antisense oligodeoxyribonucleotides


Summary: Short fragments of DNA that are used to alter the function of target RNAs or DNAs to which they hybridize.

Top Publications

  1. Guo Q, Xiao G, Li R, Guan S, Zhu X, Wu J. Treatment of Streptococcus mutans with antisense oligodeoxyribonucleotides to gtfB mRNA inhibits GtfB expression and function. FEMS Microbiol Lett. 2006;264:8-14 pubmed
    We examined the effects of phosphorothioate-modified antisense oligodeoxyribonucleotides (PS-ODN) targeted to mRNA transcribed from gtfB, which encodes synthesis of water-insoluble glucans in Streptococcus mutans. Treatment of S...
  2. Tang X, Dmochowski I. Synthesis of light-activated antisense oligodeoxynucleotide. Nat Protoc. 2006;1:3041-8 pubmed
    ..Here, we provide a detailed procedure for synthesizing photoactive asODNs in good yields. Synthesis, purification and analysis of the light-activated asODN can be completed within 1-2 weeks. ..
  3. Tang X, Swaminathan J, Gewirtz A, Dmochowski I. Regulating gene expression in human leukemia cells using light-activated oligodeoxynucleotides. Nucleic Acids Res. 2008;36:559-69 pubmed
    ..Two-fold photomodulation of c-MYB protein levels was also observed with S-C5. However, no photomodulation of c-MYB protein levels was observed with S-C6, perhaps due to the greater stability of this duplex. ..
  4. Kalota A, Karabon L, Swider C, Viazovkina E, Elzagheid M, Damha M, et al. 2'-deoxy-2'-fluoro-beta-D-arabinonucleic acid (2'F-ANA) modified oligonucleotides (ON) effect highly efficient, and persistent, gene silencing. Nucleic Acids Res. 2006;34:451-61 pubmed
    ..Therefore, our data demonstrate that PS-2'F-ANA-DNA chimeras are efficient gene silencing molecules, and suggest that they could have significant therapeutic potential. ..
  5. Zhao X, Lee R. Tumor-selective targeted delivery of genes and antisense oligodeoxyribonucleotides via the folate receptor. Adv Drug Deliv Rev. 2004;56:1193-204 pubmed
    ..In addition, FR-targeted liposomes have been evaluated for the targeted delivery of antisense oligodeoxyribonucleotides (ODNs)...
  6. Pineda R, Heiser R, Ribera A. Developmental, molecular, and genetic dissection of INa in vivo in embryonic zebrafish sensory neurons. J Neurophysiol. 2005;93:3582-93 pubmed
    ..Finally, analysis of macho mutants indicated that developmental upregulation of INa was absent in RB cells. These results indicate that MOs are a useful tool for the molecular dissection and analysis of ion channel function in vivo. ..
  7. Opalinska J, Kalota A, Gifford L, Lu P, Jen K, Pradeepkumar P, et al. Oxetane modified, conformationally constrained, antisense oligodeoxyribonucleotides function efficiently as gene silencing molecules. Nucleic Acids Res. 2004;32:5791-9 pubmed
    ..We conclude that rationally targeted, OXE modified ODNs, can function efficiently as gene silencing agents, and hypothesize that they will prove useful for therapeutic purposes. ..
  8. Opalinska J, Machalinski B, Ratajczak J, Ratajczak M, Gewirtz A. Multigene targeting with antisense oligodeoxynucleotides: an exploratory study using primary human leukemia cells. Clin Cancer Res. 2005;11:4948-54 pubmed
    ..We hypothesize that exposing primary leukemic cells to antisense oligodeoxynucleotides targeted to two, or possibly more, genes might significantly augment the therapeutic utility of these molecules. ..
  9. Gifford L, Opalinska J, Jordan D, Pattanayak V, Greenham P, Kalota A, et al. Identification of antisense nucleic acid hybridization sites in mRNA molecules with self-quenching fluorescent reporter molecules. Nucleic Acids Res. 2005;33:e28 pubmed
    ..The general utility of this method is demonstrated by SQRM identification of targetable sequence within c-myb and bcl-6 mRNA. Corresponding antisense oligonucleotides reduce these gene products in cells. ..

More Information


  1. Yacyshyn B, Chey W, Wedel M, Yu R, Paul D, Chuang E. A randomized, double-masked, placebo-controlled study of alicaforsen, an antisense inhibitor of intercellular adhesion molecule 1, for the treatment of subjects with active Crohn's disease. Clin Gastroenterol Hepatol. 2007;5:215-20 pubmed
    ..In the subject population studied, alicaforsen failed to demonstrate efficacy in any of its primary outcome measures. Alicaforsen was well-tolerated. ..
  2. Redell J, Xue Bian J, Bubb M, Crow T. One-trial in vitro conditioning regulates an association between the beta-thymosin repeat protein Csp24 and actin. Neuroscience. 2007;148:413-20 pubmed
    ..These data suggest Csp24 may influence intrinsic excitability by regulating cytoskeletal dynamics. ..
  3. Kratz E, Eimon P, Mukhyala K, Stern H, Zha J, Strasser A, et al. Functional characterization of the Bcl-2 gene family in the zebrafish. Cell Death Differ. 2006;13:1631-40 pubmed
    ..These data indicate substantial functional similarity between zebrafish and mammalian Bcl-2 family members, and establish the zebrafish as a relevant model for studying the intrinsic apoptosis pathway. ..
  4. Petursdottir A, Farr S, Morley J, Banks W, Skuladottir G. Lipid peroxidation in brain during aging in the senescence-accelerated mouse (SAM). Neurobiol Aging. 2007;28:1170-8 pubmed
    ..The oldest age group contained the highest concentration of alpha-tocopherol, indicating a protection against oxidative damage of PUFA in brain membrane phospholipids. ..
  5. Ding L, Chen X, Jing K, Wang H, Zhang W. Inhibition of the VEGF expression and cell growth in hepatocellular carcinoma by blocking HIF-1alpha and Smad3 binding site in VEGF promoter. J Huazhong Univ Sci Technolog Med Sci. 2006;26:75-8 pubmed
  6. Chu S, Ma Y, Feng D, Zhang H, Qiu J, Zhu Z. c-Met antisense oligodeoxynucleotides increase sensitivity of human glioma cells to paclitaxel. Oncol Rep. 2010;24:189-94 pubmed
    ..01). Thus, c-Met antisense oligodeoxynucleotides increase the sensitivity of human glioma cells to paclitaxel. Combined use of the two agents could be a novel and attractive strategy in human glioma treatment. ..
  7. Omae T, Yoshioka H, Tanaka T, Nagai H, Saji M, Noda K, et al. Antisense in vivo knockdown of synaptotagmin I by HVJ-liposome mediated gene transfer attenuates ischemic brain damage in neonatal rats. Brain Dev. 2008;30:313-20 pubmed publisher
    ..It was also suggested that this treatment was more effective in the neocortex than in the striatum in neonatal rats. ..
  8. Fossat P, Dobremez E, Bouali Benazzouz R, Favereaux A, Bertrand S, Kilk K, et al. Knockdown of L calcium channel subtypes: differential effects in neuropathic pain. J Neurosci. 2010;30:1073-85 pubmed publisher
    ..2 activation. We propose that L-type calcium channels in the spinal dorsal horn play an important role in pain processing, and that the maintenance of chronic neuropathic pain depends specifically on channels comprising Ca(V)1.2. ..
  9. Han Z, Xu G, Zhou J, Xing H, Wang S, Wu M, et al. Inhibition of motile and invasive properties of ovarian cancer cells by ASODN against Rho-associated protein kinase. Cell Commun Adhes. 2005;12:59-69 pubmed
    ..Our data suggested that p160ROCK was involved in ovarian cancer cell invasion and metastasis by facilitating cancer cell migration, and that p160ROCK might be a potential new effective target for preventing metastasis of ovarian cancer. ..
  10. Tseng D, Chou M, Tseng Y, Hsiao C, Huang C, Kaneko T, et al. Effects of stanniocalcin 1 on calcium uptake in zebrafish (Danio rerio) embryo. Am J Physiol Regul Integr Comp Physiol. 2009;296:R549-57 pubmed publisher
    ..These data suggest that zSTC-1 negatively regulates ECaC gene expression to reduce Ca(2+) uptake in zebrafish embryos. ..
  11. Chen J, Li C, Pei D, Han D, Liu X, Jiang H, et al. GluR6-containing KA receptor mediates the activation of p38 MAP kinase in rat hippocampal CA1 region during brain ischemia injury. Hippocampus. 2009;19:79-89 pubmed publisher
  12. van Deventer S, Wedel M, Baker B, Xia S, Chuang E, Miner P. A phase II dose ranging, double-blind, placebo-controlled study of alicaforsen enema in subjects with acute exacerbation of mild to moderate left-sided ulcerative colitis. Aliment Pharmacol Ther. 2006;23:1415-25 pubmed
    ..18%, P=0.04) to week 30 (50% vs. 11%, P=0.03). Alicaforsen enema was safe and well tolerated at all doses studied. The durability of the response to alicaforsen enema treatment may suggests a disease-modifying effect. ..
  13. Bravo J, Parra C, Arancibia S, Andrés S, Morales P, Herrera Marschitz M, et al. Adrenalectomy promotes a permanent decrease of plasma corticoid levels and a transient increase of apoptosis and the expression of Transforming Growth Factor beta1 (TGF-beta1) in hippocampus: effect of a TGF-beta1 oligo-antisense. BMC Neurosci. 2006;7:40 pubmed
    ..Sustained intracerebral administration of TGF-beta1 ASO increased the apoptosis promoted by ADX, suggesting that TGF-beta1 plays an anti-apoptotic role in vivo in hippocampus. ..
  14. Zhao F, Zhang S, Ma L, Gao H, Zhong Z. Efficacy of c-erbB-2 antisense oligonucleotide transfection on uterine endometrial cancer HEC-1A cell lines. Eur J Gynaecol Oncol. 2007;28:263-9 pubmed
    ..Transfecting c-erbB-2 ASODNs can obviously suppress the mRNA and protein expression in HEC-1A cells, cause cellular apoptosis and inhibit cell growth. It may be a more useful gene therapy for endometrial cancer. ..
  15. He L, Guan K, Yan Z, Ye H, Xu K, Ren L, et al. Enhanced sensitivity to mitomycin C by abating heat shock protein 70 expression in human bladder cancer cell line of BIU-87. Chin Med J (Engl). 2005;118:1965-72 pubmed
    ..05). The abating level of HSP70 expression can strengthen the sensitivity of BIU-87 to MMC. One of this effect might be related to the induction of apoptosis by abating HSP70 expression. ..
  16. Beeram M, Patnaik A, Rowinsky E. Regulation of c-Raf-1: therapeutic implications. Clin Adv Hematol Oncol. 2003;1:476-81 pubmed
    ..that regulate pleiotropic cellular processes using such strategies as isoprenylation inhibitors, antisense oligodeoxyribonucleotides, and inhibitors of the kinase function represent attractive therapeutic options...
  17. Carbonell A, de la Peña M, Flores R, Gago S. Effects of the trinucleotide preceding the self-cleavage site on eggplant latent viroid hammerheads: differences in co- and post-transcriptional self-cleavage may explain the lack of trinucleotide AUC in most natural hammerheads. Nucleic Acids Res. 2006;34:5613-22 pubmed
    ..Comparisons with other natural hammerheads showed that the ELVd-(+)-GUC and ELVd-(+)-AUC hammerheads are the catalytically most active in a post-transcriptional context with low magnesium...
  18. Hsieh Y, Yang S, Chiou H, Kuo D. Activations of c-fos/c-jun signaling are involved in the modulation of hypothalamic superoxide dismutase (SOD) and neuropeptide Y (NPY) gene expression in amphetamine-mediated appetite suppression. Toxicol Appl Pharmacol. 2006;212:99-109 pubmed
    ..It was suggested that c-fos/c-jun signaling might involve in the central regulation of AMPH-mediated feeding suppression via the modulation of NPY gene expression. ..
  19. Lekishvili T, Hesketh S, Brazier M, Brown D. Mouse galectin-1 inhibits the toxicity of glutamate by modifying NR1 NMDA receptor expression. Eur J Neurosci. 2006;24:3017-25 pubmed
    ..These results suggest that the astrocytic lectin galectin-1 could protect neurons against the effects of excitotoxicity as seen in stroke and ischemic injury. ..
  20. Mishra R, Carnevale K, Cathcart M. iPLA2beta: front and center in human monocyte chemotaxis to MCP-1. J Exp Med. 2008;205:347-59 pubmed publisher
  21. Hegde G, Peterson K, Emanuel K, Mittal A, Joshi A, Dickinson J, et al. Hedgehog-induced survival of B-cell chronic lymphocytic leukemia cells in a stromal cell microenvironment: a potential new therapeutic target. Mol Cancer Res. 2008;6:1928-36 pubmed publisher
    ..Together, these results reveal that Hh signaling is important in the pathogenesis of B-CLL and, hence, may be a potential therapeutic target. ..
  22. Nowak M, Wyszko E, Fedoruk Wyszomirska A, Pospieszny H, Barciszewska M, Barciszewski J. A new and efficient method for inhibition of RNA viruses by DNA interference. FEBS J. 2009;276:4372-80 pubmed publisher
    ..We showed that Dicer processed dsDNA, which suggests activation of the cellular machinery involved in silencing of RNA. For the silencing of viral RNA effected with dsDNA, we coined the term DNA interference technology. ..
  23. Montero Balaguer M, Lang M, Sachdev S, Knappmeyer C, Stewart R, De La Guardia A, et al. The mother superior mutation ablates foxd3 activity in neural crest progenitor cells and depletes neural crest derivatives in zebrafish. Dev Dyn. 2006;235:3199-212 pubmed
    ..Further analysis of mosm188 mutants and foxd3 morphants revealed that NC cells are initially formed, suggesting that foxd3 function is required to maintain the pool of NC progenitors. ..
  24. Laczkó I, Váró G, Bottka S, Balint Z, Illyes E, Vass E, et al. N-terminal acylation of the SV40 nuclear localization signal peptide enhances its oligonucleotide binding and membrane translocation efficiencies. Arch Biochem Biophys. 2006;454:146-54 pubmed
    ..Cell translocation experiments revealed a highly efficient cell transport of the ODN by palmitoylated SV40 peptide at rM>10. ..
  25. Choi K, Whisler K, Graham D, Self D. Antisense-induced reduction in nucleus accumbens cyclic AMP response element binding protein attenuates cocaine reinforcement. Neuroscience. 2006;137:373-83 pubmed
  26. Zhang W, Liu L, Xu T. Reduced potassium-chloride co-transporter expression in spinal cord dorsal horn neurons contributes to inflammatory pain hypersensitivity in rats. Neuroscience. 2008;152:502-10 pubmed publisher
    ..The data also support the notion that disinhibition in the spinal cord is a general feature of inflammatory and neuropathic pain conditions, and suggest new therapeutic intervention. ..
  27. Miner P, Wedel M, Xia S, Baker B. Safety and efficacy of two dose formulations of alicaforsen enema compared with mesalazine enema for treatment of mild to moderate left-sided ulcerative colitis: a randomized, double-blind, active-controlled trial. Aliment Pharmacol Ther. 2006;23:1403-13 pubmed
    ..The extended length of remission suggests that alicaforsen enema treatment may have a disease modifying effect. ..
  28. Kanangat S, Postlethwaite A, Higgins G, Hasty K. Novel functions of intracellular IL-1ra in human dermal fibroblasts: implications in the pathogenesis of fibrosis. J Invest Dermatol. 2006;126:756-65 pubmed
    ..Our data indicate novel functions for icIL-1ra, which might be relevant to the genesis of fibrotic diseases such as SSc. ..
  29. Jung S, Park Y, Park Y, Cha S, Lee M, Suh C. Na+-Ca2+ exchanger modulates Ca2+ content in intracellular Ca2+ stores in rat osteoblasts. Exp Mol Med. 2007;39:458-68 pubmed
    ..These results strongly suggest that NCX has a regulatory role in cellular Ca2+ pathways in osteoblasts by modulating intracellular Ca2+ content. ..
  30. Semenova M, Zakharova E, Zaletov S, Zaeva V, Kosheleva N. [The effect of antisense oligonucleoties specific to the harakiri mRNA on spontaneous and induced defects of mouse preimplantation embryo development]. Genetika. 2008;44:1290-3 pubmed
  31. Xuan D, Li X, Deng Z, Zhang H, Feng P, Duan X, et al. Identification and characterization of a novel gene, Mcpr1, and its possible function in the proliferation of embryonic palatal mesenchymal cells. J Biol Chem. 2006;281:33997-4008 pubmed
  32. Wang Y, Qiao H, Peng T, Li Y, Zhang M, Liang H, et al. [Suppression of osteosarcoma in vitro by coexpression of antisense VEGF165 cDNA and thymidine kinase gene]. Zhonghua Bing Li Xue Za Zhi. 2007;36:190-5 pubmed
    ..The double-gene co-expression system in study provides experimental basis for therapy against osteosarcoma by a synchronous antiangiogenic and suicide gene approach. ..
  33. Schuldt A. MicroRNAs diversify in Drosophila development. Nat Cell Biol. 2005;7:781 pubmed
  34. Yang X, Koh C, Liu S, Pan X, Santhanam R, Yu B, et al. Transferrin receptor-targeted lipid nanoparticles for delivery of an antisense oligodeoxyribonucleotide against Bcl-2. Mol Pharm. 2009;6:221-30 pubmed publisher
    ..Tf-LN-mediated delivery combined with TfR up-regulation by deferoxamine appears to be a potentially promising strategy for enhancing the delivery efficiency and therapeutic efficacy of antisense oligonucleotides. ..
  35. Canter R, Kesmodel S, Heitjan D, Veeramachaneni N, Mokadam N, Drebin J, et al. Suppression of beta-catenin by antisense oligomers augments tumor response to isolated limb perfusion in a rodent model of adenomatous polyposis coli-mutant colon cancer. Ann Surg Oncol. 2005;12:733-42 pubmed
    ..Western blotting revealed prolonged suppression of beta-catenin expression after beta-catenin-specific ILP. Short-term beta-catenin antisense treatment improves tumor response rates after ILP in a rodent model of human CRC. ..
  36. Abaza M, Al Saffar A, Al Sawan S, Al Attiyah R. c-myc antisense oligonucleotides sensitize human colorectal cancer cells to chemotherapeutic drugs. Tumour Biol. 2008;29:287-303 pubmed publisher
    ..This two-hit approach may be important in the quest to overcome drug resistance in cancer patients whose tumors carry an overexpressed c-myc gene. ..
  37. Sharma R, Ravikumar T, Raimo D, Yang W. Induction of p21WAF1 expression protects HT29 colon cancer cells from apoptosis induced by cryoinjury. Ann Surg Oncol. 2005;12:743-52 pubmed
    ..Combining antisense ODN targeted against p21WAF1 and cryotherapy may improve clinical outcomes in the treatment of colorectal cancer. ..
  38. Lupfer C, Stein D, Mourich D, Tepper S, Iversen P, Pastey M. Inhibition of influenza A H3N8 virus infections in mice by morpholino oligomers. Arch Virol. 2008;153:929-37 pubmed publisher
    ..These data indicate that PPMOs targeting highly conserved regions of FLUAV are promising novel therapeutic candidates. ..
  39. Reisoli E, De Lucchini S, Nardi I, Ori M. Serotonin 2B receptor signaling is required for craniofacial morphogenesis and jaw joint formation in Xenopus. Development. 2010;137:2927-37 pubmed publisher
  40. D Aquila P, Panin F, Castelli M, Serra G. Dopamine D3 receptor antisense oligodeoxynucleotide potentiates imipramine-induced dopaminergic behavioural supersensitivity. Behav Pharmacol. 2006;17:101-6 pubmed
  41. Locato V, Balestrazzi A, De Gara L, Carbonera D. Reduced expression of top1beta gene induces programmed cell death and alters ascorbate metabolism in Daucus carota cultured cells. J Exp Bot. 2006;57:1667-76 pubmed
    ..The relevance of these findings in relation to the signalling pathways leading to PCD is discussed. ..
  42. Turco M, Lamberti A, Bisogni R, Romano M, Petrella A, Ammirante M, et al. Modulation of cell apoptosis by AIR. Leukemia. 2007;21:2557-9 pubmed
  43. Hong X, Jiang F, Kalkanis S, Zhang Z, Zhang X, Zheng X, et al. Decrease of endogenous vascular endothelial growth factor may not affect glioma cell proliferation and invasion. J Exp Ther Oncol. 2007;6:219-29 pubmed
    ..Our data indicate that the decrease of endogenous VEGF expression may not affect glioma cell proliferation and invasion. ..
  44. Johnson Anuna L, Eckert G, Franke C, Igbavboa U, Muller W, Wood W. Simvastatin protects neurons from cytotoxicity by up-regulating Bcl-2 mRNA and protein. J Neurochem. 2007;101:77-86 pubmed
    ..These findings suggest that neuroprotection by simvastatin is dependent on the drug's previously unexplored and important effect of up-regulating Bcl-2. ..
  45. Nakamura K, Wang Y, Liu X, Kubo A, Hnatowich D. Cationic transfectors increase accumulation in cultured tumor cells of radiolabeled antisense DNAs without entrapment. Cancer Biother Radiopharm. 2007;22:629-35 pubmed
    ..In conclusion, by using radiolabeled DNAs, definitive evidence was obtained showing that the addition of Neophectin and jet PEI increased cellular accumulations of both AS and S DNA without evidence of vesicle entrapment. ..
  46. Poletini M, McKee D, Kennett J, Doster J, Freeman M. Knockdown of clock genes in the suprachiasmatic nucleus blocks prolactin surges and alters FRA expression in the locus coeruleus of female rats. Am J Physiol Endocrinol Metab. 2007;293:E1325-34 pubmed
    ..SCN neurons therefore determine PRL secretory surges, possibly by modulating LC circadian neuronal activity. ..
  47. Jha P, Sohn J, Xu Q, Wang Y, Kaplan H, Bora P, et al. Suppression of complement regulatory proteins (CRPs) exacerbates experimental autoimmune anterior uveitis (EAAU). J Immunol. 2006;176:7221-31 pubmed
  48. Zhang L, Wen H, Zhang L, Chen K, Zhang Y. [Inhibitory effects of transfected Bcl-XL antisense oligodeoxynucleotide on proliferation of esophageal cancer cells and growth of human esophageal carcinoma in nude mice]. Zhonghua Bing Li Xue Za Zhi. 2005;34:402-6 pubmed
    ..The suppression of Bcl-XL expression by ASODN may offer both a therapeutic approach and an important theoretic foundation for gene therapy against esophageal carcinoma. ..
  49. Yamashiro S, Abe H, Mabuchi I. IQGAP2 is required for the cadherin-mediated cell-to-cell adhesion in Xenopus laevis embryos. Dev Biol. 2007;308:485-93 pubmed
    ..These results strongly suggest that XIQGAP2 is crucial for cell adhesion during early development in Xenopus. ..
  50. Zhang L, Xiao C, Wang J, Zhang L, Zeng Y. Activation of extracellular signal-regulated protein kinases 5 in the spinal cord contributes to the neuropathic pain behaviors induced by CCI in rats. Neurol Res. 2009;31:1037-43 pubmed publisher
    ..The activation of ERK5 pathways contributes to neuropathic pain in CCI rats, and the function of pERK5 may partly be accomplished via the CREB protein-dependent gene expression. ..
  51. Yamanaka Y, Tagawa H, Takahashi N, Watanabe A, Guo Y, Iwamoto K, et al. Aberrant overexpression of microRNAs activate AKT signaling via down-regulation of tumor suppressors in natural killer-cell lymphoma/leukemia. Blood. 2009;114:3265-75 pubmed publisher
    ..Collectively, these results provide important new insight into the pathogenesis of NK-cell lymphoma/leukemia and suggest targeting miR-21 and/or miR-155 may represent a useful approach to treating NK-cell lymphoma/leukemia. ..
  52. Shin Y, Kang S, Jeong S, Shim Y, Kim Y, Kim B, et al. Clusterin enhances proliferation of primary astrocytes through extracellular signal-regulated kinase activation. Neuroreport. 2006;17:1871-5 pubmed
    ..These results suggest that clusterin might play an important role in astrogliosis by stimulating the proliferation of astrocytes through activation of the extracellular signal-regulated kinase 1/2 signaling pathway. ..
  53. Curzon P, Anderson D, Nikkel A, Fox G, Gopalakrishnan M, Decker M, et al. Antisense knockdown of the rat alpha7 nicotinic acetylcholine receptor produces spatial memory impairment. Neurosci Lett. 2006;410:15-9 pubmed