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https://www.readbyqxmd.com/read/29339213/nrp-2-in-tumor-lymphangiogenesis-and-lymphatic-metastasis
#1
Jingwen Wang, Yuhong Huang, Jun Zhang, Boyi Xing, Wei Xuan, Honghai Wang, He Huang, Jiayu Yang, Jianwu Tang
Neuropilin-2 (NRP-2) not only functions as a receptor for semaphorins, a family of neural axon guidance factors, but also interacts with VEGFs, a family of vascular endothelial growth factors. As an independent receptor or a co-receptor, NRP-2 binds to ligands VEGF-C/D, activates the VEGF-C/D-NRP-2 signaling axis, and further regulates lymphangiogenesis-associated factors in both lymphatic endothelial cells (LECs) and some tumor cells during tumor progression. Via VEGF-C/D-NRP-2 axis, NRP-2 induces LEC proliferation, reconstruction and lymphangiogenesis and subsequently promotes tumor cell migration, invasion and lymphatic metastasis...
January 12, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29338550/the-role-of-tumor-angiogenesis-as-a-therapeutic-target-in-colorectal-cancer
#2
Francesca Battaglin, Alberto Puccini, Rossana Intini, Marta Schirripa, Alessandra Ferro, Francesca Bergamo, Sara Lonardi, Vittorina Zagonel, Heinz-Josef Lenz, Fotios Loupakis
Angiogenesis is a complex process regulated by several pro- and anti-angiogenic factors, thus the loss of its fine equilibrium plays a key role in colorectal cancer (CRC) development and progression. Therapeutic agents targeting VEGF/VEGFR signaling, the main regulator of this process, proved to be effective across different treatment lines in metastatic CRC (mCRC) and contributed greatly to improve patients' survival in recent years. Areas covered: This review aimed to summarize the actual body of knowledge available on the VEGF pathway in CRC, including currently available anti-angiogenic drugs and treatment challenges, mechanisms of resistance, promising predictive biomarkers and future perspectives...
January 17, 2018: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/29334610/phase-ii-study-of-dovitinib-in-patients-with-castration-resistant-prostate-cancer-kcsg-gu11-05
#3
Yoon Ji Choi, Hye Sook Kim, Se Hoon Park, Bong-Seog Kim, Kyoung Ha Kim, Hyo Jin Lee, Hong Suk Song, Dong-Yeop Shin, Ha Young Lee, Hoon-Gu Kim, Kyung Hee Lee, Jae Lyun Lee, Kyong Hwa Park
Purpose: Fibroblast growth factor (FGF) signals are important in carcinogenesis and progression of prostate cancer. Dovitinib is an oral, pan-class inhibitor of vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor, and fibroblast growth factor receptor (FGFR). We evaluated the efficacy and toxicity of dovitinib in men with metastatic castration resistant prostate cancer (mCRPC). Materials and Methods: This study was a single-arm, phase II, open-label, multicenter trial of dovitinib 500mg/day (5-days-on/2-days-off schedule)...
January 2, 2018: Cancer Research and Treatment: Official Journal of Korean Cancer Association
https://www.readbyqxmd.com/read/29331754/synthesis-and-bioevaluation-and-doking-study-of-1h-pyrrolo-2-3-b-pyridine-derivatives-bearing-aromatic-hydrazone-moiety-as-c-met-inhibitors
#4
Wenhui Wang, Shan Xu, Yongli Duan, Xiaobo Liu, Xiaojing Li, Caolin Wang, Bingbing Zhao, Pengwu Zheng, Wufu Zhu
Two series of aromatic hydrazone derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety (7a-r, 8a-i, 12a-b, 13a-c, 16a-d and 17a-e) were designed, synthesized and evaluated for the IC50 values against four cancer cell lines (A549, HepG2, MCF-7and PC-3). Two selected compounds (7c and 17e) were further evaluated for the activity against c-Met, Flt-3, VEGFR-2 and EGFR kinases. The data indicated that targets compounds were selective for c-Met kinase. And the most promising compound 7c was further studied in terms of dose-dependent, time-dependent and cell apoptosis...
December 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29328399/mir%C3%A2-378a-enhances-the-sensitivity-of-liver-cancer-to-sorafenib-by-targeting-vegfr-pdgfr%C3%AE-and-c%C3%A2-raf
#5
Hongxia Fu, Jicai Zhang, Tongshan Pan, Shuying Ai, Li Tang, Fengqin Wang
Liver cancer is a globally prevalent cancer with poor prognosis. The present study investigated the link between microRNA-378a (miR‑378a) expression and the sensitivity of hepatocellular carcinoma (HCC) and hepatoblastoma (HB) cancers to sorafenib therapy. miR‑378a expression was determined in liver tissue samples from healthy candidates and patients with liver cancer using the reverse transcription‑quantitative polymerase chain reaction. The antitumor effects of miR‑378a alone and in combination with sorafenib were investigated in the HB cell line HepG2 and the HCC cell line SMMC‑7721 with methyl thiazoyl tetrazolium, colony formation, flow cytometry and Transwell migration assays...
January 8, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29323750/design-synthesis-and-molecular-docking-of-novel-indole-scaffold-based-vegfr-2-inhibitors-as-targeted-anticancer-agents
#6
Hanaa M Roaiah, Iman A Y Ghannam, Islam H Ali, Ahmed M El Kerdawy, Mamdouh M Ali, Safinaz E-S Abbas, Sally S El-Nakkady
A series of new indole derivatives 1-18 was synthesized and tested for their cytotoxic activity on a panel of 60 tumor cell lines. Additionally, molecular docking was carried out to study their binding pattern and binding affinity in the VEGFR-2 active site using sorafenib as a reference VEGFR-2 inhibitor. Based on the molecular docking results, compounds 5a, 5b, 6, 7, 14b, 18b, and 18c were selected to be evaluated for their VEGFR-2 inhibitory activity. Compound 18b exhibited a broad-spectrum antiproliferative activity on 47 cell lines, with GI % ranging from 31 to 82...
January 11, 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29322783/micrornas-in-triple-negative-breast-cancer
#7
M Koleckova, M Janikova, Z Kolar
Triple-negative breast cancer (TNBC) is a molecular subtype of breast cancer with one of the worst prognoses. Current treatment is based on chemo- and/or radiotherapy and surgery. New targets, however, offering other therapeutic approaches, have been identified. These involve poly (ADP-ribose) polymerase (PARP), vascular endothelial growth factor receptor (VEGFR), epidermal growth factor receptor (EGFR), androgen receptor (AR), long non-coding RNAs (lncRNAs) and microRNAs (miRs). The latter are non-coding RNAs which control the expression of more than 50% of human genes via regulation of basic cellular processes at post-transcriptional level and dysregulation of miRs is found in many types of tumors...
2018: Neoplasma
https://www.readbyqxmd.com/read/29317165/discovery-of-novel-2-substituted-4-phenoxypyridine-derivatives-as-potential-antitumor-agents
#8
Yongli Duan, Shan Xu, Hehua Xiong, Linxiao Wang, Bingbing Zhao, Ping Wang, Caolin Wang, Yiqing Peng, Shifan Cai, Rong Luo, Pengwu Zheng, Qidong Tang
A series of 2-substituted-4-phenoxypyridine derivatives were designed, synthesized, and evaluated for their antiproliferative activity against 4 cancer cell lines (A549, HT-29, H460, and U87MG) in vitro. Most compounds showed moderate to excellent potency. Nine tyrosine kinases (c-Met, Flt-3, ALK, VEGFR-2, VEGFR-3, PDGFR-α, PDGFR-β, c-Kit, and EGFR) were used to evaluate the inhibitory activities with the most promising analogue 39, which showed the Flt-3/c-Met IC50 values of 2.18/2.61 nM. Structure-activity relationship studies indicated that n-Pr served as R1 group showed a higher preference, and stronger mono-EWGs on the phenyl ring (such as R2 = 4-F) was benefited to the potency...
December 29, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29313954/phase-1-2-trial-of-temsirolimus-and-sorafenib-in-the-treatment-of-patients-with-recurrent-glioblastoma-north-central-cancer-treatment-group-study-alliance-n0572
#9
David Schiff, Kurt A Jaeckle, S Keith Anderson, Evanthia Galanis, Caterina Giannini, Jan C Buckner, Phillip Stella, Patrick J Flynn, Bradley J Erickson, John F Schwerkoske, Vesna Kaluza, Erin Twohy, Janet Dancey, John Wright, Jann N Sarkaria
BACKGROUND: Mitogen-activated protein kinase (MAPK) activation and mammalian target of rapamycin (mTOR)-dependent signaling are hallmarks of glioblastoma. In the current study, the authors conducted a phase 1/2 study of sorafenib (an inhibitor of Raf kinase and vascular endothelial growth factor receptor 2 [VEGFR-2]) and the mTOR inhibitor temsirolimus in patients with recurrent glioblastoma. METHODS: Patients with recurrent glioblastoma who developed disease progression after surgery or radiotherapy plus temozolomide and with ≤2 prior chemotherapy regimens were eligible...
January 3, 2018: Cancer
https://www.readbyqxmd.com/read/29298329/molecular-and-functional-analysis-of-anchorage-independent-treatment-evasive-neuroblastoma-tumorspheres-with-enhanced-malignant-properties-a-possible-explanation-for-radio-therapy-resistance
#10
Tamara J Abou-Antoun, Javad Nazarian, Anthony Ghanem, Stanislav Vukmanovic, Anthony D Sandler
Despite significant advances in cancer treatment and management, more than 60% of patients with neuroblastoma present with very poor prognosis in the form of metastatic and aggressive disease. Solid tumors including neuroblastoma are thought to be heterogeneous with a sub-population of stem-like cells that are treatment-evasive with highly malignant characteristics. We previously identified a phenomenon of reversible adaptive plasticity (RAP) between anchorage dependent (AD) cells and anchorage independent (AI) tumorspheres in neuroblastoma cell cultures...
2018: PloS One
https://www.readbyqxmd.com/read/29297707/first-line-vascular-endothelial-growth-factor-targeted-therapy-in-renal-cell-carcinoma-priming-the-tumor-microenvironment-for-immunotherapy
#11
Nizar Tannir, Hans Hammers, Asim Amin
Despite improved outcomes with systemic vascular endothelial growth factor (VEGF)-targeted agents in patients with advanced renal cell carcinoma (RCC), the majority of patients will eventually develop treatment resistance and disease progression. With the emergence of checkpoint inhibitors as potential treatment approaches, studies suggest that ideally combining or sequencing them with VEGF receptor (VEGFR)-tyrosine kinase inhibitors (TKIs) may provide more effective treatments that reduce or delay disease progression...
January 3, 2018: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/29297179/vascular-endothelial-growth-factor-receptor-inhibition-enhances-copd-picture-in-mice-exposed-to-waterpipe-smoke
#12
Abdallah Alzoubi, Rawan Ghazwi, Karem Alzoubi, Mohammad Alqudah, Khalid Kheirallah, Omar Khabour, Mohammed Allouh
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is marked by destruction of alveolar architecture. Preclinical modeling for COPD is challenging. Chronic cigarette smoke exposure, the reference animal model of COPD, is time-inefficient, while exposure to waterpipe smoke (WPS), a surging smoking modality, was not fully tested for its histopathological pulmonary consequences. Since alveolar damage and pulmonary vascular endothelial dysfunction are integral to COPD pathology, lung histopathological effects of WPS were temporally evaluated, alone or in combination with vascular endothelial growth factor receptor (VEGFR) inhibition in mice...
January 3, 2018: Folia Morphologica (Warsz)
https://www.readbyqxmd.com/read/29295519/design-and-discovery-of-quinazoline-and-thiourea-containing-sorafenib-analogs-as-egfr-and-vegfr-2-dual-tk-inhibitors
#13
Shaofeng Sun, Jingwen Zhang, Ningning Wang, Xiangkai Kong, Fenghua Fu, Hongbo Wang, Jianwen Yao
Both EGFR and VEGFR-2 play a critical role in tumor growth, angiogenesis and metastasis, and targeting EGFR and VEGFR-2 simultaneously represents a promising approach to cancer treatment. In this work, a series of novel quinazoline- and thiourea-containing sorafenib analogs (10a-v) were designed and synthesized as EGFR and VEGFR-2 dual TK inhibitors. Their in vitro enzymatic inhibitory activities against EGFR and VEGFR-2, and antiproliferative activities against HCT-116, MCF-7 and B16 cell lines were evaluated and described...
December 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29291441/synthesis-and-biological-evaluation-of-new-water-soluble-photoactive-chlorin-conjugate-for-targeted-delivery
#14
Vasilii F Otvagin, Alexander V Nyuchev, Natalia S Kuzmina, Ivan D Grishin, Andrei E Gavryushin, Yuliya V Romanenko, Oscar I Koifman, Dmitrii V Belykh, Nina N Peskova, Natalia Yu Shilyagina, Irina V Balalaeva, Alexey Yu Fedorov
A new water-soluble conjugate, consisting of a chlorin-based photosensitizing part, and a 4-arylaminoquinazoline moiety with high potential affinity to an epidermal growth factor receptors (EGFR) and vascular endothelial growth factor receptors (VEGFR), suitable for photodynamic therapy (PDT), was synthesized starting from methylpheophorbide-a in seven steps. An increased accumulation of this compound in A431 cells with high level of EGFR expression, in comparison with CHO and HeLa cells with low EGFR expression was observed...
December 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29290798/ultrasound-molecular-imaging-of-vegfr-2-in-clear-cell-renal-cell-carcinoma-tracks-disease-response-to-antiangiogenic-and-notch-inhibition-therapy
#15
Juan D Rojas, Fanglue Lin, Yun-Chen Chiang, Anna Chytil, Diana C Chong, Victoria L Bautch, W Kimryn Rathmell, Paul A Dayton
Metastatic clear-cell renal cell carcinoma (ccRCC) affects thousands of patients worldwide each year. Antiangiogenic therapy has been shown to have beneficial effects initially, but resistance is eventually developed. Therefore, it is important to accurately track the response of cancer to different therapeutics in order to appropriately adjust the therapy to maximize efficacy. Change in tumor volume is the current gold standard for determining efficacy of treatment. However, functional variations can occur much earlier than measurable volume changes...
2018: Theranostics
https://www.readbyqxmd.com/read/29289530/a-vascular-endothelial-growth-factor-dependent-sprouting-angiogenesis-assay-based-on-an-in-vitro-human-blood-vessel-model-for-the-study-of-anti-angiogenic-drugs
#16
Joris Pauty, Ryo Usuba, Irene Gayi Cheng, Louise Hespel, Haruko Takahashi, Keisuke Kato, Masayoshi Kobayashi, Hiroyuki Nakajima, Eujin Lee, Florian Yger, Fabrice Soncin, Yukiko T Matsunaga
Angiogenesis is the formation of new capillaries from pre-existing blood vessels and participates in proper vasculature development. In pathological conditions such as cancer, abnormal angiogenesis takes place. Angiogenesis is primarily carried out by endothelial cells, the innermost layer of blood vessels. The vascular endothelial growth factor-A (VEGF-A) and its receptor-2 (VEGFR-2) trigger most of the mechanisms activating and regulating angiogenesis, and have been the targets for the development of drugs...
December 20, 2017: EBioMedicine
https://www.readbyqxmd.com/read/29286055/midostaurin-for-the-treatment-of-adult-patients-with-newly-diagnosed-acute-myeloid-leukemia-that-is-flt3-mutation-positive
#17
J S Garcia, M E Percival
Midostaurin is a multitargeted tyrosine kinase inhibitor (TKI) that potently inhibits activated fms-related tyrosine kinase 3 (FLT3) in the nanomolar range and other kinases including platelet-derived growth factor receptors α (PDGFR- α) and β (PDGFR- β), cyclin-dependent kinase, proto-oncogene tyrosine-protein kinase Src, tyrosine-protein kinase Fgr, spleen tyrosine kinase (Syk), KIT proto-oncogene receptor tyrosine kinase and the major vascular endothelial growth factor receptor (VEGFR). Activating mutations in FLT3, which is one of the more common acute myeloid leukemia (AML) mutations, particularly those that result in an FLT3-ITD (internal tandem duplication) mutation, confer poor prognosis and represent a therapeutic target...
October 2017: Drugs of Today
https://www.readbyqxmd.com/read/29285275/apatinib-is-effective-for-treatment-of-advanced-hepatocellular-carcinoma
#18
Yinlong Kong, Lin Sun, Zhenyu Hou, Yongqiang Zhang, Ping Chen, Yunlong Cui, Xiaolin Zhu, Tianqiang Song, Qiang Li, Huikai Li, Ti Zhang, Lunxiu Qin
As treatment options for hepatocellular carcinoma (HCC) are currently limited, we evaluated the efficacy and safety of oral apatinib, a VEGFR-2 inhibitor, on patients with advanced HCC. Twenty-two patients from Tianjin Medical University Cancer Institute and Hospital were enrolled for evaluation. Apatinib was administered at 500 mg/day or 250 mg/day continuously. Clinical endpoints were time to disease progression (TTP), overall survival (OS), and safety. The median TTP of treated patients was 10.4 months (95% CI 3...
December 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/29285210/discovery-and-evaluation-of-triple-inhibitors-of-vegfr-2-tie-2-and-ephb4-as-anti-angiogenic-and-anti-cancer-agents
#19
Lin Zhang, Yuanyuan Shan, Xingyue Ji, Mengyuan Zhu, Chuansheng Li, Ying Sun, Ru Si, Xiaoyan Pan, Jinfeng Wang, Weina Ma, Bingling Dai, Binghe Wang, Jie Zhang
Receptor tyrosine kinases (RTKs), especially VEGFR-2, TIE-2, and EphB4, play a crucial role in both angiogenesis and tumorigenesis. Moreover, complexity and heterogeneity of angiogenesis make it difficult to treat such pathological traits with single-target agents. Herein, we developed two classes of multi-target RTK inhibitors (RTKIs) based on the highly conserved ATP-binding pocket of VEGFR-2/TIE-2/EphB4, using previously reported BPS-7 as a lead compound. These multi-target RTKIs exhibited considerable potential as novel anti-angiogenic and anticancer agents...
December 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/29284120/colorimetric-immunoassays-for-the-screening-and-specificity-evaluation-of-molecules-disturbing-vegfs-vegfrs-interactions
#20
Laura Trapiella-Alfonso, Sylvain Broussy, Wang-Qing Liu, Michel Vidal, Edouard Lecarpentier, Vassilis Tsatsaris, Nathalie Gagey-Eilstein
Angiogenesis and its involved proteins, particularly Vascular Endothelial Growth Factor (VEGF) family and VEGF receptors (VEGFRs), have been considered as a target of therapeutic interest for numerous inflammatory and vascular diseases. Acting on this biological process through interaction with VEGFs or VEGFRs has received considerable attention. Indeed, VEGFs and VEGFRs are currently targeted by drugs such as monoclonal antibodies. The feasibility of a therapeutic strategy based on blocking the VEGF/VEGFR interaction by using ligands "other-than-biologics" is also explored...
December 25, 2017: Analytical Biochemistry
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