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A RNA antagonist of hypoxia-inducible factor-1α, EZN-2968, inhibits tumor cell growth
Open accessAbstract
Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that plays a critical role in angiogenesis, survival, metastasis, drug resistance, and glucose metabolism. Elevated expression of the α-subunit of HIF-1 (HIF-1α), which occurs in response to hypoxia or activation of growth factor pathways, is associated with poor prognosis in many types of cancer. Therefore, down-regulation of HIF-1α protein by RNA antagonists may control cancer growth. EZN-2968 is a RNA antagonist composed of third-generation oligonucleotide, locked nucleic acid, technology that specifically binds and inhibits the expression of HIF-1α mRNA. In vitro, in human prostate (15PC3, PC3, and DU145) and glioblastoma (U373) cells, EZN-2968 induced a potent, selective, and durable antagonism of HIF-1 mRNA and protein expression (IC50, 1-5 nmol/L) under normoxic and hypoxic conditions associated with inhibition of tumor cell growth. Additionally, down-regulation of HIF-1α protein by EZN-2968 led to reduction of its transcriptional targets and of human umbilical vein endothelial cell tube formation. In vivo, administration of EZN-2968 to normal mice led to specific, dose-dependent, and highly potent down-regulation of endogenous HIF-1α and vascular endothelial growth factor in the liver. The effect can last for days after administration of single dose of EZN-2968 and is associated with long residence time of locked nucleic acid in certain tissues. In efficacy studies, tumor reduction was found in nude mice implanted with DU145 cells treated with EZN-2968. Ongoing phase I studies of EZN-2968 in patients with advanced malignancies will determine optimal dose and schedule for the phase II program. [Mol Cancer Ther 2008;7(11):3598–608]
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“IC50 values for the HIF-2α isoform, with which EZN-2968 has a 3-base-pair mismatch, were 5 times higher in all cell lines tested compared to IC50 values for HIF-1α, supporting the relative selectivity of EZN-2968 for HIF-1α [11].”
From Pilot trial of EZN-2968, an antisense oligonucleotide inhibitor of hypoxia-inducible factor-1 alpha (HIF-1α), in patients with refractory solid tumors (2014) · cites this paper as [11]
Experimental — accuracy not yet measuredThe source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“Because preclinical biodistribution studies of EZN-2968 documented prolonged and preferential retention in the liver [11]”
From Pilot trial of EZN-2968, an antisense oligonucleotide inhibitor of hypoxia-inducible factor-1 alpha (HIF-1α), in patients with refractory solid tumors (2014) · cites this paper as [11]
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“It was reported that inhibition of HIF-1α by EZN-2698 attenuates HIF-1α protein level and tumor progression in various in vitro (human prostate and glioblastoma cell lines) and in vivo studies52.”
From HIF-1α pathway: role, regulation and intervention for cancer therapy (2015) · cites this paper as [52]
Experimental — accuracy not yet measuredThe source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“EZN-2698 (1) is an anti-sense oligonucleotide, an RNA antagonist which specifically binds and inhibits the expression of HIF-1α mRNA as well as HIF-1α target genes.”
From HIF-1α pathway: role, regulation and intervention for cancer therapy (2015) · cites this paper as [52]
Experimental — accuracy not yet measuredThe source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“The in vivo effect of EZN-2968 has also been tested in a subcutaneous prostate cancer cell line xenograft model and, although treatment did not result in a significant reduction in tumor burden, pre-treatment of cells with EZN-2968 prior to injection resulted in a significant reduction in tumor size.”
From Therapeutic targeting of hypoxia and hypoxia-inducible factors in cancer (2016) · cites this paper as Greenberger et al., 2008
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“In vitro, it potently suppresses HIF-1α protein accumulation with IC50 values in the low-nanomolar range (1–5 nM) under both normoxic and hypoxic conditions.”
From HIF inhibition: Current strategies and clinical challenges (2026) · cites this paper as [281]
Experimental — accuracy not yet measuredThe source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“EZN-2968 binds specifically to HIF1A mRNA, promoting transcript degradation and inhibiting translation [280,281].”
From HIF inhibition: Current strategies and clinical challenges (2026) · cites this paper as [281]
Experimental — accuracy not yet measuredThe source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
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“In preclinical studies, EZN-2968 effectively attenuated transcription of HIF-1 target genes and inhibited hypoxia-driven angiogenesis in multiple cancer models, including prostate cancer, glioblastoma, and DU145 xenografts [281].”
From HIF inhibition: Current strategies and clinical challenges (2026) · cites this paper as [281]
Experimental — accuracy not yet measuredThe cited source says what the claim attributes to it.
In the citing paper
“EZN-2968 is an LNA antisense oligodeoxynucleotide that has been demonstrated to hybridize with HIF-1α mRNA and block HIF-1α protein expression in preclinical models [11].”
From Pilot trial of EZN-2968, an antisense oligonucleotide inhibitor of hypoxia-inducible factor-1 alpha (HIF-1α), in patients with refractory solid tumors (2014) · cites this paper as [11]
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“Tumor growth inhibition was observed in xenograft models [11].”
From Pilot trial of EZN-2968, an antisense oligonucleotide inhibitor of hypoxia-inducible factor-1 alpha (HIF-1α), in patients with refractory solid tumors (2014) · cites this paper as [11]
The cited source says what the claim attributes to it.
In the citing paper
“EZN-2968 has a three base pair mismatch with the HIF-2α sequence and, as a consequence, only downregulates HIF-2α mRNA by 20% at 25 nM.”
From Therapeutic targeting of hypoxia and hypoxia-inducible factors in cancer (2016) · cites this paper as Greenberger et al., 2008
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“EZN-2968 binding leads to HIF-1α mRNA downregulation in a dose-dependent manner and results in near complete inhibition at 5 nM concentrations (Greenberger et al., 2008).”
From Therapeutic targeting of hypoxia and hypoxia-inducible factors in cancer (2016) · cites this paper as Greenberger et al., 2008
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In the citing paper
“EZN-2968 treatment of tumor cells in vitro downregulated HIF-1α protein levels during hypoxia and reduced the growth rate.”
From Therapeutic targeting of hypoxia and hypoxia-inducible factors in cancer (2016) · cites this paper as Greenberger et al., 2008
The cited source says what the claim attributes to it.
In the citing paper
“Due to a three-nucleotide mismatch, its activity toward EPAS1 (HIF-2α) mRNA is minimal [281].”
From HIF inhibition: Current strategies and clinical challenges (2026) · cites this paper as [281]
The cited source says what the claim attributes to it.
In the citing paper
“EZN-2968 is built on locked nucleic acid (LNA) chemistry, in which a methylene bridge between the 2′-oxygen and 4′-carbon of the ribose ring locks the sugar into a rigid conformation. This structural feature enhances base-pairing affinity, nuclease resistance, and in vivo stability relative to conventional oligonucleotides [[279], [280], [281]].”
From HIF inhibition: Current strategies and clinical challenges (2026) · cites this paper as [281]
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Citations
Cites
Angiogenesis in cancer and other diseases
Carmeliet, P., & Jain, R. K. (2000) · Nature · doi:10.1038/35025220 · Cited by 9,070
Targeting HIF-1 for cancer therapy
Semenza, G. L. (2003) · Nature Reviews Cancer · doi:10.1038/nrc1187 · Cited by 6,717
Wang, G. L., Jiang, B. H., Rue, E. A., & Semenza, G. L. (1995) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.92.12.5510 · Cited by 6,212
Angiogenesis as a therapeutic target
Ferrara, N., & Kerbel, R. S. (2005) · Nature · doi:10.1038/nature04483 · Cited by 2,653
Mitochondrial reactive oxygen species trigger hypoxia-induced transcription
Chandel, N. S., Maltepe, E., Goldwasser, E., Mathieu, C. E., Simon, M. C., & Schumacker, P. T. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.20.11715 · Cited by 1,926
Hypoxia signalling in cancer and approaches to enforce tumour regression
Pouysségur, J., Dayan, F., & Mazure, N. M. (2006) · Nature · doi:10.1038/nature04871 · Cited by 1,676
LNA-mediated microRNA silencing in non-human primates
Elmén, J., Lindow, M., Schütz, S., Lawrence, M., Petri, A., Obad, S., Lindholm, M., Hedtjärn, M., Hansen, H. F., Berger, U., et al. (2008) · Nature · doi:10.1038/nature06783 · Cited by 1,589
(2000) · PubMed · Cited by 1,445
Tian, H., McKnight, S. L., & Russell, D. W. (1997) · Genes & Development · doi:10.1101/gad.11.1.72 · Cited by 1,351
Hypoxia-Inducible Factors, Stem Cells, and Cancer
Keith, B., & Simon, M. C. (2007) · Cell · doi:10.1016/j.cell.2007.04.019 · Cited by 1,179
Cited by
Sorted by citations
Items 101–200 of 251
Chen, Y., Zhao, D., Xiao, F., Li, X., Li, J., Su, Z., & Jiang, X. (2023) · Advanced Materials · doi:10.1002/adma.202209672 · Cited by 47
Zhang, Y., Castaneda, S., Dumble, M. L., Wang, M., Mileski, M., Qu, Z., Kim, S., Shi, V., Kraft, P., Gao, Y. J., et al. (2011) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-11-0329 · Cited by 47
Self-citationHIF-1α Is a Rational Target for Future Ovarian Cancer Therapies
Wang, X., Du, Z., Xu, T., Wang, X., Li, W., Gao, J., Li, J., & Zhu, H. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.785111 · Cited by 50
Notch signaling, hypoxia, and cancer
Guo, M., Niu, Y., Xie, M., Liu, X., & Li, X. (2023) · Frontiers in Oncology · doi:10.3389/fonc.2023.1078768 · Cited by 48
Glutamine Metabolism: Molecular Regulation, Biological Functions, and Diseases
Kumar, M. A., Baba, S. K., Khan, I. R., Khan, M. S., Husain, F. M., Ahmad, S., Haris, M., Singh, M., Akil, A. A., Macha, M. A., et al. (2025) · MedComm · doi:10.1002/mco2.70120 · Cited by 52
HIF factors cooperate with PML‐RARα to promote acute promyelocytic leukemia progression and relapse
Coltella, N., Percio, S., Valsecchi, R., Cuttano, R., Guarnerio, J., Ponzoni, M., Pandolfi, P. P., Melillo, G., Pattini, L., & Bernardi, R. (2014) · EMBO Molecular Medicine · doi:10.1002/emmm.201303065 · Cited by 45
Gan, E. S., & Ooi, E. E. (2020) · Virology Journal · doi:10.1186/s12985-020-01374-2 · Cited by 46
Sapra, P., Wang, M., Bandaru, R., Zhao, H., Greenberger, L. M., & Horak, I. D. (2010) · Nucleosides Nucleotides & Nucleic Acids · doi:10.1080/15257771003597733 · Cited by 44
Self-citationSadaghianloo, N., Contenti, J., Dardik, A., & Mazure, N. M. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20215387 · Cited by 45
Islam, S. M. T., Won, J., Khan, M., Mannie, M. D., & Singh, I. (2021) · Immunology · doi:10.1111/imm.13335 · Cited by 45
HIF-1α Confers Resistance to Induced Stress in Bone Marrow-derived Mesenchymal Stem Cells
Kiani, A. A., Kazemi, A., Halabian, R., Mohammadipour, M., Jahanian‐Najafabadi, A., & Roudkenar, M. H. (2013) · Archives of Medical Research · doi:10.1016/j.arcmed.2013.03.006 · Cited by 42
Kazi, A. A., Gilani, R. A., Schech, A. J., Chumsri, S., Sabnis, G. J., Shah, P., Goloubeva, O. G., Kronsberg, S. S., & Brodie, A. (2014) · Breast Cancer Research · doi:10.1186/bcr3609 · Cited by 41
The VHL/HIF Axis in the Development and Treatment of Pheochromocytoma/Paraganglioma
Song, P., Zhang, J., Tan, X., Huang, Y., Xu, J., Silk, N., Zhang, D., Liu, Q., & Jiang, J. (2020) · Frontiers in Endocrinology · doi:10.3389/fendo.2020.586857 · Cited by 42
Hypoxia inducible factor (HIF) as a model for studying inhibition of protein–protein interactions
Burslem, G. M., Kyle, H. F., Nelson, A., Edwards, T. A., & Wilson, A. J. (2017) · Chemical Science · doi:10.1039/c7sc00388a · Cited by 39
Wu, J., Contratto, M., Shanbhogue, K. P., Manji, G. A., O’Neil, B. H., Noonan, A., Tudor, R., & Lee, R. (2019) · World Journal of Clinical Oncology · doi:10.5306/wjco.v10.i3.149 · Cited by 41
Hypoxia-inducible factor inhibitors: a survey of recent patented compounds (2004 - 2010)
Ban, H. S., Uto, Y., & Nakamura, H. (2011) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.2011.547477 · Cited by 42
Mühleisen, A., Giaisi, M., Köhler, R., Krammer, P. H., & Li-Weber, M. (2014) · Cell Death and Disease · doi:10.1038/cddis.2014.536 · Cited by 46
Marine natural products as inhibitors of hypoxic signaling in tumors
Nagle, D. G., & Zhou, Y. (2009) · Phytochemistry Reviews · doi:10.1007/s11101-009-9120-1 · Cited by 41
Kheshtchin, N., & Hadjati, J. (2021) · Journal of Cellular Physiology · doi:10.1002/jcp.30643 · Cited by 42
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Narum, S. M., Deal, B. R., Ogasawara, H., Mancuso, J. N., Zhang, J., & Salaita, K. S. (2024) · ACS Nano · doi:10.1021/acsnano.3c09027 · Cited by 41
Wu, Y., Zhang, Y., Wang, M., Li, Q., Qu, Z., Shi, V., Kraft, P., Kim, S. H., Gao, Y. J., Pak, J., et al. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-12-0838 · Cited by 39
Self-citationHypoxia inducible factor 1α inhibitor PX-478 reduces atherosclerosis in mice
Villa-Roel, N., Ryu, K., Gu, L., Esmerats, J. F., Kang, D. W., Kumar, S., & Jo, H. (2022) · Atherosclerosis · doi:10.1016/j.atherosclerosis.2022.01.002 · Cited by 40
Pre-retrieval reperfusion decreases cancer recurrence after rat ischemic liver graft transplantation
Oldani, G., Crowe, L. A., Orci, L. A., Slits, F., Rubbia‐Brandt, L., Vito, C. D., Morel, P., Mentha, G., Berney, T., Vallée, J., et al. (2014) · Journal of Hepatology · doi:10.1016/j.jhep.2014.03.036 · Cited by 38
Henríquez, J. A., Sleeman, J. P., & Garvalov, B. K. (2018) · Clinical & Experimental Metastasis · doi:10.1007/s10585-018-9930-x · Cited by 37
Shin, M., Krishnamurthy, P. M., Devi, G., & Watts, J. K. (2021) · Nucleic Acid Therapeutics · doi:10.1089/nat.2021.0040 · Cited by 36
Cheng, Y.-C., Liou, J., Kuo, C., Lai, W.-Y., Shih, K.-H., Chang, C.-Y., Pan, W., Tseng, J. T.-C., & Chang, J. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-12-0778 · Cited by 36
Raguraman, P., Balachandran, A. A., Chen, S., Diermeier, S. D., & Veedu, R. N. (2021) · Cancers · doi:10.3390/cancers13215555 · Cited by 37
Exploration of the HIF-1α/p300 interface using peptide and Adhiron phage display technologies
Kyle, H. F., Wickson, K. F., Stott, J., Burslem, G. M., Breeze, A. L., Tiede, C., Tomlinson, D. C., Warriner, S. L., Nelson, A. S., Wilson, A. J., et al. (2015) · Molecular BioSystems · doi:10.1039/c5mb00284b · Cited by 35
Prognostic Impact of Hypoxia-InduciblemiRNA-210in Patients with Lung Adenocarcinoma
Osugi, J., Kimura, Y., Owada, Y., Inoue, T., Watanabe, Y., Yamaura, T., Fukuhara, M., Muto, S., Okabe, N., Matsumura, Y., et al. (2015) · Journal of Oncology · doi:10.1155/2015/316745 · Cited by 34
siRNA Therapeutics in the Treatment of Diseases
Bakhtiyari, S., Haghani, K., Basati, G., & Karimfar, M. H. (2012) · Therapeutic Delivery · doi:10.4155/tde.12.136 · Cited by 34
The Role of Imaging Biomarkers to Guide Pharmacological Interventions Targeting Tumor Hypoxia
Gallez, B. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.853568 · Cited by 35
Shaikat, A. H., Azad, S. M. A. K., Tamim, M. A. R., Ullah, M. S., Amin, M. N., Sabbir, M. K., Tarun, M. T. I., Mostaq, M. S., Sabrin, S., Mahmud, M. Z., et al. (2025) · Cancer Pathogenesis and Therapy · doi:10.1016/j.cpt.2025.07.003 · Cited by 37
Bohonowych, J. E., Peng, S., Gopal, U., Hance, M. W., Wing, S. B., Argraves, K. M., Lundgren, K., & Isaacs, J. S. (2011) · BMC Cancer · doi:10.1186/1471-2407-11-520 · Cited by 32
“A number of generalized HIF targeted approaches have been employed, including modulation of HIF expression, transcription, translation, dimerization, transactivation, and stability [17-23].”
BackgroundTargeting hypoxia in the treatment of small cell lung cancer
Bryant, J., Meredith, S. L., Williams, K. J., & White, A. E. (2014) · Lung Cancer · doi:10.1016/j.lungcan.2014.08.003 · Cited by 32
HIF-Dependent Mechanisms of Relationship between Hypoxia Tolerance and Tumor Development
Dzhalilova, D. S., & Makarova, O. V. (2021) · Biochemistry (Moscow) · doi:10.1134/s0006297921100011 · Cited by 34
Novel and emerging targeted-based cancer therapy agents and methods
Hojjat‐Farsangi, M. (2015) · Tumor Biology · doi:10.1007/s13277-015-3184-x · Cited by 31
Nurwidya, F., Takahashi, F., Minakata, K., Murakami, A., & Takahashi, K. (2012) · Anatomy & Cell Biology · doi:10.5115/acb.2012.45.2.73 · Cited by 35
Mao, S., Liu, Y., Morgan, J. B., Jekabsons, M. B., Zhou, Y., & Nagle, D. G. (2009) · Journal of Natural Products · doi:10.1021/np900444m · Cited by 31
Borsi, E., Perrone, G., Terragna, C., Martello, M., Zamagni, E., Tacchetti, P., Pantani, L., Brioli, A., Dico, A. F., Zannetti, B. A., et al. (2014) · Experimental Cell Research · doi:10.1016/j.yexcr.2014.09.018 · Cited by 30
Tumor Microenvironment and Nitric Oxide: Concepts and Mechanisms
Vedenko, A., Panara, K., Goldstein, G., Ramasamy, R., & Arora, H. (2020) · Advances in experimental medicine and biology · doi:10.1007/978-3-030-50224-9_10 · Cited by 30
Fakhri, S., Moradi, S. Z., Faraji, F., Kooshki, L., Webber, K. J., & Bishayee, A. (2023) · Cancer and Metastasis Reviews · doi:10.1007/s10555-023-10136-9 · Cited by 32
Anti‐angiogenic therapy: Adapting strategies to overcome resistant tumors
Mitchell, D., & Bryan, B. A. (2010) · Journal of Cellular Biochemistry · doi:10.1002/jcb.22764 · Cited by 30
King, M. J., Bukantz, S. C., Phillips, S. E., Mohapatra, S. S., Tamulis, T., & Lockey, R. F. (2004) · PubMed · Cited by 30
Hypoxia as a Target for Combination with Transarterial Chemoembolization in Hepatocellular Carcinoma
Wang, Z., Li, Q., & Liang, B. (2024) · Pharmaceuticals · doi:10.3390/ph17081057 · Cited by 30
Tumor Hypoxia As an Enhancer of Inflammation-Mediated Metastasis: Emerging Therapeutic Strategies
DiGiacomo, J. W., & Gilkes, D. M. (2018) · Targeted Oncology · doi:10.1007/s11523-018-0555-4 · Cited by 29
Targeting energy metabolism to eliminate cancer cells
Shahruzaman, S. H., Fakurazi, S., & Maniam, S. (2018) · Cancer Management and Research · doi:10.2147/cmar.s167424 · Cited by 29
Using RNA-seq to Assess Off-Target Effects of Antisense Oligonucleotides in Human Cell Lines
Michel, S., Schirduan, K., Shen, Y., Klar, R., Tost, J., & Jaschinski, F. (2020) · Molecular Diagnosis & Therapy · doi:10.1007/s40291-020-00504-4 · Cited by 27
Potent Inhibition of HIF1α and p300 Interaction by a Constrained Peptide Derived from CITED2
Qin, X., Chen, H., Tu, L., Ma, Y., Liu, N., Zhang, H., Li, D., Riedl, B., Bierer, D. E., Yin, F., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01043 · Cited by 26
Li, C., Lu, H.-J., Na, F., Deng, L., Xue, J., Wang, J., Wang, Y., Li, Q., & Lü, Y. (2013) · Asian Pacific Journal of Cancer Prevention · doi:10.7314/apjcp.2013.14.6.3607 · Cited by 25
HIF inhibitors for ischemic retinopathies and cancers: options beyond anti-VEGF therapies
Subhani, S., Vavilala, D. T., & Mukherji, M. (2016) · Angiogenesis · doi:10.1007/s10456-016-9510-0 · Cited by 27
Martin, A. R., Ronco, C., Demange, L., & Benhida, R. (2016) · MedChemComm · doi:10.1039/c6md00432f · Cited by 27
Regulating the Expression of HIF-1α or lncRNA: Potential Directions for Cancer Therapy
Zhang, M., Zhang, Y., Ding, Y., Huang, J., Yao, J., Xie, Z., Lv, Y., & Zuo, J. (2022) · Cells · doi:10.3390/cells11182811 · Cited by 26
Bilgin, S., Tayhan, S. E., Yıldırım, A., & Koç, E. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2022.106230 · Cited by 26
Vavilala, D. T., Ponnaluri, V. K. C., Kanjilal, D., & Mukherji, M. (2014) · PLoS ONE · doi:10.1371/journal.pone.0113717 · Cited by 23
Percio, S., Coltella, N., Grisanti, S., Bernardi, R., & Pattini, L. (2014) · Genome Medicine · doi:10.1186/s13073-014-0084-4 · Cited by 23
Anti-hypoxia nanosized drug delivery systems improving cancer therapy
Yan, W., Lang, T., Zhu, R., Zhu, X. G., Yu, H., Wu, T., Yin, Q., & Li, Y. (2022) · Nano Today · doi:10.1016/j.nantod.2022.101376 · Cited by 21
Research progress on non-protein-targeted drugs for cancer therapy
Zhang, Y., Lu, L., Song, F., Zou, X., Liu, Y., Zheng, X., Qian, J., Gu, C., Huang, P. C., & Yang, Y. (2023) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-023-02635-y · Cited by 22
Zhang, L., Yang, L., Li, J. J., & Sun, L. (2012) · Cancer Letters · doi:10.1016/j.canlet.2012.03.030 · Cited by 21
Shin, M., Lee, H.-J., Kang, S., Auh, Q., Lee, Y.-M., Kim, Y., & Kim, E.-C. (2014) · BioMed Research International · doi:10.1155/2014/934691 · Cited by 21
Small-molecule inhibitors of the HIF pathway and synthetic lethal interactions
Jones, D. T., & Harris, A. L. (2012) · Expert Opinion on Therapeutic Targets · doi:10.1517/14728222.2012.674516 · Cited by 21
An update on RNA interference-mediated gene silencing in cancer therapy
Ren, Y., & Zhang, Y. (2014) · Expert Opinion on Biological Therapy · doi:10.1517/14712598.2014.935334 · Cited by 20
Molecular mechanisms of effectiveness of novel therapies in multiple myeloma
Bianchi, G., & Ghobrial, I. M. (2012) · Leukemia & lymphoma/Leukemia and lymphoma · doi:10.3109/10428194.2012.706287 · Cited by 19
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Current insights and future perspectives of hypoxia-inducible factor-targeted therapy in cancer
Ajith, T. A. (2018) · Journal of Basic and Clinical Physiology and Pharmacology · doi:10.1515/jbcpp-2017-0167 · Cited by 19
Shen, J., Chen, J., Ma, J., Fan, L.-L., Zhang, X., Yue, T., Yan, Y., & Zhang, Y. (2020) · Asian Journal of Pharmaceutical Sciences · doi:10.1016/j.ajps.2019.12.001 · Cited by 19
The hypoxic microenvironment: A determinant of cancer stem cell evolution
Carnero, A., & LLeonart, M. E. (2015) · Inside the Cell · doi:10.1002/icl3.1039 · Cited by 23
Zhang, Z., & Zhang, H. (2021) · Expert Opinion on Therapeutic Targets · doi:10.1080/14728222.2021.2015321 · Cited by 18
Physical Exercise and Oxidative Stress
Kruk, J. (2011) · Medicina Sportiva · doi:10.2478/v10036-011-0004-2 · Cited by 18
Akinsulie, O. C., Shahzad, S., Ogunleye, S. C., Oladapo, I. P., Joshi, M., Ugwu, C. E., Gbadegoye, J. O., Hassan, F. O., Adeleke, R. A., Akande, Q. A., et al. (2023) · Frontiers in Immunology · doi:10.3389/fimmu.2023.1224102 · Cited by 19
Target Inhibition in Antiangiogenic Therapy A Wide Spectrum of Selectivity and Specificity
Kelly, R. J., Darnell, C., & Rixe, O. (2010) · The Cancer Journal · doi:10.1097/ppo.0b013e3181ff37cf · Cited by 17
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McDermott, A., & Tavassoli, A. (2024) · Transcription · doi:10.1080/21541264.2024.2417475 · Cited by 18
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Malenfant, S., Margaillan, G., Loehr, J., Bonnet, S., & Provencher, S. (2013) · Expert Review of Respiratory Medicine · doi:10.1586/ers.12.83 · Cited by 16
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Garvalov, B. K., & Acker, T. (2016) · Advances in experimental medicine and biology · doi:10.1007/978-1-4899-7678-9_12 · Cited by 17
Shin, J.-I., Lim, H.-Y., Kim, H.-W., Seung, B., & Sur, J. (2015) · Journal of Comparative Pathology · doi:10.1016/j.jcpa.2015.05.004 · Cited by 15
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Wendt, B., Mülbaier, M., Wawro, S., Schultes, C. M., Alonso, J., Janssen, B., & Lewis, J. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm200272h · Cited by 14
Naik, R., Han, S.-H., & Lee, K. (2015) · Archives of Pharmacal Research · doi:10.1007/s12272-015-0632-5 · Cited by 14
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Shomron, N. (2009) · European Journal of Cancer · doi:10.1016/s0959-8049(09)70060-7 · Cited by 8
Wang, Y., Li, Y., Wang, D., Li, Y., Chang, A. B., & Chan, W. K. (2012) · Cancer Letters · doi:10.1016/j.canlet.2012.01.037 · Cited by 8
Assinder, S. J., Dong, Q., Mangs, H., & Richardson, D. R. (2008) · Molecular Pharmacology · doi:10.1124/mol.108.053066 · Cited by 8
Zhang, X., Achkasov, E. E., Gavrikov, L. K., Yuchen, L., Zhang, C., Dudnik, E. N., Rumyantseva, O. I., Beeraka, N. M., & Glazachev, O. S. (2024) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2024.117275 · Cited by 8
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Khouzam, R. A., Salman, S., Thiery, J., Zaarour, R. F., Vela, V., Limani, P., Janji, B., & Chouaı̈b, S. (2026) · International Journal of Molecular Sciences · doi:10.3390/ijms27093873 · Cited by 7
Boticario, C. B., & Angosto, M. C. (2010) · Anales de la Real Academia Nacional de Farmacia · Cited by 5
Wang, S., Wang, X., Shao, Y., Shao, K., Wang, Y., Guo, X., Dong, H., Zhao, W., Li, Y., & Li, G. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.105298 · Cited by 5
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Metadata
- Authors
- Greenberger, L. M., Horak, I. D., Filpula, D., Sapra, P., Westergaard, M., Frydenlund, H. F., Albæk, C., Schrøder, H., & Ørum, H.
- Affiliations
- Enzon Pharmaceuticals (United States) (US)
- 2Santaris Pharma A/S, Copenhagen, Denmark
- Venue
- Molecular Cancer Therapeutics
- Published
- 2008-11-01
- Volume
- 7
- Issue
- 11
- Pages
- 3598-3608
- ISSN
- 1535-7163 (ISSN-L)
- 1538-8514
- OpenAlex
- W2158916045
- Cited by
- 245
- References
- 49
- Citations by year
- 2026: 6 · 2025: 7 · 2024: 12 · 2023: 13 · 2022: 13 · 2021: 19 · 2020: 11 · 2019: 10 · 2018: 8 · 2017: 7 · 2016: 10 · 2015: 12 · 2014: 22 · 2013: 22 · 2012: 25
- FWCI
- 5.31
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Molecular Cancer Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- University of Southern Denmark Research Portal (University of Southern Denmark) (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Hypoxia, and Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Angiogenesis and VEGF in Cancer
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Keywords
- HIF-1α, HIF-1, RNA interference, locked nucleic acid, prostate cancer, glioblastoma, tumor growth inhibition, angiogenesis, vascular endothelial growth factor, hypoxia
- MeSH terms
- Animals, Antineoplastic Agents, Humans, Liver, Mice, Inbred C57BL, Oligonucleotides, RNA, Messenger, Transcription, Genetic, Transfection, Down-Regulation, Models, Animal, Cell Line, Tumor, Mice, Hypoxia-Inducible Factor 1, alpha Subunit
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