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HIF-1 Inhibitors for Cancer Therapy: From Gene Expression to Drug Discovery
Abstract
Hypoxia-inducible factor 1 (HIF-1) is a heterodimeric protein composed of HIF-1alpha and HIF-1alpha subunits, which is activated in response to reduced O2 availability. HIF-1 transactivates genes encoding proteins that are involved in key aspects of the cancer phenotype, including cell immortalization and de-differentiation, stem cell maintenance, genetic instability, glucose uptake and metabolism, pH regulation, autocrine growth/survival, angiogenesis, invasion/metastasis, and resistance to chemotherapy. Increased HIF-1alpha levels, as determined by immunohistochemical analysis of tumor biopsy specimens, is associated with increased mortality in many human cancers. Drugs that inhibit HIF-1 activity and have anti-cancer effects in vivo have been identified and clinical trials are warranted to establish the contexts in which addition of such agents to therapy protocols will result in increased patient survival.
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“The search for possible HIF inhibitors has led to the identification of a number of molecules that impair HIF at various transcriptional and translational stages (ranging from protein stabilization to dimerization to DNA binding) [123].”
From Hypoxia and hypoxia-inducible factors as regulators of T cell development, differentiation, and function (2013) · cites this paper as [123]
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Items 101–116 of 116
Targeting epithelial–mesenchymal transition: therapeutic reversal of the cancer stem cell phenotype
Fruehauf, J. P., & Liau, M. C. (2011) · Therapy · doi:10.2217/thy.11.72 · Cited by 1
Prognostic significance of necrosis in ampullary carcinomas
Akar, K. E., & Bağcı, P. (2024) · Irish Journal of Medical Science (1971 -) · doi:10.1007/s11845-024-03740-3 · Cited by 1
“Intratumoral hypoxia is a mechanism created through HIF-1α (hypoxia-induced factor-1α), which is known to induce tumor dedifferentiation, rapid growth, invasion, metastasis, angiogenesis, and resistance to chemotherapy, resulting in the formation of aggressive tumor morphology [31, 32].”
BackgroundSadeghi, M., Hojati, Z., & Ghaedi, K. (2014) · مجله دانشگاه علوم پزشکی اراک · Cited by 1
Nuclear Factors Linking Cancer and Inflammation
Chosdol, K., Bhagat, M., Dikshit, B., Madan, E., Chattopadhyay, P., & Sinha, S. (2013) · Cancer drug discovery and develogment/Cancer drug discovery and development · doi:10.1007/978-1-4614-8039-6_6
Role of Hypoxia-Inducible Transcription Factors in TAM Function
Rohwer, N., & Cramer, T. (2011) · Springer eBooks · doi:10.1007/978-1-4614-0662-4_12
“Based on the crucial role for a wide range of common human cancers, targeting HIF-a is commonly considered as an innovative and effective approach for cancer therapy (Semenza 2009).”
BackgroundRahman, T., & Wezen, X. C. (2018) · Royal Society of Chemistry eBooks · doi:10.1039/9781782624011-00055
Chinese herbal medicine exhibits anticancer properties via eight cancer hallmarks
Subramaniam, M., & Lim, Y. M. (2020) · Journal of Applied Pharmaceutical Science · doi:10.7324/japs.2020.10818 · Cited by 1
“Dulce, acts as a HIF-1α inhibitor (Semenza, 2009).”
Yin, J., Zeng, X., Ai, Z., et al. (2020) · Research Square · doi:10.21203/rs.3.rs-115737/v1
Uribe, D. J. (2011) · UA Campus Repository (The University of Arizona)
Eliminating the hypoxia driven immunosuppression in tumors to enable immunotherapies of cancer
Halpin-Veszeleiova, K. (2022) · Digital Repository Service (Northeastern University) · doi:10.17760/d20455931
Sheikhi, E., Aghamaali, M., & Babataheri, S. (2023) · Journal of Research in Applied and Basic Medical Sciences · doi:10.61186/rabms.9.3.176
“Therefore, increasing its expression indicates that HIF1α plays a critical role in tumor progression and expansion (3, 9).”
Davis, D. A., Shrestha, P., & Yarchoan, R. (2024) · Global Health & Medicine · doi:10.35772/ghm.2024.01069
Gao, B., Zhang, C., Wang, D., Luo, D., Shan, Z., Teng, W., Tao, T., & Li, J. (2025) · International Journal of Women s Health · doi:10.2147/ijwh.s552719
“54 63 Several cancer prognostic data analyses suggest that mild hypothyroidism may prolong survival in cancer patients.”
Influence of hypoxia on tumour cell susceptibility to cytotoxic T lymphocyte mediated lysis
Noman, M. Z. (2012) · theses.fr (ABES) · doi:10.70675/306da2eez5bc3z478ez83c5zdc39407a896e
Influence de la Transition Epithélio-Mésenchymateuse sur la réponse T cytotoxique anti-tumorale
Akalay, I. (2013) · theses.fr (ABES) · doi:10.70675/cb446c70z6112z416ez9557z9831373b9e40
Metadata
- Authors
- Semenza, G.
- Affiliations
- Johns Hopkins University (US)
- Corresponding author
- Semenza, G.
- ORCID
- Semenza, G.
- Venue
- Current Pharmaceutical Design
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2009-11-01
- Volume
- 15
- Issue
- 33
- Pages
- 3839-3843
- ISSN
- 1381-6128 (ISSN-L)
- OpenAlex
- W2077230187
- Cited by
- 116
- References
- 0
- Citations by year
- 2025: 3 · 2024: 4 · 2023: 5 · 2022: 4 · 2021: 4 · 2020: 6 · 2019: 4 · 2018: 2 · 2017: 3 · 2016: 14 · 2015: 3 · 2014: 11 · 2013: 9 · 2012: 14
- FWCI
- 4.90
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Current Pharmaceutical Design (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Johns Hopkins University
- National Institute of General Medical Sciences
- 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
- Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
- Keywords
- HIF-1, HIF-1 inhibitors, HIF-1α, tumor hypoxia, cancer therapy, drug discovery, angiogenesis, metastasis, chemoresistance, glucose metabolism, stem cell maintenance, gene expression
- MeSH terms
- Antineoplastic Agents, Humans, Neoplasms, Drug Design, Gene Expression Regulation, Neoplastic, Drug Resistance, Neoplasm, Hypoxia-Inducible Factor 1, Hypoxia-Inducible Factor 1, alpha Subunit
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