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https://www.readbyqxmd.com/read/29235893/construction-of-some-cytotoxic-agents-with-aurone-and-furoaurone-scaffolds
#1
Ghaneya S Hassan, Hanan H Georgey, Riham F George, Eman R Mohammed
AIM: In spite of the availability of different chemotherapies for cancer treatment, there is still a need for new candidates with higher efficacy and lower toxicity. METHODOLOGY: Aurones 7a-f, 8a-f and furoaurones 13a-f, 16a-c were synthesized. Some compounds were selected by the National Cancer Institute, USA, for cytotoxicity screening. RESULTS & DISCUSSION: The furoaurone derivative, 13a was the most active one exhibiting promising growth inhibition against leukemia, K562 and melanoma, MDA-MB-435 cells at concentration of 10 μM...
December 13, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29232168/high-throughput-screening-approach-for-identifying-compounds-that-inhibit-nonhomologous-end-joining
#2
Andrea L Bredemeyer, Bruce S Edwards, Mark K Haynes, Abigail J Morales, Yinan Wang, Oleg Ursu, Anna Waller, Larry A Sklar, Barry P Sleckman
DNA double-strand breaks (DSBs) are repaired primarily by homologous recombination (HR) or nonhomologous end joining (NHEJ). Compounds that modulate HR have shown promise as cancer therapeutics. The V(D)J recombination reaction, which assembles antigen receptor genes in lymphocytes, is initiated by the introduction of DNA DSBs at two recombining gene segments by the RAG endonuclease, followed by the NHEJ-mediated repair of these DSBs. Here, using HyperCyt automated flow cytometry, we develop a robust high-throughput screening (HTS) assay for NHEJ that utilizes engineered pre-B-cell lines where the V(D)J recombination reaction can be induced and monitored at a single-cell level...
December 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/29229903/loss-of-pbrm1-rescues-vhl-dependent-replication-stress-to-promote-renal-carcinogenesis
#3
Judit Espana-Agusti, Anne Warren, Su Kit Chew, David J Adams, Athena Matakidou
Inactivation of the VHL (Von Hippel Lindau) tumour suppressor has long been recognised as necessary for the pathogenesis of clear cell renal cancer (ccRCC); however, the molecular mechanisms underlying transformation and the requirement for additional genetic hits remain unclear. Here, we show that loss of VHL alone results in DNA replication stress and damage accumulation, effects that constrain cellular growth and transformation. By contrast, concomitant loss of the chromatin remodelling factor PBRM1 (mutated in 40% of ccRCC) rescues VHL-induced replication stress, maintaining cellular fitness and allowing proliferation...
December 11, 2017: Nature Communications
https://www.readbyqxmd.com/read/29228881/unravelling-novel-congeners-from-acetyllysine-mimicking-ligand-targeting-a-lysine-acetyltransferase-pcaf-bromodomain
#4
Venkatesan Suryanarayanan, Sanjeev Kumar Singh
p300/CBP Associated Factor (PCAF) bromodomain (BRD), a lysine acetyltransferases, has emerged as a promising drug target as its dysfunction is linked to onset and progression of several diseases like cancer, diabetes, AIDS etc. In this study, a three featured E-Pharmacophore (ARR) was generated based on acetyllysine mimicking inhibitor of PCAF BRD which is available as co-crystal structure (PDB ID: 5FDZ). It was used for filtering small molecule databases followed by molecular docking and consequently validated using enrichment calculation...
December 11, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29228628/drug-sensitivity-profiling-identifies-potential-therapies-for-lymphoproliferative-disorders-with-overactive-jak-stat3-signaling
#5
Heikki Kuusanmäki, Olli Dufva, Elina Parri, Arjan J van Adrichem, Hanna Rajala, Muntasir M Majumder, Bhagwan Yadav, Alun Parsons, Wing C Chan, Krister Wennerberg, Satu Mustjoki, Caroline A Heckman
Constitutive JAK/STAT3 signaling contributes to disease progression in many lymphoproliferative disorders. Recent genetic analyses have revealed gain-of-function STAT3 mutations in lymphoid cancers leading to hyperactivation of STAT3, which may represent a potential therapeutic target. Using a functional reporter assay, we screened 306 compounds with selective activity against various target molecules to identify drugs capable of inhibiting the cellular activity of STAT3. Top hits were further validated with additional models including STAT3-mutated natural killer (NK)-cell leukemia/lymphoma cell lines and primary large granular lymphocytic (LGL) leukemia cells to assess their ability to inhibit STAT3 phosphorylation and STAT3 dependent cell viability...
November 14, 2017: Oncotarget
https://www.readbyqxmd.com/read/29227193/ddx5-p68-associated-lncrna-loc284454-is-differentially-expressed-in-human-cancers-and-modulates-gene-expression
#6
Monalisa Das, Arun Renganathan, Shrinivas Nivrutti Dighe, Utsa Bhaduri, Abhijith Shettar, Geetashree Mukherjee, Paturu Kondaiah, Manchanahalli R Satyanarayana Rao
Long non-coding RNAs (lncRNAs) are emerging as important players in regulation of gene expression in higher eukaryotes. DDX5/p68 RNA helicase protein which is involved in splicing of precursor mRNAs also interacts with lncRNAs like, SRA and mrhl, to modulate gene expression. We performed RIP-seq analysis in HEK293T cells to identify the complete repertoire of DDX5/p68 interacting transcripts including 73 single exonic (SE) lncRNAs. The LOC284454 lncRNA is the second top hit of the list of SE lncRNAs which we have characterized in detail for its molecular features and cellular functions...
December 11, 2017: RNA Biology
https://www.readbyqxmd.com/read/29208522/discovery-of-new-gsk-3%C3%AE-inhibitors-through-structure-based-virtual-screening
#7
Xiaodong Dou, Lan Jiang, Yanxing Wang, Hongwei Jin, Zhenming Liu, Liangren Zhang
Glycogen synthase kinase-3β (GSK-3β) is an attractive therapeutic target for human diseases, such as diabetes, cancer, neurodegenerative diseases, and inflammation. Thus, structure-based virtual screening was performed to identify novel scaffolds of GSK-3β inhibitors, and we observed that conserved water molecules of GSK-3β were suitable for virtual screening. We found 14 hits and D1 (IC50 of 0.71 μM) were identified. Furthermore, the neuroprotection activity of D1-D3 was validated on a cellular level...
November 24, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29207941/uneven-acute-non-alcoholic-fatty-change-of-the-liver-after-percutaneous-transhepatic-portal-vein-embolization-in-a-patient-with-hilar-cholangiocarcinoma-a-case-report
#8
Chun-Yi Tsai, Motoi Nojiri, Yukihiro Yokoyama, Tomoki Ebata, Takashi Mizuno, Masato Nagino
BACKGROUND: Portal vein embolization is essential for patients with biliary cancer who undergo extended hepatectomy to induce hypertrophy of the future remnant liver. Over 830 patients have undergone the portal vein embolization at our institution since 1990. Non-alcoholic fatty liver disease is an entity of hepatic disease characterized by fat deposition in hepatocytes. It has a higher prevalence among persons with morbid obesity, type 2 diabetes, and hyperlipidemia. Neither the mechanism of hepatic hypertrophy after portal vein embolization nor the pathophysiology of non-alcoholic fatty liver disease has been fully elucidated...
December 6, 2017: BMC Gastroenterology
https://www.readbyqxmd.com/read/29207657/discovery-of-novel-frizzled-7-inhibitors-by-targeting-the-receptor-s-transmembrane-domain
#9
Wei Zhang, Wenyan Lu, Subramaniam Ananthan, Mark J Suto, Yonghe Li
Frizzled (Fzd) proteins are seven transmembrane receptors that belong to a novel and separated family of G-protein-coupled receptors (GPCRs). The Fzd receptors can respond to Wnt proteins to activate the canonical β-catenin pathway which is important for both initiation and progression of cancers. Disruption of the Wnt/β-catenin signal thus represents an opportunity for rational cancer prevention and therapy. Of the 10 members of the Fzd family, Fzd7 is the most important member involved in cancer development and progression...
October 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/29203377/proposed-terminology-and-classification-of-pre-malignant-neoplastic-conditions-a-consensus-proposal
#10
REVIEW
Peter Valent, Cem Akin, Michel Arock, Christoph Bock, Tracy I George, Stephen J Galli, Jason Gotlib, Torsten Haferlach, Gregor Hoermann, Olivier Hermine, Ulrich Jäger, Lukas Kenner, Hans Kreipe, Ravindra Majeti, Dean D Metcalfe, Alberto Orfao, Andreas Reiter, Wolfgang R Sperr, Philipp B Staber, Karl Sotlar, Charles Schiffer, Giulio Superti-Furga, Hans-Peter Horny
Cancer evolution is a step-wise non-linear process that may start early in life or later in adulthood, and includes pre-malignant (indolent) and malignant phases. Early somatic changes may not be detectable or are found by chance in apparently healthy individuals. The same lesions may be detected in pre-malignant clonal conditions. In some patients, these lesions may never become relevant clinically whereas in others, they act together with additional pro-oncogenic hits and thereby contribute to the formation of an overt malignancy...
November 26, 2017: EBioMedicine
https://www.readbyqxmd.com/read/29202410/discovery-optimization-and-biological-evaluation-for-novel-c-met-kinase-inhibitors
#11
Haoliang Yuan, Qiufeng Liu, Li Zhang, Shihe Hu, Tiantian Chen, Huifang Li, Yadong Chen, Yechun Xu, Tao Lu
The c-Met kinase has emerged as an attractive target for developing antitumor agents because of its close relationship with the development of many human cancers, poor clinical outcomes and even drug resistance. A series of novel c-Met kinase inhibitors have been identified with multiple workflow in this work, including virtual screening, X-ray crystallography, biological evaluation and structural optimization. The experimentally determined crystal structure of the best hit compound HL-11 in c-Met kinase domain was highly consistent with the computational prediction...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29202221/sperm-hybrid-micromotor-for-targeted-drug-delivery
#12
Haifeng Xu, Mariana Medina-Sánchez, Veronika Magdanz, Lukas Schwarz, Franziska Hebenstreit, Oliver G Schmidt
A sperm-driven micromotor is presented as a targeted drug delivery system, which is appealing to potentially treat diseases in the female reproductive tract. This system is demonstrated to be an efficient drug delivery vehicle by first loading a motile sperm cell with doxorubicin hydrochloride (DOX-HCl, an anticancer drug), then guiding it, using a synthetic magnetic harness, to an in vitro cultured tumor spheroid, and finally delivering the drug locally once the sperm cell is free by an integrated mechanical release mechanism...
December 4, 2017: ACS Nano
https://www.readbyqxmd.com/read/29201774/hepatitis-action-plan-and-changing-trend-of-liver-disease-in-japan-viral-hepatitis-and-nonalcoholic-fatty-liver-disease
#13
REVIEW
Tatsuya Kanto, Sachiyo Yoshio
In Japan, the estimated number of chronic hepatitis B virus infections was 1.1 to 1.4 million, and that of chronic hepatitis C virus was 1.9 to 2.3 million in 2000. The mortality of hepatocellular carcinoma had been increasing and hit the peak at around 2002, which subsequently started to decrease. Japan has a national action plan for addressing viral hepatitis called Basic Act on Hepatitis Measures, established in 2009. In 2011, basic guidelines for promotion of control measures for hepatitis were issued, comprising nine principles in order to promote measures to prevent hepatitis B and C...
January 2017: Euroasian journal of hepato-gastroenterology
https://www.readbyqxmd.com/read/29197962/structure-based-pharmacophore-design-and-virtual-screening-for-novel-potential-inhibitors-of-epidermal-growth-factor-receptor-as-an-approach-to-breast-cancer-chemotherapy
#14
Shabnam Mahernia, Malihe Hassanzadeh, Niusha Sharifi, Bita Mehravi, Fariba Paytam, Mehdi Adib, Massoud Amanlou
Cancer cells are described with features of uncontrolled growth, invasion and metastasis. The epidermal growth factor receptor subfamily of tyrosine kinases (EGFR-TK) plays a crucial regulatory role in the control of cellular proliferation and progression of various cancers. Therefore, its inhibition might lead to the discovery of a new generation of anticancer drugs. In the present study, structure-based pharmacophore modeling, molecular docking and molecular dynamics simulations were applied to identify potential hits, which exhibited good inhibition on the proliferation of MCF-7 breast cancer cell line and favorable binding interactions on EGFR-TK...
December 2, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/29194093/cdkn2a-b-deletion-and-double-hit-mutations-of-the-mapk-pathway-underlie-the-aggressive-behavior-of-langerhans-cell-tumors
#15
Luc Xerri, José Adélaïde, Cornel Popovici, Séverine Garnier, Arnaud Guille, Lenaïg Mescam-Mancini, Camille Laurent, Pierre Brousset, Carole Coze, Gérard Michel, Max Chaffanet, Reda Bouabdallah, Diane Coso, François Bertucci, Daniel Birnbaum
Langerhans cell histiocytosis (LCH) has a mostly favorable outcome, whereas Langerhans cell sarcoma (LCS) is an aggressive tumor. It is still unclear whether any specific molecular alterations could underlie the aggressive behavior of Langerhans cell proliferations. We used targeted next-generation sequencing and array-comparative genomic hybridization to profile 22 LCH samples from different patients together with 3 LCS samples corresponding to different relapses from the same patient. The third LCS relapse was a composite tumor including both B-cell chronic lymphocytic leukemia and LCS components...
November 29, 2017: American Journal of Surgical Pathology
https://www.readbyqxmd.com/read/29190092/structure-based-design-and-biological-characterization-of-selective-histone-deacetylase-8-hdac8-inhibitors-with-anti-neuroblastoma-activity
#16
Tino Heimburg, Fiona R Kolbinger, Patrik Zeyen, Ehab Ghazy, Daniel Herp, Karin Schmidtkunz, Jelena Melesina, Tajith Baba Shaik, Frank Erdmann, Matthias Schmidt, Christophe Romier, Dina Robaa, Olaf Witt, Ina Oehme, Manfred Jung, Wolfgang Sippl
Histone deacetylases (HDACs) are important modulators of epigenetic gene regulation and additionally control the activity of non-histone protein substrates. While for HDACs 1-3 and 6 many potent selective inhibitors have been obtained, for other subtypes much less is known on selective inhibitors and the consequences of their inhibition. The present report describes the development of substituted benzhydroxamic acids as potent and selective HDAC8 inhibitors. Docking studies using available crystal structures have been used for structure-based optimization of this series of compounds...
November 30, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29187845/loss-of-genome-fidelity-beta-hpvs-and-the-dna-damage-response
#17
REVIEW
Sebastian O Wendel, Nicholas A Wallace
While the role of genus alpha human papillomaviruses in the tumorigenesis and tumor maintenance of anogenital and oropharyngeal cancers is well-established, the role of genus beta human papilloviruses (β-HPVs) in non-melanoma skin cancers (NMSCs) is less certain. Persistent β-HPV infections cause NMSCs in sun-exposed skin of people with a rare genetic disorder, epidermodysplasia verruciformis. However, β-HPV infections in people without epidermodysplasia verruciformis are typically transient. Further, β-HPV gene expression is not necessary for tumor maintenance in the general population as on average there is fewer than one copy of the β-HPV genome per cell in NMSC tumor biopsies...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29180474/vitamin-c-sensitizes-melanoma-to-bet-inhibitors
#18
Gaofeng Wang, Sushmita Mustafi, Vladimir Camarena, Claude-Henry Volmar, Tyler C Huff, David W Sant, Shaun P Brothers, Zhao-Jun Liu, Claes Wahlestedt
Bromodomain and extra-terminal inhibitors (BETi) are promising cancer therapies, yet prominent side effects of BETi at effective doses have been reported in Phase I clinical trials. Here we screened a panel of small molecules targeting epigenetic modulators against human metastatic melanoma cells. Cells were pretreated with or without ascorbate (vitamin C), which promotes DNA demethylation and subsequently changes the sensitivity to drugs. Top hits were structurally unrelated BETi including JQ1, I-BET151, CPI-203, and BI-2536...
November 27, 2017: Cancer Research
https://www.readbyqxmd.com/read/29179527/hitting-the-nail-on-the-head-combining-oncolytic-adenovirus-mediated-virotherapy-and-immunomodulation-for-the-treatment-of-glioma
#19
REVIEW
Wojciech K Panek, J Robert Kane, Jacob S Young, Aida Rashidi, Julius W Kim, Deepak Kanojia, Maciej S Lesniak
Glioblastoma is a highly aggressive malignant brain tumor with a poor prognosis and the median survival 14.6 months. Immunomodulatory proteins and oncolytic viruses represent two treatment approaches that have recently been developed for patients with glioblastoma that could extend patient survival and result in better treatment outcomes for patients with this disease. Together, these approaches could potentially augment the treatment efficacy and strength of these anti-tumor therapies. In addition to oncolytic activities, this combinatory approach introduces immunomodulation locally only where cancerous cells are present...
October 24, 2017: Oncotarget
https://www.readbyqxmd.com/read/29170627/combinatorial-in-silico-strategy-towards-identifying-potential-hotspots-during-inhibition-of-structurally-identical-hdac1-and-hdac2-enzymes-for-effective-chemotherapy-against-neurological-disorders
#20
Shabir Ahmad Ganai, Ehsaan Abdullah, Romana Rashid, Mohammad Altaf
Histone deacetylases (HDACs) regulate epigenetic gene expression programs by modulating chromatin architecture and are required for neuronal development. Dysregulation of HDACs and aberrant chromatin acetylation homeostasis have been implicated in various diseases ranging from cancer to neurodegenerative disorders. Histone deacetylase inhibitors (HDACi), the small molecules interfering HDACs have shown enhanced acetylation of the genome and are gaining great attention as potent drugs for treating cancer and neurodegeneration...
2017: Frontiers in Molecular Neuroscience
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