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https://www.readbyqxmd.com/read/30517905/rational-design-of-polymer-lipid-nanoparticles-for-docetaxel-delivery
#1
Juan M R Albano, Lígia Nunes de Morais Ribeiro, Verônica Muniz Couto, Mariana Barbosa Messias, Gustavo Henrique Rodrigues da Silva, Márcia Cristina Breitkreitz, Eneida de Paula, Monica Pickholz
In this work, a stable nanocarrier for the anti-cancer drug docetaxel was rational designed. The nanocarrier was developed based on the solid lipid nanoparticle preparation process aiming to minimize the total amount of excipients used in the final formulations. A particular interest was put on the effects of the polymers in the final composition. In this direction, two poloxoamers -Pluronic F127 and F68- were selected. Some poloxamers are well known to be inhibitors of the P-glycoprotein efflux pump. Additionally, their poly-ethylene-oxide blocks can help them to escape the immune system, making the poloxamers appealing to be present in a nanoparticle designed for the treatment of cancer...
November 28, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/30517668/sox2-in-cancer-stemness-tumor-malignancy-and-therapeutic-potentials
#2
Mahfuz Al Mamun, Kaiissar Mannoor, Jun Cao, Firdausi Qadri, Xiaoyuan Song
Cancer stem cells (CSCs), a minor subpopulation of tumor bulks with self-renewal and seeding capacity to generate new tumors, posit a significant challenge to develop effective and long-lasting anti-cancer therapies. The emergence of drug resistance appears upon failure of chemo-/radiation therapy to eradicate the CSCs, thereby leading to CSC-mediated clinical relapse. Accumulating evidence suggests that transcription factor SOX2, a master regulator of embryonic and induced pluripotent stem cells, drives cancer stemness, fuels tumor initiation, and contributes to tumor aggressiveness through major drug resistance mechanisms like epithelial-to-mesenchymal transition (EMT), ATP-binding cassette (ABC) drug transporters, anti-apoptotic and/or pro-survival signaling, lineage plasticity, and evasion of immune surveillance...
December 5, 2018: Journal of Molecular Cell Biology
https://www.readbyqxmd.com/read/30516854/cocktail-strategy-based-on-spatio-temporally-controlled-nano-device-improves-therapy-of-breast-cancer
#3
Tianqun Lang, Yiran Liu, Zhong Zheng, Wei Ran, Yihui Zhai, Qi Yin, Pengcheng Zhang, Yaping Li
Metastatic breast cancer may be resistant to chemo-immunotherapy due to the existence of cancer stem cells (CSC). And the control of particle size and drug release of a drug carrier for multidrug combination is a key issue influencing therapy effect. Here, a cocktail strategy is reported, in which chemotherapy against both bulk tumor cells and CSC and immune checkpoint blockade therapy are intergraded into one drug delivery system. The chemotherapeutic agent paclitaxel (PTX), the anti-CSC agent thioridazine (THZ), and the PD-1/PD-L1 inhibitor HY19991 (HY) are all incorporated into an enzyme/pH dual-sensitive nanoparticle with a micelle-liposome double-layer structure...
December 5, 2018: Advanced Materials
https://www.readbyqxmd.com/read/30516115/biological-efficacy-of-carvacrol-analogues
#4
Z Mbese, B A Aderibigbe
BACKGROUND: Carvacrol is the major constituent of essential oils derived from plants. It exhibits antimicrobial, antioxidant, anticancer, anti-inflammatory, and anticholinesterase activity. The analogues of carvacrol can be prepared via selected synthetic routes, resulting in potent compounds. OBJECTIVE: Modifying carvacrol by the introduction of selected functionalities has the potential to enhance the biological activity of carvacrol. The functionalities on carvacrol such as the hydroxyl group, benzene ring and alkyl groups can be modified or used for hybridization with important pharmaceutical scaffolds...
December 4, 2018: Recent Patents on Anti-infective Drug Discovery
https://www.readbyqxmd.com/read/30515835/pharmacological-explorations-of-eco-friendly-amide-substituted-z-%C3%AE-enaminones-as-anti-breast-cancer-drugs
#5
Palaniraja Subramamiam, Chandrasekaran Ramasubbu, Selvaraj Athiramu, Sivakumar Arumugam, Manikandan Alagumuthu
Amide substituted (Z)-β-enaminones were synthesized by green chemistry and stereo-specific synthetic pathway as novel phosphoinositide 3-kinase (PI3K) inhibitors and breast cancer drugs. PI3K inhibition was measured by competitive ELISA. A panel of cancer cell lines including MCF-7 (breast cancer), G-361 (skin cancer), and HCT 116 (colon cancer) were used to assess the anticancer potentials. In the PI3K assay, 2c and 2f were indolent for the proposed inhibitory action, which was recognized from the obtained IC50 (>1...
December 5, 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/30515806/challenges-facing-antiangiogenesis-therapy-the-significant-role-of-hypoxia-inducible-factor-and-met-in-development-of-resistance-to-anti-vascular-endothelial-growth-factor-targeted-therapies
#6
REVIEW
Ali Mahdi, Behrad Darvishi, Keivan Majidzadeh-A, Malihe Salehi, Leila Farahmand
It is now fully recognized that along with multiple physiological functions, angiogenesis is also involved in the fundamental process and pathobiology of several disorders including cancer. Recent studies have fully established the role of angiogenesis in cancer progression as well as invasion and metastasis. Consequently, many therapeutic agents such as monoclonal antibodies targeting angiogenesis pathway have been introduced in clinic with the hope for improving the outcomes of cancer therapy. Bevacizumab (Avastin®) was the first anti-vascular endothelial growth factor (VEGF) targeting monoclonal antibody developed with this purpose and soon received its accelerated US Food and Drug Administration (FDA) approval for treatment of patients with metastatic breast cancer in 2008...
December 4, 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/30515357/model-based-in-silico-analysis-of-the-pi3k-akt-pathway-the-elucidation-of-cross-talk-between-diabetes-and-breast-cancer
#7
Sammia Rehman, Ayesha Obaid, Anam Naz, Amjad Ali, Shahzina Kanwal, Jamil Ahmad
Background: A positive association between diabetes and breast cancer has been identified by various epidemiological and clinical studies. However, the possible molecular interactions between the two heterogeneous diseases have not been fully determined yet. There are several underlying mechanisms which may increase the risk of breast cancer in diabetic patients. Introduction: In this study, we focused on the role of O-GlcNAc transferase (OGT) enzyme in the regulation of phosphatidylinositol-3 kinase (PI3K) pathway through activation/deactivation of Akt protein...
2018: PeerJ
https://www.readbyqxmd.com/read/30514779/anti-ctla-4-immunotherapy-does-not-deplete-foxp3-regulatory-t-cells-tregs-in-human-cancers-letter
#8
Roberto Ferrara, Sandrine Susini, Aurélien Marabelle
The potential role of anti-CTLA-4 antibodies in depleting intratumoral T-regulatory cells (iTregs) is still a matter of debate. In fact, if on one hand a recent study showed that ipilimumab and tremelimumab do not reduce Tregs in bladder, prostate and melanoma human cancers, on the other hand several other reports described opposite results. Basically, the depletion of iTregs may concern only CTLA-4+ iTregs and the evaluation of this population by immunohistochemistry may be challenging because CTLA-4 is highly express in the cytoplasm rather than on the membrane of these cells...
December 4, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/30514402/preclinical-pharmacokinetic-evaluation-to-facilitate-repurposing-of-tyrosine-kinase-inhibitors-nilotinib-and-imatinib-as-antiviral-agents
#9
Hari Krishna Ananthula, Scott Parker, Erin Touchette, R Mark Buller, Gopi Patel, Daniel Kalman, Johanna S Salzer, Nadia Gallardo-Romero, Victoria Olson, Inger K Damon, Tessa Moir-Savitz, Larry Sallans, Milton H Werner, Catherine M Sherwin, Pankaj B Desai
BACKGROUND: Several tyrosine kinase inhibitors (TKIs) developed as anti-cancer drugs, also have anti-viral activity due to their ability to disrupt productive replication and dissemination in infected cells. Consequently, such drugs are attractive candidates for "repurposing" as anti-viral agents. However, clinical evaluation of therapeutics against infectious agents associated with high mortality, but low or infrequent incidence, is often unfeasible. The United States Food and Drug Administration formulated the "Animal Rule" to facilitate use of validated animal models for conducting anti-viral efficacy studies...
December 4, 2018: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/30514066/therapeutic-targeting-of-the-dna-damage-response-using-an-atr-inhibitor-in-biliary-tract-cancer
#10
Ah-Rong Nam, Mei Hua Jin, Ji Eun Park, Ju-Hee Bang, Do-Youn Oh, Yung-Jue Bang
Purpose: The DNA damage response (DDR) is a multi-complex network of signaling pathways involved in DNA damage repair, cell cycle checkpoints, and apoptosis. In the case of biliary tract cancer (BTC), the strategy of DDR targeting has not been evaluated, even though many patients have DNA repair pathway alterations. The purpose of this study was to test the DDR-targeting strategy in BTC using an ataxia-telangiectasia and Rad3-related (ATR) inhibitor. Materials and Methods: A total of nine human BTC cell lines were used for evaluating anti-tumor effect of AZD6738 (ATR inhibitor) alone or combination with cytotoxic chemotherapeutic agents through MTT Assay, colony-forming assays, cell cycle analyses, and comet assays...
December 3, 2018: Cancer Research and Treatment: Official Journal of Korean Cancer Association
https://www.readbyqxmd.com/read/30513929/the-healing-promoting-properties-of-selected-cyclitols-a-review
#11
REVIEW
Agnieszka Owczarczyk-Saczonek, Lesław Bernard Lahuta, Magdalena Ligor, Waldemar Placek, Ryszard Józef Górecki, Bogusław Buszewski
INTRODUCTION: Myo -inositol and its derivatives cyclitols play an important role in the processes of cell regulation, signal transduction, osmoregulation, and ion channel physiology, and are a component of the cell membrane. Free cyclitols present in food or released during the degradation of galactosyl cyclitols by bacteria (in digestive tract) show some physiological benefits. AIM: The aim of this paper is to present and analyze the documented data about curative and healing properties of cyclitols...
December 3, 2018: Nutrients
https://www.readbyqxmd.com/read/30513611/a-soft-coral-derived-compound-11-dehydrosinulariolide-induces-g2-m-cell-cycle-arrest-and-apoptosis-in-small-cell-lung-cancer
#12
Yu-Chao Lin, Jui-Hsin Su, Shih-Chao Lin, Chia-Che Chang, Te-Chun Hsia, Yu-Tang Tung, Chi-Chien Lin
11-Dehydrosinulariolide, an active compound that is isolated from the cultured soft coral Sinularia flexibilis , has been suggested to show anti-tumor biological characteristics according to previous studies. However, its potential effect on small cell lung cancer (SCLC) remains unknown. The present study investigates the underlying mechanism for the treatment of SCLC in vitro and in vivo. Cell viability was examined using the methyl-thiazol-diphenyl-tetrazolium (MTT) assay. Flow cytometry was applied to evaluate cell cycle distribution and apoptosis...
November 30, 2018: Marine Drugs
https://www.readbyqxmd.com/read/30513596/propranolol-promotes-glucose-dependence-and-synergizes-with-dichloroacetate-for-anti-cancer-activity-in-hnscc
#13
Christopher T Lucido, W Keith Miskimins, Paola D Vermeer
Tumor cell metabolism differs from that of normal cells, conferring tumors with metabolic advantages but affording opportunities for therapeutic intervention. Accordingly, metabolism-targeting therapies have shown promise. However, drugs targeting singular metabolic pathways display limited efficacy, in part due to the tumor's ability to compensate by using other metabolic pathways to meet energy and growth demands. Thus, it is critical to identify novel combinations of metabolism-targeting drugs to improve therapeutic efficacy in the face of compensatory cellular response mechanisms...
November 30, 2018: Cancers
https://www.readbyqxmd.com/read/30512923/oxygen-production-of-modified-core-shell-cuo-zro2-nanocomposites-by-microwave-radiation-to-alleviate-cancer-hypoxia-for-enhanced-chemo-microwave-thermal-therapy
#14
Zengzhen Chen, Meng Niu, Gen Chen, Qiong Wu, Longfei Tan, Changhui Fu, Xiangling Ren, Hongshan Zhong, Ke Xu, Xianwei Meng
There are acknowledged risks of metastasis of cancer cells and obstructing cancer treatment from hypoxia. In this work, we design a multifunctional nanocomposite for treating hypoxia based on the oxygen release capability of CuO triggered by microwave (MW). Core-shell CuO@ZrO2 nanocomposites are prepared by confining CuO nanoparticles within the cavities of mesoporous ZrO2 hollow nanospheres. The 1-butyl-3-methylimidazolium hexafluorophosphate (IL) is loaded to the CuO@ZrO2 nanocomposites for improving microwave thermal therapy (MWTT)...
December 4, 2018: ACS Nano
https://www.readbyqxmd.com/read/30510774/lipid-accumulation-facilitates-mitotic-slippage-induced-adaptation-to-anti-mitotic-drug-treatment
#15
Alex Wong, Sixun Chen, Lay Kien Yang, Yoganathan Kanagasundaram, Karen Crasta
Aberrant lipid accumulation is a hallmark of cancer known to contribute to its aggressiveness and malignancy. Emerging studies have demonstrated context-dependent changes in lipid metabolism during chemotherapy. However, there is little known regarding the mechanisms linking lipid metabolism to chemotherapy-induced cell fates. Here, we describe lipid accumulation in cells following antimitotic drug treatment. Cells arrested in mitosis, as well as cells that escaped mitotic arrest and underwent mitotic slippage, showed elevated cytoplasmic lipid droplets...
2018: Cell Death Discovery
https://www.readbyqxmd.com/read/30510417/a-tf-modified-tripterine-loaded-coix-seed-oil-microemulsion-enhances-anti-cervical-cancer-treatment
#16
Yunyan Chen, Ding Qu, Rongping Fu, Mengfei Guo, Yue Qin, Jian Guo, Yan Chen
Purpose: A transferrin-modified microemulsion carrying coix seed oil and tripterine (Tf-CT-MEs) was developed for improved tumor-specific accumulation and penetration to enhance cervical cancer treatment. Materials and methods: Tripterine-loaded coix seed oil microemulsion (CT-MEs) was prepared through one-step emulsion method. The morphology, size, and zeta potential of CT-MEs and Tf-CT-MEs were examined by transmission electron microscopy and dynamic light scattering...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/30509398/a-new-screening-method-for-atp-independent-kinase-inhibitors-identifies-repurposed-anti-cancer-drugs
#17
Michael Timaner, Yuval Shaked
No abstract text is available yet for this article.
November 2018: EBioMedicine
https://www.readbyqxmd.com/read/30508853/-systemic-treatment-of-early-and-metastatic-breast-cancer
#18
Tanja Fehm, Volkmar Müller
Within the last years significant improvements have been achieved in early and metastatic breast cancer treatment by innovative targeted therapies and new drug combinations. GnRH-analogues have been confirmed as an important part of endocrine treatment in premenopausal patients. Endocrine based strategies including CDK-4/6-Inhibitors substantially improve progression-free survival in metastatic patients. For patients with HER2-positive disease the addition of Pertuzumab to Trastuzumab in combination with chemotherapy has achieved a significant improvement in anti-HER2 therapy in early as well as metastatic breast cancer...
December 2018: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/30508182/mutant-p53-in-cancer-therapy-the-barrier-or-the-path
#19
Xiang Zhou, Qian Hao, Hua Lu
Since wild-type p53 is central for maintaining genomic stability and preventing oncogenesis, its coding gene TP53 is highly mutated in ~50% of human cancers, and its activity is almost abrogated in the rest of cancers. Approximately 80% of p53 mutations are single point mutations with several hotspot mutations. Besides loss of function and dominant-negative effect on the wild-type p53 activity, the hotspot mutant p53s also acquire new oncogenic functions, so-called 'gain-of-functions' (GOF). Because the GOF of mutant p53s is highly associated with late stage malignance and drug resistance, these p53 mutants have become hot targets for developing novel cancer therapies...
December 3, 2018: Journal of Molecular Cell Biology
https://www.readbyqxmd.com/read/30507322/sacituzumab-for-the-treatment-of-triple-negative-breast-cancer-is-this-the-poster-child-of-future-therapy
#20
Mark L Zangardi, Laura M Spring, Aiko Nagayama, Aditya Bardia
Triple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer that disproportionately impacts younger women and is associated with a poor prognosis. Systemic treatment options for metastatic TNBC (mTNBC) are limited to successive lines of cytotoxic chemotherapy agents with low response rates. Trop-2 has been identified as a potential target in epithelial cancers such as TNBC; this has encouraged the development of sacituzumab govitecan (IMMU-132), an anti-Trop-2 antibody-drug conjugate (ADC)...
December 3, 2018: Expert Opinion on Investigational Drugs
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