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https://www.readbyqxmd.com/read/28531811/synthesis-of-novel-indole-derivatives-as-promising-dna-binding-agents-and-evaluation-of-antitumor-and-antitopoisomerase-i-activities
#1
Elizabeth Almeida Lafayette, Sinara Mônica Vitalino de Almeida, Renata Virginia Cavalcanti Santos, Jamerson Ferreira de Oliveira, Cezar Augusto da Cruz Amorim, Rosali Maria Ferreira da Silva, Maira Galdino da Rocha Pitta, Ivan da Rocha Pitta, Ricardo Olimpio de Moura, Luiz Bezerra de Carvalho Júnior, Moacyr Jesus Barreto de Melo Rêgo, Maria do Carmo Alves de Lima
Molecules bearing indole nucleus present diverse biological properties such as antitumor and anti-inflammatory activities that can be associated both to DNA and protein interactions. This study focused on the synthesis of new indole derivatives with thiazolidines and imidazolidine rings condensed as side chains as well as the evaluation of their ability to interact with the DNA and antitumor and topoisomerase inhibition activities. All derivatives were successfully synthesized and their structures were elucidated by mass spectrometry (MS), infrared (IR), spectroscopy (1)H NMR, (13)C NMR, COSY (1)H-(1)H and HSQC (1)H-(13)C...
May 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28531166/-epiafzelechin-protects-against-ovariectomy-induced-bone-loss-in-adult-mice-and-modulate-osteoblastic-and-osteoclastic-functions-in-vitro
#2
Ka-Chun Wong, Sisi Cao, Xiaoli Dong, Man-Chun Law, Tak-Hang Chan, Man-Sau Wong
The present study was designed to characterize the bone protective effects of (-)-epiafzelechin (EAF), a flavan-3-ol, in mature ovariectomized mice model and its ability to stimulate osteoblastic activity and inhibit osteoclastic activity. Mature C57BL/6 mice (three to four months old) were either ovariectomised (OVX) or sham-operated and subjected to treatment (vehicle, 17β-oestradiol (E2, 200 μg/kg/day) or EAF (500 μg/kg/day) orally for six weeks. EAF and E2 significantly reduced urinary calcium (Ca) excretion, serum osteocalcin (OCN), and urinary deoxy-pyridinoline (DPD); increased bone mineral density (BMD); and improved micro-architectural properties in OVX mice...
May 22, 2017: Nutrients
https://www.readbyqxmd.com/read/28530852/long-term-risk-of-subsequent-malignant-neoplasms-after-treatment-of-childhood-cancer-in-the-dcog-later-study-cohort-role-of-chemotherapy
#3
Jop C Teepen, Flora E van Leeuwen, Wim J Tissing, Eline van Dulmen-den Broeder, Marry M van den Heuvel-Eibrink, Helena J van der Pal, Jacqueline J Loonen, Dorine Bresters, Birgitta Versluys, Sebastian J C M M Neggers, Monique W M Jaspers, Michael Hauptmann, Margriet van der Heiden-van der Loo, Otto Visser, Leontien C M Kremer, Cécile M Ronckers
Purpose Childhood cancer survivors (CCSs) are at increased risk for subsequent malignant neoplasms (SMNs). We evaluated the long-term risk of SMNs in a well-characterized cohort of 5-year CCSs, with a particular focus on individual chemotherapeutic agents and solid cancer risk. Methods The Dutch Childhood Cancer Oncology Group-Long-Term Effects After Childhood Cancer cohort includes 6,165 5-year CCSs diagnosed between 1963 and 2001 in the Netherlands. SMNs were identified by linkages with the Netherlands Cancer Registry, the Dutch Pathology Registry, and medical chart review...
May 22, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28530640/genetic-regulation-of-the-runx-transcription-factor-family-has-antitumor-effects
#4
Ken Morita, Kensho Suzuki, Shintaro Maeda, Akihiko Matsuo, Yoshihide Mitsuda, Chieko Tokushige, Gengo Kashiwazaki, Junichi Taniguchi, Rina Maeda, Mina Noura, Masahiro Hirata, Tatsuki Kataoka, Ayaka Yano, Yoshimi Yamada, Hiroki Kiyose, Mayu Tokumasu, Hidemasa Matsuo, Sunao Tanaka, Yasushi Okuno, Manabu Muto, Kazuhito Naka, Kosei Ito, Toshio Kitamura, Yasufumi Kaneda, Paul P Liu, Toshikazu Bando, Souichi Adachi, Hiroshi Sugiyama, Yasuhiko Kamikubo
Runt-related transcription factor 1 (RUNX1) is generally considered to function as a tumor suppressor in the development of leukemia, but a growing body of evidence suggests that it has pro-oncogenic properties in acute myeloid leukemia (AML). Here we have demonstrated that the antileukemic effect mediated by RUNX1 depletion is highly dependent on a functional p53-mediated cell death pathway. Increased expression of other RUNX family members, including RUNX2 and RUNX3, compensated for the antitumor effect elicited by RUNX1 silencing, and simultaneous attenuation of all RUNX family members as a cluster led to a much stronger antitumor effect relative to suppression of individual RUNX members...
May 22, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28530540/novel-n-mustard-benzimidazoles-benzothiazoles-hybrids-synthesis-and-anticancer-evaluation
#5
Dilip P Detroja, Tai-Lin Chen, Yi-Wen Lin, Tsai-Yi Yen, Ming-Hsi Wu, Tung-Hu Tsai, Krunal Maheriya, Rajesh Kakadiya, Te-Chang Lee, Anamik Shah, Tsann-Long Su
BACKGROUND: Bendamustine, an N-mustard-benzoimidazole hybrid conjugate, was recently approved for the treatment of chronic lymphocytic leukemia. However, the short half-life of bendamustine may limit its clinical applications. OBJECTIVE: The purpose of this study is to design and synthesize compounds with a more favorable pharmacokinetic profile. METHODS: We synthesized a series of hybrid molecules comprising a phenyl N-mustard moiety and benzothiazole or benzimidazole scaffold linked via an ureido linker and evaluated their antitumor activity and plasma stability...
May 22, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28530458/-early-symptoms-of-childhood-malignant-diseases
#6
Zsuzsanna Erzsébet Papp, Izabella Kelemen, Adrienne Horváth
INTRODUCTION: Childhood malignant diseases are rare in pediatric pathology. Early symptoms are not specific, fatigue, pallor, compression signs and bone marrow failure are often mentioned. AIM: To summarize the most frequent early symptoms of childhood malignancies in order to help the physicians in the early recognition. METHOD: In our retrospective study, we processed a period of 5 years between 2012-2016, with an accent on the onset manifestations of malignancies...
May 2017: Orvosi Hetilap
https://www.readbyqxmd.com/read/28529924/regulation-of-cancer-cell-responsiveness-to-ionizing-radiation-treatment-by-cyclic-amp-response-element-binding-nuclear-transcription-factor
#7
REVIEW
Francesca D'Auria, Lucia Centurione, Maria Antonietta Centurione, Antonio Angelini, Roberta Di Pietro
Cyclic AMP response element binding (CREB) protein is a member of the CREB/activating transcription factor (ATF) family of transcription factors that play an important role in the cell response to different environmental stimuli leading to proliferation, differentiation, apoptosis, and survival. A number of studies highlight the involvement of CREB in the resistance to ionizing radiation (IR) therapy, demonstrating a relationship between IR-induced CREB family members' activation and cell survival. Consistent with these observations, we have recently demonstrated that CREB and ATF-1 are expressed in leukemia cell lines and that low-dose radiation treatment can trigger CREB activation, leading to survival of erythro-leukemia cells (K562)...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28529810/molecular-profiling-a-case-of-zbtb16-rara-acute-promyelocytic-leukemia
#8
Stephen E Langabeer, Lisa Preston, Johanna Kelly, Matt Goodyer, Ezzat Elhassadi, Amjad Hayat
Several variant RARA translocations have been reported in acute promyelocytic leukemia (APL) of which the t(11;17)(q23;q21), which results in a ZBTB16-RARA fusion, is the most widely identified and is largely resistant to therapy with all-trans retinoic acid (ATRA). The clinical course together with the cytogenetic and molecular characterization of a case of ATRA-unresponsive ZBTB16-RARA APL is described. Additional mutations potentially cooperating with the translocation fusion product in leukemogenesis have been hitherto unreported in ZBTB16-RARA APL and were sought by application of a next-generation sequencing approach to detect those recurrently found in myeloid malignancies...
2017: Case Reports in Hematology
https://www.readbyqxmd.com/read/28529740/copy-number-variation-and-protein-expression-of-dot1l-in-pancreatic-adenocarcinoma-as-a-potential-drug-target
#9
Heike Loeser, Dirk Waldschmidt, Fabian Kuetting, Carina Heydt, Thomas Zander, Patrick Plum, Hakan Alakus, Reinhard Buettner, Alexander Quaas
Adenocarcinoma of the pancreas has a poor prognosis. At present, no relevant personalized targets have been identified. Sequencing studies have implicated gene alterations of disruptor of telomeric silencing 1 like histone lysine methyltransferase (DOT1L) in pancreatic adenocarcinoma. DOT1L is part of the histone modification system and catalyzes methylation of H3K79, which is crucial in cell signaling and DNA damage repair. DOT1L is considered to be a target of therapy in mixed lineage leukemia gene-deficient leukemia cases and a potential target in breast carcinoma...
May 2017: Molecular and Clinical Oncology
https://www.readbyqxmd.com/read/28529625/tuberostemonine-reverses-multidrug-resistance-in-chronic-myelogenous-leukemia-cells-k562-adr
#10
Yu Jia Wang, Huan Dong Zhao, Cai Feng Zhu, Jian Li, Hong Juan Xie, Yu Xiang Chen
Objective: To investigate the reversal effect of tuberostemonine on MDR in myelogenous leukemia cells K562/ADR. Methods: Human myelogenous leukemia cells K562 and their adriamycin-resistance cells K562/ADR were used. The growth curve of cells treated by tuberostemonine and the Non-toxic concentration of tuberostemonine were determined by MTT, Cell apoptosis was determined by MTT and flow cytometry. The expression of MDR1, Survivin and Livin was detected by RT-PCR. The activity of P-gp was detected by flow cytometry...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28529314/a-critical-role-of-periostin-in-b-cell-acute-lymphoblastic-leukemia
#11
Z Ma, X Zhao, J Huang, X Jia, M Deng, D Cui, Z Du, G Fu, G Ouyang, C Xiao
Leukemia accepted article preview online, 22 May 2017. doi:10.1038/leu.2017.149.
May 22, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28529313/impact-of-killer-immunoglobulin-like-receptor-and-human-leukocyte-antigen-genotypes-on-the-efficacy-of-immunotherapy-in-acute-myeloid-leukemia
#12
E Bernson, A Hallner, F E Sander, O Wilsson, O Werlenius, A Rydström, R Kiffin, M Brune, R Foà, J Aurelius, A Martner, K Hellstrand, F B Thorén
Interactions between killer-immunoglobulin-like receptors (KIRs) and their HLA class I ligands are instrumental in natural killer (NK) cell regulation and protect normal tissue from NK cell attack. Human KIR haplotypes comprise genes encoding mainly inhibitory receptors (KIR A) or activating and inhibitory receptors (KIR B). A substantial fraction of humans lack ligands for inhibitory KIRs (iKIRs), i.e. a 'missing ligand' genotype. KIR B/x and missing ligand genotypes may thus give rise to potentially autoreactive, unlicensed NK cells...
May 22, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28529312/prognostic-impact-of-ikzf1-deletions-in-association-with-vincristine-dexamethasone-pulses-during-maintenance-treatment-of-childhood-acute-lymphoblastic-leukemia-on-trial-all-bfm-95
#13
L Hinze, A Möricke, M Zimmermann, S Junk, G Cario, E Dagdan, C P Kratz, V Conter, M Schrappe, M Stanulla
Leukemia accepted article preview online, 22 May 2017. doi:10.1038/leu.2017.154.
May 22, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28529311/spotlight-on-pomalidomide-could-less-be-more
#14
T J Zander, S Aebi, T Pabst, C Renner, C Driessen
Leukemia accepted article preview online, 22 May 2017. doi:10.1038/leu.2017.156.
May 22, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28529310/a-revisionist-history-of-adult-marrow-stem-cell-biology-or-they-forgot-about-the-discard
#15
REVIEW
P Quesenberry, L Goldberg
Leukemia accepted article preview online, 22 May 2017. doi:10.1038/leu.2017.155.
May 22, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28529309/an-unusual-activating-insertion-deletion-mpl-mutant-in-primary-myelofibrosis
#16
J-P Defour, Y Hoade, A-M Reuther, A Callaway, D Ward, F Chen, S N Constantinescu, N C P Cross
Leukemia accepted article preview online, 22 May 2017. doi:10.1038/leu.2017.153.
May 22, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28529308/assessing-the-thrombotic-risk-of-patients-with-essential-thrombocythemia-in-the-genomic-era
#17
REVIEW
L Falchi, H M Kantarjian, S Verstovsek
The molecular characterization of myeloproliferative neoplasms (MPN), including essential thrombocythemia (ET), has enabled deeper understanding of their pathogenesis. A driver lesion, namely, Janus kinase (JAK)2V617F, calreticulin (CALR) or myeloproliferative leukemia (MPL) gene mutation can be identified in the vast majority of patients. Each of these mutations is associated with distinct clinical features and may modulate the patients' clinical course, risk of complications, including vascular events, and survival...
May 22, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28529307/genetic-deletion-of-sost-or-pharmacological-inhibition-of-sclerostin-prevent-multiple-myeloma-induced-bone-disease-without-affecting-tumor-growth
#18
J Delgado-Calle, J Anderson, M D Cregor, K W Condon, S A Kuhstoss, L I Plotkin, T Bellido, G D Roodman
Multiple myeloma (MM) causes lytic bone lesions due to increased bone resorption and concomitant marked suppression of bone formation. Sclerostin (Scl) levels, an osteocyte-derived inhibitor of Wnt/β-catenin signaling, are elevated in MM patient sera and are increased in osteocytes in MM-bearing mice. We show here that genetic deletion of Sost, the gene encoding Scl, prevented MM-induced bone disease in an immune-deficient mouse model of early MM, and that administration of anti-Scl antibody (Scl-Ab) increased bone mass and decreases osteolysis in immune-competent mice with established MM...
May 22, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28529020/nosocomial-legionellosis-and-invasive-aspergillosis-in-a-child-with-t-lymphoblastic-leukemia
#19
Rhoikos Furtwängler, Uwe Schlotthauer, Barbara Gärtner, Norbert Graf, Arne Simon
Invasive aspergillosis of the lungs and the central nervous system and Legionella pneumophilia serotype 1 infection of the lungs were diagnosed in a 22-month old child during inpatient induction treatment for T-lymphoblastic leukemia. Environmental investigations i.e. samples from the hospital water system did not reveal any Legionella. The patient may have been exposed to waterborne pathogens despite terminal water filtration due to a technical device to release residual tap water from the hose after showering...
May 13, 2017: International Journal of Hygiene and Environmental Health
https://www.readbyqxmd.com/read/28528709/association-between-the-killer-cell-immunoglobulin-like-receptor-a-haplotype-and-childhood-acute-lymphoblastic-leukemia
#20
Awad E Osman, Abdullah Aljuryan, Hanan Al-Harthi, Mai Almeshari
Killer immunoglobulin-like receptors (KIRs) have the ability to regulate Natural killer (NK) cell function through inhibition/activation mechanisms. Healthy human cells express HLA class I ligands on their surface, which are recognized by NK cells to avoid spontaneous cell destruction. The associations of KIRs and/or HLA class 1 ligands in leukemic patients have been studied in some populations, with some of these studies demonstrating an association of specific types with leukemia. KIRs and their corresponding HLA class 1 ligands were investigated in Saudi patients with ALL and AML and compared to healthy controls...
May 18, 2017: Human Immunology
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