“…We exploit ligand binding and inhibitor screens to uncover a susceptibility of TPST1 and TPST2 to different classes of small molecules, including the anti-angiogenic compound suramin and the kinase inhibitor rottlerin. By screening the Published Kinase Inhibitor Set, we identified oxindole-based inhibitors of the Ser/Thr kinase RAF (rapidly accelerated fibrosarcoma) as low-micromolar inhibitors of TPST1 and TPST2. …”
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“…We confirmed that it does so in a concentration-dependent manner with a low micromolar half-maximal inhibitory concentration (IC(50) = 3 μM) in our protein-based ELISA-type setup, while chloroquine, siramesine, and suramin showed no inhibitory activity in this assay. …”
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“…The ATP analog, Bz-ATP, was a less effective agonist than ATP, and PPADS was a more potent inhibitor of the AcP2X receptors than the suramin. AcP2X were uniquely expressed within the cerebral F-cluster, the multifunctional integrative neurosecretory center. …”
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“…The rats in intervention group received intraperitoneal injection of 100uM suramin (a P2Y12 receptor antagonist). In control group, the escape latency, level of microglia activation and ATP content were similar between different time points. …”
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“…From this, we have identified FPA-124 and several suramin-related compounds as novel inhibitors of nsp13 helicase activity in vitro. …”
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“…However, activation of purinergic receptors by the non-selective purinergic agonist ATP (10(−8)–10(−3) M) caused a concentration-dependent increase in intracellular [Ca(2+)] that could be blocked by the P2 antagonists PPADS and suramin. CONCLUSIONS: Primary cultures of rat lacrimal gland myoepithelial cells were established that displayed a heterogeneous expression of muscarinic receptors. …”
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“…Also, treatment with the antiapoptosis drug suramin prevented YopJ-mediated macrophage cytotoxicity and enhanced Y. pseudotuberculosis virulence in vivo. …”
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“…Furthermore, compound 42 could selectively inhibited PTP1B as a mix-type inhibitor with IC(50) value of 134.9 μM, which was 2.5-fold higher than the positive control, suramin sodium (IC(50) 339.0 μM), but not inhibit α-glucosidase. …”
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“…Most of the drugs used for the treatment, e.g., Suramin, have shown several problems, including the high level of toxicity. …”
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“…Vortex keratopathy is commonly caused by certain cationic amphiphilic drugs such as amiodarone, antimalarials, suramin, tamoxifen, chlorpromazine and non-steroidal anti-inflammatory drugs. …”
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“…We further confirmed the antiviral function of silkworm Sirt5 through its effects on viral titers during both knockdown and overexpression experiments. Additionally, Suramin, a Sirt5 inhibitor, was found to promote BmNPV replication. …”
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“…Furthermore, results showed that while administering ATP could mimic EA function, it could be reversed by the ATP P2 receptor antagonist, suramin. (4) Conclusions: Our data provide novel information, indicating that changes in neurotransmitter and cytokine levels can offer insight into acupuncture mechanisms and clinical targeting.…”
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“…Two other anionic fusion inhibitors tested, dextran sulphate and suramin, inhibited movements similarly. Removal of the NH4Cl from the cell medium reversed the lysosomal stasis and restored P-L fusion. …”
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“…The inhibition of the channel by ATP was reversible, concentration dependent (K (i) = 64 μM), and could be completely prevented by pretreatment with suramin, a specific purinergic receptor (P(2)) blocker. …”
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“…The currents evoked by 300 μm ATP were not inhibited by 100 μm suramin, pyridoxal-phosphate-6-azophenyl-2′,4′-disulfonic acid, 2′,3′-O-(2,4,6-trinitrophenol)-ATP, or copper. …”
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“…To evidence the participation of T. cruzi Ecto-NTPDase1 in the infective process, we evaluated the effect of known Ecto-ATPDase inhibitors (ARL 67156, Gadolinium and Suramin), or anti-NTPDase-1 polyclonal antiserum on ATPase and ADPase hydrolytic activities in recombinant T. cruzi NTPDase-1 and in live trypomastigotes. …”
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“…RESULTS: The protease activity was blocked in the presence of the purinergic receptor blockers suramin (50 μM) and PPADS (50 μM) or the extracellular and intracellular calcium chelators EGTA (5 mM) and BAPTA/AM (25, 100, 200 and 500 μM), respectively for P. yoelii and P. berghei. …”
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“…Four LOPAC compounds inhibited the FP-based assay: aurintricarboxylic acid (ATA) (IC(50) = 1.4 μM), suramin sodium salt (IC(50) = 3.6 μM), NF 023 hydrate (IC(50) = 6.2 μM) and tyrphostin AG 538 (IC(50) = 3.6 μM). …”
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“…The general P2 receptor antagonists PPADS and suramin both inhibited LymP2X currents with IC(50) values of 8.1 and 27.4 µM respectively. …”
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“…EFS responses in ICC-LP were significantly reduced by atropine or suramin. SMC and vascular SMC (VSM) also responded to EFS. …”
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