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https://www.readbyqxmd.com/read/28819150/the-g%C3%AE-i-giv-binding-interface-is-a-druggable-protein-protein-interaction
#1
Vincent DiGiacomo, Alain Ibáñez de Opakua, Maria P Papakonstantinou, Lien T Nguyen, Nekane Merino, Juan B Blanco-Canosa, Francisco J Blanco, Mikel Garcia-Marcos
Heterotrimeric G proteins are usually activated by the guanine-nucleotide exchange factor (GEF) activity of GPCRs. However, some non-receptor proteins are also GEFs. GIV (a.k.a Girdin) was the first non-receptor protein for which the GEF activity was ascribed to a well-defined protein sequence that directly binds Gαi. GIV expression promotes metastasis and disruption of its binding to Gαi blunts the pro-metastatic behavior of cancer cells. Although this suggests that inhibition of the Gαi-GIV interaction is a promising therapeutic strategy, protein-protein interactions (PPIs) are considered poorly "druggable" targets requiring case-by-case validation...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28809439/in-silico-profiling-of-the-biological-activities-of-amaryllidaceae-alkaloids
#2
Eman Shawky
OBJECTIVES: The large number of publications about Amaryllidaceae alkaloids reflects the abundance and variety in biological activity of these alkaloids. An in-silico approach was implemented in this work to rationalize the individual alkaloids to molecular biological activity. METHODS: A database was generated containing 313 Amaryllidaceae alkaloids which were then subjected to in-silico-validated structure-based virtual screening using extra precision (XP) approach of Glide docking program...
August 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28806777/a-synthetic-sickness-screen-for-senescence-re-engagement-targets-in-mutant-cancer-backgrounds
#3
Claire J Cairney, Lauren S Godwin, Alan E Bilsland, Sharon Burns, Katrina H Stevenson, Lynn McGarry, John Revie, Jon D Moore, Ceri M Wiggins, Rebecca S Collinson, Clare Mudd, Elpida Tsonou, Mahito Sadaie, Dorothy C Bennett, Masashi Narita, Christopher J Torrance, W Nicol Keith
Senescence is a universal barrier to immortalisation and tumorigenesis. As such, interest in the use of senescence-induction in a therapeutic context has been gaining momentum in the past few years; however, senescence and immortalisation remain underserved areas for drug discovery owing to a lack of robust senescence inducing agents and an incomplete understanding of the signalling events underlying this complex process. In order to address this issue we undertook a large-scale morphological siRNA screen for inducers of senescence phenotypes in the human melanoma cell line A375P...
August 14, 2017: PLoS Genetics
https://www.readbyqxmd.com/read/28800793/upregulation-of-hint2-inhibits-non-small-cell-lung-cancer-cell-invasion-via-cox-2-pge%C3%A2-mediated-activation-of-%C3%A3-catenin-signaling
#4
Jie Li, Siwen Chen, Bin Ni
Histidine triad nucleotide binding protein 2 (HINT2) belongs to a HIT superfamily. It is ubiquitous and can be detectedin all forms of life. Recently, this protein has been reported to function as a tumor suppressor in some kind of cancers. However, little is known about its precise role in non-small cell lung cancer (NSCLC). In the present study, we explored the effects of HINT2 on the invasive potential of NSCLC cells. Our results showed that the expression of HINT2 was reduced in NSCLC tissues and cell lines...
August 11, 2017: Oncology Research
https://www.readbyqxmd.com/read/28783712/machine-learning-for-predicting-lifespan-extending-chemical-compounds
#5
Diogo G Barardo, Danielle Newby, Daniel Thornton, Taravat Ghafourian, João Pedro de Magalhães, Alex A Freitas
Increasing age is a risk factor for many diseases; therefore developing pharmacological interventions that slow down ageing and consequently postpone the onset of many age-related diseases is highly desirable. In this work we analyse data from the DrugAge database, which contains chemical compounds and their effect on the lifespan of model organisms. Predictive models were built using the machine learning method random forests to predict whether or not a chemical compound will increase Caenorhabditis elegans' lifespan, using as features Gene Ontology (GO) terms annotated for proteins targeted by the compounds and chemical descriptors calculated from each compound's chemical structure...
July 18, 2017: Aging
https://www.readbyqxmd.com/read/28780159/pyridine-pyrimidine-amides-that-prevent-hgf-induced-epithelial-scattering-by-two-distinct-mechanisms
#6
Adam Siddiqui-Jain, Jacob P Hoj, J Blade Hargiss, Taylor H Hoj, Carter J Payne, Collin A Ritchie, Steven R Herron, Colette Quinn, Jeffrey T Schuler, Marc D H Hansen
Stimulation of cultured epithelial cells with scatter factor/hepatocyte growth factor (HGF) results in individual cells detaching and assuming a migratory and invasive phenotype. Epithelial scattering recapitulates cancer progression and studies have implicated HGF signaling as a driver of cancer metastasis. Inhibitors of HGF signaling have been proposed to act as anti-cancer agents. We previously screened a small molecule library for compounds that block HGF-induced epithelial scattering. Most hits identified in this screen exhibit anti-mitotic properties...
July 25, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28774426/novel-anti-prostate-cancer-scaffold-identified-by-the-combination-of-in-silico-and-cell-based-assays-targeting-the-pi3k-akt-mtor-pathway
#7
Marta Érica Saidel, Karen C Dos Santos, Luís F P Nagano, Carlos Alberto Montanari, Andrei Leitão
Phenotypic assays were performed in prostate cancer cell lines to describe the biological activity of PI3K-AKT-mTOR pathway inhibitors retrieved from the virtual screening initiative. These novel chemicals share in common the aminopyridine scaffold, hitting PC-3 cells in macromolar range, with selectivity index over fibroblast cell lines. Moreover, a preliminary study of the mode of action by flow cytometry assay pointed out that these compounds had a rapamycin-like response for the PI3K-AKT-mTOR pathway modulation...
July 24, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28771473/novel-application-of-the-published-kinase-inhibitor-set-to-identify-therapeutic-targets-and-pathways-in-triple-negative-breast-cancer-subtypes
#8
Margarite D Matossian, Steven Elliott, Van T Hoang, Hope E Burks, Theresa B Phamduy, Douglas B Chrisey, William J Zuercher, David H Drewry, Carrow Wells, Bridgette Collins-Burow, Matthew E Burow
Triple negative breast cancers (TNBCs) have high recurrence and metastasis rates. Acquisition of a mesenchymal morphology and phenotype in addition to driving migration is a consequential process that promotes metastasis. Although some kinases are known to regulate a mesenchymal phenotype, the role for a substantial portion of the human kinome remains uncharacterized. Here we evaluated the Published Kinase Inhibitor Set (PKIS) and screened a panel of TNBC cell lines to evaluate the compounds' effects on a mesenchymal phenotype...
2017: PloS One
https://www.readbyqxmd.com/read/28768863/hras-egfr-met-and-ron-are-recurrently-activated-by-provirus-insertion-in-mav-2-retrovirus-induced-liver-tumors
#9
Vladimir Pecenka, Petr Pajer, Vít Karafiat, Petra Kasparova, Jana Dudlova, Michal Dvorak
Myeloblastosis-associated virus-2 (MAV-2) is a highly tumorigenic simple avian retrovirus. Chickens infected in ovo with MAV-2 develop tumors in kidneys, lungs, and liver with a short latency of less then 8 weeks. Here we report the results of molecular analyses of MAV-2-induced liver tumors that fall into three classes: hepatic hemangiosarcomas (HHS), intrahepatic cholangiocarcinomas (ICC), and hepatocellular carcinomas (HCC). Comprehensive inverse PCR-based screening of 92 chicken liver tumors revealed that in ca 86 % of these tumors, MAV-2 provirus had integrated into one of four gene loci: HRAS, EGFR, MET, and RON Insertionally mutated genes correlated with tumor type - HRAS was hit in HHSs, MET in ICCs, RON mostly in ICCs and EGFR mostly in HCC...
August 2, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28760529/discovery-of-a-novel-b-cell-lymphoma-6-bcl6-corepressor-interaction-inhibitor-by-utilizing-structure-based-drug-design
#10
Takeshi Yasui, Takeshi Yamamoto, Nozomu Sakai, Kouhei Asano, Takafumi Takai, Yayoi Yoshitomi, Melinda Davis, Terufumi Takagi, Kotaro Sakamoto, Satoshi Sogabe, Yusuke Kamada, Weston Lane, Gyorgy Snell, Masashi Iwata, Masayuki Goto, Hiroshi Inooka, Jun-Ichi Sakamoto, Yoshihisa Nakada, Yasuhiro Imaeda
B-cell lymphoma 6 (BCL6) is a transcriptional repressor that can form complexes with corepressors via protein-protein interactions (PPIs). The complexes of BCL6 and corepressors play an important role in the formation of germinal centers (GCs), and differentiation and proliferation of lymphocytes. Therefore, BCL6-corepressor interaction inhibitors would be drug candidates for managing autoimmune diseases and cancer. Starting from high-throughput screening hits 1a and 2a, we identified a novel BCL6-corepressor interaction inhibitor 8c (cell-free enzyme-linked immunosorbent assay [ELISA] IC50=0...
September 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28758515/approaches-for-discovering-novel-bioactive-small-molecules-targeting-autophagy
#11
Hui-Yun Hwang, Sung Min Cho, Ho Jeong Kwon
In recent years, development of novel bioactive small molecules targeting autophagy has been implicated for autophagy-related disease treatment. Screening new small molecules regulating autophagy allows for the discovery of novel autophagy machinery and therapeutic agents. Areas covered: Two major screening methods for novel autophagy modulators are introduced in this review, namely target based screening and phenotype based screening. With increasing attention focused on chemical compound libraries, coupled with the development of new assay systems, this review attempts to provide an efficient strategy to explore autophagy biology and discover small molecules for the treatment of autophagy-related diseases...
July 30, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28756009/flaws-in-the-lnt-single-hit-model-for-cancer-risk-an-historical-assessment
#12
REVIEW
Edward J Calabrese
The LNT single-hit model was derived from the Nobel Prize-winning research of Herman J. Muller who showed that x-rays could induce gene mutations in Drosophila and that the dose response for these so-called mutational events was linear. Lewis J. Stadler, another well-known and respected geneticist at the time, strongly disagreed with and challenged Muller's claims. Detailed evaluations by Stadler over a prolonged series of investigations revealed that Muller's experiments had induced gross heritable chromosomal damage instead of specific gene mutations as had been claimed by Muller at his Nobel Lecture...
July 26, 2017: Environmental Research
https://www.readbyqxmd.com/read/28753844/transcriptome-wide-analysis-of-magnetic-resonance-imaging-targeted-biopsy-and-matching-surgical-specimens-from-high-risk-prostate-cancer-patients-treated-with-radical-prostatectomy-the-target-must-be-hit
#13
Jan Philipp Radtke, Mandeep Takhar, David Bonekamp, Claudia Kesch, Nicholas Erho, Marguerite du Plessis, Christine Buerki, Kaye Ong, Elai Davicioni, Markus Hohenfellner, Boris A Hadaschik
BACKGROUND: The most suspicious lesions on multiparametric magnetic resonance imaging (MRI) may be representative of final pathology. OBJECTIVE: We connect imaging with high-precision spatial annotation of biopsies and genomic cancer signatures to compare the genomic signals of the index lesion and biopsy cores of adjacent and far away locations. DESIGN, SETTING, AND PARTICIPANTS: Eleven patients diagnosed with high-risk prostate cancer on MRI/transrectal ultrasound-fusion biopsy (Bx) and treated with radical prostatectomy (RP)...
January 26, 2017: European Urology Focus
https://www.readbyqxmd.com/read/28749548/c-myc-positive-relapsed-and-refractory-diffuse-large-b-cell-lymphoma-impact-of-additional-hits-and-outcomes-with-subsequent-therapy
#14
Narendranath Epperla, Kami J Maddocks, Mohammed Salhab, Julio C Chavez, Nishitha Reddy, Reem Karmali, Elvira Umyarova, Veronika Bachanova, Cristiana Costa, Martha Glenn, Oscar Calzada, Ana C Xavier, Zheng Zhou, Nasheed M Hossain, Francisco J Hernandez-Ilizaliturri, Zeina Al-Mansour, Stefan K Barta, Saurabh Chhabra, Frederick Lansigan, Amitkumar Mehta, Michael V Jaglal, Andrew Evans, Christopher R Flowers, Jonathon B Cohen, Timothy S Fenske, Mehdi Hamadani, Luciano J Costa
BACKGROUND: The impact of MYC proto-oncogene, basic helix-loop-helix (MYC) translocations (with or without additional rearrangements involving the B-cell lymphoma 2 [BCL2] or BCL6 genes) on the response to salvage therapy and survival in patients with diffuse large B-cell lymphoma (DLBCL) who experience primary treatment failure is not well defined. METHODS: This was a multicenter, retrospective study of the impact of MYC, BCL2, and BCL6 rearrangements in patients with DLBCL who failed to achieve complete remission or relapsed within 6 months after they completed upfront chemoimmunotherapy...
July 27, 2017: Cancer
https://www.readbyqxmd.com/read/28739687/rational-design-of-a-potent-pan-pim-kinases-inhibitor-with-a-rhodanine-benzoimidazole-structure
#15
Yuichi Sawaguchi, Ryuta Yamazaki, Yukiko Nishiyama, Toshio Sasai, Masayuki Mae, Atsuhiro Abe, Takashi Yaegashi, Hiroyuki Nishiyama, Takeshi Matsuzaki
BACKGROUND/AIM: The serine/threonine Pim kinases are overexpressed in various types of solid carcinomas and hematological malignancies, and contribute to regulating cell-cycle progression and cell survival. The aim of this study was to discover a novel pan-Pim kinases inhibitor with potent anti-proliferative activities against cancer cell lines. MATERIALS AND METHODS: We screened a panel of small molecule compounds for their ability to inhibit Pim-1 kinase activity, and the hit compound was optimized using the docking analysis to Pim-1...
August 2017: Anticancer Research
https://www.readbyqxmd.com/read/28733251/rna-binding-protein-raly-promotes-protein-arginine-methyltransferase-1-alternatively-spliced-isoform-v2-relative-expression-and-metastatic-potential-in-breast-cancer-cells
#16
Emma Bondy-Chorney, R Mitchell Baldwin, Andréanne Didillon, Benoît Chabot, Bernard J Jasmin, Jocelyn Côté
Aberrant expression of Protein Arginine Methyltransferases (PRMTs) has been observed in several cancer types, including breast cancer. We previously reported that the PRMT1v2 isoform, which is generated through inclusion of alternative exon 2, is overexpressed in breast cancer cells and promotes their invasiveness. However, the precise mechanism by which expression of this isoform is controlled and how it is dysregulated in breast cancer remains unknown. Using a custom RNA interference-based screen, we identified several RNA binding proteins (RBP) which, when knocked down, altered the relative abundance of the alternatively spliced PRMT1v2 isoform...
July 18, 2017: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/28732184/high-throughput-identification-of-mir-596-inducing-p53-mediated-apoptosis-in-hela-and-hct116-cells-using-cell-microarray
#17
Ming Ma, Junyu Yang, Bolun Wang, Zhihua Zhao, Jianzhong Jeff Xi
miRNAs play a key role in the regulation of gene networks in mammalian cells. However, little is known about their roles and functions in the apoptosis pathway. Here, we conducted a whole-genome miRNA screening for apoptosis and identified more than 100 miRNAs as apoptosis inducers. To further explain the roles of these mRNAs in apoptosis, a second round of screening was conducted between p53 +/+ and -/- cells. Among the hits, miR-596 was identified as a regulator of p53. The overexpression of miR-596 significantly increased p53 at the protein level, thereby inducing apoptosis...
July 1, 2017: SLAS Technology
https://www.readbyqxmd.com/read/28729623/3d-qsar-studies-on-maslinic-acid-analogs-for-anticancer-activity-against-breast-cancer-cell-line-mcf-7
#18
Sarfaraz Alam, Feroz Khan
Global prevalence of breast cancer and its rising frequency makes it a key area of research in drug discovery programs. The research article describes the development of field based 3D-QSAR model based on human breast cancer cell line MCF7 in vitro anticancer activity, which defines the molecular level understanding and regions of structure-activity relationship for triterpene maslinic acid and its analogs. The key features such as average shape, hydrophobic regions and electrostatic patterns of active compounds were mined and mapped to virtually screen potential analogs...
July 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28726519/cancer-stem-cells-cd133-inhibition-and-cytotoxicity-of-certain-3-phenylthiazolo-3-2-a-benzimidazoles-design-direct-synthesis-crystal-study-and-in-vitro-biological-evaluation
#19
Ghada H Al-Ansary, Wagdy M Eldehna, Hazem A Ghabbour, Sara T A Al-Rashood, Khalid A Al-Rashood, Radwa A Eladwy, Abdullah Al-Dhfyan, Maha M Kabil, Hatem A Abdel-Aziz
Cancer stem cells (CSCs) have been objects of intensive study since their identification in 1994. Adopting a structural rigidification approach, a novel series of 3-phenylthiazolo[3,2-a]benzimidazoles 4a-d was designed and synthesised, in an attempt to develop potent anticancer agent that can target the bulk of tumour cells and CSCs. The anti-proliferative activity of the synthesised compounds was evaluated against two cell lines, namely; colon cancer HT-29 and triple negative breast cancer MDA-MB-468 cell lines...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28724888/crosscheck-an-open-source-web-tool-for-high-throughput-screen-data-analysis
#20
Jamil Najafov, Ayaz Najafov
Modern high-throughput screening methods allow researchers to generate large datasets that potentially contain important biological information. However, oftentimes, picking relevant hits from such screens and generating testable hypotheses requires training in bioinformatics and the skills to efficiently perform database mining. There are currently no tools available to general public that allow users to cross-reference their screen datasets with published screen datasets. To this end, we developed CrossCheck, an online platform for high-throughput screen data analysis...
July 19, 2017: Scientific Reports
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