当前位置： SCI文献检索 > CANCER LETTERS期刊下所有文献 > Novel anticancer compound [trifluoromethyl-substituted pyrazole N-nucleoside] inhibits FLT3 activity to induce differentiation in acute myeloid leukemia cells.

Novel anticancer compound [trifluoromethyl-substituted pyrazole N-nucleoside] inhibits FLT3 activity to induce differentiation in acute myeloid leukemia cells.

Abstract：

:Anticancer properties of chemically synthesized compounds have continuously been optimized for better efficacy and selectivity. Derivatives of heterocyclic compounds are well known to have selective antiproliferative effect against many types of cancer. In this study, we investigated the ability of an indigenously synthesized anticancer molecule, G-11 [1-(2",3",4",6"-Tetra-O-acetyl-β-D-glucopyranosyl)-4-(3'-trifluoromethylphenylhydrazono)-3-trifluoromethyl-1,4-dihydropyrazol-5-one], to cause selective cytotoxicity and induce differentiation in the acute myeloid leukemia HL-60 cells. G-11 was able to exert cytotoxic effect on hematological (Jurkat, U937, K562, HL-60, CCRF-SB) and solid tumor (MCF-7, HepG2, HeLa, Caco-2) cell lines, with IC50 values significantly lower than noncancerous cells (HEK-293, BJ and Vero) and normal peripheral blood mononuclear cells. G-11 induced differentiation of HL-60 cells to granulocytes and monocytes/macrophages by inhibiting the activation of FLT3 (CD135 tyrosine kinase). ITD-FLT3 mutation found in many acute myeloid leukemia patients could also be targeted by G-11 as exhibited by its inhibitory effect on MOLM-13 and MV4-11 cell lines. Molecular docking studies suggest the involvement of Leu616, Asp698, Cys694 and Cys828 residues in binding of G-11 to FLT3. The ability of G-11 to cause selective cytotoxicity and induce differentiation in cancer cells could be clinically relevant for therapeutic gains.

journal_name

Cancer Lett

journal_title

Cancer letters

authors

Saleh AM,Taha MO,Aziz MA,Al-Qudah MA,AbuTayeh RF,Rizvi SA

doi

10.1016/j.canlet.2016.02.028

subject

Has Abstract

pub_date

2016-06-01 00:00:00

pages

199-208

issue

2

eissn

0304-3835

issn

1872-7980

pii

S0304-3835(16)30096-9

journal_volume

375

pub_type

杂志文章

相关文献

CANCER LETTERS文献大全
  • Combination therapy: histone deacetylase inhibitors and platinum-based chemotherapeutics for cancer.

    abstract：:One of the most promising strategies to increase the efficacy of standard chemotherapy drugs is by combining them with low doses of histone deacetylases inhibitors (HDACis). Regarded as chemosensitizers, the addition of well-tolerated doses of HDACis to platinum-based chemotherapeutics has been proven in vitro and in ...

    journal_title：Cancer letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.canlet.2012.09.018

    authors： Diyabalanage HV,Granda ML,Hooker JM

    更新日期：2013-02-01 00:00:00

  • Alterations at the Ink4a locus in transplacentally induced murine lung tumors.

    abstract：:The malignant phenotype results from multiple genetic alterations, including the activation of oncogenes and inactivation of tumor suppressor genes. Activation of the Ki-ras oncogene has been implicated as an early event in the pathogenesis of lung adenocarcinomas in humans and experimental animal models. Previous stu...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/s0304-3835(01)00647-4

    authors： Mizesko MC,Grewe C,Grabner A,Miller MS

    更新日期：2001-10-22 00:00:00

  • Role of mitochondrial complexes I and II, reactive oxygen species and arachidonic acid metabolism in deoxycholate-induced apoptosis.

    abstract：:Bile acids are promoters of colon cancer; however, the mechanism(s) of action of this tumor promoter are largely unknown. Bile acids induce apoptosis in colon epithelial cells and it is probable that the modulation of apoptosis contributes, in part, to colon carcinogenesis. We tested the hypothesis that damage to mito...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/s0304-3835(01)00786-8

    authors： Washo-Stultz D,Crowley-Weber CL,Dvorakova K,Bernstein C,Bernstein H,Kunke K,Waltmire CN,Garewal H,Payne CM

    更新日期：2002-03-28 00:00:00

  • Targeting LRP8 inhibits breast cancer stem cells in triple-negative breast cancer.

    abstract：:Triple-negative breast cancer (TNBC) is the most difficult subtype of breast cancer to treat due to a paucity of effective targeted therapies. Many studies have reported that breast cancer stem cells (BCSCs) are enriched in TNBC and are responsible for chemoresistance and metastasis. In this study, we identify LRP8 as...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2018.09.022

    authors： Lin CC,Lo MC,Moody R,Jiang H,Harouaka R,Stevers N,Tinsley S,Gasparyan M,Wicha M,Sun D

    更新日期：2018-12-01 00:00:00

  • Small molecule BKM1972 inhibits human prostate cancer growth and overcomes docetaxel resistance in intraosseous models.

    abstract：:Bone metastasis is a major cause of prostate cancer (PCa) mortality. Although docetaxel chemotherapy initially extends patients' survival, in most cases PCa becomes chemoresistant and eventually progresses without a cure. In this study, we developed a novel small-molecule compound BKM1972, which exhibited potent in vi...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2019.01.010

    authors： Chen Y,Gera L,Zhang S,Li X,Yang Y,Mamouni K,Wu AY,Liu H,Kucuk O,Wu D

    更新日期：2019-04-01 00:00:00

  • Dietary genistein suppresses chemically induced prostate cancer in Lobund-Wistar rats.

    abstract：:Epidemiological reports suggest that Asians consuming a diet high in soy have a low incidence of clinically manifested prostate cancer. We have tested the hypothesis that life-time exposure to genistein, the primary isoflavone component of soy, is responsible for this protective effect. Lobund-Wistar rats were exposed...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/s0304-3835(01)00811-4

    authors： Wang J,Eltoum IE,Lamartiniere CA

    更新日期：2002-12-01 00:00:00

  • The potentiation of radiation response on murine tumor by fludarabine phosphate.

    abstract：:Fludarabine phosphate is a synthetic analog of beta-arabinofuranosyl adenine (beta-ara-A), an anti-viral agent. Since beta-ara-A has been shown to be an effective inhibitor of potentially lethal damage (PLD) repair in cell culture system but ineffective in in vivo tumors, we carried out experiments to determine whethe...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/0304-3835(86)90168-0

    authors： Kim JH,Alfieri AA,Kim SH,Fuks Z

    更新日期：1986-04-01 00:00:00

  • Inhibition by zinc of hepatic lysosomal release of beta-glucuronidase induced by phorbol-12-myristate-13-acetate (PMA).

    abstract：:The tumor promoter, phorbol-12-myristate-13-acetate (PMA), elicited a significant increase in lysosomal membrane permeability, as measured by release of free beta-glucurnidase, in guinea pig and hamster isolated hepatic lysosomes in vitro. This response was antagonized by zinc sulfate; zinc compounds having previously...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/0304-3835(80)90065-8

    authors： Pfeiffer CJ,Cho CH

    更新日期：1980-07-01 00:00:00

  • MDM2-NFAT1 dual inhibitor, MA242: Effective against hepatocellular carcinoma, independent of p53.

    abstract：:The overexpression of the MDM2 oncoprotein frequently occurs in hepatocellular carcinoma (HCC). Small molecules that inhibit MDM2-p53 binding show efficacy against p53 wild-type HCC, but most patients have p53-mutant tumors and intrinsic resistance to such MDM2 inhibitors. We have recently discovered that the NFAT1 tr...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2019.114429

    authors： Wang W,Cheng JW,Qin JJ,Hu B,Li X,Nijampatnam B,Velu SE,Fan J,Yang XR,Zhang R

    更新日期：2019-09-10 00:00:00

  • Promotion of mouse two-stage skin carcinogenesis by diacylglycerol-rich edible oil.

    abstract：:Tumor promotion potential of diacylglycerol (DAG)-rich edible oil was examined using a two-stage mouse skin carcinogenesis model initiated with 7,12-dimethylbenz[a]anthracene (DMBA). Topical treatment with 75 mg DAG oil once a day for 5 days/week for 35 weeks caused papillomas in 4 of 23 (17%) DMBA-treated female ICR ...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2008.10.016

    authors： Takasuka N,Takahashi M,Hori Y,Kitahashi T,Iigo M,Imai T,Yoshimi N,Sugimura T,Wakabayashi K

    更新日期：2009-03-08 00:00:00

  • A novel integrated system using patient-derived glioma cerebral organoids and xenografts for disease modeling and drug screening.

    abstract：:A physiologically relevant glioma tumor model is important to the study of disease progression and screening drug candidates. However, current preclinical glioma models lack the brain microenvironment, and the established tumor cell lines do not represent glioma biology and cannot be used to evaluate the therapeutic e...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2020.12.013

    authors： Zhang L,Liu F,Weygant N,Zhang J,Hu P,Qin Z,Yang J,Cheng Q,Fan F,Zeng Y,Tang Y,Li Y,Tang A,He F,Peng J,Liao W,Hu Z,Li M,Liu Z

    更新日期：2021-03-01 00:00:00

  • Hypericin-mediated photodynamic therapy elicits differential interleukin-6 response in nasopharyngeal cancer.

    abstract：:Cytokines induce inflammatory and immune responses in tumors after photodynamic therapy (PDT). Since there are no reports of IL-6 in nasopharyngeal cancer (NPC) cells following PDT, we evaluated IL-6 expression in two different NPC tumors after hypericin mediated PDT. Interleukin-6 transcription was significantly upre...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2005.04.013

    authors： Du H,Bay BH,Mahendran R,Olivo M

    更新日期：2006-04-28 00:00:00

  • Oral artemisinin prevents and delays the development of 7,12-dimethylbenz[a]anthracene (DMBA)-induced breast cancer in the rat.

    abstract：:Artemisinin, a compound isolated from the sweet wormwood Artemisia annua L., has previously been shown to have selective toxicity towards cancer cells in vitro. In the present experiment, we studied the potential of artemisinin to prevent breast cancer development in rats treated with a single oral dose (50mg/kg) of 7...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2005.01.019

    authors： Lai H,Singh NP

    更新日期：2006-01-08 00:00:00

  • Resistance factors in colon cancer tissue and the adjacent normal colon tissue: glutathione S-transferases alpha and pi, glutathione and aldehyde dehydrogenase.

    abstract：:Glutathione S-transferases (GST) alpha and pi, glutathione (GSH) and aldehyde dehydrogenase (ADH) were determined in colorectal cancer tissue specimens and in the adjacent normal colon tissue. The median contents in normal and cancer tissue were 8.1 (2.3-30.3) (5-95% quantiles) and 15.1 (5.3-50.3) microg/mg protein fo...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/s0304-3835(98)00059-7

    authors： Hengstler JG,Böttger T,Tanner B,Dietrich B,Henrich M,Knapstein PG,Junginger T,Oesch F

    更新日期：1998-06-05 00:00:00

  • An inverse correlation between expression of NCAM-A and the matrix-metalloproteinases gelatinase-A and gelatinase-B in human glioma cells in vitro.

    abstract：:Matrix metalloproteinases (MMPs) are an homologous family of proteolytic enzymes capable of degrading components of the extracellular matrix (ECM) and thereby facilitating the invasion of tumour cells into normal tissues. The neural cell adhesion molecules (NCAMs) of neuronal and glial cells provide a Ca2+-independent...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/s0304-3835(97)00171-7

    authors： Maidment SL,Rucklidge GJ,Rooprai HK,Pilkington GJ

    更新日期：1997-06-03 00:00:00

  • Targeting autophagy by small molecule inhibitors of vacuolar protein sorting 34 (Vps34) improves the sensitivity of breast cancer cells to Sunitinib.

    abstract：:Resistance to chemotherapy is a challenging problem for treatment of cancer patients and autophagy has been shown to mediate development of resistance. In this study we systematically screened a library of 306 known anti-cancer drugs for their ability to induce autophagy using a cell-based assay. 114 of the drugs were...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2018.07.028

    authors： Dyczynski M,Yu Y,Otrocka M,Parpal S,Braga T,Henley AB,Zazzi H,Lerner M,Wennerberg K,Viklund J,Martinsson J,Grandér D,De Milito A,Pokrovskaja Tamm K

    更新日期：2018-10-28 00:00:00

  • Secretory Stanniocalcin 1 promotes metastasis of hepatocellular carcinoma through activation of JNK signaling pathway.

    abstract：:The hypoxic microenvironment is well-characterized in hepatocellular carcinoma (HCC). Delineation of hypoxia-responsive events is an integral part to understand the pathogenesis of HCC. We studied the functional role and clinical relevance of Stanniocalcin 1 (STC1), a hypoxia-induced molecular target, in HCC. In our c...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2017.06.034

    authors： Chan KK,Leung CO,Wong CC,Ho DW,Chok KS,Lai CL,Ng IO,Lo RC

    更新日期：2017-09-10 00:00:00

  • Radiation promotes malignant progression of glioma cells through HIF-1alpha stabilization.

    abstract：:Given its contribution to malignant phenotypes of cancer, tumor hypoxia has been considered as a potential therapeutic problem. In the stressful microenvironment condition, hypoxia inducible factor 1 (HIF1) is well known to mediate the transcriptional adaptation of cells to hypoxia and acts as a central player for the...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2014.07.048

    authors： Kim YH,Yoo KC,Cui YH,Uddin N,Lim EJ,Kim MJ,Nam SY,Kim IG,Suh Y,Lee SJ

    更新日期：2014-11-01 00:00:00

  • Metformin displays anti-myeloma activity and synergistic effect with dexamethasone in in vitro and in vivo xenograft models.

    abstract：:Epidemiologic studies and meta-analyses have suggested that patients with type 2 diabetes mellitus (T2DM) have a higher incidence of malignancies, including myeloma. Metformin is a widely prescribed antidiabetic drug. Recently, researchers have shown that metformin has direct anticancer activity against many tumor cel...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2014.09.050

    authors： Zi FM,He JS,Li Y,Wu C,Yang L,Yang Y,Wang LJ,He DH,Zhao Y,Wu WJ,Zheng GF,Han XY,Huang H,Yi Q,Cai Z

    更新日期：2015-01-28 00:00:00

  • Influence of supplemental ascorbate on the antitumor activity of 5-hydroxydopa, a purported cytotoxic metabolite.

    abstract：:The present study was conducted to clarify the mechanism responsible for enhancement of the anti-melanoma activity of levodopa methylester by supplemental ascorbate in vivo. 5-Hydroxydopa, a known cytotoxic agent and the major metabolite formed from levodopa in the presence of ascorbate and mushroom tyrosinase in vitr...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/0304-3835(85)90154-5

    authors： Pierson HF,Meadows GG

    更新日期：1985-11-01 00:00:00

  • Apicidin down-regulates human papillomavirus type 16 E6 and E7 transcripts and proteins in SiHa cervical cancer cells.

    abstract：:Virtually all cervical cancer morbidities are associated with genital skin or mucosa cell infection with human papillomavirus (HPV). The HPV oncogenic proteins E6 and E7 are able to inactivate p53 and Rb proteins, which results in malignant transformation. Employing quantitative real-time PCR and Western blot analysis...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2008.06.030

    authors： Luczak MW,Jagodzinski PP

    更新日期：2008-12-08 00:00:00

  • c-Met upregulates aquaporin 3 expression in human gastric carcinoma cells via the ERK signalling pathway.

    abstract：:Aquaporin 3 (AQP3) and c-Met are both overexpressed in human gastric carcinoma and highly associated with its metastasis and invasion. However, it still remains unknown whether c-Met and AQP3 correlate with each other. Herein, we demonstrated that c-Met expression in gastric cancer tissues significantly correlated wit...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2011.12.040

    authors： Wang J,Gui Z,Deng L,Sun M,Guo R,Zhang W,Shen L

    更新日期：2012-06-01 00:00:00

  • Metastasis of breast tumor cells to brain is suppressed by targeting RLIP alone and in combination with 2'-Hydroxyflavanone.

    abstract：:Brain metastasis is an important cause of morbidity and mortality in cancer-patients. Breast tumor cells frequently metastasize to brain and initiate severe therapeutic complications. In the present study, we evaluated the anti-metastatic effects of 2'-hydroxyflavanone (2HF) alone and in combination with RLIP targeted...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2018.09.015

    authors： Singhal J,Singhal P,Horne D,Salgia R,Awasthi S,Singhal SS

    更新日期：2018-12-01 00:00:00

  • Induction of anti-cancer T cell immunity by in situ vaccination using systemically administered nanomedicines.

    abstract：:Patients with inadequate anti-cancer T cell responses experience limited benefit from immune checkpoint inhibitors and other immunotherapies that require T cells. Therefore, treatments that induce de novo anti-cancer T cell immunity are needed. One strategy - referred to as in situ vaccination - is to deliver chemothe...

    journal_title：Cancer letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.canlet.2019.114427

    authors： Lynn GM,Laga R,Jewell CM

    更新日期：2019-09-10 00:00:00

  • Interaction of tamoxifen with cytosolic and nuclear type II estrogen binding sites (type II EBS).

    abstract：:The aim of this study was to investigate the interaction of tamoxifen (TAM) with the so-called Type II estrogen binding sites (Type II EBS) in both the cytosolic and the nuclear fraction of the ER-negative A 2780 human ovarian cancer cell line and in an ER-negative ovarian cancer tissue. Although cytosolic and nuclear...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/0304-3835(95)03922-j

    authors： Ferrandina G,Ranelletti FO,Scambia G,Benedetti Panici P,D'Agostino G,Piantelli M,Isola G,Mancuso S

    更新日期：1995-09-04 00:00:00

  • Variability of origin for the neocentromeric sequences in analphoid supernumerary marker chromosomes of well-differentiated liposarcomas.

    abstract：:Well-differentiated liposarcomas (WDLPS) and dedifferentiated liposarcomas are cytogenetically characterized by the presence of supernumerary ring or giant chromosomes containing amplified material from the 12q14-15 region. These chromosomes contain neocentromeres, which are able to bind the kinetochore proteins and t...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2008.08.025

    authors： Italiano A,Maire G,Sirvent N,Nuin PA,Keslair F,Foa C,Louis C,Aurias A,Pedeutour F

    更新日期：2009-01-18 00:00:00

  • The cellular myb oncogene is amplified, rearranged and activated in human glioblastoma cell lines.

    abstract：:The human c-myb gene which encodes a DNA binding protein and which is rarely amplified in neoplastic cells was found to be altered in four human glioblastoma cell lines. It exists in multiple copies in 2 out of 4 cases studied. The degree of amplification as determined by densitometry was about 10-fold, a rearrangemen...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/0304-3835(90)90077-b

    authors： Welter C,Henn W,Theisinger B,Fischer H,Zang KD,Blin N

    更新日期：1990-06-30 00:00:00

  • SOX7, down-regulated in colorectal cancer, induces apoptosis and inhibits proliferation of colorectal cancer cells.

    abstract：:The sex-determining region Y-box 7 (Sox7) is a member of high mobility group (HMG) transcription factor family, essential for embryonic development and endoderm differentiation. Deregulation of Wnt signaling pathway is a hallmark of colorectal cancer. Our results showed that the expression level of SOX7 was frequently...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2008.11.014

    authors： Zhang Y,Huang S,Dong W,Li L,Feng Y,Pan L,Han Z,Wang X,Ren G,Su D,Huang B,Lu J

    更新日期：2009-05-08 00:00:00

  • Magnetic polyethyleneimine (PEI) microcapsules as retrievable traps for carcinogen electrophiles formed in the gastrointestinal tract.

    abstract：:Semi-permeable magnetic microcapsules containing polyethyleneimine (PEI) have been developed as retrievable carcinogen traps. In vitro, the soluble core PEI and membrane both bound reactive substances of limited aqueous stability, such as from [14C]N-methyl-N-nitrosourea ([14C]NMU), and aqueous stable dyes of molecula...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/0304-3835(87)90101-7

    authors： Povey AC,Bartsch H,O'Neill IK

    更新日期：1987-07-01 00:00:00

  • Induction of Plac8 promotes pro-survival function of autophagy in cadmium-induced prostate carcinogenesis.

    abstract：:Chronic exposure to cadmium is known to be a risk factor for human prostate cancer. Despite over-whelming evidence of cadmium causing carcinogenicity in humans, the specific underlying molecular mechanisms that govern metal-induced cellular transformation remain unclear. Acute exposure (up to 72 h) to cadmium induces ...

    journal_title：Cancer letters

    pub_type： 杂志文章

    doi：10.1016/j.canlet.2017.08.023

    authors： Kolluru V,Pal D,Papu John AMS,Ankem MK,Freedman JH,Damodaran C

    更新日期：2017-11-01 00:00:00