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https://www.readbyqxmd.com/read/28651231/evaluation-of-in-vitro-anticancer-activity-of-1-8-cineole-containing-n-hexane-extract-of-callistemon-citrinus-curtis-skeels-plant-and-its-apoptotic-potential
#1
Sowndarya Sampath, Vidhya Veeramani, Gopal Shankar Krishnakumar, Udhayakumar Sivalingam, Suguna Lakshmi Madurai, Rose Chellan
Plants are the source of a variety of secondary metabolites, which are often used in the anticancer activity. Discovering new anticancer drug from herbal source is more important in both biological and pharmacological activities. Hence, the objective of this study is to identify the anticancer agent in Callistemon citrinus (Curtis) Skeels (CC) for the treatment of cancer. Very recently we have reported an increased antioxidant activity in the ethanolic and methanolic extracts (EE and ME) of CC but significantly reduced activity (rather increased cytotoxicity), in the n-hexane extract (HE)...
June 23, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28650658/a-potent-selective-and-cell-active-protein-arginine-methyltransferase-5-prmt5-inhibitor-developed-by-structure-based-virtual-screening-and-hit-optimization
#2
Ruifeng Mao, Jingwei Shao, Kongkai Zhu, Yuanyuan Zhang, Hong Ding, Chenhua Zhang, Zhe Shi, Hualiang Jiang, De-Qun Sun, Wenhu Duan, Cheng Luo
PRMT5 plays important roles in diverse cellular processes and is upregulated in several human malignancies. Besides, PRMT5 has been validated as anti-cancer target in mantle cell lymphoma. In this study, we found a potent and selective PRMT5 inhibitor by performing structure-based virtual screening and hit optimization. The identified compound 17 (IC50 = 0.33 μM) exhibited a broad selectivity against a panel of other methyltransferases. The direct binding of 17 to PRMT5 was validated by surface plasmon resonance experiments, with a Kd of 0...
June 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28649702/dose-considerations-for-anti-cancer-drugs-in-metastatic-prostate-cancer
#3
REVIEW
Megan Crumbaker, Howard Gurney
Despite a growing number of treatment options, metastatic castrate resistant prostate cancer remains almost universally fatal. Dose individualization ensures patients receive the maximal benefit from each line of treatment potentially leading to improved outcomes, a reduction in quality of life impairment and minimization of premature cessation for avoidable toxicity. Herein, we review drug-specific issues that may be associated with unexpected or unrecognized variations in drug systemic exposure despite the use of protocol doses...
June 26, 2017: Prostate
https://www.readbyqxmd.com/read/28649130/dopamine-d2-receptor-antagonist-sulpiride-enhances-dexamethasone-responses-in-the-treatment-of-drug-resistant-and-metastatic-breast-cancer
#4
Jian Li, Qing-Yu Yao, Jun-Sheng Xue, Li-Jie Wang, Yin Yuan, Xiu-Yun Tian, Hong Su, Si-Yuan Wang, Wen-Jun Chen, Wei Lu, Tian-Yan Zhou
Recent evidence shows that dopamine D2-like receptor (D2DR) antagonists, such as trifluoperazine and thioridazine, are effective for cancer therapy and inhibition of cancer stem-like cells (CSCs). In this study, we investigated the anti-cancer effects of combination therapy of dexamethasone (DEX) and sulpiride (SUL), an atypical antipsychotic, against drug-resistant and metastatic breast cancers and further explored the underlying mechanisms. Oral administration of SUL (25, 100 mg·kg(-1)·d(-1)) alone did not inhibit the tumor growth in human breast cancer MCF-7/Adr xenograft model, but dose-dependently decreased the proportion of CSCs in vitro and in vivo...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28648866/cytokines-in-immunogenic-cell-death-applications-for-cancer-immunotherapy
#5
REVIEW
Anne Showalter, Arati Limaye, Jeremiah L Oyer, Robert Igarashi, Christina Kittipatarin, Alicja J Copik, Annette R Khaled
Despite advances in treatments like chemotherapy and radiotherapy, metastatic cancer remains a leading cause of death for cancer patients. While many chemotherapeutic agents can efficiently eliminate cancer cells, long-term protection against cancer is not achieved and many patients experience cancer recurrence. Mobilizing and stimulating the immune system against tumor cells is one of the most effective ways to protect against cancers that recur and/or metastasize. Activated tumor specific cytotoxic T lymphocytes (CTLs) can seek out and destroy metastatic tumor cells and reduce tumor lesions...
June 22, 2017: Cytokine
https://www.readbyqxmd.com/read/28648521/ratiometric-co-delivery-of-multiple-chemodrugs-in-a-single-nanocarrier
#6
Chao Chen, Ran Tao, Dan Ding, Deling Kong, Aiping Fan, Zheng Wang, Yanjun Zhao
Co-delivery of multiple anti-cancer drugs in a single nanoplatform has shown great promise in enhancing therapeutic efficacy and reducing adverse effects. However, the ratiometric dose control is pivotal, but often challenging in combinational nanomedicine. Here, we report the employment of cyclodextrin-bearing amphiphilic polymer conjugate micelles for ratiometric, non-covalent loading of three hydrophobic model drugs, curcumin (CUR), camptothecin (CPT), and doxorubicin (DOX) in one single nanocarrier. Each drug was physically encapsulated in the cyclodextrin-bearing polymer conjugate via guest-host complexation...
June 22, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28648461/the-structural-requirements-of-histone-deacetylase-inhibitors-saha-analogs-modified-at-the-c5-position-display-dual-hdac6-8-selectivity
#7
Ahmed T Negmeldin, Mary Kay H Pflum
Histone deacetylase (HDAC) proteins have emerged as important targets for anti-cancer drugs, with four small molecules approved for use in the clinic. Suberoylanilide hydroxamic acid (Vorinostat, SAHA) was the first FDA-approved HDAC inhibitor for cancer treatment. However, SAHA inhibits most of the eleven HDAC isoforms. To understand the structural requirements of HDAC inhibitor selectivity and develop isoform selective HDAC inhibitors, SAHA analogs modified in the linker at the C5 position were synthesized and tested for potency and selectivity...
June 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28648146/emerging-roles-of-protein-disulfide-isomerase-in-cancer
#8
Eunyoug Lee, Do Hee Lee
Protein disulfide isomerase (PDI) family is a group of multifunctional endoplasmic reticulum (ER) enzymes mediating the formation of disulfide bonds, catalyzing the cysteine-based redox reactions and assisting the quality control of the client proteins. Recent structural and functional studies have demonstrated that PDI members not only play an essential role in the proteostasis in the ER but also exert diverse effects in numerous human diseases including cancer and neurodegenerative diseases. Increasing evidence suggests that PDI is actively involved in the proliferation, survival, and metastasis of several types of cancer cells...
June 26, 2017: BMB Reports
https://www.readbyqxmd.com/read/28648052/anti-cancer-therapeutic-alginate-based-tissue-sealants-for-lung-repair
#9
Spencer Lincoln Fenn, Patrick N Charron, Rachael Ann Oldinski
Injury to the connective tissue that lines the lung, the pleura, or to the lung itself can occur from many causes including trauma or surgery, as well as lung diseases or cancers. To address current limitations for patching lung injuries, to stop air or fluid leaks, an adherent hydrogel sealant patch system was developed, based on methacrylated alginate (AMA) and AMA di-aldehyde (AMA-DA) blends, which is capable of sealing damaged tissues and sustaining physiological pressures. Methacrylation of alginate hydroxyl groups rendered the polysaccharide capable of photo-crosslinking when mixed with an eosin Y-based photo-initiator system, and exposed to visible green light...
June 24, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28647884/fluoxetine-induces-apoptosis-through-endoplasmic-reticulum-stress-via-mitogen-activated-protein-kinase-activation-and-histone-hyperacetylation-in-sk-n-be-2-m17-human-neuroblastoma-cells
#10
Ji Hyun Choi, Yeon Ju Jeong, Ah-Ran Yu, Kyung-Sik Yoon, Wonchae Choe, Joohun Ha, Sung Soo Kim, Eui-Ju Yeo, Insug Kang
Fluoxetine (FLX) is an antidepressant drug that belongs to the class of selective serotonin reuptake inhibitors. FLX is known to induce apoptosis in multiple types of cancer cells. In this study, the molecular mechanisms underlying the anti-cancer effects of FLX were investigated in SK-N-BE(2)-M17 human neuroblastoma cells. FLX induced apoptotic cell death, activation of caspase-4, -9, and -3, and expression of endoplasmic reticulum (ER) stress-associated proteins, including C/EBP homologous protein (CHOP)...
June 24, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28647529/-linking-secondary-metabolites-to-biosynthesis-genes-in-the-fungal-endophyte-cyanodermella-asteris-the-anti-cancer-bisanthraquinone-skyrin
#11
Linda Jahn, Thomas Schafhauser, Daniel Wibberg, Christian Rückert, Anika Winkler, Andreas Kulik, Tilmann Weber, Liane Flor, Karl-Heinz van Pée, Jörn Kalinowski, Jutta Ludwig-Müllera, Wolfgang Wohlleben
Fungal aromatic polyketides display a very diverse and widespread group of natural products. Due to their excellent light absorption properties and widely studied biological activities, they offer numerous application for food, textile and pharmaceutical industry. The biosynthetic pathways of fungal aromatic polyketides usually involve a set of successive enzymes, in which a non-reductive polyketide synthases iteratively catalyzes the essential assembly of simple building blocks into (often polycyclic) aromatic compounds...
June 21, 2017: Journal of Biotechnology
https://www.readbyqxmd.com/read/28647509/a-review-of-acalypha-indica-l-euphorbiaceae-as-traditional-medicinal-plant-and-its-therapeutic-potential
#12
REVIEW
Nor Syahiran Zahidin, Syafiqah Saidin, Razauden Mohamed Zulkifli, Ida Idayu Muhamad, Harisun Ya'akob, Hadi Nur
ETHNOPHARMACOLOGICAL RELEVANCE: Acalypha indica is an herbal plant that grows in wet, temperate and tropical region, primarily along the earth's equator line. This plant is considered by most people as a weed and can easily be found in these regions. Although this plant is a weed, Acalypha indica has been acknowledged by local people as a useful source of medicine for several therapeutic treatments. They consume parts of the plant for many therapeutics purposes such as anthelmintic, anti-ulcer, bronchitis, asthma, wound healing, anti-bacterial and other applications...
June 21, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28647489/a-high-throughput-assay-to-identify-substrate-selective-inhibitors-of-the-erk-protein-kinases
#13
Chad J Miller, Yagmur Muftuoglu, Benjamin E Turk
Extracellular signal-regulated kinases 1 and 2 (ERK1/2) phosphorylate a variety of substrates important for survival and proliferation, and their activity is frequently deregulated in tumors. ERK pathway inhibitors have shown clinical efficacy as anti-cancer drugs, but most patients eventually relapse due to reactivation of the pathway. One factor limiting the efficacy of current therapeutics is the difficulty in reaching clinically effective inhibition of the ERK pathway in the absence of on-target toxicities...
June 21, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28646535/targeting-stat3-by-ho3867-induces-apoptosis-in-ovarian-clear-cell-carcinoma
#14
Kristin Bixel, Uksha Saini, Hemant Kumar Bid, John Fowler, Maria Riley, Ross Wanner, Kalpana Deepa Priya Dorayappan, Sneha Rajendran, Ikuo Konishi, Noriomi Matsumura, David E Cohn, Karuppaiyah Selvendiran
Advanced ovarian clear cell carcinoma (OCCC) carries a very poor prognosis in large part secondary to the extremely high rate of resistance to standard platinum and taxane chemotherapy. STAT3 expression and activation has been shown to regulate tumor progression in various human cancers, though has not been well studied in OCCC. Preliminary work in our lab has demonstrated constitutive activation of STAT3 (pSTAT3Tyr705 or pSTAT3727) in OCCC cell lines as well as human OCCC tumor tissue samples. Significantly, pSTAT3 is expressed in the absence of other forms of activated STAT (pSTAT1, 2, 6)...
June 24, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28645831/synthesis-and-biological-evaluation-of-jl-a7-derivatives-as-potent-abcb1-inhibitors
#15
Miaobo Pan, Jian Cui, Lei Jiao, Hesham Ghaleb, Chen Liao, Jiaqi Zhou, Mutta Kairuki, Haiyan Lin, Wenlong Huang, Hai Qian
Cancer chemotherapy failure is often due to the overexpression of ATP-binding cassette (ABC) transporters (particularly ABCB1), resulting in a variety of structurally and pharmacologically unrelated drugs efflux. The multidrug resistance (MDR) phenomenon could be reversed by ABCB1 inhibitors. Now, JL-A7 as the lead compound based on a triazol-N-ethyl-tetrahydroisoquinoline scaffold, 18 compounds were designed and synthesized. Substitution in para positions yielded high activities toward ABCB1. Moreover, compound 5 could effectively block the drug efflux function of ABCB1 and increase the accumulation of anti-cancer drugs to achieve effective treatment concentration in MDR cells...
June 13, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28645267/a-rapid-and-quantitative-method-to-detect-human-circulating-tumor-cells-in-a-preclinical-animal-model
#16
Shih-Hsin Tu, Yi-Chen Hsieh, Li-Chi Huang, Chun-Yu Lin, Kai-Wen Hsu, Wen-Shyang Hsieh, Wei-Ming Chi, Chia-Hwa Lee
BACKGROUND: As cancer metastasis is the deadliest aspect of cancer, causing 90% of human deaths, evaluating the molecular mechanisms underlying this process is the major interest to those in the drug development field. Both therapeutic target identification and proof-of-concept experimentation in anti-cancer drug development require appropriate animal models, such as xenograft tumor transplantation in transgenic and knockout mice. In the progression of cancer metastasis, circulating tumor cells (CTCs) are the most critical factor in determining the prognosis of cancer patients...
June 23, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28644837/real-world-first-line-treatment-and-overall-survival-in-non-small-cell-lung-cancer-without-known-egfr-mutations-or-alk-rearrangements-in-us-community-oncology-setting
#17
Amy P Abernethy, Ashwini Arunachalam, Thomas Burke, Caroline McKay, Xiting Cao, Rachael Sorg, David P Carbone
PURPOSE: To establish a baseline for care and overall survival (OS) based upon contemporary first-line treatments prescribed in the era before the introduction of immune checkpoint inhibitors, for people with metastatic non-small cell lung cancer (NSCLC) without common actionable mutations. METHODS: Using a nationally representative electronic health record data from the Flatiron dataset which included 162 practices from different regions in US, we identified patients (≥18 years old) newly diagnosed with stage IV NSCLC initiating first-line anticancer therapy (November 2012- January 2015, with follow-up through July 2015)...
2017: PloS One
https://www.readbyqxmd.com/read/28644429/cytotoxic-and-genotoxic-studies-of-essential-oil-from-rosa-damascene-mill-kashan-iran
#18
Mohammad Shokrzadeh, Emran Habibi, Mona Modanloo
Aim Rosa damascene Mill. belongs to the family of Roseaceae and its essential oil is produced in large amounts in Iran. The wide application of rose oil has raised questions about potential adverse health effects. We have investigated cytotoxic activity and genotoxic effects of Rosa oil from Kashan, Iran. Methods The cytotoxic effect and IC50 of the essential oil on the cell lines was studied followed by MTT assay. In this assay mitochondrial oxidoreductase enzymes with reducing the tetrazolium dye MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) reflect the number of viable cells...
August 1, 2017: Medicinski Glasnik
https://www.readbyqxmd.com/read/28644051/brief-overview-of-nanoparticulate-therapy-in-cancer
#19
Rajesh R Wakaskar
Nanoparticles govern an all-important role, in this day and age, in determining the tissue distribution of either hydrophobic or hydrophilic anti-cancer drugs by encapsulating them or by covalent attachment. The whole purpose is to systematically improve upon the existing anti-tumor efficacy of these drugs. Selective delivery of these chemotherapeutic agents to the compromised or diseased tissue is the key to avoid any potential toxicity problems. Certain types of nanoparticles, through various mechanisms such as active targeting or reversing multi-drug resistance, display immense potential in adding to the existing anti-tumor efficacy profile...
June 23, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28643475/tailoring-of-physicochemical-properties-of-nanocarriers-for-effective-anti-cancer-applications
#20
REVIEW
Swaroop Chakraborty, Geethanjali S Dhakshinamurthy, Superb K Misra
Nanotechnology has emerged strongly as a viable option to overcome the challenge of early diagnosis and effective drug delivery, for cancer treatment. Emerging research articles have expounded the advantages of using a specific type of nanomaterial-based system called as "nanocarriers," for anti-cancer therapy. The nanocarrier system is used as a transport unit for targeted drug delivery of the therapeutic drug moiety. In order for the nanocarriers to be effective for anticancer therapy, their physicochemical parameter needs to be tuned so that bio-functionalisation can be achieved to a) allow drugs being attached to the substrate and for their controlled release, b) ensure the stability of the nanocarrier up to the point of delivery, and c) clearance of the nanocarrier after the delivery...
June 23, 2017: Journal of Biomedical Materials Research. Part A
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