The DOI matches its Crossref record; 50 of the 50 references it cites were found in a registry or an index.
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]
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
The source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“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]
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
“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
Experimental — accuracy not yet measured
The source backs part of the claim, not all of it — or backs it for a different population, condition or comparison.
In the citing paper
“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.
In the citing paper
“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]
The cited source says what the claim attributes to it.
In the citing paper
“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
The cited source says what the claim attributes to it.
In the citing paper
“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
The cited source says what the claim attributes to it.
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]
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
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
Hypoxia-inducible factors and the response to hypoxic stress
Majmundar, A. J., Wong, W. J., & Simon, M. C. (2010) · Molecular Cell · doi:10.1016/j.molcel.2010.09.022 · Cited by 2,380
The role of hypoxia in cancer progression, angiogenesis, metastasis, and resistance to therapy
Muz, B., de la Puente, P., Azab, F., & Azab, A. K. (2015) · Hypoxia · doi:10.2147/hp.s93413 · Cited by 2,066
“gave effective results and a safe toxicity in a Phase I clinical trial in metastatic, advanced solid malignancy.(85) Targeting”
BackgroundHIF-1α pathway: role, regulation and intervention for cancer therapy
Masoud, G. N., & Li, W. (2015) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2015.05.007 · Cited by 1,871
Hypoxia-inducible factors: mediators of cancer progression and targets for cancer therapy
Semenza, G. L. (2012) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2012.01.005 · Cited by 1,514
Therapeutic targeting of hypoxia and hypoxia-inducible factors in cancer
Wigerup, C., Påhlman, S., & Bexell, D. (2016) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2016.04.009 · Cited by 687
“…Glyceollins AKT/mTOR, Hsp90 Lee et al., 2015 Topotecan, PEG-SN38 Topoisomerase 1 Rapisarda et al., 2004, Pastorino et al., 2010 EZN-2968 HIF-1α mRNA Greenberger et al., 2008 2ME2, ENMD-1198 Microtubules Mabjeesh et al., 2003; LaVallee et al., 2008 Geldanamycin and analogs Hsp90 Isaacs et al.,…”
BackgroundRohwer, N., & Cramer, T. (2011) · Drug Resistance Updates · doi:10.1016/j.drup.2011.03.001 · Cited by 632
Anticancer Targets in the Glycolytic Metabolism of Tumors: A Comprehensive Review
Porporato, P. E., Dhup, S., Dadhich, R. K., Copetti, T., & Sonveaux, P. (2011) · Frontiers in Pharmacology · doi:10.3389/fphar.2011.00049 · Cited by 449
Hypoxia and Hypoxia Inducible Factors: Diverse Roles in Liver Diseases
Nath, B., & Szabó, G. (2011) · Hepatology · doi:10.1002/hep.25497 · Cited by 295
Pharmacologic Targeting of Hypoxia-Inducible Factors
Semenza, G. L. (2019) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010818-021637 · Cited by 288
Jensen, R. L. (2009) · Journal of Neuro-Oncology · doi:10.1007/s11060-009-9827-2 · Cited by 294
Up-down regulation of HIF-1α in cancer progression
Rashid, M., Zadeh, L. R., Baradaran, B., Molavi, O., Ghesmati, Z., Sabzichi, M., & Ramezani, F. (2021) · Gene · doi:10.1016/j.gene.2021.145796 · Cited by 302
Bai, R., Li, Y., Jian, L., Yue-hui, Y., Zhao, L., & Wei, M. (2022) · Molecular Cancer · doi:10.1186/s12943-022-01645-2 · Cited by 296
Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors
Xia, Y., Choi, H.-K., & Lee, K. (2012) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2012.01.033 · Cited by 278
Development of HIF‐1 inhibitors for cancer therapy
Onnis, B., Rapisarda, A., & Melillo, G. (2009) · Journal of Cellular and Molecular Medicine · doi:10.1111/j.1582-4934.2009.00876.x · Cited by 268
Targeting hypoxia-inducible factors: therapeutic opportunities and challenges
Yuan, X., Ruan, W., Bobrow, B., Carmeliet, P., & Eltzschig, H. K. (2024) · Nature Reviews Drug Discovery · doi:10.1038/s41573-023-00848-6 · Cited by 245
Ellinghaus, P., Heisler, I., Unterschemmann, K., Haerter, M., Beck, H., Greschat, S., Ehrmann, A., Summer, H., Flamme, I., Oehme, F., et al. (2013) · Cancer Medicine · doi:10.1002/cam4.112 · Cited by 230
Crosstalk between TGF-β signaling and the microRNA machinery
Butz, H., Rácz, K., Hunyady, L., & Patócs, A. (2012) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2012.04.003 · Cited by 216
Targeting the hypoxia-inducible factor (HIF) pathway in cancer
Poon, E., Harris, A. L., & Ashcroft, M. A. (2009) · Expert Reviews in Molecular Medicine · doi:10.1017/s1462399409001173 · Cited by 215
Noman, M. Z., Hasmim, M., Lequeux, A., Xiao, M., Duhem, C., Chouaı̈b, S., Berchem, G., & Janji, B. (2019) · Cells · doi:10.3390/cells8091083 · Cited by 220
Wilson, G. K., Tennant, D. A., & McKeating, J. A. (2014) · Journal of Hepatology · doi:10.1016/j.jhep.2014.08.025 · Cited by 205
Antisense oligonucleotides: modifications and clinical trials
Sharma, V. K., Sharma, R. K., & Singh, S. K. (2014) · MedChemComm · doi:10.1039/c4md00184b · Cited by 206
The hypoxic microenvironment: A determinant of cancer stem cell evolution
Carnero, A., & LLeonart, M. E. (2016) · BioEssays · doi:10.1002/bies.201670911 · Cited by 204
Zheng, F., Chen, J., Zhang, X., Wang, Z., Chen, J., Lin, X., Huang, H., Fu, W., Liang, J., Wu, W., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-21535-3 · Cited by 208
Tumor angiogenesis revisited: Regulators and clinical implications
Ronca, R., Benkheil, M., Mitola, S. M. F., Struyf, S., & Liekens, S. (2017) · Medicinal Research Reviews · doi:10.1002/med.21452 · Cited by 198
Development of Inhibitors Targeting Hypoxia-Inducible Factor 1 and 2 for Cancer Therapy
Yu, T., Tang, B., & Sun, X. (2017) · Yonsei Medical Journal · doi:10.3349/ymj.2017.58.3.489 · Cited by 202
HIFs, angiogenesis, and cancer
Yang, Y., Sun, M., Wang, L., & Jiao, B. (2012) · Journal of Cellular Biochemistry · doi:10.1002/jcb.24438 · Cited by 193
Beyond microRNA – Novel RNAs derived from small non-coding RNA and their implication in cancer
Martens‐Uzunova, E. S., Olvedy, M., & Jenster, G. W. (2013) · Cancer Letters · doi:10.1016/j.canlet.2012.11.058 · Cited by 191
Kang, J., Kim, E., Kim, W., Seong, K. M., Youn, H., Kim, J. W., Kim, J., & Youn, B. (2013) · Journal of Biological Chemistry · doi:10.1074/jbc.m113.490482 · Cited by 189
Interfering with Tumor Hypoxia for Radiotherapy Optimization
Telarović, I., Wenger, R. H., & Pruschy, M. N. (2021) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-021-02000-x · Cited by 208
Hypoxia-inducible factors and innate immunity in liver cancer
Yuen, V. W., & Wong, C. C. (2020) · Journal of Clinical Investigation · doi:10.1172/jci137553 · Cited by 187
Hypoxia: The Cornerstone of Glioblastoma
Doménech, M., Hernández, A., Plaja, A., Martinez‐Balibrea, E., & Balañá, C. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms222212608 · Cited by 187
Burdick, A. D., Sciabola, S., Mantena, S. R., Hollingshead, B. D., Stanton, R. V., Warneke, J. A., Zeng, M., Martsen, E., Medvedev, A. V., Makarov, S. S., et al. (2014) · Nucleic Acids Research · doi:10.1093/nar/gku142 · Cited by 185
Overcoming disappointing results with antiangiogenic therapy by targeting hypoxia
Rapisarda, A., & Melillo, G. (2012) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2012.64 · Cited by 178
Cell‐specific blood–brain barrier regulation in health and disease: a focus on hypoxia
Engelhardt, S., Patkar, S., & Ogunshola, O. O. (2013) · British Journal of Pharmacology · doi:10.1111/bph.12489 · Cited by 168
Jeong, W., Rapisarda, A., Park, S. R., Kinders, R. J., Chen, A., Melillo, G., Turkbey, B., Steinberg, S. M., Choyke, P., Doroshow, J. H., et al. (2014) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-013-2362-z · Cited by 159
“Tumor growth inhibition was observed in xenograft models [11].”
InfluentialGlaviano, A., Lau, H., Carter, L. M., Lee, E. H. C., Lam, H. Y., Okina, E., Tan, D. J. J., Tan, W., Ang, H. L., Carbone, D., et al. (2025) · Journal of Hematology & Oncology · doi:10.1186/s13045-024-01634-6 · Cited by 169
Hypoxia-inducible factor pathway and diseases of the vascular wall
Lim, C. S., Kiriakidis, S., Sandison, A., Paleolog, E. M., & Davies, A. H. (2013) · Journal of Vascular Surgery · doi:10.1016/j.jvs.2013.02.240 · Cited by 154
Targeting the Metabolic Microenvironment of Tumors
Bailey, K. M., Wojtkowiak, J. W., Hashim, A. I., & Gillies, R. J. (2012) · Advances in pharmacology · doi:10.1016/b978-0-12-397927-8.00004-x · Cited by 157
Lipid Metabolism and Lipid Droplets in Pancreatic Cancer and Stellate Cells
Sunami, Y., Rebelo, A., & Kleeff, J. H. (2017) · Cancers · doi:10.3390/cancers10010003 · Cited by 157
A systems biology view of blood vessel growth and remodelling
Logsdon, E. A., Finley, S. D., Popel, A. S., & Gabhann, F. M. (2013) · Journal of Cellular and Molecular Medicine · doi:10.1111/jcmm.12164 · Cited by 163
Navarro, C., Ortega, Á., Santeliz, R., Garrido, B., Chacín, M., Galbán, N., Vera, I., Sanctis, J. B. D., & Bermúdez, V. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14061303 · Cited by 152
Vadlapatla, R. K., Vadlapudi, A. D., & Mitra, A. K. (2013) · Current Drug Targets · doi:10.2174/13894501113149990015 · Cited by 148
Role of the hypoxic tumor microenvironment in the resistance to anti-angiogenic therapies
Rapisarda, A., & Melillo, G. (2009) · Drug Resistance Updates · doi:10.1016/j.drup.2009.03.002 · Cited by 142
Promise and Challenge of RNA Interference–Based Therapy for Cancer
Petrocca, F., & Lieberman, J. (2010) · Journal of Clinical Oncology · doi:10.1200/jco.2009.27.6287 · Cited by 138
Frolova, O., Samudio, I. J., Benito, J. M., Jacamo, R. O., Kornblau, S. M., Marković, A. K., Schober, W. D., Lu, H., Qiu, Y. H., Buglio, D., et al. (2012) · Cancer Biology & Therapy · doi:10.4161/cbt.20838 · Cited by 130
Zhang, J., Yao, M., Xia, S., Zeng, F., & Liu, Q. (2025) · Cellular & Molecular Biology Letters · doi:10.1186/s11658-024-00682-7 · Cited by 150
The emerging role of hypoxia, HIF-1 and HIF-2 in multiple myeloma
Martin, S. K., Diamond, P., Gronthos, S., Peet, D. J., & Zannettino, A. C. W. (2011) · Leukemia · doi:10.1038/leu.2011.122 · Cited by 126
The potential role of HIF on tumour progression and dissemination
Unwith, S., Zhao, H., Hennah, L., & Ma, D. (2014) · International Journal of Cancer · doi:10.1002/ijc.28889 · Cited by 130
Benito, J., Shi, Y., Szymanska, B., Carol, H., Boehm, I., Lu, H., Konoplev, S. N., Fang, W., Zweidler‐McKay, P. A., Campana, D., et al. (2011) · PLoS ONE · doi:10.1371/journal.pone.0023108 · Cited by 122
The relevance of a hypoxic tumour microenvironment in prostate cancer
Stewart, G. D., Ross, J. A., McLaren, D. B., Parker, C. C., Habib, F. K., & Riddick, A. C. P. (2009) · British Journal of Urology · doi:10.1111/j.1464-410x.2009.08921.x · Cited by 116
Dirin, M., & Winkler, J. (2013) · Expert Opinion on Biological Therapy · doi:10.1517/14712598.2013.774366 · Cited by 115
Liu, X., Xiong, M., Shu, X., Tang, R.-Z., & Wang, J. (2012) · Molecular Pharmaceutics · doi:10.1021/mp300193f · Cited by 112
Chemical Modification Study of Antisense Gapmers
Stanton, R. V., Sciabola, S., Salatto, C. T., Weng, Y., Moshinsky, D., Little, J., Walters, E., Kreeger, J. M., DiMattia, D. A., Chen, T. X., et al. (2012) · Nucleic Acid Therapeutics · doi:10.1089/nat.2012.0366 · Cited by 110
Targeting HIF-2 α in clear cell renal cell carcinoma: A promising therapeutic strategy
Martínez‐Sáez, O., Borau, P. G., Alonso‐Gordoa, T., Molina‐Cerrillo, J., & Grande, E. (2017) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2017.01.013 · Cited by 111
Biological Activity and Biotechnological Aspects of Locked Nucleic Acids
Lundin, K. E., Højland, T., Hansen, B. R., Persson, R., Bramsen, J. B., Kjems, J., Koch, T., Wengel, J., & Smith, C. I. E. (2013) · Advances in genetics · doi:10.1016/b978-0-12-407676-1.00002-0 · Cited by 114
Hypoxia inducible factors in the tumor microenvironment as therapeutic targets of cancer stem cells
Hajizadeh, F., Okoye, I., Esmaily, M., Chaleshtari, M. G., Masjedi, A., Azizi, G., Irandoust, M., Ghalamfarsa, G., & Jadidi‐Niaragh, F. (2019) · Life Sciences · doi:10.1016/j.lfs.2019.116952 · Cited by 105
Storti, P., Bolzoni, M., Donofrío, G., Airoldi, I., Guasco, D., Toscani, D., Martella, E., Lazzaretti, M., Mancini, C., Agnelli, L., et al. (2013) · Leukemia · doi:10.1038/leu.2013.24 · Cited by 107
Belaïdi, E., Morand, J., Gras, E., Pépin, J., & Godin‐Ribuot, D. (2016) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2016.07.010 · Cited by 116
Liu, K., Zhang, X., Xu, W., Chen, J., Yu, J. Q., Gamble, J. R., & McCaughan, G. W. (2017) · Clinical and Translational Gastroenterology · doi:10.1038/ctg.2017.28 · Cited by 104
Zhang, J., Hu, Z., Horta, C. A., & Yang, J. (2022) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2022.12.002 · Cited by 106
Tafani, M., Pucci, B., Russo, A., Schito, L., Pellegrini, L., Perrone, G. A., Villanova, L., Salvatori, L., Ravenna, L., Petrangeli, E., et al. (2013) · Frontiers in Pharmacology · doi:10.3389/fphar.2013.00013 · Cited by 100
Gacche, R. N., & Meshram, R. J. (2013) · Progress in Biophysics and Molecular Biology · doi:10.1016/j.pbiomolbio.2013.10.001 · Cited by 97
Progress toward Overcoming Hypoxia-Induced Resistance to Solid Tumor Therapy
Reginato, M., & Karakashev, S. (2015) · Cancer Management and Research · doi:10.2147/cmar.s58285 · Cited by 95
Chambers, A. M., & Matosevic, S. (2019) · Frontiers in Molecular Biosciences · doi:10.3389/fmolb.2019.00060 · Cited by 100
Tang, X., Zhang, Q., Shi, S., Yen, Y., Li, X., Zhang, Y., Zhou, K., & Le, A. D. (2009) · International Journal of Cancer · doi:10.1002/ijc.24710 · Cited by 95
Hypoxia-mediated cancer stem cell resistance and targeted therapy
Sun, X., Lv, X., Yan, Y., Zhao, Y., Ma, R., He, M., & Wei, M. (2020) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2020.110623 · Cited by 93
Wojtkowiak-Szlachcic, A., Taylor, K., Stępniak-Konieczna, E., Sznajder, Ł. J., Mykowska, A., Sroka, J., Thornton, C. A., & Sobczak, K. (2015) · Nucleic Acids Research · doi:10.1093/nar/gkv163 · Cited by 90
Kao, T.-W., Bai, G.-H., Wang, T.-L., Shih, I.-M., Chuang, C.-M., Lo, C.-L., Tsai, M.-C., Chiu, L.-Y., Lin, C.-C., & Shen, Y.-A. (2023) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-023-02724-y · Cited by 89
Hypoxia-inducible factor-1α: A promising therapeutic target for vasculopathy in diabetic retinopathy
Li, H.-Y., Yuan, Y., Fu, Y.-H., Wang, Y., & Gao, X.-Y. (2020) · Pharmacological Research · doi:10.1016/j.phrs.2020.104924 · Cited by 88
Bouhamida, E., Morciano, G., Perrone, M., Kahsay, A. E., Della Sala, M., Wieckowski, M. R., Fiorica, F., Pinton, P., Giorgi, C., & Patergnani, S. (2022) · Biology · doi:10.3390/biology11020300 · Cited by 87
Hypoxia and Hypoxia-Inducible Factors in Leukemias
Deynoux, M., Sunter, N. J., Hérault, O., & Mazurier, F. (2016) · Frontiers in Oncology · doi:10.3389/fonc.2016.00041 · Cited by 91
Aurora kinases in childhood acute leukemia: the promise of aurora B as therapeutic target
Hartsink-Segers, S. A., Zwaan, C. M., Exalto, C., Luijendijk, M. W. J., Calvert, V. S., Petricoin, E., We, E., Reinhardt, D., de Haas, V., Hedtjärn, M., et al. (2012) · Leukemia · doi:10.1038/leu.2012.256 · Cited by 82
A therapeutic role for targeting c-Myc/Hif-1- dependent signaling pathways
Podar, K., & Anderson, K. C. (2010) · Cell Cycle · doi:10.4161/cc.9.9.11358 · Cited by 82
Hypoxia‐inducible factor‐1 as a therapeutic target in cancer
Tang, C., & Yu, J. Q. (2012) · Journal of Gastroenterology and Hepatology · doi:10.1111/jgh.12038 · Cited by 80
Cardoso, R., Love, R., Nilsson, C. L., Bergqvist, S., Nowlin, D., Yan, J., Liu, K. K. ‐., Zhu, J., Chen, P., Deng, Y., et al. (2012) · Protein Science · doi:10.1002/pro.2172 · Cited by 79
Silva, V. L., & Al-Jamal, W. T. (2017) · Journal of Controlled Release · doi:10.1016/j.jconrel.2017.03.013 · Cited by 77
Oberemok, V. V., Laikova, K. V., Repetskaya, A., Kenyo, I., Владимирович, Г. М., Касич, И. Н., Krasnodubets, A. M., Gal’chinsky, N. V., Фомочкина, И. И., Zaitsev, A. S., et al. (2018) · Molecules · doi:10.3390/molecules23061302 · Cited by 77
An Overview of the Recent Development of Anticancer Agents Targeting the HIF-1 Transcription Factor
Shirai, Y., Chow, C. C. T., Kambe, G., Suwa, T., Kobayashi, M., Takahashi, I., Harada, H., & Nam, J. (2021) · Cancers · doi:10.3390/cancers13112813 · Cited by 76
Autophagy, a double-edged sword in anti-angiogenesis therapy
Liu, J., Fan, L., Wang, H., & Sun, G. (2015) · Medical Oncology · doi:10.1007/s12032-015-0721-9 · Cited by 72
Gariboldi, M. B., Ravizza, R., & Monti, E. (2010) · Biochemical Pharmacology · doi:10.1016/j.bcp.2010.05.011 · Cited by 70
Zhang, Y., Qu, Z., Kim, S., Shi, V., Liao, B., Kraft, P., Bandaru, R., Wu, Y. S., Greenberger, L. M., & Horak, I. D. (2010) · Gene Therapy · doi:10.1038/gt.2010.133 · Cited by 71
Self-citationHu, J., Valckenborgh, E. V., Menu, E., Bruyne, E. D., & Vanderkerken, K. (2012) · Disease Models & Mechanisms · doi:10.1242/dmm.008961 · Cited by 69
The molecular therapy of colorectal cancer
Waldner, M. J., & Neurath, M. F. (2010) · Molecular Aspects of Medicine · doi:10.1016/j.mam.2010.02.005 · Cited by 67
HIF-1 and HIF-2 in cancer: structure, regulation, and therapeutic prospects
Shi, Y., & Gilkes, D. M. (2025) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-024-05537-0 · Cited by 81
The Caulerpa Pigment Caulerpin Inhibits HIF-1 Activation and Mitochondrial Respiration
Liu, Y., Morgan, J. B., Coothankandaswamy, V., Liu, R., Jekabsons, M. B., Mahdi, F., Nagle, D. G., & Zhou, Y. (2009) · Journal of Natural Products · doi:10.1021/np9005794 · Cited by 64
Hsp90 as a Gatekeeper of Tumor Angiogenesis: Clinical Promise and Potential Pitfalls
Bohonowych, J. E. S., Gopal, U., & Isaacs, J. S. (2010) · Journal of Oncology · doi:10.1155/2010/412985 · Cited by 64
Li, Z., You, Q., & Zhang, X. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01596 · Cited by 64
Sadri, N., & Zhang, P. J. (2013) · Cancers · doi:10.3390/cancers5020320 · Cited by 65
Bioanalysis of siRNA and Oligonucleotide Therapeutics in Biological Fluids and Tissues
Tremblay, G. A., & Oldfield, P. R. (2009) · Bioanalysis · doi:10.4155/bio.09.66 · Cited by 61
Understanding the Oxygen-Sensing Pathway and Its Therapeutic Implications in Diseases
Liao, C., & Zhang, Q. H. (2020) · American Journal Of Pathology · doi:10.1016/j.ajpath.2020.04.003 · Cited by 64
Therapeutic targeting of hypoxia and hypoxia-inducible factor 1 alpha in multiple myeloma
Borsi, E., Terragna, C., Brioli, A., Tacchetti, P., Martello, M., & Cavo, M. (2014) · Translational research · doi:10.1016/j.trsl.2014.12.001 · Cited by 61
Valsecchi, R., Coltella, N., Belloni, D., Ponente, M., ten Hacken, E., Scielzo, C., Scarfò, L., Bertilaccio, M. T. S., Brambilla, P., Lenti, E., et al. (2016) · Blood · doi:10.1182/blood-2015-07-657056 · Cited by 59
Hypoxia inducible factor-1 alpha as a therapeutic target in multiple myeloma
Borsi, E., Perrone, G., Terragna, C., Martello, M., Dico, A. F., Solaini, G., Baracca, A., Sgarbi, G., Pasquinelli, G., Valente, S., et al. (2014) · Oncotarget · doi:10.18632/oncotarget.1736 · Cited by 57
Renal toxicity of targeted therapies
Kelly, R. J., Billemont, B., & Rixe, O. (2009) · Targeted Oncology · doi:10.1007/s11523-009-0109-x · Cited by 53
Ikeda, H., & Kakeya, H. (2021) · The Journal of Antibiotics · doi:10.1038/s41429-021-00451-0 · Cited by 61
Increased activation of the hypoxia-inducible factor pathway in varicose veins
Lim, C. S., Kiriakidis, S., Paleolog, E. M., & Davies, A. H. (2012) · Journal of Vascular Surgery · doi:10.1016/j.jvs.2011.10.111 · Cited by 53
Action Sites and Clinical Application of HIF-1α Inhibitors
Xu, R., Wang, F., Yang, H., & Wang, Z. (2022) · Molecules · doi:10.3390/molecules27113426 · Cited by 59
The osteoblastic niche in the context of multiple myeloma
Toscani, D., Bolzoni, M., Accardi, F., Aversa, F., & Giuliani, N. (2015) · Annals of the New York Academy of Sciences · doi:10.1111/nyas.12578 · Cited by 52
Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors
Minegishi, H., Fukashiro, S., Ban, H. S., & Nakamura, H. (2013) · ACS Medicinal Chemistry Letters · doi:10.1021/ml3004632 · Cited by 54
Papargyri, N., Stoico, M. P., Andersen, M. R., Koch, T., & Hagedorn, P. (2019) · Molecular Therapy — Nucleic Acids · doi:10.1016/j.omtn.2019.12.011 · Cited by 50
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
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
