DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation.

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：:The inverse association between a high enterolactone (ENL) concentration in both urine and serum, and the risk of breast cancer found in epidemiological studies suggests a chemopreventive action for ENL. However, no causal relationship has been established in clinical studies or in experimental models for breast cance...

journal_title：Molecular cancer therapeutics

authors： Saarinen NM,Huovinen R,Wärri A,Mäkelä SI,Valentín-Blasini L,Sjöholm R,Ammälä J,Lehtilä R,Eckerman C,Collan YU,Santti RS

更新日期：2002-08-01 00:00:00

abstract：:Gallium nitrate is a metallodrug with clinical efficacy in non-Hodgkin's lymphoma. Its mechanisms of antineoplastic action are not fully understood. In the present study, we investigated the roles of transferrin receptor (TfR) targeting and apoptotic pathways in gallium-induced cell death. Although DoHH2 lymphoma cell...

journal_title：Molecular cancer therapeutics

authors： Chitambar CR,Wereley JP,Matsuyama S

更新日期：2006-11-01 00:00:00

abstract：:Stem cell factor (SCF)/Kit and insulin-like growth factor-I (IGF-I)/IGF-I receptor (IGF-IR) autocrine loops play a prominent role in the growth of small cell lung cancer (SCLC). Previous data suggested that IGF-I protects cells from apoptosis induced by STI571, an efficient inhibitor of Kit signal transduction, by act...

journal_title：Molecular cancer therapeutics

authors： Warshamana-Greene GS,Litz J,Buchdunger E,Hofmann F,García-Echeverría C,Krystal GW

更新日期：2004-05-01 00:00:00

abstract：:The extracellular pH of tumor tissue is significantly lower than the extracellular pH of normal tissue, whereas the intracellular pH of both tissues is similar. In principle, extracellular acidity may be expected to enhance the intracellular uptake and cytotoxicity of weak acid chemotherapeutics that are membrane perm...

journal_title：Molecular cancer therapeutics

authors： Gerweck LE,Vijayappa S,Kozin S

更新日期：2006-05-01 00:00:00

abstract：:Several studies have identified silibinin as an anticarcinogenic agent. Recently, we showed that silibinin inhibits cell growth via G1 arrest, leading to differentiation of androgen-dependent human prostate carcinoma LNCaP cells (X. Zi and R. Agarwal, Proc. Natl. Acad. Sci. USA, 96: 7490-7495,1999). Here, we extend th...

journal_title：Molecular cancer therapeutics

authors： Tyagi A,Agarwal C,Agarwal R

更新日期：2002-05-01 00:00:00

abstract：:Phortress is a novel, potent, and selective experimental antitumor agent. Its mechanism of action involves induction of CYP1A1-catalyzed biotransformation of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203) to generate electrophilic species, which covalently bind to DNA, exacting lethal damage to sensitive tu...

journal_title：Molecular cancer therapeutics

authors： Leong CO,Suggitt M,Swaine DJ,Bibby MC,Stevens MF,Bradshaw TD

更新日期：2004-12-01 00:00:00

abstract：:Radiotherapy can be synergistically combined with immunotherapy in mouse models, extending its efficacious effects outside of the irradiated field (abscopal effects). We previously reported that a regimen encompassing local radiotherapy in combination with anti-CD137 plus anti-PD-1 mAbs achieves potent abscopal effect...

journal_title：Molecular cancer therapeutics

authors： Rodríguez-Ruiz ME,Rodríguez I,Mayorga L,Labiano T,Barbes B,Etxeberria I,Ponz-Sarvise M,Azpilikueta A,Bolaños E,Sanmamed MF,Berraondo P,Calvo FA,Barcelos-Hoff MH,Perez-Gracia JL,Melero I

更新日期：2019-03-01 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：:Previously, we constructed a recombinant Bifidobacterium longum displaying a partial mouse Wilms' tumor 1 (WT1) protein (B. longum 420) as an oral cancer vaccine using a bacterial vector and demonstrated that oral administration of B. longum 420 significantly inhibited tumor growth compared with the Db126 WT1 peptide ...

journal_title：Molecular cancer therapeutics

authors： Kitagawa K,Gonoi R,Tatsumi M,Kadowaki M,Katayama T,Hashii Y,Fujisawa M,Shirakawa T

更新日期：2019-05-01 00:00:00

abstract：:Although proteasome inhibitors such as bortezomib had significant therapeutic effects in multiple myeloma and mantel cell lymphoma, they exhibited minimal clinical activity as a monotherapy for solid tumors, including colorectal cancer. We found in this study that proteasome inhibition induced a remarkable nuclear exp...

journal_title：Molecular cancer therapeutics

authors： Wu T,Chen W,Zhong Y,Hou X,Fang S,Liu CY,Wang G,Yu T,Huang YY,Ouyang X,Li HQ,Cui L,Yang Y

更新日期：2017-04-01 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：:RX-5902 is a first-in-class anticancer agent targeting phosphorylated-p68 and attenuating nuclear shuttling of β-catenin. The purpose of this study was to evaluate the efficacy of RX-5902 in preclinical models of triple-negative breast cancer (TNBC) and to explore effects on β-catenin expression. A panel of 18 TNBC ce...

journal_title：Molecular cancer therapeutics

authors： Capasso A,Bagby SM,Dailey KL,Currimjee N,Yacob BW,Ionkina A,Frank JG,Kim DJ,George C,Lee YB,Benaim E,Gittleman B,Hartman SJ,Tan AC,Kim J,Pitts TM,Eckhardt SG,Tentler JJ,Diamond JR

更新日期：2019-11-01 00:00:00

abstract：:The androgen receptor (AR) is a key driver and therapeutic target in androgen-sensitive prostate cancer, castration-resistant prostate cancer (CRPC), and CRPC resistant to abiraterone and enzalutamide, two second-generation inhibitors of AR signaling. Because current AR inhibitors target a functioning C-terminal ligan...

journal_title：Molecular cancer therapeutics

authors： Dong J,Wu Z,Wang D,Pascal LE,Nelson JB,Wipf P,Wang Z

更新日期：2019-01-01 00:00:00

abstract：:The KiSS-1 gene has been reported to be a metastasis suppressor gene in human melanoma. The gene product was isolated from human placenta as the ligand of GPR54, a G protein-coupled receptor, and the C-terminally amidated peptide of 54 amino acids is called metastin. The binding of metastin to GPR54 has been shown to ...

journal_title：Molecular cancer therapeutics

authors： Takeda T,Kikuchi E,Mikami S,Suzuki E,Matsumoto K,Miyajima A,Okada Y,Oya M

更新日期：2012-04-01 00:00:00

abstract：:Farnesyl transferase inhibitors (FTI) exhibit anticancer activity as a single agent in preclinical studies and show promise in combination with other therapeutics in clinical trials. Previous studies show that FTIs arrest cancer cells in mitosis; however, the mechanism by which this occurs is unclear. Here, we observe...

journal_title：Molecular cancer therapeutics

authors： Schafer-Hales K,Iaconelli J,Snyder JP,Prussia A,Nettles JH,El-Naggar A,Khuri FR,Giannakakou P,Marcus AI

更新日期：2007-04-01 00:00:00

abstract：:Interference with endothelial cell metabolism is a promising, yet unexploited strategy for angiogenesis inhibition. We reported that the glucose analogue 2-deoxy-D-glucose (2-DG) inhibits angiogenesis at significantly lower concentrations than those required for tumor cytotoxicity. Here, we found that hypersensitivity...

journal_title：Molecular cancer therapeutics

authors： Kovács K,Decatur C,Toro M,Pham DG,Liu H,Jing Y,Murray TG,Lampidis TJ,Merchan JR

更新日期：2016-02-01 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：:Rac1 GTPase regulates a variety of signaling pathways that are implicated in malignant phenotypes. Here, we show that selective inhibition of Rac1 activity by the pharmacologic inhibitor NSC23766 suppressed cell growth in a panel of human breast cancer cell lines, whereas it had little toxicity to normal mammary epith...

journal_title：Molecular cancer therapeutics

authors： Yoshida T,Zhang Y,Rivera Rosado LA,Chen J,Khan T,Moon SY,Zhang B

更新日期：2010-06-01 00:00:00

abstract：:There is considerable interest in the clinical development of inhibitors of mTOR complexes mTORC1 and 2. Because mTORC1 and its downstream mRNA translation effectors may protect against genotoxic DNA damage, we investigated the inhibition of mTORC1 and mTORC1/2 in the ability to reverse platinum resistance in tissue c...

journal_title：Molecular cancer therapeutics

authors： Musa F,Alard A,David-West G,Curtin JP,Blank SV,Schneider RJ

更新日期：2016-07-01 00:00:00

abstract：:Recombinant immunotoxins, consisting of single-chain variable fragments (scFv) genetically fused to polypeptide toxins, represent potentially effective candidates for cancer therapeutics. We evaluated the affinity of various anti-Her2/neu scFv fused to recombinant gelonin (rGel) and its effect on antitumor efficacy an...

journal_title：Molecular cancer therapeutics

authors： Cao Y,Marks JD,Huang Q,Rudnick SI,Xiong C,Hittelman WN,Wen X,Marks JW,Cheung LH,Boland K,Li C,Adams GP,Rosenblum MG

更新日期：2012-01-01 00:00:00

abstract：:To date, there is no effective therapy for hormone-independent prostate cancer. Therefore, as a new strategy for refractory cancer, gene therapy is showing increasing promise. In this study, we attempted to use a nonviral gene transfer system, in vivo electroporation, in prostate cancer cell PC-3 xenografts with the w...

journal_title：Molecular cancer therapeutics

authors： Mikata K,Uemura H,Ohuchi H,Ohta S,Nagashima Y,Kubota Y

更新日期：2002-02-01 00:00:00

abstract：:At the present time, the optimal development of molecularly targeted anticancer agents is limited by the lack of clinically applicable tools to predict drug effects. This study aimed to develop methods that might be useful in predicting the efficacy of targeted agents in a novel model system of human pancreatic cancer...

journal_title：Molecular cancer therapeutics

authors： Rubio-Viqueira B,Mezzadra H,Nielsen ME,Jimeno A,Zhang X,Iacobuzio-Donahue C,Maitra A,Hidalgo M,Altiok S

更新日期：2007-02-01 00:00:00

abstract：:Breast cancer resistance to the antiestrogens tamoxifen (OHT) and fulvestrant is accompanied by alterations in both estrogen-dependent and estrogen-independent signaling pathways. Consequently, effective inhibition of both pathways may be necessary to block proliferation of antiestrogen-resistant breast cancer cells. ...

journal_title：Molecular cancer therapeutics

authors： Long X,Fan M,Bigsby RM,Nephew KP

更新日期：2008-07-01 00:00:00

abstract：:Because the majority of cancers exhibit direct or indirect deregulation of cyclin-dependent kinase (CDK) function, members of the CDK family are attractive targets for the development of anticancer agents. As part of an ongoing program, novel imidazopyridines were identified and developed as potent and selective CDK i...

journal_title：Molecular cancer therapeutics

authors： Byth KF,Geh C,Forder CL,Oakes SE,Thomas AP

更新日期：2006-03-01 00:00:00

abstract：:Tissue transglutaminase 2 belongs to a family of transglutaminase proteins that confers mechanical resistance from proteolysis and stabilizes proteins. Transglutaminase 2 promotes transamidation between glutamine and lysine residues with the formation of covalent linkages between proteins. Transglutaminase 2 also inte...

journal_title：Molecular cancer therapeutics

authors： Yuan L,Choi K,Khosla C,Zheng X,Higashikubo R,Chicoine MR,Rich KM

更新日期：2005-09-01 00:00:00

abstract：:Chemopreventive agents in colorectal cancer possess either antiproliferative or anti-inflammatory actions. Nonsteroidal anti-inflammatory drugs (NSAID) and cyclooxygenase-2 inhibitors have shown promise, but are compromised by side effects. Nitric oxide donor NSAIDs are organic nitrates conjugated via a labile linker ...

journal_title：Molecular cancer therapeutics

authors： Hagos GK,Carroll RE,Kouznetsova T,Li Q,Toader V,Fernandez PA,Swanson SM,Thatcher GR

更新日期：2007-08-01 00:00:00

abstract：:Synthetic retinoid-related molecules (RRMs) have been described that show strong antiproliferative activity and induce apoptosis in cancer cells. These RRMs induce caspase activity independently of the retinoid receptors in Jurkat T cells. We observed that the inhibitor of cathepsins B and L Z-FA-fmk blocks the induct...

journal_title：Molecular cancer therapeutics

authors： Lopez-Hernandez FJ,Ortiz MA,Bayon Y,Piedrafita FJ

更新日期：2003-03-01 00:00:00

abstract：:TAS-121 is a novel orally active selective covalent inhibitor of the mutant EGFR. We performed preclinical characterization of TAS-121 and compared its efficacy and selectivity for common EGFR mutations (Ex19del and L858R), first- and second- generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) resistance mutation (T7...

journal_title：Molecular cancer therapeutics

authors： Ito K,Nishio M,Kato M,Murakami H,Aoyagi Y,Ohe Y,Okayama T,Hashimoto A,Ohsawa H,Tanaka G,Nonoshita K,Ito S,Matsuo K,Miyadera K

更新日期：2019-05-01 00:00:00

abstract：:Ligation of OX40 (CD134, TNFRSF4) on activated T cells by its natural ligand (OX40L, CD252, TNFSF4) enhances cellular survival, proliferation, and effector functions such as cytokine release and cellular cytotoxicity. We engineered a recombinant human OX40L IgG4P Fc fusion protein termed MEDI6383 that assembles into a...

journal_title：Molecular cancer therapeutics

authors： Oberst MD,Augé C,Morris C,Kentner S,Mulgrew K,McGlinchey K,Hair J,Hanabuchi S,Du Q,Damschroder M,Feng H,Eck S,Buss N,de Haan L,Pierce AJ,Park H,Sylwester A,Axthelm MK,Picker L,Morris NP,Weinberg A,Hammond SA

更新日期：2018-05-01 00:00:00