The DOI matches its Crossref record.
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.
Overview
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
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?
In the citing paper
“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]
Citations
Cited by
Sorted by citations
Tumour hypoxia induces a metabolic shift causing acidosis: a common feature in cancer
Chiche, J., Brahimi-Horn, M. C., & Pouysségur, J. (2010) · Journal of Cellular and Molecular Medicine · doi:10.1111/j.1582-4934.2009.00994.x · Cited by 700
Oxygen availability and metabolic adaptations
Nakazawa, M. S., Keith, B., & Simon, M. C. (2016) · Nature reviews. Cancer · doi:10.1038/nrc.2016.84 · Cited by 446
Noman, M. Z., Hasmim, M., Messai, Y., Terry, S., Kiéda, C., Janji, B., & Chouaı̈b, S. (2015) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.00207.2015 · Cited by 420
“HIFs are dimeric proteins composed of an O2-sensitive -subunit (HIF-1 , HIF-2 , or HIF-3 ) and a -subunit (HIF-1 /aryl hydrocarbon receptor nuclear translocator).”
BackgroundInfluentialHypoxic stress: obstacles and opportunities for innovative immunotherapy of cancer
Chouaı̈b, S., Noman, M. Z., Kosmatopoulos, K., & Curran, M. A. (2016) · Oncogene · doi:10.1038/onc.2016.225 · Cited by 370
Noman, M. Z., Janji, B., Kaminska, B., Van Moer, K., Pierson, S., Przanowski, P., Buart, S., Berchem, G., Romero, P., Mami-Chouaib, F., et al. (2011) · Cancer Research · doi:10.1158/0008-5472.can-11-1094 · Cited by 256
“Signaling pathways involving hypoxia-inducible factor HIF-1a (11) and hypoxia-dependent activation of STAT3 (12) have been well elucidated (13).”
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
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
