Decitabine maintains hematopoietic precursor self-renewal by preventing repression of stem cell genes by a differentiation-inducing stimulus.

abstract：:Constitutive activation of Janus kinases (JAKs) and signal transducers and activators of transcription (STAT) occurs at very high frequency in various hematopoietic malignancies and solid tumors. It has been demonstrated that the tyrosine kinase inhibitor, AG-490, selectively blocks JAK activity and completely elimina...

journal_title：Molecular cancer therapeutics

authors： Burdelya L,Catlett-Falcone R,Levitzki A,Cheng F,Mora LB,Sotomayor E,Coppola D,Sun J,Sebti S,Dalton WS,Jove R,Yu H

更新日期：2002-09-01 00:00:00

abstract：:Antibody-drug conjugates (ADC), potent cytotoxic drugs linked to antibodies via chemical linkers, allow specific targeting of drugs to neoplastic cells. We have used this technology to develop the ADC DCDT2980S that targets CD22, an antigen with expression limited to B cells and the vast majority of non-Hodgkin lympho...

journal_title：Molecular cancer therapeutics

authors： Li D,Poon KA,Yu SF,Dere R,Go M,Lau J,Zheng B,Elkins K,Danilenko D,Kozak KR,Chan P,Chuh J,Shi X,Nazzal D,Fuh F,McBride J,Ramakrishnan V,de Tute R,Rawstron A,Jack AS,Deng R,Chu YW,Dornan D,Williams M,Ho W,

更新日期：2013-07-01 00:00:00

abstract：:A novel series of 3,5-diaryl-oxadiazoles was identified as apoptosis-inducing agents through our cell and chemical genetics-based screening assay for compounds that induce apoptosis using a chemical genetics approach. Several analogues from this series including MX-74420 and MX-126374 were further characterized. MX-12...

journal_title：Molecular cancer therapeutics

authors： Jessen KA,English NM,Yu Wang J,Maliartchouk S,Archer SP,Qiu L,Brand R,Kuemmerle J,Zhang HZ,Gehlsen K,Drewe J,Tseng B,Cai SX,Kasibhatla S

更新日期：2005-05-01 00:00:00

abstract：:Tumor cells are efficiently killed after incubation with alpha-emitter immunoconjugates targeting tumor-specific antigens. Therefore, application of alpha-emitter immunoconjugates is a promising therapeutic option for treatment of carcinomas that are characterized by dissemination of single tumor cells in the peritone...

journal_title：Molecular cancer therapeutics

authors： Seidl C,Port M,Gilbertz KP,Morgenstern A,Bruchertseifer F,Schwaiger M,Röper B,Senekowitsch-Schmidtke R,Abend M

更新日期：2007-08-01 00:00:00

abstract：:Previous work has shown that cisplatin (CDDP) becomes concentrated in lysosomes, and that acquired resistance to CDDP is associated with abnormalities of protein trafficking and secretion. The lysosomal compartment in CDDP-sensitive 2008 human ovarian carcinoma cells was compared with that in CDDP-resistant 2008/C13*5...

journal_title：Molecular cancer therapeutics

authors： Safaei R,Larson BJ,Cheng TC,Gibson MA,Otani S,Naerdemann W,Howell SB

更新日期：2005-10-01 00:00:00

abstract：:Cytochrome P450 1B1 (CYP1B1) is found in tumor tissue and is suspected to play a role in oncogenesis and drug resistance. CYP1B1 gene polymorphisms have been associated with the risk of developing lung and other cancers. They may be associated with tumor response to anticancer drugs. We have determined 4 frequent nons...

journal_title：Molecular cancer therapeutics

authors： Laroche-Clary A,Le Morvan V,Yamori T,Robert J

更新日期：2010-12-01 00:00:00

abstract：:DNA double-strand breaks (DSB) are the most cytotoxic lesions induced by topoisomerase II poisons. Nonhomologous end joining (NHEJ) is a major pathway for DSB repair and requires DNA-dependent protein kinase (DNA-PK) activity. DNA-PK catalytic subunit (DNA-PKcs) is structurally similar to PI-3K, which promotes cell su...

journal_title：Molecular cancer therapeutics

authors： Munck JM,Batey MA,Zhao Y,Jenkins H,Richardson CJ,Cano C,Tavecchio M,Barbeau J,Bardos J,Cornell L,Griffin RJ,Menear K,Slade A,Thommes P,Martin NM,Newell DR,Smith GC,Curtin NJ

更新日期：2012-08-01 00:00:00

abstract：:Why does it seem that, repeatedly, when a new treatment with a striking effect is discovered in the cancer field, it is effective for a very rare cancer type? For example, groundbreaking therapeutic discoveries have been made for extremely uncommon malignancies such as hairy cell leukemia, chronic myelogenous leukemia...

journal_title：Molecular cancer therapeutics

authors： Braiteh F,Kurzrock R

更新日期：2007-04-01 00:00:00

abstract：:In bone metastatic lesions, osteoclasts play a key role in the development of osteolysis. Previous studies have shown that macrophage colony-stimulating factor (M-CSF) is important for the differentiation of osteoclasts. In this study, we investigated whether an inhibitor of M-CSF receptor (c-Fms) suppresses osteoclas...

journal_title：Molecular cancer therapeutics

authors： Ohno H,Kubo K,Murooka H,Kobayashi Y,Nishitoba T,Shibuya M,Yoneda T,Isoe T

更新日期：2006-11-01 00:00:00

abstract：:Tumor recurrence after curative resection remains a major problem in patients with locally advanced colorectal cancer treated with adjuvant chemotherapy. Genetic single-nucleotide polymorphisms (SNP) may serve as useful molecular markers to predict clinical outcomes in these patients and identify targets for future dr...

journal_title：Molecular cancer therapeutics

authors： Ning Y,Gerger A,Zhang W,Hanna DL,Yang D,Winder T,Wakatsuki T,Labonte MJ,Stintzing S,Volz N,Sunakawa Y,Stremitzer S,El-Khoueiry R,Lenz HJ

更新日期：2014-02-01 00:00:00

abstract：:Isodon diterpenoids have received considerable phytochemical and biological attention for their strong antitumor activity with low toxicity. In this study, ExcisaninA, a diterpenoid compound purified from Isodon MacrocalyxinD, was tested on human Hep3B and MDA-MB-453 cell lines and Hep3B xenograft models. The results ...

journal_title：Molecular cancer therapeutics

authors： Deng R,Tang J,Xia LP,Li DD,Zhou WJ,Wang LL,Feng GK,Zeng YX,Gao YH,Zhu XF

更新日期：2009-04-01 00:00:00

abstract：:The efficacy of photodynamic therapy (PDT) for epithelial cancers is increased when PDT is combined with calcitriol (Vit D), a form of differentiation therapy (DT). Here, we describe an underlying mechanism for this effect. Differentiation-promoting agents are known to upregulate CCAAT/enhancer-binding proteins (C/EBP...

journal_title：Molecular cancer therapeutics

authors： Anand S,Hasan T,Maytin EV

更新日期：2013-08-01 00:00:00

abstract：:Hepatocellular carcinoma (HCC) can arise from chronic inflammation due to viral infection, organ damage, drug toxicity, or alcohol abuse. Moreover, gene desensitization via aberrant CpG island methylation is a frequent epigenetic defect in HCC. However, the details of how inflammation is linked with epigenetic-mediate...

journal_title：Molecular cancer therapeutics

authors： Li CF,Tsai HH,Ko CY,Pan YC,Yen CJ,Lai HY,Yuh CH,Wu WC,Wang JM

更新日期：2015-11-01 00:00:00

abstract：:Targeting death receptor-mediated apoptosis has emerged as an effective strategy for cancer therapy. However, certain types of cancer cells are intrinsically resistant to death receptor-mediated apoptosis. In an effort to identify agents that can sensitize cancer cells to death receptor-induced apoptosis, we have iden...

journal_title：Molecular cancer therapeutics

authors： Raja SM,Chen S,Yue P,Acker TM,Lefkove B,Arbiser JL,Khuri FR,Sun SY

更新日期：2008-07-01 00:00:00

abstract：:Chronic myelogenous leukemia is characterized by the presence of the chimeric BCR-ABL gene, which is expressed as the constitutively active Bcr-Abl kinase. Although kinase activity is directly responsible for the clinical phenotype, current diagnostic and prognostic methods focus on a genetic classification system in ...

journal_title：Molecular cancer therapeutics

authors： Sylvester JE,Kron SJ

更新日期：2010-05-01 00:00:00

abstract：:Several antiangiogenic drugs targeting VEGF/VEGF receptor (VEGFR) that were approved by the Food and Drug Administration for many cancer types, including colorectal and lung cancer, can effectively reduce tumor growth. However, targeting the VEGF signaling pathway will probably influence the normal function of endothe...

journal_title：Molecular cancer therapeutics

authors： Chen CT,Yamaguchi H,Lee HJ,Du Y,Lee HH,Xia W,Yu WH,Hsu JL,Yen CJ,Sun HL,Wang Y,Yeh ET,Hortobagyi GN,Hung MC

更新日期：2011-08-01 00:00:00

abstract：:Eribulin (E7389), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules. At low concentrations, it suppresses the growth phase of microtubule dynamic instability in interphase cells, arrests mitosis, and induces apoptosis, suggesting that suppression o...

journal_title：Molecular cancer therapeutics

authors： Okouneva T,Azarenko O,Wilson L,Littlefield BA,Jordan MA

更新日期：2008-07-01 00:00:00

abstract：:This study aims to explore whether E545K, the most common hotspot mutation of PIK3CA in cervical cancer, confers radioresistance to cervical cancer cells, to demonstrate the underling mechanism, and to develop the effective targets. SiHa and MS751 cells with PIK3CA-WT and PIK3CA-E545K were established by lentiviral tr...

journal_title：Molecular cancer therapeutics

authors： Jiang W,Wu Y,He T,Zhu H,Ke G,Xiang L,Yang H

更新日期：2020-02-01 00:00:00

abstract：:Patients with non-small cell lung carcinoma (NSCLC) with activating mutations in epidermal growth factor receptor (EGFR) initially respond well to the EGFR inhibitors erlotinib and gefitinib. However, all patients relapse because of the emergence of drug-resistant mutations, with T790M mutations accounting for approxi...

journal_title：Molecular cancer therapeutics

authors： Tjin Tham Sjin R,Lee K,Walter AO,Dubrovskiy A,Sheets M,Martin TS,Labenski MT,Zhu Z,Tester R,Karp R,Medikonda A,Chaturvedi P,Ren Y,Haringsma H,Etter J,Raponi M,Simmons AD,Harding TC,Niu D,Nacht M,Westlin WF,Pette

更新日期：2014-06-01 00:00:00

abstract：:Activation of beta-catenin is a critical step in the pathogenesis of many common human cancers and is the initiating event in adenocarcinoma of the colon. Because activation of beta-catenin provides a gain-of-function, it is tempting to speculate that specific pharmacological inhibition of activated beta-catenin might...

journal_title：Molecular cancer therapeutics

authors： Kim JS,Crooks H,Foxworth A,Waldman T

更新日期：2002-12-01 00:00:00

abstract：:Mis-expression of microRNAs (miRNA) is widespread in human cancers, including in pancreatic cancer. Aberrations of miRNA include overexpression of oncogenic miRs (Onco-miRs) or downregulation of so-called tumor suppressor TSG-miRs. Restitution of TSG-miRs in cancer cells through systemic delivery is a promising avenue...

journal_title：Molecular cancer therapeutics

authors： Pramanik D,Campbell NR,Karikari C,Chivukula R,Kent OA,Mendell JT,Maitra A

更新日期：2011-08-01 00:00:00

abstract：:Epidermal growth factor receptor (EGFR) vIII is a mutated EGFR that is frequently overexpressed in glioblastomas and implicated in response to receptor tyrosine kinase inhibitors. In this study, we investigate the effect of ZD6474 (ZACTIMA, vandetanib), a dual inhibitor for vascular endothelial growth factor receptor ...

journal_title：Molecular cancer therapeutics

authors： Yiin JJ,Hu B,Schornack PA,Sengar RS,Liu KW,Feng H,Lieberman FS,Chiou SH,Sarkaria JN,Wiener EC,Ma HI,Cheng SY

更新日期：2010-04-01 00:00:00

abstract：:The two-step transcriptional activation (TSTA) mechanism in gene therapy amplifies cell type-specific promoter activity, allowing for increased levels of gene expression in target tissues. In this system, the specific promoter drives expression of a strong transcriptional activator that binds to DNA target sequences l...

journal_title：Molecular cancer therapeutics

authors： Arendt ML,Nasir L,Morgan IM

更新日期：2009-12-01 00:00:00

abstract：:Nonselective inhibitors of human histone deacetylases (HDAC) are known to have antitumor activity in mice in vivo, and several of them are under clinical investigation. The first of these, Vorinostat (SAHA), has been approved for treatment of cutaneous T-cell lymphoma. Questions remain concerning which HDAC isotype(s)...

journal_title：Molecular cancer therapeutics

authors： Fournel M,Bonfils C,Hou Y,Yan PT,Trachy-Bourget MC,Kalita A,Liu J,Lu AH,Zhou NZ,Robert MF,Gillespie J,Wang JJ,Ste-Croix H,Rahil J,Lefebvre S,Moradei O,Delorme D,Macleod AR,Besterman JM,Li Z

更新日期：2008-04-01 00:00:00

abstract：:Cell cycle regulators, such as the CDC25 phosphatases, are potential targets for the development of new anticancer drugs. Here we report the identification and the characterization of BN82685, a quinone-based CDC25 inhibitor that is active in vitro and in vivo. BN82685 inhibits recombinant CDC25A, B, and C phosphatase...

journal_title：Molecular cancer therapeutics

authors： Brezak MC,Quaranta M,Contour-Galcera MO,Lavergne O,Mondesert O,Auvray P,Kasprzyk PG,Prevost GP,Ducommun B

更新日期：2005-09-01 00:00:00

abstract：:Tumor-associated urokinase plasminogen activator (uPA) is a critical marker of invasion and metastasis, has strong prognostic relevance, and is thus a potential therapeutic target. Experimental data published to date has established the proof-of-principle of uPA targeting by (213)Bi-labeled plasminogen activator inhib...

journal_title：Molecular cancer therapeutics

authors： Stutchbury TK,Al-Ejeh F,Stillfried GE,Croucher DR,Andrews J,Irving D,Links M,Ranson M

更新日期：2007-01-01 00:00:00

abstract：:The ability of the epidermal growth factor receptor inhibitor gefitinib (Iressa) to prevent/treat methylnitrosourea (MNU)-induced mammary cancers and to modulate biomarkers in female Sprague-Dawley rats was examined. Rats were given a single dose of MNU (75 mg/kg body weight) at 50 days of age. In the prevention studi...

journal_title：Molecular cancer therapeutics

authors： Lubet RA,Szabo E,Christov K,Bode AM,Ericson ME,Steele VE,Juliana MM,Grubbs CJ

更新日期：2008-04-01 00:00:00

abstract：:The present studies have determined whether interactions between the cyclin-dependent kinase inhibitor flavopiridol and the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA; vorinostat; Zolinza) occur in breast cancer cells. MDA-MB-231 and MCF7 cells were treated with flavopiridol (25-100 nmol/L) an...

journal_title：Molecular cancer therapeutics

authors： Mitchell C,Park MA,Zhang G,Yacoub A,Curiel DT,Fisher PB,Roberts JD,Grant S,Dent P

更新日期：2007-12-01 00:00:00

abstract：:Patients with non-small cell lung cancer (NSCLC) harboring activating mutations in the epidermal growth factor receptor (EGFR) kinase domain tend to respond well to the tyrosine kinase inhibitors, gefitinib and erlotinib. However, following clinical response, these patients typically relapse within a year of treatment...

journal_title：Molecular cancer therapeutics

authors： Godin-Heymann N,Ulkus L,Brannigan BW,McDermott U,Lamb J,Maheswaran S,Settleman J,Haber DA

更新日期：2008-04-01 00:00:00

abstract：:Melanoma is a highly drug-resistant cancer with resistance developing to agents targeting single proteins. To circumvent this problem, a new class of agent inhibiting multiple key pathways important in this disease is being developed to reduce the likelihood of developing resistant disease. The phosphoinositide 3-kina...

journal_title：Molecular cancer therapeutics

authors： Gowda R,Madhunapantula SV,Kuzu OF,Sharma A,Robertson GP

更新日期：2014-07-01 00:00:00