octamer transcription factor 1


Summary: A ubiquitously expressed octamer transcription factor that regulates GENETIC TRANSCRIPTION of SMALL NUCLEAR RNA; IMMUNOGLOBULIN GENES; and HISTONE H2B genes.

Top Publications

  1. Wang P, Wang Q, Sun J, Wu J, Li H, Zhang N, et al. POU homeodomain protein Oct-1 functions as a sensor for cyclic AMP. J Biol Chem. 2009;284:26456-65 pubmed publisher
    ..Our study therefore identifies a novel mechanism by which cAMP regulates hormone-gene expression and suggests that ubiquitously expressed Oct-1 may play a role in metabolic homeostasis by functioning as a sensor for cAMP...
  2. Shu Y, Brown C, Castro R, Shi R, Lin E, Owen R, et al. Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics. Clin Pharmacol Ther. 2008;83:273-80 pubmed
    ..Our studies suggest that OCT1 genotype is a determinant of metformin pharmacokinetics. ..
  3. Shakya A, Cooksey R, Cox J, Wang V, McClain D, Tantin D. Oct1 loss of function induces a coordinate metabolic shift that opposes tumorigenicity. Nat Cell Biol. 2009;11:320-7 pubmed publisher
    ..We show that these metabolic changes directly oppose tumorigenicity. Collectively, our findings show that Oct1, the genes it regulates and the pathways these genes affect could be used as targets for new modes of cancer therapy. ..
  4. Sirek A, Liu L, Naples M, Adeli K, Ng D, Jin T. Insulin stimulates the expression of carbohydrate response element binding protein (ChREBP) by attenuating the repressive effect of Pit-1, Oct-1/Oct-2, and Unc-86 homeodomain protein octamer transcription factor-1. Endocrinology. 2009;150:3483-92 pubmed publisher
    ..Our observations therefore identify Oct-1 as a transcriptional repressor of ChREBP and suggest that insulin stimulates ChREBP expression via attenuating the repressive effect of Oct-1. ..
  5. Faure C, Patey N, Gauthier C, Brooks E, Mawe G. Serotonin signaling is altered in irritable bowel syndrome with diarrhea but not in functional dyspepsia in pediatric age patients. Gastroenterology. 2010;139:249-58 pubmed publisher
    ..01) and 5-HT content (P < .01) and a high SERT mRNA expression (P < .01). These results confirm the role of 5-HT signaling in IBS in children and argue against such a role in FD. ..
  6. Kaku H, Rothstein T. Octamer binding protein 2 (Oct2) regulates PD-L2 gene expression in B-1 cells through lineage-specific activity of a unique, intronic promoter. Genes Immun. 2010;11:55-66 pubmed publisher
    ..Thus, PD-L2 expression is regulated by two different promoters that function in a lineage-specific manner, with the B-1-specific promoter being constitutively active as a result of Oct1 and Oct2 binding. ..
  7. Tzvetkov M, Vormfelde S, Balen D, Meineke I, Schmidt T, Sehrt D, et al. The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin. Clin Pharmacol Ther. 2009;86:299-306 pubmed publisher
    ..Renal OCT1 expression may be important not only in relation to metformin but with respect to other drugs as well. ..
  8. Park K, Guo Z, Shao L, Du Q, Geller D. A far-upstream Oct-1 motif regulates cytokine-induced transcription of the human inducible nitric oxide synthase gene. J Mol Biol. 2009;390:595-603 pubmed publisher
    ..2 kb in the hiNOS promoter that regulates cytokine-induced hiNOS gene transcription and further underscores tight control mechanisms regulating the expression of the hiNOS gene. ..
  9. Nakakariya M, Shima Y, Shirasaka Y, Mitsuoka K, Nakanishi T, Tamai I. Organic anion transporter OAT1 is involved in renal handling of citrulline. Am J Physiol Renal Physiol. 2009;297:F71-9 pubmed publisher
    ..Accordingly, citrulline may be useful for diagnosis of kidney function as is creatinine. ..

More Information


  1. Galetti M, Alfieri R, Cavazzoni A, La Monica S, Bonelli M, Fumarola C, et al. Functional characterization of gefitinib uptake in non-small cell lung cancer cell lines. Biochem Pharmacol. 2010;80:179-87 pubmed publisher
    ..Moreover, our results suggest that the extrusion of lactate by crowded cells may contribute in decreasing the pH, which in turn can influence the uptake of gefinitib and as a result the inhibition of EGFR autophosphorylation. ..
  2. Xu X, Hong X, Wang G. Induction of endogenous gamma-globin gene expression with decoy oligonucleotide targeting Oct-1 transcription factor consensus sequence. J Hematol Oncol. 2009;2:15 pubmed publisher
    ..It also provides an innovative strategy for the treatment of many disease conditions, including sickle cell anemia and beta-thalassemia. ..
  3. Vuzman D, Polonsky M, Levy Y. Facilitated DNA search by multidomain transcription factors: cross talk via a flexible linker. Biophys J. 2010;99:1202-11 pubmed publisher
    ..The results we obtained by examining various multidomain DNA-binding proteins support the necessity of discrepancies between the DNA-binding affinities of the constituent domains. ..
  4. Kang K, Im Y, Go W, Han H. C-myc amplification altered the gene expression of ABC- and SLC-transporters in human breast epithelial cells. Mol Pharm. 2009;6:627-33 pubmed publisher
    ..05) altered by c-Myc overexpression. In conclusion, c-Myc amplification appeared to be coupled with the modulation of gene expression of certain drug transporters in human breast epithelial cells. ..
  5. Franke R, Kosloske A, Lancaster C, Filipski K, Hu C, Zolk O, et al. Influence of Oct1/Oct2-deficiency on cisplatin-induced changes in urinary N-acetyl-beta-D-glucosaminidase. Clin Cancer Res. 2010;16:4198-206 pubmed publisher
    ..1; 95% confidence interval, 2.1-31; P = 0.0078). Cimetidine is able to inhibit OCT2-mediated uptake of cisplatin in the kidney, and subsequently ameliorate nephrotoxicity likely with minimal effect on uptake in tumor cells. ..
  6. Lin C, Tai Y, Huang M, Tsai Y, Hsu H, Tzen K, et al. Cellular localization of the organic cation transporters, OCT1 and OCT2, in brain microvessel endothelial cells and its implication for MPTP transport across the blood-brain barrier and MPTP-induced dopaminergic toxicity in rodents. J Neurochem. 2010;114:717-27 pubmed publisher
    ..In conclusion, OCT1 and OCT2 are important for MPTP transfer across the blood-brain barrier and amantadine reduces the blood-brain barrier transfer of MPTP and MPTP-induced dopaminergic toxicity in rodents. ..
  7. Kang J, Shakya A, Tantin D. Stem cells, stress, metabolism and cancer: a drama in two Octs. Trends Biochem Sci. 2009;34:491-9 pubmed publisher
    ..The molecular underpinnings of these phenomena are emerging, as are the consequences for adult stem cells and cancer, and thereby hangs a tale. ..
  8. Hernández A, Villegas A, Anguita E. Human promoter mutations unveil Oct-1 and GATA-1 opposite action on Gfi1b regulation. Ann Hematol. 2010;89:759-65 pubmed publisher
    ..This is also the first report of Gfi1b mutations with a functional implication; further investigation and follow-up will clarify the involvement of these mutations in hematological disease. ..
  9. Wang P, Jin T. Hydrogen peroxide stimulates nuclear import of the POU homeodomain protein Oct-1 and its repressive effect on the expression of Cdx-2. BMC Cell Biol. 2010;11:56 pubmed publisher
    ..These observations suggest that Oct-1 functions as a sensor for both metabolic and stress/survival signaling pathways via altering its nuclear-cytoplasmic shuttling. ..
  10. Astrand C, Belikov S, Wrange O. Histone acetylation characterizes chromatin presetting by NF1 and Oct1 and enhances glucocorticoid receptor binding to the MMTV promoter. Exp Cell Res. 2009;315:2604-15 pubmed publisher
    ..Previously, we showed that Nuclear Factor 1 (NF1) and Octamer Transcription Factor 1 (Oct1) bind constitutively to the MMTV promoter and thereby induce translational nucleosome ..
  11. Harte M, O Brien G, Ryan N, Gorski J, Savage K, Crawford N, et al. BRD7, a subunit of SWI/SNF complexes, binds directly to BRCA1 and regulates BRCA1-dependent transcription. Cancer Res. 2010;70:2538-47 pubmed publisher
    ..These results support a model whereby the regulation of ERalpha transcription by BRD7 is mediated by its recruitment of BRCA1 and Oct-1 to the ESR1 promoter. ..
  12. Dong B, Huang C, Li D, Zhao F. Oct-1 functions as a transactivator in the hormonal induction of beta-casein gene expression. Mol Cell Biochem. 2009;328:93-9 pubmed publisher
  13. Zhou K, Donnelly L, Kimber C, Donnan P, Doney A, Leese G, et al. Reduced-function SLC22A1 polymorphisms encoding organic cation transporter 1 and glycemic response to metformin: a GoDARTS study. Diabetes. 2009;58:1434-9 pubmed publisher
    ..44 and P = 0.75), or the hazard of monotherapy failure (P = 0.85 and P = 0.56). The SLC22A1 loss-of-function variants, R61C and 420del, do not attenuate the A1C reduction achieved by metformin in patients with type 2 diabetes. ..
  14. He H, Meyer C, Shin H, Bailey S, Wei G, Wang Q, et al. Nucleosome dynamics define transcriptional enhancers. Nat Genet. 2010;42:343-7 pubmed publisher
    ..Therefore, quantitative modeling of enhancer structure provides a powerful predictive method to infer the identity of transcription factors involved in cellular responses to specific stimuli. ..
  15. Xu L, Matsumoto A, Sasaki A, Harada H, Taniguchi A. Identification of a suppressor element in the amelogenin promoter. J Dent Res. 2010;89:246-51 pubmed publisher
    ..Mutation of the Oct-1 binding sites reversed the suppressor activity, suggesting that Oct-1 sites are essential for suppression. These results suggest that Oct-1 and intron 1 may contribute to cell-type-specific amelogenin expression. ..
  16. Gallagher P, Liem R, Wong E, Weiss M, Bodine D. GATA-1 and Oct-1 are required for expression of the human alpha-hemoglobin-stabilizing protein gene. J Biol Chem. 2005;280:39016-23 pubmed
    ..The AHSP promoter is an excellent candidate region for mutations associated with decreased AHSP gene expression. ..
  17. Laurent B, Randrianarison Huetz V, Marechal V, Marchal V, Mayeux P, Dusanter Fourt I, et al. High-mobility group protein HMGB2 regulates human erythroid differentiation through trans-activation of GFI1B transcription. Blood. 2010;115:687-95 pubmed publisher
    ..We propose that HMGB2 potentiates GATA-1-dependent transcription of GFI1B by Oct-1 and thereby controls erythroid differentiation. ..
  18. Jang E, Kim H, Park C, Kang J. Increased expression of hepatic organic cation transporter 1 and hepatic distribution of metformin in high-fat diet-induced obese mice. Drug Metab Pharmacokinet. 2010;25:392-7 pubmed
    ..In conclusion, our results suggest, at least in part, that obesity might have an effect on the absorption or distribution pharmacokinetics of metformin through an increase in hepatic OCT1 expression...
  19. Li Weber M, Salgame P, Hu C, Davydov I, Laur O, Klevenz S, et al. Th2-specific protein/DNA interactions at the proximal nuclear factor-AT site contribute to the functional activity of the human IL-4 promoter. J Immunol. 1998;161:1380-9 pubmed
    ..These findings suggest that besides c-Maf, another Th2-specific factor(s) may be involved in tissue-specific expression of the IL-4 gene. ..
  20. Nenoi M, Daino K, Nakajima T, Wang B, Taki K, Kakimoto A. Involvement of Oct-1 in the regulation of CDKN1A in response to clinically relevant doses of ionizing radiation. Biochim Biophys Acta. 2009;1789:225-31 pubmed publisher
    ..Thus, our results reveal that Oct-1 is crucial to the TP53-mediated regulation of the CDKN1A gene promoter following exposure to clinically relevant doses of IR. ..
  21. Lents C, Farmerie T, Cherrington B, Clay C. Multiple core homeodomain binding motifs differentially contribute to transcriptional activity of the murine gonadotropin-releasing hormone receptor gene promoter. Endocrine. 2009;35:356-64 pubmed publisher
  22. Kim D, Sriharsha L, Xu W, Kamel Reid S, Liu X, Siminovitch K, et al. Clinical relevance of a pharmacogenetic approach using multiple candidate genes to predict response and resistance to imatinib therapy in chronic myeloid leukemia. Clin Cancer Res. 2009;15:4750-8 pubmed publisher
    ..Several cellular and genetic mechanisms of imatinib resistance have been proposed, including amplification and overexpression of the BCR/ABL gene, the tyrosine kinase domain point mutations, and MDR1 gene overexpression...
  23. Kiesler P, Shakya A, Tantin D, Vercelli D. An allergy-associated polymorphism in a novel regulatory element enhances IL13 expression. Hum Mol Genet. 2009;18:4513-20 pubmed publisher
    ..Our results illustrate how a functional variant in a regulatory element enhances transcription of an allergy-associated gene, thereby modulating disease susceptibility. ..
  24. Luca F, Kashyap S, Southard C, Zou M, Witonsky D, Di Rienzo A, et al. Adaptive variation regulates the expression of the human SGK1 gene in response to stress. PLoS Genet. 2009;5:e1000489 pubmed publisher
    ..Identifying such functional variants may shed light on the mechanisms underlying inter-individual variation in response to environmental stressors and to hormonal therapy, as well as in the susceptibility to hormone-dependent diseases. ..
  25. Rytting E, Bryan J, Southard M, Audus K. Low-affinity uptake of the fluorescent organic cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (4-Di-1-ASP) in BeWo cells. Biochem Pharmacol. 2007;73:891-900 pubmed
    ..Transport of 4-Di-1-ASP into the nuclear region of BeWo cells was also observed, which is likely mediated by a nucleoside transporter. ..
  26. Meng X, Luo Y, Xiao W, Li M, Shi J. Cloning and characterization of the promoter of the human AHI1 gene. Biochem Genet. 2009;47:427-38 pubmed publisher
    ..Our research provides an important basis for further investigations on the transcriptional regulation of the human AHI1 gene. ..
  27. Dennis M, Paracchini S, Scerri T, Prokunina Olsson L, Knight J, Wade Martins R, et al. A common variant associated with dyslexia reduces expression of the KIAA0319 gene. PLoS Genet. 2009;5:e1000436 pubmed publisher
    ..Our study thus pinpoints a common variant as altering the function of a dyslexia candidate gene and provides an illustrative example of the strategic approach needed to dissect the molecular basis of complex genetic traits. ..
  28. Marin D, Bazeos A, Mahon F, Eliasson L, Milojkovic D, Bua M, et al. Adherence is the critical factor for achieving molecular responses in patients with chronic myeloid leukemia who achieve complete cytogenetic responses on imatinib. J Clin Oncol. 2010;28:2381-8 pubmed publisher
    ..66; P = .006). In patients with CML treated with imatinib for some years, poor adherence may be the predominant reason for inability to obtain adequate molecular responses. ..
  29. D Apolito D, Baiamonte E, Bagliesi M, Di Marzo R, Calzolari R, Ferro L, et al. The sea urchin sns5 insulator protects retroviral vectors from chromosomal position effects by maintaining active chromatin structure. Mol Ther. 2009;17:1434-41 pubmed publisher
  30. Becker M, Visser L, Van Schaik R, Hofman A, Uitterlinden A, Stricker B. Genetic variation in the organic cation transporter 1 is associated with metformin response in patients with diabetes mellitus. Pharmacogenomics J. 2009;9:242-7 pubmed publisher
    ..09-0.47, P=0.005). After Bonferroni correction, the P-value was 0.050. To conclude, genetic variation at rs622342 in the SLC22A1 gene was associated with the glucose-lowering effect of metformin in patients with diabetes mellitus. ..
  31. Chen J, Randeva H. Genomic organization and regulation of the human orexin (hypocretin) receptor 2 gene: identification of alternative promoters. Biochem J. 2010;427:377-90 pubmed publisher
  32. Hughes T, Hochhaus A. Clinical strategies to achieve an early and successful response to tyrosine kinase inhibitor therapy. Semin Hematol. 2009;46:S11-5 pubmed
    ..Regular monitoring of response is crucial to maximize therapeutic success, and improved understanding of the factors affecting response will guide future clinical strategies. ..
  33. Zheng C, Zhu H, Liu H, Hu N, Meng W. [Expression of hOCT1 in patients with chronic myelogeneous leukemia treated by imatinib mesylate]. Sichuan Da Xue Xue Bao Yi Xue Ban. 2009;40:893-6 pubmed
    ..5110+/-0.1629, P=0.001), there was no significant correlation between the increase of hOCT1 and the decrease of BCR-ABL (P=0.821). hOCT1 has no association with the stage and course of CML, nor with the effectiveness of IM therapy. ..
  34. Zolk O. Current understanding of the pharmacogenomics of metformin. Clin Pharmacol Ther. 2009;86:595-8 pubmed publisher
    ..After a brief historical review of the discovery of the transporters for cationic drugs, the pharmacogenetics of metformin is discussed here in the light of recent literature. ..
  35. Becker M, Visser L, van Schaik R, Hofman A, Uitterlinden A, Stricker B. Interaction between polymorphisms in the OCT1 and MATE1 transporter and metformin response. Pharmacogenet Genomics. 2010;20:38-44 pubmed publisher
    ..The effect in incident users with the OCT1 rs622342 AC genotype is in between. ..
  36. Gervaziev Y, Olenina L, Krasotkina J, Lupatov A, Mazurina S, Gervazieva V. Oct-1 is responsible for the C-33T polymorphism effect in the IL-4 promoter. Int J Immunogenet. 2010;37:13-20 pubmed publisher
    ..Our findings suggest that the interplay between Oct-1 and unknown TFs may be responsible for the C-33T polymorphism effects. ..
  37. Belikov S, Astrand C, Wrange O. FoxA1 binding directs chromatin structure and the functional response of a glucocorticoid receptor-regulated promoter. Mol Cell Biol. 2009;29:5413-25 pubmed publisher
    ..Three constitutively binding factors, nuclear factor 1 (NF1), octamer transcription factor 1 (Oct1), and the Forkhead box A1 (FoxA1), were shown to act in concert, to direct the chromatin ..
  38. Fahrmayr C, Fromm M, Konig J. Hepatic OATP and OCT uptake transporters: their role for drug-drug interactions and pharmacogenetic aspects. Drug Metab Rev. 2010;42:380-401 pubmed publisher
  39. Nies A, Koepsell H, Winter S, Burk O, Klein K, Kerb R, et al. Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver. Hepatology. 2009;50:1227-40 pubmed publisher
    ..0001), and four variants in OCT3 (rs2292334, rs2048327, rs1810126, rs3088442) were associated with reduced OCT3 mRNA levels (P = 0.03)...
  40. Zhu X, Wu L, Zhang L, Hao P, Zhang S, Huang J, et al. Distinct regulatory mechanism of immunoglobulin gene transcription in epithelial cancer cells. Cell Mol Immunol. 2010;7:279-86 pubmed publisher
    ..These results suggested the presence of a distinct regulatory mechanism for Ig gene expression in non-B cancer cells. ..