Comparison of biological effects of non-nucleoside DNA methylation inhibitors versus 5-aza-2'-deoxycytidine.

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：:Karyopherin beta 1 (Kpnβ1) is a nuclear transport receptor that imports cargoes into the nucleus. Recently, elevated Kpnβ1 expression was found in certain cancers and Kpnβ1 silencing with siRNA was shown to induce cancer cell death. This study aimed to identify novel small molecule inhibitors of Kpnβ1, and determine t...

journal_title：Molecular cancer therapeutics

authors： van der Watt PJ,Chi A,Stelma T,Stowell C,Strydom E,Carden S,Angus L,Hadley K,Lang D,Wei W,Birrer MJ,Trent JO,Leaner VD

更新日期：2016-04-01 00:00:00

abstract：:The majority of patients with HER2-overexpressing metastatic breast cancer who initially respond to the HER2-targeted antibody trastuzumab show disease progression within 1 year. The identification of novel agents that effectively inhibit survival of cancer cells that have progressed on trastuzumab is critical for imp...

journal_title：Molecular cancer therapeutics

authors： Rowe DL,Ozbay T,Bender LM,Nahta R

更新日期：2008-07-01 00:00:00

abstract：:DNA repair mechanisms are crucial for cell survival. It increases the cancer cell's ability to resist DNA damage. FEN1 is involved in DNA replication and repair, specifically long-patch base excision repair. Although the gene function and post-translational modification of FEN1 are well studied, the regulatory mechani...

journal_title：Molecular cancer therapeutics

authors： Zhu H,Wu C,Wu T,Xia W,Ci S,He W,Zhang Y,Li L,Zhou S,Zhang J,Edick AM,Zhang A,Pan FY,Hu Z,He L,Guo Z

更新日期：2019-12-01 00:00:00

abstract：:Preclinical data suggest that combined EGF receptor (EGFR) targeting with an EGFR tyrosine kinase inhibitor and an anti-EGFR monoclonal antibody may be superior over single-agent targeting. Therefore, as part of a phase I study, we analyzed the outcome of 20 patients with non-small cell lung cancer treated with the co...

journal_title：Molecular cancer therapeutics

authors： Wheler JJ,Tsimberidou AM,Falchook GS,Zinner RG,Hong DS,Fok JY,Fu S,Piha-Paul SA,Naing A,Kurzrock R

更新日期：2013-10-01 00:00:00

abstract：:We previously reported that a pan-PAD inhibitor, YW3-56, activates p53 target genes to inhibit cancer growth. However, the p53-independent anticancer activity and molecular mechanisms of YW3-56 remain largely elusive. Here, gene expression analyses found that ATF4 target genes involved in endoplasmic reticulum (ER) st...

journal_title：Molecular cancer therapeutics

authors： Wang S,Chen XA,Hu J,Jiang JK,Li Y,Chan-Salis KY,Gu Y,Chen G,Thomas C,Pugh BF,Wang Y

更新日期：2015-04-01 00:00:00

abstract：:Contrary to other anticancer targets, topoisomerase I (TOP1) is targeted by only one chemical class of FDA-approved drugs: topotecan and irinotecan, the derivatives of the plant alkaloid, camptothecin. The indenoisoquinolines LMP400, LMP744, and LMP776 are novel noncamptothecin TOP1 inhibitors in clinical trial, which...

journal_title：Molecular cancer therapeutics

authors： Marzi L,Agama K,Murai J,Difilippantonio S,James A,Peer CJ,Figg WD,Beck D,Elsayed MSA,Cushman M,Pommier Y

更新日期：2018-08-01 00:00:00

abstract：:DNA damaging agents such as cisplatin arrest cell cycle progression at either G1, S, or G2 phase, although the G1 arrest is only seen in cells expressing the wild-type p53 tumor suppressor protein. We have reported that 7-hydroxystaurosporine (UCN-01) overcomes S and G2 phase arrest and enhances the cytotoxicity of ci...

journal_title：Molecular cancer therapeutics

authors： Eastman A,Kohn EA,Brown MK,Rathman J,Livingstone M,Blank DH,Gribble GW

更新日期：2002-10-01 00:00:00

abstract：:The TGFβ-mediated alteration of the tumor microenvironment plays a crucial role in tumor progression. Mesothelial cells are the primary components of the tumor microenvironment for ovarian cancer cells; however, the exact role of TGFβ-stimulated mesothelial cells in ovarian cancer progression remains uncertain. In thi...

journal_title：Molecular cancer therapeutics

authors： Sugiyama K,Kajiyama H,Shibata K,Yuan H,Kikkawa F,Senga T

更新日期：2014-08-01 00:00:00

abstract：:Transforming growth factor (TGF)-β contributes to the malignant phenotype of glioblastoma by promoting invasiveness and angiogenesis and creating an immunosuppressive microenvironment. So far, TGF-β1 and TGF-β2 isoforms have been considered to act in a similar fashion without isoform-specific function in glioblastoma....

journal_title：Molecular cancer therapeutics

authors： Seystahl K,Papachristodoulou A,Burghardt I,Schneider H,Hasenbach K,Janicot M,Roth P,Weller M

更新日期：2017-06-01 00:00:00

abstract：:DNA topoisomerase I (Top1) inhibition by camptothecin derivatives can impair the hypoxia-induced cell transcriptional response. In the present work, we determined molecular aspects of the mechanism of camptothecin's effects on hypoxia-inducible factor-1α (HIF-1α) activity in human cancer cells. In particular, we provi...

journal_title：Molecular cancer therapeutics

authors： Bertozzi D,Marinello J,Manzo SG,Fornari F,Gramantieri L,Capranico G

更新日期：2014-01-01 00:00:00

abstract：:Upregulation of HER2 is a hallmark of 20% to 30% of invasive breast cancers, rendering this receptor an attractive target for cancer therapy. Although HER2-targeting agents have provided substantial clinical benefit as cancer therapeutics, there is a need for the development of new agents aiming at circumventing anti-...

journal_title：Molecular cancer therapeutics

authors： Brack S,Attinger-Toller I,Schade B,Mourlane F,Klupsch K,Woods R,Hachemi H,von der Bey U,Koenig-Friedrich S,Bertschinger J,Grabulovski D

更新日期：2014-08-01 00:00:00

abstract：:Radiotherapy, a frequent mode of cancer treatment, is often restricted by dose-related toxicity and development of therapeutic resistance. To develop a novel and selective radiosensitizer, we studied the radiosensitizing effects and associated mechanisms of silibinin in prostate cancer. The radiosensitizing effect of ...

journal_title：Molecular cancer therapeutics

authors： Nambiar DK,Rajamani P,Deep G,Jain AK,Agarwal R,Singh RP

更新日期：2015-12-01 00:00:00

abstract：:Dietary phytochemicals exhibit chemopreventive potential in vivo through persistent low-dose exposures, whereas mechanistic in vitro studies with these agents generally use a high-dose single treatment. Because the latter approach is not representative of an in vivo steady state, we investigated antitumor activity of ...

journal_title：Molecular cancer therapeutics

authors： Moiseeva EP,Almeida GM,Jones GD,Manson MM

更新日期：2007-11-01 00:00:00

abstract：:The effect of vascular endothelial growth factor (VEGF) ligands and cediranib on tumor cell proliferation, migration, and invasion was determined. It has recently been suggested that autocrine signaling through the VEGF receptor (VEGFR) pathway may play a role in tumor cell survival, invasion, and migration. The purpo...

journal_title：Molecular cancer therapeutics

authors： Morelli MP,Brown AM,Pitts TM,Tentler JJ,Ciardiello F,Ryan A,Jürgensmeier JM,Eckhardt SG

更新日期：2009-09-01 00:00:00

abstract：:Trabectedin (ET-743) is a marine alkaloid isolated from the Caribbean tunicate Ecteinascidia turbinata, with a chemical structure characterized by three fused tetrahydroisoquinoline rings. Two of these rings (subunits A and B) provide the framework for covalent interaction with the minor groove of the DNA double helix...

journal_title：Molecular cancer therapeutics

authors： D'Incalci M,Galmarini CM

更新日期：2010-08-01 00:00:00

abstract：:Tivantinib (ARQ197) was first reported as a highly selective inhibitor of c-MET and is currently being investigated in a phase III clinical trial. However, as recently reported by us and another group, tivantinib showed cytotoxic activity independent of cellular c-MET status and also disrupted microtubule dynamics. To...

journal_title：Molecular cancer therapeutics

authors： Aoyama A,Katayama R,Oh-Hara T,Sato S,Okuno Y,Fujita N

更新日期：2014-12-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor γ (PPARγ) is an important transcription factor that modulates lipid metabolism and inflammation. However, it remains unclear whether PPARγ is involved in modulation of estrogen (E2)-induced inflammation, thus affecting apoptosis of E2-deprived breast cancer cells, MCF-7:5C an...

journal_title：Molecular cancer therapeutics

authors： Fan P,Abderrahman B,Chai TS,Yerrum S,Jordan VC

更新日期：2018-12-01 00:00:00

abstract：:Several caged Garcinia xanthone natural products have potent bioactivity and a documented value in traditional Eastern medicine. Previous synthesis and structure activity relationship studies of these natural products resulted in the identification of the pharmacophore represented by the structure of cluvenone. In the...

journal_title：Molecular cancer therapeutics

authors： Batova A,Altomare D,Chantarasriwong O,Ohlsen KL,Creek KE,Lin YC,Messersmith A,Yu AL,Yu J,Theodorakis EA

更新日期：2010-11-01 00:00:00

abstract：:The application of cancer gene therapy has heretofore been restricted to local, or locoregional, neoplastic disease contexts. This is owing to the lack of gene transfer vectors, which embody the requisite target cell selectivity in vivo required for metastatic disease applications. To this end, we have explored novel ...

journal_title：Molecular cancer therapeutics

authors： Lee M,Lu ZH,Li J,Kashentseva EA,Dmitriev IP,Mendonca SA,Curiel DT

更新日期：2020-03-01 00:00:00

abstract：:Amplification of human epidermal growth factor receptor 2 (HER2) has been detected in 20% to 30% of gastric cancers and is associated with a poor outcome. Combination therapies with HER2-targeting agents and cytotoxic agents are considered a potential therapeutic option for gastric cancer with HER2 amplification. We h...

journal_title：Molecular cancer therapeutics

authors： Tanizaki J,Okamoto I,Takezawa K,Tsukioka S,Uchida J,Kiniwa M,Fukuoka M,Nakagawa K

更新日期：2010-05-01 00:00:00

abstract：:Histone deacetylase inhibitors represent a promising new class of anticancer agents. In the current investigation, we examined the activity of PXD101, a potent histone deacetylase inhibitor, used alone or in combination with clinically relevant chemotherapeutics (docetaxel, paclitaxel, and carboplatin), in preclinical...

journal_title：Molecular cancer therapeutics

authors： Qian X,LaRochelle WJ,Ara G,Wu F,Petersen KD,Thougaard A,Sehested M,Lichenstein HS,Jeffers M

更新日期：2006-08-01 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：:TRC105 is an anti-endoglin antibody currently being tested in combination with VEGF inhibitors. In the phase Ib trial, 38 patients were treated with both TRC105 and bevacizumab (BEV), and improved clinical outcomes were observed, despite the fact that 30 patients (79%) were refractory to prior anti-VEGF therapy. Plasm...

journal_title：Molecular cancer therapeutics

authors： Liu Y,Starr MD,Brady JC,Rushing C,Pang H,Adams B,Alvarez D,Theuer CP,Hurwitz HI,Nixon AB

更新日期：2018-10-01 00:00:00

abstract：:17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) converts estrone (E1) into estradiol (E2) and is expressed in many steroidogenic tissues and breast cancer cell lines. Because the potent estrogen E2 stimulates the growth and development of hormone-dependent diseases, inhibition of the final step of E2 synthesis is c...

journal_title：Molecular cancer therapeutics

authors： Ayan D,Maltais R,Roy J,Poirier D

更新日期：2012-10-01 00:00:00

abstract：:DMOT4039A, a humanized anti-mesothelin mAb conjugated to the antimitotic agent monomethyl auristatin E (MMAE), was given to patients with pancreatic and ovarian cancer every 3 weeks (0.2-2.8 mg/kg; q3w) or weekly (0.8-1.2 mg/kg). A 3+3 design was used for dose escalation followed by expansion at the recommended phase ...

journal_title：Molecular cancer therapeutics

authors： Weekes CD,Lamberts LE,Borad MJ,Voortman J,McWilliams RR,Diamond JR,de Vries EG,Verheul HM,Lieu CH,Kim GP,Wang Y,Scales SJ,Samineni D,Brunstein F,Choi Y,Maslyar DJ,Colon-Otero G

更新日期：2016-03-01 00:00:00

abstract：:Tumor-specific tissue-penetrating peptides deliver drugs into extravascular tumor tissue by increasing tumor vascular permeability through interaction with neuropilin (NRP). Here, we report that a prototypic tumor-penetrating peptide iRGD (amino acid sequence: CRGDKGPDC) potently inhibits spontaneous metastasis in mic...

journal_title：Molecular cancer therapeutics

authors： Sugahara KN,Braun GB,de Mendoza TH,Kotamraju VR,French RP,Lowy AM,Teesalu T,Ruoslahti E

更新日期：2015-01-01 00:00:00

abstract：:Erlotinib is a tyrosine kinase inhibitor approved for the treatment of patients with advanced non-small cell lung cancer (NSCLC). In these patients, erlotinib prolongs survival but its benefit remains modest because many tumors express wild-type (wt) EGFR or develop a second-site EGFR mutation. To test drug combinatio...

journal_title：Molecular cancer therapeutics

authors： Dermawan JK,Gurova K,Pink J,Dowlati A,De S,Narla G,Sharma N,Stark GR

更新日期：2014-09-01 00:00:00

abstract：:Overexpression of Notch receptors and ligands has been associated with various cancers and developmental disorders, making Notch a potential therapeutic target. Here, we report characterization of Notch1 monoclonal antibodies (mAb) with therapeutic potential. The mAbs generated against epidermal growth factor (EGF) re...

journal_title：Molecular cancer therapeutics

authors： Sharma A,Paranjape AN,Rangarajan A,Dighe RR

更新日期：2012-01-01 00:00:00

abstract：:To investigate the mechanism by which 5-aminoimidazole-4-carboxamide-1-β-riboside (AICAr) induces apoptosis in multiple myeloma cells, we conducted an unbiased metabolomics screen. AICAr had selective effects on nucleotide metabolism, resulting in an increase in purine metabolites and a decrease in pyrimidine metaboli...

journal_title：Molecular cancer therapeutics

authors： Bardeleben C,Sharma S,Reeve JR,Bassilian S,Frost P,Hoang B,Shi Y,Lichtenstein A

更新日期：2013-07-01 00:00:00