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Current Cancer Drug Targets

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https://www.readbyqxmd.com/read/27875952/in-vitro-sensitivity-profiling-of-neuroblastoma-cells-against-a-comprehensive-small-molecule-kinase-inhibitor-library-to-identify-agents-for-future-therapeutic-studies
#1
Anjali Singh, Vanessa Meier-Stephenson, Aarthi Jayanthan, Aru Narendran
Solid tumors represent one of the most widespread causes of death in children across the world. Neuroblastoma (NB) constitutes about 8% of all childhood tumors, yet accounts for more than 15% of death, with an unacceptable overall survival rate. Despite the current multimodal therapeutic approaches involving surgery, radiation, chemotherapy with myeloablative therapy and hematopoietic stem cell rescue, there is growing realization of the limitations of conventional agents to improve the outcome in high risk metastatic disease...
November 22, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27903215/identification-of-novel-agents-for-the-treatment-of-brain-metastases-of-breast-cancer
#2
Vinay Kumar Venishetty, Werner J Geldenhuys, Tori B Terell-Hall, Jessica I G Griffith, Gregory R Sondag, Fayez F Safadi, Paul R Lockman
BACKGROUND: Brain cancer from metastasized breast cancer has a high mortality rate in women. The treatment of lesions is hampered in large part by the blood-brain barrier (BBB), which prevents adequate distribution of anti-cancer compounds to brain metastases. METHOD: In this study we used a novel screening method to identify candidate molecules that are well-suited to utilizing the BBB choline transporter for distribution into the brain parenchyma. RESULTS: From our screen we identified two compounds, Ch-1 and Ch-2 that were able to reduce the brain tumor burden in a murine mouse model of brain metastasis of breast cancer...
November 21, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27903214/chemotherapy-and-cardiotoxicity-in-hematologic-malignancies-a-review
#3
Antonio Stellitano, Roberta Fedele, Santina Barillà, Antonino Iaria, Carmelo Massimiliano Rao, Massimo Martino
Antineoplastic agents affect the cardiovascular system, and the incidence of cardiotoxicity is continuously growing in patients with hematologic malignancies and treated with antineoplastic therapy. Cardio-oncology is a quite young discipline, designed for diagnosis, prevention and treatment of cardiovascular complications of anticancer agents. Nowadays, with the current treatments and an accurate pharmacological control of comorbidities present at the time of the oncological diagnosis, early clinical events are infrequent, and it seems indeed that cardiotoxicity could emerge as time and years go by, after therapies completion...
November 21, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27834128/studies-on-non-synonymous-polymorphisms-altering-human-dna-topoisomerase-ii-alpha-interaction-with-amsacrine-and-mitoxantrone-an-in-silico-approach
#4
Farzaneh Mohamadi Farsani, Mohamad Reza Ganjalikhany, Sadeq Vallian
DNA topoisomerase II-α (Top2-α), an essential enzyme for the management of DNA during replication, transcription, recombination, and chromatin remodeling, is one of the most important anticancer targets. Numerous molecules have been designed as Top2-α inhibitors. However, several studies have shown that polymorphisms and mutations in Top2 have conferred resistance to most of these anticancer drugs. The aim of this study was to computationally examine the mechanisms by which genomic variations in Top2-α could affect its resistance to Amsacrine and Mitoxantrone as important inhibitors of the enzyme...
November 9, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27799031/calcium-calpain-dependent-pathways-regulate-vesiculation-in-malignant-breast-cells
#5
Jack Taylor, Ritu Jaiswal, Mary Bebawy
Multidrug resistance in cancer (MDR) occurs when tumours become cross-resistant to a range of different anticancer agents. One mechanism by which MDR can be acquired is through cell to cell communication pathways. Membrane-derived microparticles (MPs) are emerging as important signaling molecules in this process. MPs are released from most eukaryotic cells and transfer functional proteins and nucleic acids to recipient cells conferring deleterious traits within the cancer cell population including MDR, metastasis, and angiogenesis...
October 26, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27784207/does-hypoxic-response-mediate-primary-resistance-to-sunitinib-in-untreated-locally-advanced-breast-cancer
#6
Sofia Braga, Joana Cardoso, Saudade André, Margarida Brito, Pedro Sánchez, Lurdes Orvalho, Lucilia Salgado, Sérgio Dias, José B Pereira-Leal, José Luis Passos-Coelho
BACKGROUND: The antiangiogenic drug sunitinib has never been evaluated as single agent in untreated breast cancer patients. OBJECTIVE: We aimed to characterize the activity of sunitinib, alone and with docetaxel, in untreated locally advanced or operable breast cancer and to uncover the mechanisms of response. METHOD: Patients were treated with an upfront window of sunitinib followed by four cycles of sunitinib plus docetaxel. Response, resistance and toxicity were evaluated according to standard clinical parameters, magnetic resonance imaging, positron emission tomography, standard pathology characterization, molecular pathology and gene expression profiling...
October 25, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27774879/strong-anti-tumorous-potential-of-nardostachys-jatamansi-rhizome-extract-on-glioblastoma-and-in-silico-analysis-of-its-molecular-drug-targets
#7
Himanshi Kapoor, Nalini Yadav, Madhu Chopra, Sushil Chandra Mahapatra, Veena Agrawal
Glioblastoma has been reckoned as the prime cause of death due to brain tumours, being most invasive and lethal. Available treatment options, i.e. surgery, radiotherapy, chemotherapy and targeted therapies are not effective in improving prognosis, so an alternate therapy is insistent. Plant based drugs are efficient due to their synergistic action, multi-targeted approach and least side effects. Present investigation reports the strong anti-tumorous potential of Nardostachys jatamansi rhizome extract (NJRE) on U87 MG glioblastoma cells...
October 19, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27739365/egfr-high-expression-but-not-kras-status-predicts-sensitivity-of-pancreatic-cancer-cells-to-nimotuzumab-treatment-in-vivo
#8
Chenfei Zhou, Liangjun Zhu, Jun Ji, Fangmi Ding, Chao Wang, Qu Cai, Yingyan Yu, Zhenggang Zhu, Jun Zhang
Nimotuzumab, a monoclonal antibody against EGFR, has been shown to be efficacious in the treatment of advanced pancreatic cancer, but its predictive marker has not been established. The present study was designed to investigate the impact of EGFR and KRAS status on the antitumor efficacy of nimotuzumab and to explore its underlying mechanism of action. EGFR expression levels of pancreatic cancer cell lines, BxPC3, Panc-1, and Patu-8988, were analyzed by Western blot and immunocytochemistry, and their KRAS status was determined by gene sequencing...
October 13, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27697026/mechanisms-of-tubulin-binding-ligands-to-target-cancer-cells-updates-on-their-therapeutic-potential-and-clinical-trials
#9
Bhupinder Kumar, Rakesh Kumar, Ira-Ida Skvortsova, Vinod Kumar
A number of chemically diverse substances bind to the tubulin and inhibit cell proliferation by disrupting microtubule dynamics. There are four binding sites for the ligands binding to the tubulin; taxane/epothilone and laulimalide/peloruside binding ligands stabilize microtubule while vinca and colchicine binding site agents promote microtubule depolymerization. Most of the tubulin binding ligands disturb the tubulin-microtubule dynamic equilibrium but these may exhibit anticancer activities through different mechanisms...
September 28, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27677955/role-of-oxidative-stress-in-hepatitis-c-virus-induced-hepatocellular-carcinoma
#10
Na Fu, Hui Yao, Yuemin Nan, Liang Qiao
Hepatocellular carcinoma (HCC) is a leading cause of cancer-related death worldwide. Hepatitis C virus (HCV) infection is the predominant cause of chronic liver diseases and HCC, particularly in Western countries. Multiple molecular mechanisms are involved in the development and progression of HCV-related HCC, of which oxidative stress plays a pivotal role. HCV infection induces overproduction of reactive oxygen species (ROS) and impairs the function of endogenous antioxidants. Excessive amount of ROS directly damages DNA, lipids and proteins...
September 26, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27677954/hepatitis-b-virus-hbv-infection-and-hepatocellular-carcinoma-new-insights-for-an-old-topic
#11
Shi-Yan Yan, Jian-Gao Fan, Liang Qiao
Liver cancer is a common disease and the third leading cause of cancer-related deaths worldwide [1]. Hepatocellular carcinoma (HCC) is the most deadly form of liver cancer. Chronic hepatitis and subsequent liver fibrosis and cirrhosis are the major causes of HCC [2]. Chronic hepatitis B (CHB) is one of the most common infections worldwide. It is estimated that two billion people have been infected with hepatitis B virus (HBV), and up to 400,000 people worldwide are believed to have chronic HBV infection [3]...
September 26, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27677953/epstein-barr-virus-associated-gastric-cancer-and-potential-mechanisms-of-oncogenesis
#12
Ezequiel M Fuentes-Pananá, Abigail Morales-Sánchez
EBV-associated Gastric Cancer (EBVaGC) comprises about 9% of all cases of GC and constitutes a distinct clinicopathological and molecular entity. The pattern of viral expression in EBVaGC cannot be set to any of the previously EBV-associated malignancies. Several lines of evidence support that viral expression in EBVaGC is characterized by high transcription of the BamH1-A rightward transcript (BART), low-levels of EBNA-1 and lack of LMP1. The high transcription activity of the BamH1-A region is importantly directed to express BART miRNAs, supporting a critical role for these miRNAs during epithelial cell infection and carcinogenesis...
September 26, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27659430/udp-n-acetyl-d-galactosamine-polypeptide-n-acetylgalactosaminyltransferase-6-pp-galnac-t6-role-in-cancer-and-prospects-as-a-drug-target
#13
Samantha Banford, David J Timson
UDP-N-acetyl-D-galactosamine: polypeptide N-acetylgalactosaminyl transferase-6 (pp-GalNAc-T6) is a member of the N-acetyl-D-galactosamine transferase family. It catalyzes the addition of N-acetyl-D-galactosamine to proteins, often the first step in O-glycosylation of proteins. Glycosylated proteins play important roles in vivo in the cell membrane. These are often involved in cell-cell adhesion, cytoskeleton regulation and immune recognition. pp-GalNAc-T6 has been shown to be upregulated in a number of types of cancer...
September 22, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27659429/stem-cell-transplantation-in-multiple-myeloma
#14
Massimo Offidani, Silvia Gentili, Francesca Gay, Elena Aghemo, Laura Maracci, Laura Corvatta, Antonio Palumbo
High-dose therapy (HDT) followed by autologous stem cell transplantation (ASCT) remains the standard of care for patients younger than 65 years of age with multiple myeloma (MM). However, this therapeutic approach has undergone substantial advances in this last decade, mainly due to the introduction of new drugs such as thalidomide, lenalidomide and bortezomib. These new drugs, in different combinations, have shown to significantly increase response rates after induction therapy and ASCT. Moreover, the positive results obtained with these agents in consolidation and maintenance strategies after ASCT strongly support the concept of continuous therapy, whose ultimate goal is the long-term control of the disease and the improvement of outcome...
September 19, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27628597/lrigs-a-prognostically-significant-family-with-emerging-therapeutic-competence-against-cancers
#15
Uzma Malik, Aneela Javed
The human leucine-rich repeats and immunoglobulin like domains (LRIG) are evolutionary conserved family of single-pass transmembrane proteins. LRIG gene family includes three members, LRIG1 (formerly LIG1), LRIG2 and LRIG3, all of which are differentially expressed in human tissues and have long been proposed to be tumor suppressors. However, recently accumulated evidence on LRIG protein expression in human cancer appears to be inconsistent with this belief, as LRIG proteins have been found to be upregulated in certain tumors...
September 7, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27585695/grid-independent-descriptors-grind-analysis-and-sar-guided-molecular-docking-studies-to-probe-selectivity-profiles-of-inhibitors-of-multidrug-resistance-transporters-abcb1-and-abcg2
#16
Talha Shafi, Ishrat Jabeen
ATP-binding cassette (ABC) transporters, P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP/ABCG2) are major determinant of pharmacokinetic, safety and efficacy profiles of drugs thereby effluxing a broad range of endogenous substances across the plasma membrane. Overexpression of these transporters in various tumors is also implicated in the development of multidrug resistance (MDR) and thus, hampers the success of cancer chemotherapy. Modulators of these efflux transporters in combination with chemotherapeutics could be a promising concept to increase the effective intracellular concentration of anticancer drugs...
August 31, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27528364/extracellular-vesicles-in-glioblastoma-role-in-biological-processes-and-in-therapeutic-applications
#17
Ilaria Giusti, Marianna Di Francesco, Vincenza Dolo
Glioblastoma is the most common and most malignant form of primary brain cancer and it is characterized by one of the highest mortality among human cancers. Maximal and aggressive surgical resection is the first approach treatment but it is not usually definitive, being the tumor characterized by a high proliferative rate and an extensive invasion. An early diagnosis, associated to a careful monitoring, is pivotal in glioblastoma treatment; the Magnetic Resonance Imaging is used for monitoring purpose, but it's not sensitive enough to detect very small tumors; a valid alternative could be a repeated biopsy, but it is associated to a significant morbidity: less invasive options for diagnosis and therapeutic monitoring are unfailingly researched...
August 13, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27528363/new-approaches-in-glioblastoma-multiforme-the-potential-role-of-immune-check-point-inhibitors
#18
Francesca De Felice, Daniela Musio, Raffaele Cassese, Giovanni Luca Gravina, Vincenzo Tombolini
BACKGROUND: Glioblastoma multiforme (GBM) is the most frequent brain tumor. Despite recent advances in treatment approaches the prognosis remains poor, with a median overall survival of 14.6 months. Immunotherapy is the subject of ongoing research and its benefit is becoming evident in other malignancies. Immune check-points such as cytotoxic T lymphocyte associated antigen 4 (CTLA-4), programmed cell death receptor (PD-1) and indoleamine 2,3-dioxygenase (IDO) reduce immune response. OBJECTIVE: To clarify the role of immune check point inhibitors in GBM management...
August 13, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27528362/new-perspectives-in-glioblastoma-nanoparticles-based-approaches
#19
Rosa Luciano, Rossana Saracino, Giulia Battafarano, Antonio Perrotta, Melania Manco, Maurizio Muraca, Andrea Del Fattore, Michela Rossi
Glioblastoma multiforme represents one of the most aggressive tumor of central nervous system. Current therapy includes surgery, radiation and chemotherapy. These treatments are rarely curative and glioma are associated with a poor prognosis. Nanomedicine represents the most innovative branch of medicine since many studies demonstrated great advantage in the diagnosis and therapy of several diseases. In this review we will summarize the results obtained by the use of nanoparticles and extracellular vesicles in glioblastoma...
August 13, 2016: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/27528361/exploiting-microglial-functions-for-the-treatment-of-glioblastoma
#20
Cinzia Dello Russo, Lucia Lisi, Lucio Tentori, Pierluigi Navarra, Grazia Graziani, Colin K Combs
Glioblastoma is the most common brain tumor in adults and is associated with a very low survival rate. The heterogeneity of the tumor microenvironment, its resistance to drug and radiation therapy, and its robust invasiveness all contribute to the poor outcome. Large numbers of glioma associated microglia and macrophages can accumulate within the tumor where they appear to have a role in prognosis. This has stimulated considerable interest in understanding the contribution of these cells to disease progression...
August 13, 2016: Current Cancer Drug Targets
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