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Suramin

Suramin, a symmetrical, polysulfonated naphthyl-amine, inhibits a number of trypanosomal enzymes however, the importance of these effects on parasite killing is not clear. [Pg.179]

Haemolymphatic stage (acute stage) For the last two decades, the first line treatment for the acute stage are Pentamidine and Suramin [2]. One compound, the prodrug DB 289 (a diamidine), is currently in phase III clinical trials. [Pg.179]

P2X2 Smooth muscle, CNS, retina, chromaffin cells, autonomic and sensory ganglia ATP>ATPyS>2- MeSATP > > a,p-meATP (pH + zinc sensitive) Suramin, isoPPADS, RB2, NF770, NF279 Intrinsic ion channel (particularly Ca2+)... [Pg.1049]

P2X5 Proliferating cells in skin, gut, bladder, thymus, spinal cord ATP > > a,p-meATP, ATPyS Suramin, PPADS, BBG Intrinsic ion channel... [Pg.1049]

P2Y2 Immune cells, epithelial and endothelial cells, kidney tubules, osteoblasts UTP= ATP, UTPyS, INS 37217, INS 365 Suramin > RB2, AR-C126313 Gq/Gn and possibly Gj PLC-p activation... [Pg.1050]

P2Y Spleen, intestine, granulocytes AR- C67085MX > BzATPSATPyS > ATP Suramin > RB2, NF157, 5 -AMPS Gq/Gn and Ggl PLC-p activation... [Pg.1050]

Figure 13.3 Whole-cell patch-clamp recordings of excitatory postsynaptic currents (EPSCs) from dorsal horn neurons of rat (prenatal P2-13) spinal cord slices. The normal evoked EPSC of about 160pA obtained by focal stimulation of nearby tissue was dramatically reduced by addition of a cocktail (CABS) of CNQX 10 pM, D-APV 50 pM, bicuculline 10 pM and strychnine 5 pM to block glutamate, GABAa and glycine receptors. The small residual EPSC shown was blocked by the ATP P2 receptor antagonist suramin and is therefore probably mediated by released ATP. (Prom Bardoni et al. 1997 and reproduced by permission of the Journal of Neuroscience)... Figure 13.3 Whole-cell patch-clamp recordings of excitatory postsynaptic currents (EPSCs) from dorsal horn neurons of rat (prenatal P2-13) spinal cord slices. The normal evoked EPSC of about 160pA obtained by focal stimulation of nearby tissue was dramatically reduced by addition of a cocktail (CABS) of CNQX 10 pM, D-APV 50 pM, bicuculline 10 pM and strychnine 5 pM to block glutamate, GABAa and glycine receptors. The small residual EPSC shown was blocked by the ATP P2 receptor antagonist suramin and is therefore probably mediated by released ATP. (Prom Bardoni et al. 1997 and reproduced by permission of the Journal of Neuroscience)...
Already, the virion-associated reverse transcriptase has been highlighted as a target. The RT gene has been cloned, and the gene product can be produced in large quantities. Several molecules of very diverse molecular structure, such as zidovudine, suramin, and rifabutin, have been shown to cause inhibition of the... [Pg.230]

A. R. Gagliardi, M. Kassack, A. Kremeyer, G. Muller, P. Nickel, and D. C. Collins. Antiangiogenic and antiproliferative activity of suramin analogues. Cancer Chemother. Pharmacol. 41 117-124 (1998). [Pg.613]

Figure 3.10 Molecular structure of the sirtuin inhibitors suramin and NF675. Figure 3.10 Molecular structure of the sirtuin inhibitors suramin and NF675.
Structure-activity studies on suramin analogues as inhibitors of NAD( + )-dependent histone deacetylases (sirtuins). ChemMedChem, 2, 1419-1431. [Pg.83]

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