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Hypoxia-inducible factor inhibitors: a survey of recent patented compounds (2004 - 2010)
Abstract
Introduction Hypoxia-inducible factor (HIF) is a heterodimeric transcription factor consisting of α and β subunits that regulates the expression of angiogenic factors, including VEGF, which are involved in angiogenesis, invasion/metastasis, glucose uptake and cell survival during cancer development. Areas covered This review summarizes the information about patented HIF inhibitors over the last 7 years (2004 - 2010). The reader will gain an outline of the structure and biological activity of recently developed HIF inhibitors. Expert opinion Inhibition of HIF is an attractive therapeutic target for tumor angiogenesis and, until now, various HIF inhibitors have been discovered and evaluated. It is expected that development of more potent and selective HIF inhibitors will provide an effective treatment of cancer and other HIF-related diseases, including inflammation and cardiovascular disorder. As VEGF plays an important role in angiogenesis during tumor growth and ischemic diseases, the inhibition of VEGF-induced HIF is an attractive approach for the suppression of hypoxia-mediated pathological angiogenesis. HIF inhibitors may not only have cytostatic antitumor effects with fewer side effects, but also synergetic effects combined with radiotherapy.
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“PX-478 has shown anti-tumor activity in several xenograft models (Welsh et al., 2004), and a phase 1 doseescalation study of PX-478 in patients with advanced solid tumors or lymphoma showed, at best, stable disease in 14 out of 36 evaluable patients (Ban et al., 2011).”
From Therapeutic targeting of hypoxia and hypoxia-inducible factors in cancer (2016) · cites this paper as Ban et al., 2011
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“PX-478 has shown anti-tumor activity in several xenograft models (Welsh et al., 2004), and a phase 1 doseescalation study of PX-478 in patients with advanced solid tumors or lymphoma showed, at best, stable disease in 14 out of 36 evaluable patients (Ban et al., 2011).”
From Therapeutic targeting of hypoxia and hypoxia-inducible factors in cancer (2016) · cites this paper as Ban et al., 2011
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Metadata
- Authors
- Ban, H. S., Uto, Y., & Nakamura, H.
- Affiliations
- Gakushuin University (JP)
- Venue
- Expert Opinion on Therapeutic Patents
- Publisher
- Informa UK Limited
- Published
- 2011-01-06
- Volume
- 21
- Issue
- 2
- Pages
- 131-146
- ISSN
- 1354-3776 (ISSN-L)
- 1744-7674
- OpenAlex
- W2037524661
- Cited by
- 42
- References
- 87
- Citations by year
- 2024: 1 · 2022: 2 · 2021: 1 · 2019: 5 · 2018: 2 · 2017: 4 · 2016: 3 · 2015: 6 · 2014: 3 · 2013: 5 · 2012: 8
- FWCI
- 2.27
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Expert Opinion on Therapeutic Patents (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Japan Society for the Promotion of Science (22790113, 23390013)
- 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
- hypoxia-inducible factor, vascular endothelial growth factor, tumor angiogenesis, anticancer drug development, hypoxia, inflammation, cardiovascular disease, combined radiotherapy, metastasis
- MeSH terms
- Animals, Antineoplastic Agents, Disulfides, Estradiol, Furans, Humans, Imidazoles, Indazoles, Mustard Compounds, Patents as Topic, Phenylpropionates, Piperazines, Hypoxia-Inducible Factor 1, alpha Subunit
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