“…To showcase the potential of microcalorimetry for measuring drug action on pathogenic organisms, we tested the method with three antitrypanosomal drugs, melarsoprol, suramin and pentamidine and three antiplasmodial drugs, chloroquine, artemether and dihydroartemisinin, each at two concentrations on the respective parasite. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Besides that, the ICER was stable for 32 days, enough time to investigate samples of possible inhibitors, including especially the compound Suramin, that inhibited 51% the enzyme activity at 100 µmol·L(−1), which is in accordance with the data for the enzyme in solution.…”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Moreover, cilium induction by these drugs was hampered in the presence of the ATP degrading enzyme, apyrase, and in the presence of the pan-purinergic receptor inhibitor, suramin. Our findings reveal that ciliogenic drug-induced re-expression of the primary cilium in pancreatic cancer cells is, at least in certain contexts, dependent on a hitherto unrecognized autocrine/paracrine loop involving the extracellular ATP-purinergic receptor signaling pathway that can be exploited in a therapeutic approach targeting at restoring the primary cilium.…”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Suramin was the first urea-based drug to be approved in clinic, and in the following century a number of milestone drugs based on this scaffold were developed. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Exposing the control compound DMSO, negative compound sucrose, and known CIPN-causing drugs (paclitaxel, vincristine, oxaliplatin, suramin, bortezomib) for 24 h, results show the somatic area-learning AI detected significant cytotoxicity for paclitaxel (* p < 0.05) and oxaliplatin (* p < 0.05). …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The inhibition studies revealed pronounced differences in the potency of reactive blue 2, pyridoxalphosphate-6-azophenyl-2-4-disulfonic acid (PPADS), suramin, and N(6)-diethyl-β,γ-dibromomethylene-ATP (ARL67156) towards the NTPDase isoforms. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Transport of v- sis protein beyond the Golgi correlated with acquisition of the transformed phenotype. Furthermore, suramin treatment reversed transformation and upregulated the expression of cell surface PDGF receptors, suggesting an important role for receptor-ligand complexes localized to the cell surface.…”
Enlace del recurso
Enlace del recurso

“…The asymmetric growth cone filopodia extension that precedes turning can be blocked with CNQX (10 µM), but not with the ATP and adenosine receptor antagonists suramin (100 µM) and alloxazine (4 µM), suggesting non-NMDA glutamate receptors on the growth cone mediate the interaction with astrocytes. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The agonist sequence for activation was ATP = αβ-MeATP > BzATP = 2-MeSATP, and P2X(f) was inhibited by suramin, PPADS and TNP-ATP. Activation of P2X(f) attenuated the rundown of a quinidine-sensitive K(+) conductance, suggesting that P2X(f) plays a role in K(+) channel regulation. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The addition of eflornithine caused no change in the accumulation of nifurtimox, nor did the addition of clinically relevant doses of the other anti-HAT drugs suramin, nifurtimox or melarsoprol, but a significant increase was observed with the addition of pentamidine. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Interestingly, the cluster morphology caused by N-methyllevamisole was different than the clusters observed for levamisole, and a third “cord-like” morphology resembling that of the known drug suramin was observed for an aniline-containing derivative. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Five well know inhibitors such as suramin, mol-6, sirtinol, 67, and nf675 were selected to establish the nature of the binding mode of the inhibitors in the SIRT2 active site. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…ADP-stimulated ATP release was significantly inhibited by suramin (100 µM, P = 0.002). RT4 urothelial cells break down nucleotides (100 µM) including ATP, ADP, and UTP to liberate phosphate. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The positive control, suramin, inhibited PTP1B with an IC50 (half minimal (50%) inhibitory concentration) value of 16.34 µM; CNB-001 did not affect enzyme activity across the range of 1nM–0.1mM. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Interestingly, enzyme activity assays reveal an interaction between Ap4A hydrolase and the parasite growth inhibitor suramin. We also present a high resolution crystal structure of Ap4A hydrolase in apo- and sulphate- bound state, where the sulphate resides in the enzyme active site by mimicking the phosphate of substrates like Ap4A. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…An inward current was also induced by high concentrations of ATP (100 μM to 10 mM), which was reversibly blocked by 100 μM suramin (a purinergic antagonist) and blocked by nifedipine (an L-type calcium channel blocker). …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…These predictions suggest the use of specific monoclonal antibodies or suramin to target interleukin-2 and tumor necrosis factor [Formula: see text] , followed by mifepristone to inhibit the GCR. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Additionally, the androgen and estrogen targets were screened to avoid pharmaceuticals with off-target interactions. RESULTS: While suramin bound to both immune targets with high affinity, top binders of the hormonal and glucocorticoid targets were non-specific towards their respective proteins, possibly due to high structure similarity between these proteins. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The alpha-adrenoceptor antagonist phentolamine diminished EFS-induced vasoconstriction to a lower extent in HT arteries, while the purinergic receptor antagonist suramin reduced contractile response to EFS only in segments from CT. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Oncogenic Ras-induced proliferation is abolished by addition of an anti–FGF-2 blocking antibody, suramin, or treatment with either sodium chlorate or heparitinase, demonstrating an autocrine requirement for FGF-2. …”
Enlace del recurso
Enlace del recurso