular perfusion have been demonstrated in healthy volunteers after doses of 5 to 15 micrograms [28].


  1. Prostacylin receptor activation inhibits proliferation of aortic smooth muscle cells by regulating cAMP response element-binding protein- and pocket protein-dependent cyclin a gene expression. Kothapalli, D., Stewart, S.A., Smyth, E.M., Azonobi, I., Pure, E., Assoian, R.K. Mol. Pharmacol. (2003) [Pubmed]
  2. Rodent model of systemic mammary tumor disease by surgical removal of the spontaneously metastasizing SMT2A mammary carcinoma: inhibitory effect of the stable prostacyclin analogue cicaprost on occult metastasis. Schirner, M., Schneider, M.R. Int. J. Cancer (1995) [Pubmed]
  3. Antiatherosclerotic effects of oral cicaprost in experimental hypercholesterolemia in rabbits. Braun, M., Hohlfeld, T., Kienbaum, P., Weber, A.A., Sarbia, M., Schrör, K. Atherosclerosis (1993) [Pubmed]
  4. Activation of IP prostanoid receptors prevents cardiomyocyte hypertrophy via cAMP-dependent signaling. Ritchie, R.H., Rosenkranz, A.C., Huynh, L.P., Stephenson, T., Kaye, D.M., Dusting, G.J. Am. J. Physiol. Heart Circ. Physiol. (2004) [Pubmed]
  5. The prostacyclin analogue cicaprost inhibits metastasis of tumours of R 3327 MAT Lu prostate carcinoma and SMT 2A mammary carcinoma. Schirner, M., Schneider, M.R. J. Cancer Res. Clin. Oncol. (1992) [Pubmed]
  6. Internalization and Recycling of the Human Prostacyclin Receptor Is Modulated through Its Isoprenylation-dependent Interaction with the {delta} Subunit of cGMP Phosphodiesterase 6. Wilson, S.J., Smyth, E.M. J. Biol. Chem. (2006) [Pubmed]
  7. Antimitogenesis linked to regulation of Skp2 gene expression. Stewart, S.A., Kothapalli, D., Yung, Y., Assoian, R.K. J. Biol. Chem. (2004) [Pubmed]
  8. The alpha, but not the beta, isoform of the human thromboxane A2 receptor is a target for nitric oxide-mediated desensitization. Independent modulation of Tp alpha signaling by nitric oxide and prostacyclin. Reid, H.M., Kinsella, B.T. J. Biol. Chem. (2003) [Pubmed]
  9. Localization of IP in rabbit kidney and functional role of the PGI(2)/IP system in cortical collecting duct. Nasrallah, R., Nusing, R.M., Hébert, R.L. Am. J. Physiol. Renal Physiol. (2002) [Pubmed]
  10. Evidence that inward rectifier K+ channels mediate relaxation by the PGI2 receptor agonist cicaprost via a cyclic AMP-independent mechanism. Orie, N.N., Fry, C.H., Clapp, L.H. Cardiovasc. Res. (2006) [Pubmed]
  11. Effects of cicaprost and fosinopril on the progression of rat diabetic nephropathy. Villa, E., Rábano, A., Ruilope, L.M., García-Robles, R. Am. J. Hypertens. (1997) [Pubmed]
  12. The alpha, but not the beta, isoform of the human thromboxane A2 receptor is a target for prostacyclin-mediated desensitization. Walsh, M.T., Foley, J.F., Kinsella, B.T. J. Biol. Chem. (2000) [Pubmed]
  13. Protein kinase A-mediated phosphorylation of serine 357 of the mouse prostacyclin receptor regulates its coupling to G(s)-, to G(i)-, and to G(q)-coupled effector signaling. Lawler, O.A., Miggin, S.M., Kinsella, B.T. J. Biol. Chem. (2001) [Pubmed]
  14. Differential effects of stable prostacyclin analogs on smooth muscle proliferation and cyclic AMP generation in human pulmonary artery. Clapp, L.H., Finney, P., Turcato, S., Tran, S., Rubin, L.J., Tinker, A. Am. J. Respir. Cell Mol. Biol. (2002) [Pubmed]
  15. Inhibition of rat colon contractility by prostacyclin (IP-) receptor agonists: involvement of NANC neurotransmission. Qian, Y.M., Jones, R.L. Br. J. Pharmacol. (1995) [Pubmed]
  16. Distinction between relaxations induced via prostanoid EP(4) and IP(1) receptors in pig and rabbit blood vessels. Jones, R.L., Chan, K. Br. J. Pharmacol. (2001) [Pubmed]
  17. Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Jones, R.L., Wise, H., Clark, R., Whiting, R.L., Bley, K.R. Br. J. Pharmacol. (2006) [Pubmed]
  18. Functional and ligand binding studies suggest heterogeneity of platelet prostacyclin receptors. Armstrong, R.A., Lawrence, R.A., Jones, R.L., Wilson, N.H., Collier, A. Br. J. Pharmacol. (1989) [Pubmed]
  19. Cyclooxygenase-2 regulates granulocyte-macrophage colony-stimulating factor, but not interleukin-8, production by human vascular cells: role of cAMP. Stanford, S.J., Pepper, J.R., Mitchell, J.A. Arterioscler. Thromb. Vasc. Biol. (2000) [Pubmed]
  20. Expression of prostacyclin receptors in luteinizing hormone-releasing hormone immortalized neurons: role in the control of hormone secretion. Pimpinelli, F., Rovati, G.E., Capra, V., Piva, F., Martini, L., Maggi, R. Endocrinology (1999) [Pubmed]
  21. Anti-inflammatory activities of cAMP-elevating agents: enhancement of IL-10 synthesis and concurrent suppression of TNF production. Eigler, A., Siegmund, B., Emmerich, U., Baumann, K.H., Hartmann, G., Endres, S. J. Leukoc. Biol. (1998) [Pubmed]
  22. Regulation of tumor necrosis factor alpha- and interleukin-1-beta-induced induced adhesion molecule expression in human vascular smooth muscle cells by cAMP. Braun, M., Pietsch, P., Zepp, A., Schrör, K., Baumann, G., Felix, S.B. Arterioscler. Thromb. Vasc. Biol. (1997) [Pubmed]
  23. Prostacyclin receptor induces STAT1 and STAT3 phosphorylations in human erythroleukemia cells: a mechanism requiring PTX-insensitive G proteins, ERK and JNK. Lo, R.K., Wise, H., Wong, Y.H. Cell. Signal. (2006) [Pubmed]
  24. Cicaprost, an orally active prostacyclin analogue: its effects on platelet aggregation and skin blood flow in normal volunteers. Belch, J.J., McLaren, M., Lau, C.S., Mackay, I.R., Bancroft, A., McEwen, J., Thompson, J.M. British journal of clinical pharmacology. (1993) [Pubmed]
  25. Cicaprost, a prostacyclin analog, protects renal function in uninephrectomized dogs in the absence of changes in blood pressure. Villa, E., Martinez, J., Ruilope, L.M., Mampaso, F., Sancho, J.M., Robles, R.G. Am. J. Hypertens. (1993) [Pubmed]
  26. Tumor metastasis inhibition with the prostacyclin analogue cicaprost depends on discontinuous plasma peak levels. Schirner, M., Kraus, C., Lichtner, R.B., Schneider, M.R., Hildebrand, M. Prostaglandins Leukot. Essent. Fatty Acids (1998) [Pubmed]
  27. A randomised, double-blind study of cicaprost, an oral prostacyclin analogue, in the treatment of Raynaud's phenomenon secondary to systemic sclerosis. Lau, C.S., Belch, J.J., Madhok, R., Cappell, H., Herrick, A., Jayson, M., Thompson, J.M. Clinical and experimental rheumatology. (1993) [Pubmed]
  28. Pharmacokinetics and pharmacodynamics of cicaprost in healthy volunteers after oral administration of 5 to 20 micrograms. Hildebrand, M., Staks, T., Nieuweboer, B. Eur. J. Clin. Pharmacol. (1990) [Pubmed]
WikiGenes - Universities