Summary: Nucleotides in which the base moiety is substituted with one or more sulfur atoms.

Top Publications

  1. Saad F, Hotte S, North S, Eigl B, Chi K, Czaykowski P, et al. Randomized phase II trial of Custirsen (OGX-011) in combination with docetaxel or mitoxantrone as second-line therapy in patients with metastatic castrate-resistant prostate cancer progressing after first-line docetaxel: CUOG trial P-06c. Clin Cancer Res. 2011;17:5765-73 pubmed publisher
    ..Pain relief was higher than expected, with interesting correlations between serum CLU and survival. A phase III trial evaluating the pain palliation benefit of custirsen with taxane therapy is ongoing. ..
  2. Minakawa N, Sanji M, Kato Y, Matsuda A. Investigations toward the selection of fully-modified 4'-thioRNA aptamers: optimization of in vitro transcription steps in the presence of 4'-thioNTPs. Bioorg Med Chem. 2008;16:9450-6 pubmed publisher
  3. Srinivasan S, Mir F, Huang J, Khasawneh F, Lam S, Le Breton G. The P2Y12 antagonists, 2-methylthioadenosine 5'-monophosphate triethylammonium salt and cangrelor (ARC69931MX), can inhibit human platelet aggregation through a Gi-independent increase in cAMP levels. J Biol Chem. 2009;284:16108-17 pubmed publisher
    ..This inhibition is in addition to that derived from antagonism of P2Y12 receptors. ..
  4. Quintas C, Fraga S, Goncalves J, Queiroz G. The P2Y(1) and P2Y(12) receptors mediate autoinhibition of transmitter release in sympathetic innervated tissues. Neurochem Int. 2009;55:505-13 pubmed publisher
    ..P2Y(1) and P2Y(12) receptors are coupled to G(i/o)-proteins and operate as autoreceptors in the vas deferens where they interact with alpha(2)-adrenoceptors on the modulation of noradrenaline release. ..
  5. Misra U, Pizzo S. Upregulation of mTORC2 activation by the selective agonist of EPAC, 8-CPT-2Me-cAMP, in prostate cancer cells: assembly of a multiprotein signaling complex. J Cell Biochem. 2012;113:1488-500 pubmed publisher
  6. Kwan L, Devlin S, Mirocha J, Papadakis K. Thiopurine methyltransferase activity combined with 6-thioguanine metabolite levels predicts clinical response to thiopurines in patients with inflammatory bowel disease. Dig Liver Dis. 2008;40:425-32 pubmed publisher
    ..Thiopurine methyltransferase enzyme activity below 30.5 U combined with a post-treatment 6-thioguanine nucleotide level > 230 pmol/8 x 10(8) erythrocytes was the best predictor of response. ..
  7. Muramaki M, So A, Hayashi N, Sowery R, Miyake H, Fujisawa M, et al. Chemosensitization of gemcitabine-resistant human bladder cancer cell line both in vitro and in vivo using antisense oligonucleotide targeting the anti-apoptotic gene, clusterin. BJU Int. 2009;103:384-90 pubmed publisher
  8. Matsugami A, Ohyama T, Inada M, Inoue N, Minakawa N, Matsuda A, et al. Unexpected A-form formation of 4'-thioDNA in solution, revealed by NMR, and the implications as to the mechanism of nuclease resistance. Nucleic Acids Res. 2008;36:1805-12 pubmed publisher
    ..The origin of the formation of the A-form is discussed. The remarkable biochemical properties reported for fully modified 4'-thioDNA, including nuclease-resistance, are rationalized in the light of the elucidated structure. ..
  9. Redondo M, Tellez T, Roldan M. The role of clusterin (CLU) in malignant transformation and drug resistance in breast carcinomas. Adv Cancer Res. 2009;105:21-43 pubmed publisher
    ..This review summarizes our current understanding of the role of CLU in tumorigenesis, progression, and response to treatment in breast carcinomas. ..

More Information


  1. Laskin J, Nicholas G, Lee C, Gitlitz B, Vincent M, Cormier Y, et al. Phase I/II trial of custirsen (OGX-011), an inhibitor of clusterin, in combination with a gemcitabine and platinum regimen in patients with previously untreated advanced non-small cell lung cancer. J Thorac Oncol. 2012;7:579-86 pubmed publisher
    ..1 compared with 16.1 months for patients who did not (p = 0.02). Based on the above results, a randomized phase 3 trial to evaluate the survival benefit of custirsen in patients with NSCLC is warranted. ..
  2. Sowery R, Hadaschik B, So A, Zoubeidi A, Fazli L, Hurtado Coll A, et al. Clusterin knockdown using the antisense oligonucleotide OGX-011 re-sensitizes docetaxel-refractory prostate cancer PC-3 cells to chemotherapy. BJU Int. 2008;102:389-97 pubmed publisher
  3. Chi K, Siu L, Hirte H, Hotte S, Knox J, Kollmansberger C, et al. A phase I study of OGX-011, a 2'-methoxyethyl phosphorothioate antisense to clusterin, in combination with docetaxel in patients with advanced cancer. Clin Cancer Res. 2008;14:833-9 pubmed publisher
    ..OGX-011 can be given at a biologically effective dose with standard doses of docetaxel. Phase II trials of combined OGX-011 and chemotherapy are ongoing in patients with prostate, breast, and lung cancers. ..
  4. Chi K, Hotte S, Yu E, Tu D, Eigl B, Tannock I, et al. Randomized phase II study of docetaxel and prednisone with or without OGX-011 in patients with metastatic castration-resistant prostate cancer. J Clin Oncol. 2010;28:4247-54 pubmed publisher
    ..50; 95% CI, 0.29 to 0.87). Treatment with OGX-011 and docetaxel was well tolerated with evidence of biologic effect and was associated with improved survival. Further evaluation is warranted. ..
  5. Gonzalez Lama Y, Bermejo F, Lopez Sanroman A, Garcia Sanchez V, Esteve M, Cabriada J, et al. Thiopurine methyl-transferase activity and azathioprine metabolite concentrations do not predict clinical outcome in thiopurine-treated inflammatory bowel disease patients. Aliment Pharmacol Ther. 2011;34:544-54 pubmed publisher
    ..Our results do not support determination of TPMT activity or 6TGN concentrations to predict treatment outcome, and no useful serum metabolites threshold value to adjust the drug's dose was identified. ..
  6. Lamoureux F, Thomas C, Yin M, Kuruma H, Beraldi E, Fazli L, et al. Clusterin inhibition using OGX-011 synergistically enhances Hsp90 inhibitor activity by suppressing the heat shock response in castrate-resistant prostate cancer. Cancer Res. 2011;71:5838-49 pubmed publisher
    ..Together, our findings indicate that Hsp90 inhibitor-induced activation of the heat shock response and CLU is attenuated by OGX-011, with synergistic effects on delaying CRPC progression. ..
  7. Nie H, Chen L, Han D, Li J, Song W, Wei S, et al. Regulation of epithelial sodium channels by cGMP/PKGII. J Physiol. 2009;587:2663-76 pubmed publisher
    ..We therefore conclude that PKGII is an activator of lung epithelial Na(+) channels, which may expedite the resolution of oedematous fluid in alveolar sacs. ..
  8. Hoffmann K, Sixel U, Di Pasquale F, von Kügelgen I. Involvement of basic amino acid residues in transmembrane regions 6 and 7 in agonist and antagonist recognition of the human platelet P2Y(12)-receptor. Biochem Pharmacol. 2008;76:1201-13 pubmed publisher
    ..Arg256 appears to play a role in the recognition of nucleotide agonists and the non-nucleotide antagonist reactive blue-2, but no role in the recognition of the nucleotide antagonist cangrelor. ..
  9. Leonetti C, Biroccio A, D Angelo C, Semple S, Scarsella M, Zupi G. Therapeutic integration of c-myc and bcl-2 antisense molecules with docetaxel in a preclinical model of hormone-refractory prostate cancer. Prostate. 2007;67:1475-85 pubmed
    ..These data indicate that the combined targeting of genes involved in uncontrolled proliferation and evasion of apoptosis renders HRPC responsive to chemotherapy making this treatment a promising antineoplastic strategy. ..
  10. Zhang Y, Sanchez D, Gorelik J, Klenerman D, Lab M, Edwards C, et al. Basolateral P2X4-like receptors regulate the extracellular ATP-stimulated epithelial Na+ channel activity in renal epithelia. Am J Physiol Renal Physiol. 2007;292:F1734-40 pubmed
    ..This requires a mechanism within the cell that leads to either basolateral or apical ATP release to regulate renal tubular function. ..
  11. Bedikian A, Millward M, Pehamberger H, Conry R, Gore M, Trefzer U, et al. Bcl-2 antisense (oblimersen sodium) plus dacarbazine in patients with advanced melanoma: the Oblimersen Melanoma Study Group. J Clin Oncol. 2006;24:4738-45 pubmed
    ..The addition of oblimersen to dacarbazine significantly improved multiple clinical outcomes in patients with advanced melanoma and increased overall survival in patients without an elevated baseline serum LDH. ..
  12. So A, Sinnemann S, Huntsman D, Fazli L, Gleave M. Knockdown of the cytoprotective chaperone, clusterin, chemosensitizes human breast cancer cells both in vitro and in vivo. Mol Cancer Ther. 2005;4:1837-49 pubmed
    ..These data identify clusterin as a valid therapeutic target and provides preclinical proof-of-principle to test OGX-011 in multimodality therapies for breast cancer. ..
  13. Mita M, Ochoa L, Rowinsky E, Kuhn J, Schwartz G, Hammond L, et al. A phase I, pharmacokinetic and biologic correlative study of oblimersen sodium (Genasense, G3139) and irinotecan in patients with metastatic colorectal cancer. Ann Oncol. 2006;17:313-21 pubmed
    ..5-10 months. The combination is well tolerated at the recommended phase II oblimersen sodium dose of 7 mg/kg/day CIVI days 1-8 with irinotecan 280 mg/m2 intravenously on day 6 every 3 weeks. ..
  14. Chi K, Eisenhauer E, Fazli L, Jones E, Goldenberg S, Powers J, et al. A phase I pharmacokinetic and pharmacodynamic study of OGX-011, a 2'-methoxyethyl antisense oligonucleotide to clusterin, in patients with localized prostate cancer. J Natl Cancer Inst. 2005;97:1287-96 pubmed
    ..001 and Ptrend = .01, respectively). OGX-011 is well tolerated and reduces clusterin expression in primary prostate tumors. The optimal biologic dose for OGX-011 at the schedule used is 640 mg. ..
  15. Inoue N, Shionoya A, Minakawa N, Kawakami A, Ogawa N, Matsuda A. Amplification of 4'-thioDNA in the presence of 4'-thio-dTTP and 4'-thio-dCTP, and 4'-thioDNA-directed transcription in vitro and in mammalian cells. J Am Chem Soc. 2007;129:15424-5 pubmed
  16. Matranga C, Tomari Y, Shin C, Bartel D, Zamore P. Passenger-strand cleavage facilitates assembly of siRNA into Ago2-containing RNAi enzyme complexes. Cell. 2005;123:607-20 pubmed
    ..For siRNAs, virtually all RISC is assembled through this cleavage-assisted mechanism. In contrast, passenger-strand cleavage is not important for the incorporation of miRNAs that derive from mismatched duplexes. ..
  17. Chen X, Wang L, Zhou Y, Cai Q, Prakriya M, Duan K, et al. Activation of GPCRs modulates quantal size in chromaffin cells through G(betagamma) and PKC. Nat Neurosci. 2005;8:1160-8 pubmed
    ..Thus, a variety of G protein pathways exist to modulate Ca2+-evoked secretion at specific steps in fusion pore formation. ..
  18. Jackson J, Gleave M, Gleave J, Burt H. The inhibition of angiogenesis by antisense oligonucleotides to clusterin. Angiogenesis. 2005;8:229-38 pubmed
    ..These data demonstrate a strong antiangiogenic action of clusterin aso's, that is not necessarily related to any chemosensitization effect of this agent. ..
  19. Gilissen L, Derijks L, Verhoeven H, Bierau J, Hooymans P, Hommes D, et al. Pancytopenia due to high 6-methylmercaptopurine levels in a 6-mercaptopurine treated patient with Crohn's disease. Dig Liver Dis. 2007;39:182-6 pubmed
    ..Apparently, 6-methylmercaptopurine ribonucleotides metabolites can cause pancytopenia, as was already known for 6-thioguanine nucleotides. ..
  20. Schlingensiepen K, Schlingensiepen R, Steinbrecher A, Hau P, Bogdahn U, Fischer Blass B, et al. Targeted tumor therapy with the TGF-beta 2 antisense compound AP 12009. Cytokine Growth Factor Rev. 2006;17:129-39 pubmed
    ..A phase I/II study in pancreatic carcinoma and malignant melanoma is currently ongoing. Our results implicate targeted TGF-beta2 suppression as a promising therapeutic approach for malignant tumor therapy. ..
  21. Osterman M, Kundu R, Lichtenstein G, Lewis J. Association of 6-thioguanine nucleotide levels and inflammatory bowel disease activity: a meta-analysis. Gastroenterology. 2006;130:1047-53 pubmed
    ..Again, excluding the 1 outlier study eliminated this heterogeneity. Although prior studies yielded inconsistent conclusions, this analysis strongly supports that higher 6-TGN levels are associated with clinical remission. ..
  22. Fangbin Z, Xiang G, Liang D, Hui L, Xueding W, Baili C, et al. Prospective Evaluation of Pharmacogenomics and Metabolite Measurements upon Azathioprine Therapy in Inflammatory Bowel Disease: An Observational Study. Medicine (Baltimore). 2016;95:e3326 pubmed publisher
    ..The value of TPMT genotyping before thiopurine therapy is limited in Chinese patients with IBD, considering the low sensitivity of predicting leucopenia. ..
  23. Narukawa M, Kitagawa Iseki K, Oike H, Abe K, Mori T, Hayashi Y. Characterization of umami receptor and coupling G protein in mouse taste cells. Neuroreport. 2008;19:1169-73 pubmed publisher
    ..Thus, we demonstrated that umami stimuli were received by G protein-coupled receptors that function together with some of the Galphai family members. ..
  24. Absillis G, Cartuyvels E, Van Deun R, Parac Vogt T. Hydrolytic cleavage of an RNA-model phosphodiester catalyzed by a highly negatively charged polyoxomolybdate [Mo7O24]6- cluster. J Am Chem Soc. 2008;130:17400-8 pubmed publisher
    ..31)P NMR and Mo K-edge EXAFS spectra measured during different stages of the hydrolysis indicated that under catalytic conditions a partial conversion of [Mo(7)O(24)](6-) into [P(2)Mo(5)O(23)](6-) occurs. ..
  25. Davids M, Letai A. Targeting the B-cell lymphoma/leukemia 2 family in cancer. J Clin Oncol. 2012;30:3127-35 pubmed publisher
    ..Further exploitation of our understanding of the BCL-2 family promises to offer improved predictive biomarkers for oncologists and improved therapies for patients with cancer...
  26. Chang C, Chang G, Chen H. A novel cyclic AMP/Epac1/CaMKI signaling cascade promotes GCM1 desumoylation and placental cell fusion. Mol Cell Biol. 2011;31:3820-31 pubmed publisher
    ..Our study has identified a novel cAMP/Epac1/CaMKI/GCM1 signaling cascade that stimulates trophoblast fusion through promoting GCM1 phosphorylation and desumoylation. ..
  27. Stratton R, Squires P, Green A. ANP stimulates hepatocyte Ca2+ efflux via plasma membrane recruitment of PKGIalpha. Biochem Biophys Res Commun. 2008;368:965-70 pubmed publisher
    ..We propose that ANP, through localized cGMP elevation, promotes plasma membrane recruitment of PKGIalpha, which, in turn, stimulates Ca(2+) efflux. ..
  28. Jiang L, Lan T, Chen Y, Sang J, Li Y, Wu M, et al. PKG II inhibits EGF/EGFR-induced migration of gastric cancer cells. PLoS ONE. 2013;8:e61674 pubmed publisher
  29. Penzo M, Pena J. Endocannabinoid-mediated long-term depression in the avian midbrain expressed presynaptically and postsynaptically. J Neurosci. 2009;29:4131-9 pubmed publisher
    ..Both the presynaptic and the postsynaptic effects depend on CB1R activation. The reduction of postsynaptic NMDAR currents represents a novel role of endocannabinoids in synaptic modulation. ..
  30. Mueller D, Porter J, Quirk G. Noradrenergic signaling in infralimbic cortex increases cell excitability and strengthens memory for fear extinction. J Neurosci. 2008;28:369-75 pubmed publisher
    ..Thus, emotional arousal evoked by conditioned fear paradoxically promotes the subsequent extinction of that fear, thereby ensuring behavioral flexibility. ..
  31. Li P, Sun H, Han Y, Wang J, Zhang F, Tang C, et al. Intermedin enhances sympathetic outflow via receptor-mediated cAMP/PKA signaling pathway in nucleus tractus solitarii of rats. Peptides. 2013;47:1-6 pubmed publisher
    ..These results suggest that IMD participates in the sympathetic nerve activity and central regulation of the cardiovascular system and a receptor-mediated cAMP/PKA signaling pathway is involved in IMD-induced effects in the NTS. ..
  32. Eguchi K, Nakanishi S, Takagi H, Taoufiq Z, Takahashi T. Maturation of a PKG-dependent retrograde mechanism for exoendocytic coupling of synaptic vesicles. Neuron. 2012;74:517-29 pubmed publisher
    ..We conclude that maturation of the PKG-dependent retrograde signal cascade strengthens the homeostatic plasticity for the maintenance of high-frequency synaptic transmission at the fast glutamatergic synapse. ..
  33. Lanteri M, Lamattina L, Laxalt A. Mechanisms of xylanase-induced nitric oxide and phosphatidic acid production in tomato cells. Planta. 2011;234:845-55 pubmed publisher
    ..Data collectively indicate that upon xylanase perception, cells activate a protein kinase pathway required for NO formation and that, S-nitrosylation-dependent mechanisms are involved in downstream signaling leading to PA and ROS. ..
  34. Mukhlall J, Hersh W. Sulfurization of dinucleoside phosphite triesters with chiral disulfides. Nucleosides Nucleotides Nucleic Acids. 2011;30:706-25 pubmed publisher
    ..The highest de values for R(PS) and S(PS) phosphorothioates were 14.7% and 7.9%, respectively, both using MEDITH analogues...
  35. Santafe M, Garcia N, Lanuza M, Tomas M, Tomas J. Interaction between protein kinase C and protein kinase A can modulate transmitter release at the rat neuromuscular synapse. J Neurosci Res. 2009;87:683-90 pubmed publisher
    ..There was therefore some dependence of PKC on PKA activity in the fine control of the neuromuscular synaptic functionalism and ACh release. ..
  36. Mink S, Kasian K, Santos Martinez L, Jacobs H, Bose R, Cheng Z, et al. Lysozyme, a mediator of sepsis that produces vasodilation by hydrogen peroxide signaling in an arterial preparation. Am J Physiol Heart Circ Physiol. 2008;294:H1724-35 pubmed publisher
    ..Lzm-S may contribute to the vasodilation that occurs in septic shock. ..
  37. Liu Y, Franzen S. Factors determining the efficacy of nuclear delivery of antisense oligonucleotides by gold nanoparticles. Bioconjug Chem. 2008;19:1009-16 pubmed publisher
    ..We conclude that sequestration of cargo from the harsh conditions of the endosome is a desirable strategy for cell-targeting nanoparticles. ..
  38. Fu Y, Han J, Ishola T, Scerbo M, Adwanikar H, Ramsey C, et al. PKA and ERK, but not PKC, in the amygdala contribute to pain-related synaptic plasticity and behavior. Mol Pain. 2008;4:26 pubmed publisher
    ..The data suggest that in the amygdala PKA and ERK, but not PKC, contribute to pain-related synaptic facilitation and behavior by increasing NMDA receptor function through independent signaling pathways. ..
  39. Melaouhia S, Fekih M, Ferchichi H, Bouissorra H, Ben Mustapha N, Boubaker J, et al. [Is there any interest to dose the azathioprine's metabolites during inflammatory bowel diseases?]. Therapie. 2013;68:313-20 pubmed publisher
    ..Our work confirms the relation between the doses of azathioprine metabolites and the myelotoxicity due to this molecule. ..
  40. Zhang Y, Quock L, Chung E, Ohgami Y, Quock R. Involvement of a NO-cyclic GMP-PKG signaling pathway in nitrous oxide-induced antinociception in mice. Eur J Pharmacol. 2011;654:249-53 pubmed publisher
    ..These results support the hypothesis that N(2)O-induced antinociception in mice is mediated by a NO-cyclic GMP-PKG pathway...
  41. Dismuke W, Mbadugha C, Ellis D. NO-induced regulation of human trabecular meshwork cell volume and aqueous humor outflow facility involve the BKCa ion channel. Am J Physiol Cell Physiol. 2008;294:C1378-86 pubmed publisher
    ..Additionally, the time course for NO-induced decreases in TM cell volume correlated with NO-induced increases in outflow facility, suggesting that the NO-induced alterations in cell volume may influence outflow facility. ..
  42. McDermott C, Schrader L. Activation of ? opioid receptors increases intrinsic excitability of dentate gyrus granule cells. J Physiol. 2011;589:3517-32 pubmed publisher
    ..2 subunit protein at the cell surface. These results are consistent with an increase in cell excitability in response to KOR activation and may reflect new possibilities for additional opioid functions. ..
  43. Zeng J, Liu X, Zhang J, Wu X, Ruan H. P2Y1 receptor-mediated glutamate release from cultured dorsal spinal cord astrocytes. J Neurochem. 2008;106:2106-18 pubmed publisher
    ..We speculate that P2Y(1) receptors-evoked glutamate efflux, occurring under pathological condition, may modulate the activity of synapses in spinal cord. ..
  44. Agarwala S, Keilholz U, Gilles E, Bedikian A, Wu J, Kay R, et al. LDH correlation with survival in advanced melanoma from two large, randomised trials (Oblimersen GM301 and EORTC 18951). Eur J Cancer. 2009;45:1807-14 pubmed publisher
    ..LDH was highly predictive of oblimersen effect. In designing studies, LDH should be considered, regardless of tumour size or disease site. ..
  45. Di S, Maxson M, Franco A, Tasker J. Glucocorticoids regulate glutamate and GABA synapse-specific retrograde transmission via divergent nongenomic signaling pathways. J Neurosci. 2009;29:393-401 pubmed publisher
    ..The simultaneous rapid stimulation of nitric oxide and endocannabinoid synthesis by glucocorticoids has important implications for the impact of stress on the brain as well as on neural-immune interactions in the hypothalamus. ..
  46. Maly J, Pedziwiatr Werbicka E, Maly M, Semerádtová A, Appelhans D, Danani A, et al. Highly organized self-assembled dendriplexes based on poly(propylene imine) glycodendrimer and anti-HIV oligodeoxynucleotides. Curr Med Chem. 2012;19:4708-19 pubmed
    ..Space symmetry of the oligonucleotides and the resulting dendriplex monomeric units are probably the most important factors which influence the way of self-assembling. ..
  47. Sternberg C, Dumez H, Van Poppel H, Skoneczna I, Sella A, Daugaard G, et al. Docetaxel plus oblimersen sodium (Bcl-2 antisense oligonucleotide): an EORTC multicenter, randomized phase II study in patients with castration-resistant prostate cancer. Ann Oncol. 2009;20:1264-9 pubmed publisher
    ..The primary end points of the study were not met: a rate of confirmed PSA response >30% and a major toxic event rate <45% were not observed with docetaxel-oblimersen. ..
  48. Chia S, Dent S, Ellard S, Ellis P, Vandenberg T, Gelmon K, et al. Phase II trial of OGX-011 in combination with docetaxel in metastatic breast cancer. Clin Cancer Res. 2009;15:708-13 pubmed publisher
  49. Geddawy A, Shimosato T, Tawa M, Imamura T, Okamura T. Mechanism underlying endothelium-dependent relaxation by 2-methylthio-ADP in monkey cerebral artery. J Pharmacol Sci. 2010;114:180-8 pubmed
    ..Furthermore, phospholipase A(2), cytochrome P450-derived epoxyeicosatrienoic acids and Ca(2+)-activated K(+) channels appear to be involved in the relaxation. ..
  50. Franco W, Leite R. Dobutamine inhibits vasopressin-mediated water transport across toad bladder epithelium. Comp Biochem Physiol C Toxicol Pharmacol. 2008;148:68-71 pubmed publisher
    ..The current study may provide a better understanding of the effects of dobutamine on renal function by contributing towards the elucidation of its action mechanism. ..
  51. Stessl M, Marchetti Deschmann M, Winkler J, Lachmann B, Allmaier G, Noe C. A proteomic study reveals unspecific apoptosis induction and reduction of glycolytic enzymes by the phosphorothioate antisense oligonucleotide oblimersen in human melanoma cells. J Proteomics. 2009;72:1019-30 pubmed publisher
    ..The observed effects may be caused by a phosphorothioate mediated blockage of the mitochondrial voltage dependent anion channel (VDAC). ..
  52. Stocco G, Londero M, Campanozzi A, Martelossi S, Marino S, Malusa N, et al. Usefulness of the measurement of azathioprine metabolites in the assessment of non-adherence. J Crohns Colitis. 2010;4:599-602 pubmed publisher
  53. Dagnas M, Guillou J, Prévôt T, Mons N. HDAC inhibition facilitates the switch between memory systems in young but not aged mice. J Neurosci. 2013;33:1954-63 pubmed publisher
  54. Li N, Frederiksen J, Koo S, Lu J, Wilson T, Lilley D, et al. A general and efficient approach for the construction of RNA oligonucleotides containing a 5'-phosphorothiolate linkage. Nucleic Acids Res. 2011;39:e31 pubmed publisher
  55. Robinson B, Behling K, Gupta M, Zhang A, Moore J, Bantly A, et al. Abundant anti-apoptotic BCL-2 is a molecular target in leukaemias with t(4;11) translocation. Br J Haematol. 2008;141:827-39 pubmed publisher
    ..The abundant BCL-2 affords a molecular target in leukaemias with t(4;11). G3139 exhibits preclinical activity and synergy with select cytotoxic agents in RS4:11 and MV4-11 cells, and these effects occur through apoptosis. ..
  56. Ferrero J, Ramírez Franco J, Martín R, Bartolomé Martín D, Torres M, Sánchez Prieto J. Cross-talk between metabotropic glutamate receptor 7 and beta adrenergic receptor signaling at cerebrocortical nerve terminals. Neuropharmacology. 2016;101:412-25 pubmed publisher
  57. Lee J, Yedavalli V, Jeang K. Activation of HIV-1 expression and replication by cGMP dependent protein kinase type 1-beta (PKG1beta). Retrovirology. 2007;4:91 pubmed
    ..These findings provide evidence that cGMP and PKG serve to regulate HIV-1 infection in human cells. ..
  58. Maeda M, Mizuno Y, Wakita M, Yamaga T, Nonaka K, Shin M, et al. Potent and direct presynaptic modulation of glycinergic transmission in rat spinal neurons by atrial natriuretic peptide. Brain Res Bull. 2013;99:19-26 pubmed publisher
    ..Moreover, both ANP and BNP had no effect on glutamatergic EPSCs in hippocampal CA3 neurons. The results indicate a potent and selective presynaptic inhibitory action of ANP on glycinergic transmission in spinal cord sensory circuits. ..
  59. Rebolledo Antúnez S, Farías J, Arenas I, Garcia D. Gating charges per channel of Ca(V)2.2 channels are modified by G protein activation in rat sympathetic neurons. Arch Biochem Biophys. 2009;486:51-7 pubmed publisher
    ..This paper shows for the first time a significant and reversible decrease in charge transfer of Ca(V)2.2 channels under G protein modulation, which might depend on the activated G protein inhibitory pathway. ..
  60. Rudin C, Salgia R, Wang X, Hodgson L, Masters G, Green M, et al. Randomized phase II Study of carboplatin and etoposide with or without the bcl-2 antisense oligonucleotide oblimersen for extensive-stage small-cell lung cancer: CALGB 30103. J Clin Oncol. 2008;26:870-6 pubmed publisher
    ..Emerging data from several groups suggest that this lack of efficacy may be due to insufficient suppression of Bcl-2 in vivo. Additional evaluation of this agent in SCLC is not warranted. ..
  61. Aoki J, Yamashiro Kanashiro E, Ramos D, Cotrim P. Efficacy of the tubercidin antileishmania action associated with an inhibitor of the nucleoside transport. Parasitol Res. 2009;104:223-8 pubmed publisher
    ..L.) amazonensis, and in vivo tests in BALB/c mice infected with L. (L.) amazonensis. We demonstrated that TUB-NBMPR combined treatment can be effective against leishmania cells protecting mammalian cells from TUB toxicity. ..
  62. Chi K, Zoubeidi A, Gleave M. Custirsen (OGX-011): a second-generation antisense inhibitor of clusterin for the treatment of cancer. Expert Opin Investig Drugs. 2008;17:1955-62 pubmed
    ..Randomized trials of custirsen in combination with chemotherapy are planned in patients with castration-resistant prostate cancer. ..
  63. Zheng C, Wang M, Liu Q, Wakui M, Whiteaker P, Lukas R, et al. U18666A, a cholesterol-inhibition agent, modulates human neuronal nicotinic acetylcholine receptors heterologously expressed in SH-EP1 cell line. J Neurochem. 2009;108:1526-38 pubmed publisher
  64. Wu Y, Li L, Mao Y, LEE L. Static micromixer-coaxial electrospray synthesis of theranostic lipoplexes. ACS Nano. 2012;6:2245-52 pubmed publisher
    ..The lipoplexes were efficiently delivered to A549 cells (non-small cell lung cancer cell line) and down-regulated the Bcl-2 gene expression by 48 ± 6%. ..
  65. Zhou H, Chen S, Chen H, Pan H. Opioid-induced long-term potentiation in the spinal cord is a presynaptic event. J Neurosci. 2010;30:4460-6 pubmed publisher
    ..This excitatory effect of opioids on primary afferents can counteract the inhibitory effect of opioids on synaptic transmission at the spinal level and is likely involved in opioid-induced hyperalgesia and tolerance. ..
  66. Stephens R, Rentsendorj O, Servinsky L, Moldobaeva A, Damico R, Pearse D. cGMP increases antioxidant function and attenuates oxidant cell death in mouse lung microvascular endothelial cells by a protein kinase G-dependent mechanism. Am J Physiol Lung Cell Mol Physiol. 2010;299:L323-33 pubmed publisher
    ..We conclude that cGMP, through PKG(I), attenuated H(2)O(2)-induced cytotoxicity in MLMVEC by increasing catalase and Gpx-1 expression through an unknown posttranscriptional effect. ..
  67. Jaschinski F, Rothhammer T, Jachimczak P, Seitz C, Schneider A, Schlingensiepen K. The antisense oligonucleotide trabedersen (AP 12009) for the targeted inhibition of TGF-?2. Curr Pharm Biotechnol. 2011;12:2203-13 pubmed
    ..Intravenous application of trabedersen for the treatment of patients with advanced pancreatic carcinoma, metastasizing melanoma, or metastatic colorectal carcinoma is assessed in a currently ongoing phase I/II dose escalation study. ..
  68. Gao Z, Jacobson K. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Mol Pharmacol. 2017;92:613-626 pubmed publisher
    ..Thus, antagonism can be surmountable or insurmountable depending on the signaling pathways measured and the agonists used, which should be of broad relevance to drug discovery and disease treatment. ..
  69. Danino O, Giladi N, Grossman S, Fischer B. Nucleoside 5'-phosphorothioate derivatives are highly effective neuroprotectants. Biochem Pharmacol. 2014;88:384-92 pubmed publisher
    ..Based on its high potency as a neuroprotectant, we propose ATP-?-S as a highly promising, biocompatible, and water-soluble drug candidate for the treatment of neurodegenerative disorders. ..
  70. Jain H, Takeda K, Tami C, Verthelyi D, Beaucage S. Assessment of the cellular internalization of thermolytic phosphorothioate DNA oligonucleotide prodrugs. Bioorg Med Chem. 2013;21:6224-32 pubmed publisher
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