(Q38003390)

26 August 2017

title

Small-molecule inhibitors of the HIF pathway and synthetic lethal interactions (English)

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26 August 2017

2

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26 August 2017

Dylan T Jones

1

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26 August 2017

language of work or name

English

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publication date

18 April 2012

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Expert Opinion on Therapeutic Targets

26 August 2017

published in

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26 August 2017

volume

16

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26 August 2017

issue

5

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26 August 2017

page(s)

463-480

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Regulation of angiogenesis by hypoxia-inducible factor 1.

26 August 2017

cites work

1 reference

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An endoplasmic reticulum transmembrane prolyl 4-hydroxylase is induced by hypoxia and acts on hypoxia-inducible factor alpha

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HIF prolyl-hydroxylase 2 is the key oxygen sensor setting low steady-state levels of HIF-1alpha in normoxia

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Abnormal sympathoadrenal development and systemic hypotension in PHD3-/- mice

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Oxygen sensing by HIF hydroxylases

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Hypoxia signalling through mTOR and the unfolded protein response in cancer

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Regulation of hypoxia-inducible factor-1alpha by NF-kappaB

21 January 2018

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Heat shock protein 90: the cancer chaperone

21 January 2018

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GSK-3β regulates cell growth, migration, and angiogenesis via Fbw7 and USP28-dependent degradation of HIF-1α

21 January 2018

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Identification of MAPK phosphorylation sites and their role in the localization and activity of hypoxia-inducible factor-1alpha.

21 January 2018

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Dephosphorylated hypoxia-inducible factor 1alpha as a mediator of p53-dependent apoptosis during hypoxia

21 January 2018

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Hypoxia-inducible factor-1 (HIF-1)-independent microvascular angiogenesis in the aged rat brain

21 January 2018

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Genome-wide association of hypoxia-inducible factor (HIF)-1alpha and HIF-2alpha DNA binding with expression profiling of hypoxia-inducible transcripts

21 January 2018

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High-resolution genome-wide mapping of HIF-binding sites by ChIP-seq.

21 January 2018

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Silencing of hypoxia inducible factor-1alpha by RNA interference attenuates human glioma cell growth in vivo.

21 January 2018

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Contrasting properties of hypoxia-inducible factor 1 (HIF-1) and HIF-2 in von Hippel-Lindau-associated renal cell carcinoma.

21 January 2018

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https://api.crossref.org/works/10.1517%2F14728222.2012.674516

HIF-1 and HIF-2 transcription factors--similar but not identical

21 January 2018

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https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Akt signalling in health and disease.

21 January 2018

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https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Inhibiting the hypoxia response for cancer therapy: the new kid on the block

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Everolimus (RAD001) and anti-angiogenic cyclophosphamide show long-term control of gastric cancer growth in vivo

21 January 2018

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https://api.crossref.org/works/10.1517%2F14728222.2012.674516

mTOR in renal cell cancer: modulator of tumor biology and therapeutic target.

21 January 2018

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Thioredoxin and thioredoxin reductase: current research with special reference to human disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A cellular and molecular investigation of the action of PMX464, a putative thioredoxin inhibitor, in normal and colorectal cancer cell lines.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Novel thioredoxin inhibitors paradoxically increase hypoxia-inducible factor-alpha expression but decrease functional transcriptional activity, DNA binding, and degradation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A randomized phase II study of PX-12, an inhibitor of thioredoxin in patients with advanced cancer of the pancreas following progression after a gemcitabine-containing combination.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

HIF-1alpha modulation by topoisomerase inhibitors in non-small cell lung cancer cell lines

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Cell type-specific, topoisomerase II-dependent inhibition of hypoxia-inducible factor-1alpha protein accumulation by NSC 644221.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Histone-deacetylase inhibitors: novel drugs for the treatment of cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Inhibition of hypoxia-induced angiogenesis by FK228, a specific histone deacetylase inhibitor, via suppression of HIF-1alpha activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Phase I pharmacokinetic and pharmacodynamic study of LAQ824, a hydroxamate histone deacetylase inhibitor with a heat shock protein-90 inhibitory profile, in patients with advanced solid tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Complex molecular mechanisms cooperate to mediate histone deacetylase inhibitors anti-tumour activity in neuroblastoma cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Phase 2 trial of romidepsin in patients with peripheral T-cell lymphoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Microtubules as a target for anticancer drugs

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

2ME2 inhibits tumor growth and angiogenesis by disrupting microtubules and dysregulating HIF.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Phase I trial of 2-methoxyestradiol NanoCrystal dispersion in advanced solid malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A phase II study of 2-methoxyestradiol nanocrystal colloidal dispersion alone and in combination with sunitinib malate in patients with metastatic renal cell carcinoma progressing on sunitinib malate

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Significant antitumor activity in vivo following treatment with the microtubule agent ENMD-1198.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A phase I dose-escalation, safety and pharmacokinetic study of the 2-methoxyestradiol analog ENMD-1198 administered orally to patients with advanced cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

17 AAG for HSP90 inhibition in cancer--from bench to bedside

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Monitoring therapeutic response of human ovarian cancer to 17-DMAG by noninvasive PET imaging with (64)Cu-DOTA-trastuzumab

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

HSP90 inhibition is effective in breast cancer: a phase II trial of tanespimycin (17-AAG) plus trastuzumab in patients with HER2-positive metastatic breast cancer progressing on trastuzumab.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Phase I trial of 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG), a heat shock protein inhibitor, administered twice weekly in patients with advanced malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

An activator of PHD2, KRH102140, decreases angiogenesis via inhibition of HIF-1α.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Rapid degradation of hypoxia-inducible factor-1alpha by KRH102053, a new activator of prolyl hydroxylase 2.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

p300 relieves p53-evoked transcriptional repression of hypoxia-inducible factor-1 (HIF-1).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Small-molecule activation of p53 blocks hypoxia-inducible factor 1alpha and vascular endothelial growth factor expression in vivo and leads to tumor cell apoptosis in normoxia and hypoxia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A RNA antagonist of hypoxia-inducible factor-1alpha, EZN-2968, inhibits tumor cell growth

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Inhibition of hypoxia inducible factor-1alpha (HIF-1alpha) decreases vascular endothelial growth factor (VEGF) secretion and tumor growth in malignant gliomas.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Cisplatin and doxorubicin repress Vascular Endothelial Growth Factor expression and differentially down-regulate Hypoxia-inducible Factor I activity in human ovarian cancer cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Anthracycline chemotherapy inhibits HIF-1 transcriptional activity and tumor-induced mobilization of circulating angiogenic cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Modulating hypoxia-inducible transcription by disrupting the HIF-1-DNA interface

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Identification of novel small-molecule inhibitors of hypoxia-inducible factor-1 transactivation and DNA binding

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Effects of HIF-1 inhibition by chetomin on hypoxia-related transcription and radiosensitivity in HT 1080 human fibrosarcoma cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Acriflavine inhibits HIF-1 dimerization, tumor growth, and vascularization

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Targeting the PAS-A domain of HIF-1alpha for development of small molecule inhibitors of HIF-1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Artificial ligand binding within the HIF2 PAS-B domain of the HIF2 transcription factor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A novel mode of action of YC-1 in HIF inhibition: stimulation of FIH-dependent p300 dissociation from HIF-1{alpha}.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A novel approach to cancer therapy using PX-478 as a HIF-1α inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1alpha

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

FDA drug approval summary: bevacizumab (Avastin) as treatment of recurrent glioblastoma multiforme

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Bevacizumab in Combination With Oxaliplatin, Fluorouracil, and Leucovorin (FOLFOX4) for Previously Treated Metastatic Colorectal Cancer: Results From the Eastern Cooperative Oncology Group Study E3200

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Paclitaxel-carboplatin alone or with bevacizumab for non-small-cell lung cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

FDA drug approval summary: bevacizumab plus interferon for advanced renal cell carcinoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Paclitaxel plus bevacizumab versus paclitaxel alone for metastatic breast cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Avastin's commercial march suffers setback.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Antiangiogenic therapy elicits malignant progression of tumors to increased local invasion and distant metastasis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Accelerated metastasis after short-term treatment with a potent inhibitor of tumor angiogenesis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Differential toxic mechanisms of 2-deoxy-D-glucose versus 2-fluorodeoxy-D-glucose in hypoxic and normoxic tumor cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Phase II study of lonidamine and diazepam in the treatment of recurrent glioblastoma multiforme

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Molecular and cellular regulation of glucose transporter (GLUT) proteins in cancer.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Differential expression of Glut 1 mRNA and protein levels correlates with increased sensitivity to the glyco-conjugated nitric oxide donor (2-glu-SNAP) in different tumor cell types

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A novel inhibitor of glucose uptake sensitizes cells to FAS-induced cell death

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Phase I clinical and pharmacokinetic study of the glucose-conjugated cytotoxic agent D-19575 (glufosfamide) in patients with solid tumors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Inhibition of tumor lactate oxidation: consequences for the tumor microenvironment.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

CD147 subunit of lactate/H+ symporters MCT1 and hypoxia-inducible MCT4 is critical for energetics and growth of glycolytic tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

The plasma membrane lactate transporter MCT4, but not MCT1, is up-regulated by hypoxia through a HIF-1alpha-dependent mechanism.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

HIF-1 regulates hypoxic induction of NHE1 expression and alkalinization of intracellular pH in pulmonary arterial myocytes.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Hypoxia-inducible carbonic anhydrase IX and XII promote tumor cell growth by counteracting acidosis through the regulation of the intracellular pH.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Carbonic anhydrases as drug targets--an overview

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A phase II clinical and pharmacodynamic study of E7070 in patients with metastatic, recurrent, or refractory squamous cell carcinoma of the head and neck: modulation of retinoblastoma protein phosphorylation by a novel chloroindolyl sulfonamide cell

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Natural product-derived small molecule activators of hypoxia-inducible factor-1 (HIF-1)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

HIF-1 or HIF-2 induction is sufficient to achieve cell cycle arrest in NIH3T3 mouse fibroblasts independent from hypoxia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

The impact of O2 availability on human cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Suppression of hypoxia-inducible factor 2alpha restores p53 activity via Hdm2 and reverses chemoresistance of renal carcinoma cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Genetic and functional studies implicate HIF1α as a 14q kidney cancer suppressor gene

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

HIF-2alpha deletion promotes Kras-driven lung tumor development.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Genetic evidence for a tumor suppressor role of HIF-2alpha.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Comparison of Helzel and OxyLite systems in the measurements of tumor partial oxygen pressure (pO2).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Imaging oxygenation of human tumours

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Where are we with imaging oxygenation in human tumours?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Correlation of [18F]FMISO autoradiography and pimonidazole [corrected] immunohistochemistry in human head and neck carcinoma xenografts

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Dynamic contrast-enhanced and diffusion MRI show rapid and dramatic changes in tumor microenvironment in response to inhibition of HIF-1alpha using PX-478.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Dynamic contrast-enhanced-MRI of tumor hypoxia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

[18F] fluoromisonidazole and [18F] fluorodeoxyglucose positron emission tomography in response evaluation after chemo-/radiotherapy of non-small-cell lung cancer: a feasibility study

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Is ¹⁸F-fluorodeoxyglucose positron emission tomography-based metabolic response superior to Response Evaluation Criteria In Solid Tumors-based response after two cycles of platinum-based chemotherapy in predicting clinical outcome of untreated patie

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Planning study for available dose of hypoxic tumor volume using fluorine-18-labeled fluoromisonidazole positron emission tomography for treatment of the head and neck cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Prognostic significance of [18F]-misonidazole positron emission tomography-detected tumor hypoxia in patients with advanced head and neck cancer randomly assigned to chemoradiation with or without tirapazamine: a substudy of Trans-Tasman Radiation O

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Using YC-1 to overcome the radioresistance of hypoxic cancer cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Combination strategy targeting the hypoxia inducible factor-1 alpha with mammalian target of rapamycin and histone deacetylase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Marked activity of irinotecan and rapamycin combination toward colon cancer cells in vivo and in vitro is mediated through cooperative modulation of the mammalian target of rapamycin/hypoxia-inducible factor-1alpha axis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Combined treatment targeting HIF-1α and Stat3 is a potent strategy for prostate cancer therapy.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Degradation of HIF-1alpha under hypoxia combined with induction of Hsp90 polyubiquitination in cancer cells by hypericin: a unique cancer therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Increased antitumor activity of bevacizumab in combination with hypoxia inducible factor-1 inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

Antiangiogenic therapy, hypoxia, and metastasis: risky liaisons, or not?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A phase I/II trial of weekly topotecan and carboplatin in potentially platinum-sensitive relapsed ovarian and peritoneal carcinoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A phase II trial of bevacizumab plus everolimus for patients with refractory metastatic colorectal cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A phase I study of bevacizumab (B) in combination with everolimus (E) and erlotinib (E) in advanced cancer (BEE).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

A phase I trial of liposomal doxorubicin, bevacizumab, and temsirolimus in patients with advanced gynecologic and breast malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F14728222.2012.674516

10.1517/14728222.2012.674516

21 January 2018

Identifiers

DOI

1 reference

26 August 2017

1 reference