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Anti-angiogenesis

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https://www.readbyqxmd.com/read/28810190/design-synthesis-and-biological-evaluation-of-novel-2-methoxyestradiol-analogs-as-dual-selective-estrogen-receptor-modulators-serms-and-antiangiogenic-agents
#1
Kejing Lao, Yejun Wang, Mingqi Chen, Jingjing Zhang, Qidong You, Hua Xiang
2-methoxyestradiol is a novel agent showing both anti-angiogenic and vascular disrupting properties. In this study, a series of 11α-substituted 2-methoxyestradiol analogs have been designed and synthesized targeting dual ERα and microtubulin. Biological evaluation was performed on their anti-proliferative activities against 5 different cell lines. The results indicated that most compounds exhibited good activities, in which compound 24c and 30c showed the best activity with low micromolar IC50 (2.73 μM -7...
August 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28798939/orphan-nuclear-receptor-tr3-nur77-is-a-specific-therapeutic-target-for-hepatic-cancers
#2
Yingling Zeng, Xiaoguang Ye, Degui Liao, Shizhang Huang, Huinan Mao, Dezheng Zhao, Huiyan Zeng
OBJECTIVE: Although great success has been achieved in cancer treatment, current cancer therapies, including anti-tumorigenesis and anti-angiogenesis, still face the problems of insufficient efficacy, resistance and intrinsic refractoriness, in addition to their toxic side effects. There is a demand to identify additional targets that can be blocked to turn off the downstream effects of most, if not all, pathways. Our previous studies suggest that orphan nuclear receptor TR3 (human) / Nur77 (mouse) is such a target...
June 2017: Journal of Clinical & Experimental Oncology
https://www.readbyqxmd.com/read/28795691/evaluation-of-in-vitro-and-in-vivo-activity-of-a-multityrosine-kinase-inhibitor-al3810-against-human-thyroid-cancer
#3
Qin Xie, Hui Chen, Jing Ai, Ying-Lei Gao, Mei-Yu Geng, Jian Ding, Yi Chen
Thyroid cancer is the most common type of endocrine neoplasia. Despite recent breakthroughs in treatment of the disease, the treatment of advanced, progressive thyroid cancers remains challenging with limited therapeutic options available. In this study, we evaluated a novel and orally bioavailable small-molecule multiple tyrosine kinases inhibitor, AL3810, in preclinical models of thyroid cancer in vitro and in vivo. AL3810 (2-5 μmol/L) dose-dependently inhibited the proliferation of human thyroid cancer cell lines TT, SW579 and TPC-1 in vitro with IC50 values ranging from 0...
August 10, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28757066/design-synthesis-and-biological-evaluation-of-lenalidomide-derivatives-as-tumor-angiogenesis-inhibitor
#4
Shengquan Hu, Libin Yuan, Hong Yan, Zhigang Li
Lenalidomide is a type of immunomodulatory agent with anti-tumor activity by mainly expressed in the anti-angiogenesis. In order to enhance the pharmacological activity of Lenalidomide, a series of Lenalidomide derivatives were designed as tumor angiogenesis inhibitors. The potential anti-angiogenesis targets of Lenalidomide derivatives were virtual screened on Auto-Dock 4.0 by using reverse docking method. The six target proteins, such as vascular endothelial growth factor receptor, epidermal growth factor receptor, fibroblast growth factor receptor, BCR-ABL tyrosine kinase, p38 mitogen activated protein kinase and metal protein kinase, were chosen as the targets...
July 19, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28754008/combination-therapy-of-peg-hm-3-and-methotrexate-retards-adjuvant-induced-arthritis
#5
Jingchao Hao, Xiaodong Wu, Sarra Setrerrahmane, Kun Qian, Yueying Hou, Liting Yu, Chenyu Lin, Qianqian Wu, Hanmei Xu
At present, the early phenomenon of inflammatory angiogenesis is rarely studied in Rheumatoid arthritis (RA). Previous research found that PEG-HM-3, an integrin inhibitor, possessed anti-angiogenesis and anti-rheumatic activity. In this study, the advantages of inhibiting angiogenesis and immune cell adhesion and migration, as well as the benefits of anti-arthritis effects, were evaluated using a combination of PEG-HM-3 and methotrexate (MTX). In vitro, spleen cell proliferation and the levels of tumor necrosis factor α (TNF-α) in macrophage supernatant were assessed...
July 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28753317/natural-particulates-inspired-specific-targeted-co-delivery-of-sirna-and-paclitaxel-for-collaborative-antitumor-therapy
#6
Ruoning Wang, Ziqiang Zhao, Yue Han, Shihao Hu, Yaw Opoku-Damoah, Jianping Zhou, Lifang Yin, Yang Ding
The effective combination of drugs promoting anti-angiogenesis and apoptosis effects has proven to be a promising collaborative tumor antidote; and the co-delivery of small interfering RNA (siRNA) and chemotherapy agents within one efficient vehicle has gained more attentions over single regimen administration. Herein, vascular endothelial growth factor specific siRNA (siVEGF) and paclitaxel (PTX) were introduced as therapeutic companions and co-encapsulated into naturally mimic high-density lipoproteins (rHDL/siVEGF-PTX), so that various mechanisms of treatment can occur simultaneously...
July 28, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28740548/modulation-of-salmonella-tumor-colonization-and-intratumoral-anti-angiogenesis-by-triptolide-and-its-mechanism
#7
Jianxiang Chen, Yiting Qiao, Bo Tang, Guo Chen, Xiufeng Liu, Bingya Yang, Jing Wei, Xiangyu Zhang, Xiawei Cheng, Pan Du, Wenhui Jiang, Qingang Hu, Zi-Chun Hua
The weakened tumour colonization of attenuated Salmonella has severely hampered its clinical development. In this study, we investigated whether an anti-inflammation and antiangiogenesis compound triptolide could improve the efficacy of VNP20009, a highly attenuated Salmonella strain, against mice melanoma. By comparing the effects of conventional VNP20009 monotherapy and a combination therapy that uses both triptolide and VNP20009, we found that triptolide significantly improved the tumour colonization of VNP20009 by reducing the number of infiltrated neutrophils in the melanoma, which led to a larger necrotic area in the melanoma...
2017: Theranostics
https://www.readbyqxmd.com/read/28739731/identification-of-novel-proteins-interacting-with-vascular-endothelial-growth-inhibitor-174-in-renal-cell-carcinoma
#8
Qiang Zhao, Duoer Kun, Baoan Hong, Xiaohu Deng, Sheng Guo, Xingxing Tang, Yong Yang, Kan Gong, Qing Li, Lin Ye, Wen G Jiang, Ning Zhang
BACKGROUND/AIM: Vascular endothelial growth inhibitor (VEGI) is a multipotential cytokine that plays a role in regulating immunity, anti-angiogenesis, and inhibiting tumor growth. However, the proteins that interact with it are still unknown. In the present study, we examined the proteins that interact with VEGI174 and their expression in renal cell carcinoma (RCC). MATERIALS AND METHODS: The proteins that interact with VEGI174 were identified using western blot, pull-down assay, and mass spectrometry...
August 2017: Anticancer Research
https://www.readbyqxmd.com/read/28738964/-clinical-research-on-albumin-bound-paclitaxel-based-therapy-in-advanced-lung-cancer
#9
Xu Li, Bin Ai, Ping Zhang, Lin Li, Xiaonan Wu
BACKGROUND: Albumin-bound paclitaxel is a novel paclitaxel formulation formed by the combination of paclitaxel and human serum albumin (HSA) to improve the efficacy of paclitaxel and reduce its adverse reactions. The aim of this retrospective study is to observe the efficacy and safety of albumin-bound paclitaxel-based therapy in the treatment of lung cancer. METHODS: We have enrolled 50 patients with advanced or unresectable retreatment lung cancer who were admitted from November 2011 to December 2014...
July 20, 2017: Zhongguo Fei Ai za Zhi, Chinese Journal of Lung Cancer
https://www.readbyqxmd.com/read/28734166/naturally-occurring-immunomodulators-with-antitumor-activity-an-insight-on-their-mechanisms-of-action
#10
REVIEW
Shimaa Ibrahim Abdelmonym Mohamed, Ibrahim Jantan, Md Areeful Haque
Natural products with immunomodulatory activity are widely used in treatment of many diseases including autoimmune diseases, inflammatory disorders in addition to cancer. They gained a great interest in the last decades as therapeutic agents since they provide inexpensive and less toxic products than the synthetic chemotherapeutic agents. Immunomodulators are the agents that have the ability to boost or suppress the host defense response that can be used as a prophylaxis as well as in combination with other therapeutic modalities...
July 19, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28715647/the-role-of-netrin-1-in-angiogenesis-and-diabetic-retinopathy-a-promising-therapeutic-strategy
#11
Wenyi Wu, Hetian Lei, Junhui Shen, Luosheng Tang
Netrin-1 is an axon guidance cue and is necessary for neural and vascular development. It is involved in regulating axon guidance for attraction or repulsion, and it has a dual function in endothelial tip cell migration during angiogenesis. Netrin-1 has been shown to play an important role in angiogenesis, cancer progression, and inflammatory disease. Here we review the role of netrin-1 in retinal and angiogenesis development and the associated signaling pathways in diabetic retinopathy. The currently available data suggest that netrin-1 is a promising target for the development of anti-angiogenesis drugs...
May 2017: Discovery Medicine
https://www.readbyqxmd.com/read/28712852/osteonecrosis-of-the-jaws-a-review-and-update-in-etiology-and-treatment
#12
Guilherme H Ribeiro, Emanuely S Chrun, Kamile L Dutra, Filipe I Daniel, Liliane J Grando
INTRODUCTION: Osteonecrosis of the jaws can result either from radiation, used in radiotherapy for treatment of malignant tumors, or medications used for bone remodeling and anti-angiogenesis such as bisphosphonates. These conditions can be associated with triggering factors such as infection, trauma and decreased vascularity. The management of patients with osteonecrosis of the jaws requires caution since there is no specific treatment that acts isolated and decidedly. However, different treatment modalities can be employed in an associated manner to control and stabilize lesions...
June 24, 2017: Brazilian Journal of Otorhinolaryngology
https://www.readbyqxmd.com/read/28710312/aspirin-inhibits-cancer-metastasis-and-angiogenesis-via-targeting-heparanase
#13
Xiao-Yang Dai, Juan Yan, Xuhong Fu, Qiuming Pan, Danni Sun, Yuan Xu, Jiang Wang, Litong Nie, Lin-Jiang Tong, Aijun Shen, Mingyue Zheng, Min Huang, Minjia Tan, Hong Liu, Xun Huang, Jian Ding, Meiyu Geng
<br />Recent epidemiological and clinical studies have suggested the benefit of aspirin for cancer patients, which inspired increasing efforts to demonstrate the anti-cancer ability of aspirin and reveal the molecular mechanisms behind. Nevertheless, the anti-cancer activity and related mechanisms of aspirin remain largely unknown. This study aimed to confirm this observation, and more importantly, to investigate the potential target contributed to the anti-cancer of aspirin.<br /><br />Experimental Design:<br /><span style="font-size: 11px;">A homogeneous time resolved fluorescence (HTRF) assay was used to examine the impact of aspirin on heparanase...
July 14, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28700975/astilbin-decreases-proliferation-and-improves-differentiation-in-hacat-keratinocytes
#14
Chunhong Zhang, Qingqing Xu, Xi Tan, Liya Meng, Guo Wei, Ying Liu, Chunmin Zhang
Psoriasis is a common chronic dermatosis characterized by keratinocyte hyperproliferation accompanied by inflammatory reactions. Pathological changes upset the balance between keratinocyte proliferation, differentiation, and death in psoriatic lesions, suggesting that molecules with topical anti-inflammatory, anti-proliferation and anti-angiogenesis abilities may be useful for its treatment. The flavonoid astilbin is the major active component extracted from the rhizome of Smilax glabra, which has been widely used in China to treat inflammatory and autoimmune diseases...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28699667/mantle-cell-lymphoma-2017-update-on-diagnosis-risk-stratification-and-clinical-management
#15
REVIEW
Julie M Vose
DISEASE OVERVIEW: Mantle cell lymphoma (MCL) is a non-Hodgkin lymphoma characterized by involvement of the lymph nodes, spleen, blood and bone marrow with a short remission duration to standard therapies and a median overall survival (OS) of 4-5 years. DIAGNOSIS: Diagnosis is based on lymph node, bone marrow, or tissue morphology of centrocytic lymphocytes, small cell type, or blastoid variant cells. A chromosomal translocation t (11:14) is the molecular hallmark of MCL, resulting in the overexpression of cyclin D1...
August 2017: American Journal of Hematology
https://www.readbyqxmd.com/read/28694103/coe-inhibits-vasculogenic-mimicry-in-hepatocellular-carcinoma-via-suppressing-notch1-signaling
#16
Chen Jue, Zhao Min, Zhang Zhisheng, Cui Lin, Qian Yayun, Wang Xuanyi, Jin Feng, Wang Haibo, Shi Youyang, Hisamitsu Tadashi, Ishikawa Shintaro, Guo Shiyu, Liu Yanqing
ETHNOPHARMACOLOGICAL RELEVANCE: Vasculogenic mimicry (VM) has been suggested to be present in various malignant tumors and associated with tumor nutrition supply and metastasis, leading to poor prognosis of patients. Notch1 has been demonstrated to contribute to VM formation in hepathocellular carcinoma (HCC). Celastrus orbiculatus extract (COE), a mixture of 11 terpenoids isolated from the Chinese Herb Celastrus orbiculatus Vine, has been suggested to be effective in cancer treatment...
July 8, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28691643/rap2b-promotes-angiogenesis-via-pi3k-akt-vegf-signaling-pathway-in-human-renal-cell-carcinoma
#17
Jiehui Di, Keyu Gao, Debao Qu, Jing Yang, Junnian Zheng
Human renal cell carcinoma which is a highly vascular tumor is the leading cause of death from urologic cancers. Angiogenesis has a pivotal role in oncogenesis and in the viability and expansion of renal cell carcinoma. Rap2B, as a small guanosine triphosphate-binding protein of the Ras family, was first discovered in the early 1990s during the screening of a platelet complementary DNA library. Previous studies have shown that Rap2B aberrantly expressed in human carcinogenesis and promoted the development of tumors via multiple signaling pathways...
July 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/28684188/ascorbate-lacks-significant-influence-in-rats-with-bile-duct-ligation-induced-liver-injury
#18
Hsin-Ling Ho, Teh-Ia Huo, Ting Chang, Wen-Shin Lee, I-Fang Hsin, Fa-Yauh Lee, Hui-Chun Huang, Ming-Chih Hou, Shou-Dong Lee
BACKGROUND: Liver inflammation may induce fibrogenesis, cirrhosis and portal hypertension. Liver cirrhosis is characterized by increased intrahepatic resistance and enhanced vasoconstrictive response. The splanchnic vasodilatation, angiogenesis and portosystemic collaterals formation further bring about lethal complications. Ascorbate is a potent antioxidant with anti-inflammation, anti-fibrosis, and anti-angiogenesis effects. However, the relevant influences in chronic liver injury have not been sufficiently explored...
July 3, 2017: Journal of the Chinese Medical Association: JCMA
https://www.readbyqxmd.com/read/28683823/sema3a-drastically-suppresses-tumor-growth-in-oral-cancer-xenograft-model-of-mice
#19
Chao Huang, Yi Wang, Jian-Hua Huang, Weixian Liu
BACKGROUND: Multiple studies suggest anti-angiogenesis to be a promising and rational option in cancer treatment. Interestingly, the axonal sprouting inhibitor semaphorin 3A (Sema3A), a potent suppressor of tumor angiogenesis in various cancer models, is lowly expressed in human oral cancer. Thus, we hypothesized that overexpression of Sema3A in human oral cancer cells may have potential therapeutic effects. METHODS: The LentiSema3A-EGFP was first constructed and transduced to the tongue squamous cell carcinoma cell line SSC-9...
July 6, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28678611/successful-treatment-of-advanced-pancreatic-liposarcoma-with-apatinib-a-case-report-and-literature-review
#20
Tao Han, Yuting Luan, Ying Xu, Xiaodan Yang, Jing Li, Ran Liu, Qing Li, Zhendong Zheng
Pancreatic liposarcoma is a malignant tumor originated from the pancreas mesenchymal tissue and mostly presented in skin, subcutaneous, periosteum, and long bone on both sides. Both conventional chemotherapy and radiotherapy have limited efficacy and poor prognosis for advanced pancreatic liposarcoma. Here, we reported a case of advanced pancreatic liposarcoma and reviewed the literature specific for liposarcoma of the pancreas and discuss the emerging options of treatment. The patient was treated with apatinib and a cross-line rescue therapy combined with paclitaxel after progressive disease...
July 5, 2017: Cancer Biology & Therapy
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