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https://www.readbyqxmd.com/read/28332352/development-of-inhibitors-targeting-hypoxia-inducible-factor-1-and-2-for-cancer-therapy
#1
REVIEW
Tianchi Yu, Bo Tang, Xueying Sun
Hypoxia is frequently observed in solid tumors and also one of the major obstacles for effective cancer therapies. Cancer cells take advantage of their ability to adapt hypoxia to initiate a special transcriptional program that renders them more aggressive biological behaviors. Hypoxia-inducible factors (HIFs) are the key factors that control hypoxia-inducible pathways by regulating the expression of a vast array of genes involved in cancer progression and treatment resistance. HIFs, mainly HIF-1 and -2, have become potential targets for developing novel cancer therapeutics...
May 2017: Yonsei Medical Journal
https://www.readbyqxmd.com/read/28323589/preventing-high-altitude-cerebral-edema-in-rats-with-repurposed-anti-angiogenesis-pharmacotherapy
#2
Samantha Tarshis, Joanne Maltzahn, Zoe Loomis, David C Irwin
BACKGROUND: High altitude cerebral edema (HACE) is a fulminant, deadly, and yet still unpredictable brain disease. A new prophylactic treatment for HACE and its predecessor, acute mountain sickness (AMS), needs to be developed without the contraindications or adverse effect profiles of acetazolamide and dexamethasone. Since neovascularization signals are likely key contributors to HACE/AMS, our approach was to examine already existing anti-angiogenic drugs to inhibit potential initiating HACE pathway(s)...
December 1, 2016: Aerospace Medicine and Human Performance
https://www.readbyqxmd.com/read/28228260/chemotherapy-induced-ca-2-release-stimulates-breast-cancer-stem-cell-enrichment
#3
Haiquan Lu, Ivan Chen, Larissa A Shimoda, Youngrok Park, Chuanzhao Zhang, Linh Tran, Huimin Zhang, Gregg L Semenza
Breast cancer stem cells (BCSCs) play a critical role in tumor recurrence and metastasis. Exposure of breast cancer cells to chemotherapy leads to an enrichment of BCSCs. Here, we find that chemotherapy induces the expression of glutathione S-transferase omega 1 (GSTO1), which is dependent on hypoxia-inducible factor 1 (HIF-1) and HIF-2. Knockdown of GSTO1 expression abrogates carboplatin-induced BCSC enrichment, decreases tumor initiation and metastatic capacity, and delays tumor recurrence after chemotherapy...
February 21, 2017: Cell Reports
https://www.readbyqxmd.com/read/28017781/inotropic-support-against-early-brain-injury-improves-cerebral-hypoperfusion-and-outcomes-in-a-murine-model-of-subarachnoid-hemorrhage
#4
Tomoko Mutoh, Tatsushi Mutoh, Kazuhiro Nakamura, Kazumasu Sasaki, Yasuko Tatewaki, Tatsuya Ishikawa, Yasuyuki Taki
Early brain injury/ischemia is a recent therapeutic target that contributes to triggering delayed cerebral ischemia (DCI) in the setting of subarachnoid hemorrhage (SAH). This study aimed to determine the role of dobutamine for inotropic cardiac support in improving cerebral blood flow (CBF) and outcomes after experimental SAH, mediated by hypoxia-inducible factor (HIF). Thirty-one mice were subjected to SAH by endovascular perforation, and assigned to either 2% isoflurane postconditioning performed between 1 and 2...
December 23, 2016: Brain Research Bulletin
https://www.readbyqxmd.com/read/28003935/aggregation-of-engineered-human-%C3%AE-cells-into-pseudoislets-insulin-secretion-and-gene-expression-profile-in-normoxic-and-hypoxic-milieu
#5
Marie-José Lecomte, Séverine Pechberty, Cécile Machado, Sandra Da Barroca, Philippe Ravassard, Raphaël Scharfmann, Paul Czernichow, Bertrand Duvillié
Innovative treatments to cure type 1 diabetes are being actively researched. Among the different strategies, the replacement of β-cells has given promising results. Classically, islets from cadaveric donors are transplanted into diabetic patients, but recently phase I clinical trials that use stem cell-derived β-cells have been started. Such protocols require either an immunosuppressive treatment or the macroencapsulation of the β-cells. They involve cell aggregation and the exposure of the cells to hypoxia...
December 3, 2016: Cell Medicine
https://www.readbyqxmd.com/read/27999195/molecular-and-functional-evaluation-of-a-novel-hif-inhibitor-benzopyranyl-1-2-3-triazole-compound
#6
Kyunghye Park, Hye Eun Lee, Sun Hee Lee, Doohyun Lee, Taeho Lee, You Mie Lee
Hypoxia occurs in a variety of pathological events, including the formation of solid tumors. Hypoxia-inducible factor (HIF)-1α is stabilized under hypoxic conditions and is a key molecule in tumor growth and angiogenesis. Seeking to develop novel cancer therapeutics, we investigated small molecules from our in-house chemical libraries to target HIF-1α. We employed a dual-luciferase assay that uses a luciferase (Luc) reporter vector harboring five copies of hypoxia-responsive element (HRE) in the promoter...
January 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/27987431/acriflavine-inhibits-acquired-drug-resistance-by-blocking-the-epithelial-to-mesenchymal-transition-and-the-unfolded-protein-response
#7
Jeroen Dekervel, Ashenafi Bulle, Petra Windmolders, Diether Lambrechts, Eric Van Cutsem, Chris Verslype, Jos van Pelt
Epithelial-to-mesenchymal transition (EMT) is linked to tumor invasion, drug resistance and aggressive disease and this is largely dependent on the cell's microenvironment. Acriflavine (ACF) is an old antibacterial drug recently also suggested as anticancer agent and HIF inhibitor. We wanted to study the effect of acriflavine on EMT in different human cancer models. Pancreatic cancer cells (Panc-1) were exposed to TGF-β1 or cobalt chloride (to mimick severe hypoxia) to induce EMT. For our third model we exposed HepG2 liver cancer cells to sorafenib which resulted in development of acquired drug resistance with strong features of EMT and aggressive behavior...
December 14, 2016: Translational Oncology
https://www.readbyqxmd.com/read/27822416/hydroxyl-hif2-alpha-is-potential-therapeutic-target-for-renal-cell-carcinomas
#8
Takahiro Isono, Tokuhiro Chano, Tetsuya Yoshida, Susumu Kageyama, Akihiro Kawauchi, Masafumi Suzaki, Takeshi Yuasa
Dormant cancer cells are deprivation-resistant, and cause a number of problems for therapeutic approaches for cancers. Renal cell carcinomas (RCCs) include deprivation-resistant cells that are resistant to various treatments. In this study, the specific characteristics of deprivation-resistant cells were transcriptionally identified by next generation sequencing. The hypoxia-inducible factors (HIF) transcription factor network was significantly enhanced in deprivation-resistant RCCs compared to the sensitive RCCs...
2016: American Journal of Cancer Research
https://www.readbyqxmd.com/read/27602954/hypoxia-promotes-glioma-associated-macrophage-infiltration-via-periostin-and-subsequent-m2-polarization-by-upregulating-tgf-beta-and-m-csfr
#9
Xiaofan Guo, Hao Xue, Qianqian Shao, Jian Wang, Xing Guo, Xi Chen, Jinsen Zhang, Shugang Xu, Tong Li, Ping Zhang, Xiao Gao, Wei Qiu, Qinglin Liu, Gang Li
Tumor-associated macrophages (TAMs) are enriched in gliomas and help create a tumor-immunosuppressive microenvironment. A distinct M2-skewed type of macrophages makes up the majority of glioma TAMs, and these cells exhibit pro-tumor functions. Gliomas contain large hypoxic areas, and the presence of a correlation between the density of M2-polarized TAMs and hypoxic areas suggests that hypoxia plays a supportive role during TAM recruitment and induction. Here, we investigated the effects of hypoxia on human macrophage recruitment and M2 polarization...
September 2, 2016: Oncotarget
https://www.readbyqxmd.com/read/27553958/inhibition-of-notch-and-hif-enhances-the-antitumor-effect-of-radiation-in-notch-expressing-lung-cancer
#10
Yasuyuki Ikezawa, Jun Sakakibara-Konishi, Hidenori Mizugaki, Satoshi Oizumi, Masaharu Nishimura
BACKGROUND: The Notch receptor plays an important role in various cell fate decisions during development and in cancer. We have previously reported that Notch3 is upregulated by radiation in non-small cell lung cancer (NSCLC) cell lines and that the Notch pathway inhibitor γ secretase inhibitor GSI (gamma-secretase inhibitor), when combined with radiation therapy, significantly suppressed the growth of lung cancer cells. However, little is known about the mechanism of Notch upregulation induced by radiation...
February 2017: International Journal of Clinical Oncology
https://www.readbyqxmd.com/read/27228567/hypoxia-induces-myeloid-derived-suppressor-cell-recruitment-to-hepatocellular-carcinoma-through-chemokine-c-c-motif-ligand-26
#11
David Kung-Chun Chiu, Iris Ming-Jing Xu, Robin Kit-Ho Lai, Aki Pui-Wah Tse, Larry Lai Wei, Hui-Yu Koh, Lynna Lan Li, Derek Lee, Regina Cheuk-Lam Lo, Chun-Ming Wong, Irene Oi-Lin Ng, Carmen Chak-Lui Wong
UNLABELLED: A population of stromal cells, myeloid-derived suppressor cells (MDSCs), is present in tumors. Though studies have gradually revealed the protumorigenic functions of MDSCs, the molecular mechanisms guiding MDSC recruitment remain largely elusive. Hypoxia, O2 deprivation, is an important factor in the tumor microenvironment of solid cancers, whose growth often exceeds the growth of functional blood vessels. Here, using hepatocellular carcinoma as the cancer model, we show that hypoxia is an important driver of MDSC recruitment...
September 2016: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/27146677/hif-inhibitors-for-ischemic-retinopathies-and-cancers-options-beyond-anti-vegf-therapies
#12
REVIEW
Saima Subhani, Divya Teja Vavilala, Mridul Mukherji
Aberrant activation of the hypoxia inducible factor (HIF) pathway causing overexpression of angiogenic genes, like vascular endothelial growth factor (VEGF), is one of the underlying causes of ocular neovascularization (NV) and metastatic cancer. Consistently, along with surgical interventions, a number of anti-VEGF agents have been approved by FDA for the treatment of ocular neovascular diseases. These anti-VEGF agents, like ranibizumab/lucentis, have revolutionized the treatment in the past decade. However, substantial vision improvement is observed only in a subset of age-related macular degeneration patients receiving ranibizumab...
July 2016: Angiogenesis
https://www.readbyqxmd.com/read/27094790/isoflurane-postconditioning-with-cardiac-support-promotes-recovery-from-early-brain-injury-in-mice-after-severe-subarachnoid-hemorrhage
#13
Tomoko Mutoh, Tatsushi Mutoh, Kazumasu Sasaki, Yukiko Yamamoto, Yoshiharu Tsuru, Hirokazu Tsubone, Tatsuya Ishikawa, Yasuyuki Taki
AIMS: Neurocardiac dysfunction is a life-threatening systemic consequence of subarachnoid hemorrhage (SAH) that contributes to triggering delayed cerebral ischemia (DCI). This study aimed to determine the impact of dobutamine cardiac support during isoflurane postconditioning on post-SAH DCI. MAIN METHODS: Male C57BL/6 mice were subjected to SAH, SAH plus isoflurane postconditioning, or SAH plus isoflurane postconditioning with dobutamine. Severity of SAH was graded from 1 to 4 (mild, 1-2; severe, 3-4) based on T2*-weighted magnetic resonance imaging (MRI)...
May 15, 2016: Life Sciences
https://www.readbyqxmd.com/read/27009878/cisplatin-treatment-increases-stemness-through-upregulation-of-hypoxia-inducible-factors-by-interleukin-6-in-non-small-cell-lung-cancer
#14
Fuquan Zhang, Shanzhou Duan, Ying Tsai, Peter C Keng, Yongbing Chen, Soo Ok Lee, Yuhchyau Chen
Cisplatin-resistant A549 and H157 (A549CisR and H157CisR) non-small cell lung cancer cells show increased stemness of cancer stem cells (CSCs) compared to their parental cells. We investigated whether interleukin-6 (IL-6) signaling contributes to this increased stemness in cisplatin-resistant cells. When A549CisR and H157CisR cells were treated with neutralizing IL-6 antibody, decreased cisplatin resistance was observed, whereas IL-6 treatment of parental cells resulted in increased cisplatin resistance. Expression of the CSC markers was significantly upregulated in IL-6-expressing scramble cells (in vitro) and scramble cell-derived tumor tissues (in vivo) after cisplatin treatment, but not in IL-6 knocked down (IL-6si) (in vitro) cells and in IL-6si cell-derived tumor tissues (in vivo), suggesting the importance of IL-6 signaling in triggering increased stemness during cisplatin resistance development...
June 2016: Cancer Science
https://www.readbyqxmd.com/read/26882240/hypoxia-inducible-factor-hif-inhibitors-a-patent-survey-2011-2015
#15
REVIEW
Hyun Seung Ban, Yoshikazu Uto, Misun Won, Hiroyuki Nakamura
INTRODUCTION: Hypoxia-inducible factor (HIF)-1α regulates the expression of genes involved in angiogenesis, cellular energy metabolism, and cell survival during cancer development. The increased expression of HIF-1α in most solid tumors is associated with poor prognoses and therapeutic outcomes. Therefore, HIF has been recognized as an attractive target for cancer therapy, and many HIF inhibitors have been reported. AREAS COVERED: This patent survey summarizes the information about patented HIF inhibitors over the last 5 years (2011-2015)...
2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/26819450/ndufa4l2-fine-tunes-oxidative-stress-in-hepatocellular-carcinoma
#16
Robin Kit-Ho Lai, Iris Ming-Jing Xu, David Kung-Chun Chiu, Aki Pui-Wah Tse, Larry Lai Wei, Cheuk-Ting Law, Derek Lee, Chun-Ming Wong, Maria Pik Wong, Irene Oi-Lin Ng, Carmen Chak-Lui Wong
PURPOSE: Hepatocellular carcinoma (HCC) lacks effective curative therapy. Hypoxia is commonly found in HCC. Hypoxia elicits a series of protumorigenic responses through hypoxia-inducible factor-1 (HIF1). Better understanding of the metabolic adaptations of HCC cells during hypoxia is essential to the design of new therapeutic regimen. EXPERIMENTAL DESIGN: Expressions of genes involved in the electron transport chain (ETC) in HCC cell lines (20% and 1% O2) and human HCC samples were analyzed by transcriptome sequencing...
June 15, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/26679619/effect-of-hypoxia-inducible-factors-in-normal-and-leukemic-stem-cell-regulation-and-their-potential-therapeutic-impact
#17
REVIEW
Kevin Rouault-Pierre, Ashley Hamilton, Dominique Bonnet
INTRODUCTION: Hypoxia inducible factors (HIF-1α and HIF-2α) are the main mediators of hypoxic responses that operate in both normal and pathological conditions. Recent evidence indicates that HIF-1α and HIF-2α could have overlapping, unique and even sometimes opposing activities in both normal physiology and disease. Despite an increase in our understanding of the different pathways regulated by HIF-1α and HIF-2α, the role played by each factor in HSC maintenance and leukemogenesis is still controversial...
2016: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/26549347/dynamic-regulation-of-stem-cell-specification-and-maintenance-by-hypoxia-inducible-factors
#18
REVIEW
Gregg L Semenza
Stem cells are characterized by the capacity for both self-renewal and generation of all other cell types (pluripotency) or differentiated cells within a particular lineage (multipotency). Stem cells are often localized to hypoxic niches within tissues and hypoxia inducible factors (HIFs) play key roles in the maintenance of pluripotent and multipotent stem cells, as well as cancer stem cells, which are also known as tumor-initiating cells. HIF inhibitors target cancer stem cells and improve the responses to angiogenesis inhibitors and cytotoxic chemotherapy in mouse models of breast cancer...
February 2016: Molecular Aspects of Medicine
https://www.readbyqxmd.com/read/26405042/regulation-of-the-breast-cancer-stem-cell-phenotype-by-hypoxia-inducible-factors
#19
REVIEW
Gregg L Semenza
The small subpopulation of breast cancer cells that possess the capability for self-renewal and formation of secondary tumours that recapitulate the heterogeneity of the primary tumour are referred to as tumour-initiating cells or BCSCs (breast cancer stem cells). The hypoxic tumour microenvironment and chemotherapy actively induce the BCSC phenotype. HIFs (hypoxia-inducible factors) are required and molecular mechanisms by which they promote the BCSC phenotype have recently been delineated. HIF inhibitors block chemotherapy-induced enrichment of BCSCs, suggesting that their use may improve the response to chemotherapy and increase the survival of breast cancer patients...
December 2015: Clinical Science (1979-)
https://www.readbyqxmd.com/read/26310207/chemical-biology-approach-for-the-development-of-hypoxia-inducible-factor-hif-inhibitor-lw6-as-a-potential-anticancer-agent
#20
REVIEW
Ravi Naik, Seunghyeon Han, Kyeong Lee
Intratumoral hypoxia has long been considered to be a driving force in tumor progression as well as a negative prognostic factor in human cancers. The discovery of hypoxia inducible factors (HIFs), which mediate transcriptional responses to changes in oxygen levels, has renewed enthusiasm for drug discovery and the development of targeted therapies in this field. LW6 represents an important new class of small molecules that inhibit HIF-1; it has been major source for diverse lead compounds including HIF-1α inhibitors...
September 2015: Archives of Pharmacal Research
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