suramin

Summary

Summary: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.

Top Publications

  1. Gallagher C, Salter M. Differential properties of astrocyte calcium waves mediated by P2Y1 and P2Y2 receptors. J Neurosci. 2003;23:6728-39 pubmed
    ..Thus, processes that alter expression or function of these receptors may control the rate and extent of astrocyte Ca2+ waves. ..
  2. Lustberg M, Pant S, Ruppert A, Shen T, Wei Y, Chen L, et al. Phase I/II trial of non-cytotoxic suramin in combination with weekly paclitaxel in metastatic breast cancer treated with prior taxanes. Cancer Chemother Pharmacol. 2012;70:49-56 pubmed publisher
    b>Suramin, a polysulfonated naphthylurea, inhibits the actions of polypeptide growth factors including acidic and basic fibroblast growth factors (aFGF and bFGF), which confer broad spectrum chemotherapy resistance...
  3. Lee H, Chung S. The effect of subconjunctival suramin on corneal neovascularization in rabbits. Cornea. 2010;29:86-92 pubmed publisher
    To evaluate the effect of subconjunctival injection of suramin on corneal neovascularization in rabbits.
  4. Ludlow M, Durai L, Ennion S. Functional characterization of intracellular Dictyostelium discoideum P2X receptors. J Biol Chem. 2009;284:35227-39 pubmed publisher
    ..insensitive to copper and the P2 receptor antagonists pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid and suramin. Unusual for P2X channels, dP2XA and dP2XB were also Cl(-)-permeable...
  5. Jiao L, Ouyang S, Liang M, Niu F, Shaw N, Wu W, et al. Structure of severe fever with thrombocytopenia syndrome virus nucleocapsid protein in complex with suramin reveals therapeutic potential. J Virol. 2013;87:6829-39 pubmed publisher
    ..In the screening of inhibitors Suramin was identified to bind phleboviral N specifically...
  6. Zhou X, Tan T, Valiyaveettil S, Go M, Kini R, Velazquez Campoy A, et al. Structural characterization of myotoxic ecarpholin S from Echis carinatus venom. Biophys J. 2008;95:3366-80 pubmed publisher
    ..The crystal structures of native ecarpholin S and its complexes with lauric acid, and its inhibitor suramin, were elucidated. This is the first report of the structure of a member of the Ser(49)-PLA(2) subgroup...
  7. Horner S, Menke K, Hildebrandt C, Kassack M, Nickel P, Ullmann H, et al. The novel suramin analogue NF864 selectively blocks P2X1 receptors in human platelets with potency in the low nanomolar range. Naunyn Schmiedebergs Arch Pharmacol. 2005;372:1-13 pubmed
    ..means of selectively inhibiting platelet P2X1 receptors have been described, although recent work has shown that suramin is a useful lead compound for the development of high-affinity P2X1 antagonists...
  8. Zhuang S, Schnellmann R. Suramin promotes proliferation and scattering of renal epithelial cells. J Pharmacol Exp Ther. 2005;314:383-90 pubmed
    ..In this study, we show that suramin, a polysulfonated naphthylurea, stimulates outgrowth, scattering, and proliferation of primary cultures of renal ..
  9. Sim J, Broomhead H, North R. Ectodomain lysines and suramin block of P2X1 receptors. J Biol Chem. 2008;283:29841-6 pubmed publisher
    ..b>Suramin has been widely used as an antagonist at P2X receptors, and its analog 4,4',4'',4'''-[carbonylbis(imino-5,1,3-..

More Information

Publications61

  1. McGeary R, Bennett A, Tran Q, Cosgrove K, Ross B. Suramin: clinical uses and structure-activity relationships. Mini Rev Med Chem. 2008;8:1384-94 pubmed
    b>Suramin is a polysulfonated polyaromatic symmetrical urea. It is currently used to treat African river blindness and African sleeping sickness...
  2. Goto T, Takeuchi S, Miura K, Ohshima S, Mikami K, Yoneyama K, et al. Suramin prevents fulminant hepatic failure resulting in reduction of lethality through the suppression of NF-kappaB activity. Cytokine. 2006;33:28-35 pubmed
    b>Suramin is a symmetrical polysulfonated naphthylamine derivative of urea. There have been few studies on the effect of suramin on cytokines. We examined the effects of suramin on production of inflammatory cytokines...
  3. Safarinejad M. Combination chemotherapy with docetaxel, estramustine and suramin for hormone refractory prostate cancer. Urol Oncol. 2005;23:93-101 pubmed
    ..against hormone refractory prostate cancer (HRPC) with the combination of estramustine (EM), docetaxel, and suramin. A total of 42 patients with symptomatic, progressive HRPC were included in this study...
  4. Fonfria E, Clay W, Levy D, Goodwin J, Roman S, Smith G, et al. Cloning and pharmacological characterization of the guinea pig P2X7 receptor orthologue. Br J Pharmacol. 2008;153:544-56 pubmed publisher
    ..possessed higher affinity for 1-[N,O-bis(5-isoquinoline sulphonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine (KN62), suramin and Coomassie Brilliant Blue than human or rat P2X(7) receptors suggesting that it is pharmacologically different ..
  5. Zhuang S, Lu B, Daubert R, Chavin K, Wang L, Schnellmann R. Suramin promotes recovery from renal ischemia/reperfusion injury in mice. Kidney Int. 2009;75:304-11 pubmed publisher
    b>Suramin is a polysulfonated naphthylurea originally designed as a treatment for trypanosomiasis; but that has also been used to treat rodent models of fulminant hepatic failure and focal brain ischemia...
  6. Pankratov Y, Lalo U, Verkhratsky A, North R. Quantal release of ATP in mouse cortex. J Gen Physiol. 2007;129:257-65 pubmed
    ..receptor (AMPA, kainate) antagonists; smaller events were partially inhibited by P2X receptor antagonists suramin and PPADS. The decay of the larger events was selectively prolonged by cyclothiazide...
  7. Korrapati M, Shaner B, Schnellmann R. Recovery from glycerol-induced acute kidney injury is accelerated by suramin. J Pharmacol Exp Ther. 2012;341:126-36 pubmed publisher
    ..In this study, we examined the efficacy and mechanism(s) of suramin in promoting recovery from glycerol-induced AKI, a model of rhabdomyolysis-induced AKI...
  8. Liu N, Tolbert E, Ponnusamy M, Yan H, Zhuang S. Delayed administration of suramin attenuates the progression of renal fibrosis in obstructive nephropathy. J Pharmacol Exp Ther. 2011;338:758-66 pubmed publisher
    We recently showed that suramin treatment prevents the onset of renal fibrosis in a model of obstructive nephropathy induced by unilateral ureteral obstruction (UUO)...
  9. Brun R, Blum J, Chappuis F, Burri C. Human African trypanosomiasis. Lancet. 2010;375:148-59 pubmed publisher
    ..WHO has stated that if national control programmes, international organisations, research institutes, and philanthropic partners engage in concerted action, elimination of this disease might even be possible. ..
  10. Kibona S, Matemba L, Kaboya J, Lubega G. Drug-resistance of Trypanosoma b. rhodesiense isolates from Tanzania. Trop Med Int Health. 2006;11:144-55 pubmed
    ..To determine the drug resistance of Trypanosoma brucei rhodesiense strains isolated from sleeping sickness patients in Tanzania...
  11. Morgan H, McNae I, Nowicki M, Zhong W, Michels P, Auld D, et al. The trypanocidal drug suramin and other trypan blue mimetics are inhibitors of pyruvate kinases and bind to the adenosine site. J Biol Chem. 2011;286:31232-40 pubmed publisher
    ..The molecular structures of the dyes provided a starting point for the synthesis of suramin, which was developed and used as a trypanocidal drug in 1916 and is still in clinical use...
  12. Schuetz A, Min J, Antoshenko T, Wang C, Allali Hassani A, Dong A, et al. Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin. Structure. 2007;15:377-89 pubmed
    ..We identified suramin as a compound that binds to human SIRT5 and showed that it inhibits SIRT5 NAD(+)-dependent deacetylase activity ..
  13. Pearson R, Dale N, Llaudet E, Mobbs P. ATP released via gap junction hemichannels from the pigment epithelium regulates neural retinal progenitor proliferation. Neuron. 2005;46:731-44 pubmed
    ..ATP released from RPE hemichannels speeds both cell division and proliferation in the neural retina. ..
  14. Nash P, Olovsson M, Eriksson U. Placental dysfunction in Suramin-treated rats: impact of maternal diabetes and effects of antioxidative treatment. J Soc Gynecol Investig. 2005;12:174-84 pubmed
    ..rats of two different strains (U and H) were given intraperitoneal (IP) injections of the angiogenesis inhibitor Suramin (Sigma Chemical Co, St Louis, MO) or saline in early pregnancy, and fed standard or vitamin E-enriched food...
  15. Korrapati M, Shaner B, Neely B, Alge J, Arthur J, Schnellmann R. Diabetes-induced renal injury in rats is attenuated by suramin. J Pharmacol Exp Ther. 2012;343:34-43 pubmed publisher
    ..We examined the efficacy and mechanism(s) of suramin on hyperglycemia-induced renal injury before development of overt histological damage...
  16. Jagielski A, Kryskiewicz E, Bryła J. Suramin-induced reciprocal changes in glucose and lactate synthesis in renal tubules contribute to its hyperglycaemic action. Eur J Pharmacol. 2006;537:205-9 pubmed
    b>Suramin is the drug of choice for the treatment of African trypanosomiasis and onchocerciasis. It is also tested for its potential use as an anticancer agent and chemosensitizer...
  17. Huang H, Mohan S, Yu C. The NMR solution structure of human epidermal growth factor (hEGF) at physiological pH and its interactions with suramin. Biochem Biophys Res Commun. 2010;402:705-10 pubmed publisher
    ..b>Suramin, a polysulfonated naphthylurea that acts as a growth factor blocker, exhibits antiproliferative activity against ..
  18. Chung W, Kermode J. Suramin disrupts receptor-G protein coupling by blocking association of G protein alpha and betagamma subunits. J Pharmacol Exp Ther. 2005;313:191-8 pubmed
    ..b>Suramin is considered a lead compound targeting this moiety...
  19. Chan Y, Li Y, Foster W, Fu F, Huard J. The use of suramin, an antifibrotic agent, to improve muscle recovery after strain injury. Am J Sports Med. 2005;33:43-51 pubmed
    ..Muscle healing often is hindered by scar tissue formation after injury. Suramin can prevent scar tissue formation and improve muscle healing after injury because of its ability to antagonize ..
  20. Liu N, Zhuang S. Tissue protective and anti-fibrotic actions of suramin: new uses of an old drug. Curr Clin Pharmacol. 2011;6:137-42 pubmed
    b>Suramin is a polysulfonated naphthylurea, which was originally synthesized and designed as a treatment for trypanosomiasis and selected malignancies and metastatic diseases...
  21. Wolf C, Rosefort C, Fallah G, Kassack M, Hamacher A, Bodnar M, et al. Molecular determinants of potent P2X2 antagonism identified by functional analysis, mutagenesis, and homology docking. Mol Pharmacol. 2011;79:649-61 pubmed publisher
    ..acid) tetrasodium salt (NF770) as a nanomolar-potent competitive P2X2 receptor antagonist within a series of 139 suramin derivatives...
  22. Leng Y, Yamamoto T, Kadowaki M. Alteration of cholinergic, purinergic and sensory neurotransmission in the mouse colon of food allergy model. Neurosci Lett. 2008;445:195-8 pubmed publisher
    ..2%). Pretreatment with P2 purinoceptor antagonists [suramin and PPADs] significantly (P < 0.01) reduced the ATP-evoked contractions to 7.7% and 1...
  23. Qiu F, Dahl G. A permeant regulating its permeation pore: inhibition of pannexin 1 channels by ATP. Am J Physiol Cell Physiol. 2009;296:C250-5 pubmed publisher
    ..ATP analogues, including benzoylbenzoyl-ATP, suramin, and brilliant blue G were even more effective inhibitors of pannexin 1 currents than ATP...
  24. Taniguti A, Pertille A, Matsumura C, Santo Neto H, Marques M. Prevention of muscle fibrosis and myonecrosis in mdx mice by suramin, a TGF-?1 blocker. Muscle Nerve. 2011;43:82-7 pubmed publisher
    ..We evaluated the effect of suramin, a transforming growth factor-beta 1 (TGF-?1) blocker, on fibrosis in mdx mice...
  25. Trujillo C, Nery A, Martins A, Majumder P, Gonzalez F, Ulrich H. Inhibition mechanism of the recombinant rat P2X(2) receptor in glial cells by suramin and TNP-ATP. Biochemistry. 2006;45:224-33 pubmed
    ..Our objective has been to determine the pharmacological activity of the antagonist suramin, the most important antagonist of purinergic receptor function, as well as to demonstrate its noncompetitive ..
  26. Murakami M, Arruda E, Melo P, Martinez A, Calil Elias S, Tomaz M, et al. Inhibition of myotoxic activity of Bothrops asper myotoxin II by the anti-trypanosomal drug suramin. J Mol Biol. 2005;350:416-26 pubmed
    b>Suramin, a synthetic polysulfonated compound, developed initially for the treatment of African trypanosomiasis and onchocerciasis, is currently used for the treatment of several medically relevant disorders...
  27. Ikeda M. Characterization of functional P2X(1) receptors in mouse megakaryocytes. Thromb Res. 2007;119:343-53 pubmed
    ..5, respectively. P2X receptor antagonists except suramin significantly inhibited the P2X(1) responses with an IC(50) values of 0...
  28. Cao L, Young M, Broomhead H, Fountain S, North R. Thr339-to-serine substitution in rat P2X2 receptor second transmembrane domain causes constitutive opening and indicates a gating role for Lys308. J Neurosci. 2007;27:12916-23 pubmed
    ..b>Suramin, which is a noncompetitive antagonist at wild-type P2X2 receptors, had a pronounced agonist action at both P2X2[..
  29. Liu N, Tolbert E, Pang M, Ponnusamy M, Yan H, Zhuang S. Suramin inhibits renal fibrosis in chronic kidney disease. J Am Soc Nephrol. 2011;22:1064-75 pubmed publisher
    ..b>Suramin is a compound that inhibits the interaction of several cytokines and growth factors with their receptors, but ..
  30. Hausmann R, Rettinger J, Gerevich Z, Meis S, Kassack M, Illes P, et al. The suramin analog 4,4',4'',4'''-(carbonylbis(imino-5,1,3-benzenetriylbis (carbonylimino)))tetra-kis-benzenesulfonic acid (NF110) potently blocks P2X3 receptors: subtype selectivity is determined by location of sulfonic acid groups. Mol Pharmacol. 2006;69:2058-67 pubmed
    We have previously identified the suramin analog 4,4',4'',4'''-(carbonylbis(imino-5,1,3-benzenetriylbis(carbonylimino)))tetrakis-benzene-1,3-disulfonic acid (NF449) as a low nanomolar potency antagonist of recombinant P2X(1) receptors...
  31. Li C, Jiang X, Yang L, Liu X, Yue S, Li L. Involvement of sphingosine 1-phosphate (SIP)/S1P3 signaling in cholestasis-induced liver fibrosis. Am J Pathol. 2009;175:1464-72 pubmed publisher
    ..Furthermore, a selective S1P(3) receptor antagonist, suramin, markedly reduced the number of BM-derived cells during cholestasis...
  32. Karam G, Rasaee M, Mahmoodi M, Khaksari M. Inhibition of proteinase 3 (PR3) by suramin and fetal calf serum (FCS): effect of PR3 and suramin on Chinese hamster ovary cells (CHO-cells). Pak J Pharm Sci. 2005;18:46-8 pubmed
    ..A number of inhibitors for this proteinase are reported. Comprehensive studies on the inhibitory effect of suramin and heat treated fetal calf serum (deltaFCS) on PR3 have not been reported...
  33. Pankratov Y, Lalo U, Krishtal O, Verkhratsky A. P2X receptor-mediated excitatory synaptic currents in somatosensory cortex. Mol Cell Neurosci. 2003;24:842-9 pubmed
    ..We concluded that several subtypes of P2X purinoreceptors participate in synaptic transmission in neocortex. ..
  34. Uchio E, Linehan W, Figg W, Walther M. A phase I study of intravesical suramin for the treatment of superficial transitional cell carcinoma of the bladder. J Urol. 2003;169:357-60 pubmed
    b>Suramin is a polysulfonated naphthylurea that inhibits proliferation and DNA synthesis of transitional cell carcinoma cell lines...
  35. Kassack M, Braun K, Ganso M, Ullmann H, Nickel P, Böing B, et al. Structure-activity relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist. Eur J Med Chem. 2004;39:345-57 pubmed
    ..5). In conclusion, NF449 remains the most potent and selective P2X(1) antagonist known. Potential lead compounds among the suramin class for P2X(3) (16d) and P2Y(1) (16a) receptors were identified.
  36. Aguilar J, Rice M, Wagner E. The polysulfonated compound suramin blocks adsorption and lateral difusion of herpes simplex virus type-1 in vero cells. Virology. 1999;258:141-51 pubmed
    ..We analyzed the actions of the polysulfonate compound suramin on the replication of herpes simplex virus type 1 (HSV-1) and compared them with the actions of heparin...
  37. Fleck S, Birdsall B, Babon J, Dluzewski A, Martin S, Morgan W, et al. Suramin and suramin analogues inhibit merozoite surface protein-1 secondary processing and erythrocyte invasion by the malaria parasite Plasmodium falciparum. J Biol Chem. 2003;278:47670-7 pubmed
    ..b>Suramin was shown to inhibit both merozoite invasion and MSP142 proteolytic cleavage...
  38. Abdiu A, Larsson S, Wasteson A, Walz T. Suramin blocks growth-stimulatory effects of platelet-derived growth factor on malignant fibrous histiocytomas in vitro. Cancer Lett. 1999;146:189-94 pubmed
    The pattern of susceptibility of malignant cells to the cytostatic drug suramin is not fully clarified...
  39. Russell J, Gill J, Sorenson E, Schultz D, Windebank A. Suramin-induced neuropathy in an animal model. J Neurol Sci. 2001;192:71-80 pubmed
    b>Suramin is being used either alone, or in combination with other chemotherapeutic agents, in the treatment of hormone-refractory or metastatic prostate cancer...
  40. Fujiyama C, Jones A, Fuggle S, Bicknell R, Cranston D, Harris A. Human bladder cancer invasion model using rat bladder in vitro and its use to test mechanisms and therapeutic inhibitors of invasion. Br J Cancer. 2001;84:558-64 pubmed
    ..the model to test the ability of 4 compounds that interfere with tumour cell-extracellular matrix interactions (suramin, N-acetylcysteine and the urokinase plasminogen activator pathway antagonists A5 compound and monoclonal antibody ..
  41. Nok A. Arsenicals (melarsoprol), pentamidine and suramin in the treatment of human African trypanosomiasis. Parasitol Res. 2003;90:71-9 pubmed
    ..So far the treatment for the early stage of HAT involves the drugs pentamidine and suramin which have been very successful...
  42. Zanghi J, Renner W, Bailey J, Fussenegger M. The growth factor inhibitor suramin reduces apoptosis and cell aggregation in protein-free CHO cell batch cultures. Biotechnol Prog. 2000;16:319-25 pubmed
    ..in apoptosis under these conditions, we examined the effect of the growth factor inhibitor and antitumor agent suramin on CHO cell growth and apoptosis in serum-free culture...
  43. Jennings F, Rodgers J, Bradley B, Gettinby G, Kennedy P, Murray M. Human African trypanosomiasis: potential therapeutic benefits of an alternative suramin and melarsoprol regimen. Parasitol Int. 2002;51:381-8 pubmed
    ..The regimen commonly prescribed to treat CNS-stage disease involves the use of the trypanocidal drugs suramin and melarsoprol...
  44. Darsaud A, Chevrier C, Bourdon L, Dumas M, Buguet A, Bouteille B. Megazol combined with suramin improves a new diagnosis index of the early meningo-encephalitic phase of experimental African trypanosomiasis. Trop Med Int Health. 2004;9:83-91 pubmed
    ..alone at optimal doses does not cure late-stage disease tested in mouse models, however the combination of suramin and megazol is able to cure infected mice without CNS involvement...
  45. Chan Y, Li Y, Foster W, Horaguchi T, Somogyi G, Fu F, et al. Antifibrotic effects of suramin in injured skeletal muscle after laceration. J Appl Physiol (1985). 2003;95:771-80 pubmed
    ..Our studies have shown that decreased fibrosis could improve muscle healing. Suramin has been found to inhibit transforming growth factor (TGF)-beta1 expression by competitively binding to the ..
  46. de Oliveira M, Cavalcante W, Arruda E, Melo P, Dal Pai Silva M, Gallacci M. Antagonism of myotoxic and paralyzing activities of bothropstoxin-I by suramin. Toxicon. 2003;42:373-9 pubmed
    ..In this work, we evaluated the ability of suramin, a polysulfonated naphtylurea derivative, to antagonize the myotoxic and the paralyzing activities of BthTX-I on ..
  47. King B, Townsend Nicholson A, Wildman S, Thomas T, Spyer K, Burnstock G. Coexpression of rat P2X2 and P2X6 subunits in Xenopus oocytes. J Neurosci. 2000;20:4871-7 pubmed
    ..Also, H(+) ions inhibited ATP responses at low pH levels (<pH 6.3). The pH-dependent blocking activity of suramin was changed at this heteromeric receptor, although the potentiating effect of Zn(2+) on ATP responses was ..
  48. Soto F, Krause U, Borchardt K, Ruppelt A. Cloning, tissue distribution and functional characterization of the chicken P2X1 receptor. FEBS Lett. 2003;533:54-8 pubmed
    ..However, the antagonists suramin and NF023 were much less potent at chicken P2X1 receptors than at human P2X1 receptors...
  49. Lambrecht G, Braun K, Damer M, Ganso M, Hildebrandt C, Ullmann H, et al. Structure-activity relationships of suramin and pyridoxal-5'-phosphate derivatives as P2 receptor antagonists. Curr Pharm Des. 2002;8:2371-99 pubmed
    ..recently been described which to some degree are more potent and more selective than earlier antagonists like suramin or pyridoxal-5'-phosphate-6-azophenyl-2',4'-disulfonic acid (PPADS)...
  50. Marchetti D, Reiland J, Erwin B, Roy M. Inhibition of heparanase activity and heparanase-induced angiogenesis by suramin analogues. Int J Cancer. 2003;104:167-74 pubmed
    ..Heparanase activity correlates with the metastatic propensity of tumor cells. Suramin, a polysulfonated naphthylurea, is an inhibitor of heparanase with suramin analogues shown to possess ..
  51. Xu K, Ren H, Zhu J, Yang Y, Liao F. Suramin inhibits the in vitro expression of encephalitis B virus proteins NS3 and E. J Huazhong Univ Sci Technolog Med Sci. 2003;23:375-9 pubmed
    In this study, the mechanism by which Suramin inhibits the replication of epidemic encephalitis B virus was explored to provide a theoretical basis for its further application in clinical practice...
  52. Gan Y, Au J, Lu J, Wientjes M. Antiproliferative and cytotoxic effects of geldanamycin, cytochalasin E, suramin and thiacetazone in human prostate xenograft tumor histocultures. Pharm Res. 1998;15:1760-6 pubmed
    ..b>Suramin, a clinically active compound was included for comparison. Methods...