Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1.

abstract：:Notch signaling regulates cell-fate decisions during development and postnatal life. Little is known, however, about the role of Delta-like-4 (Dll4)-Notch signaling between cancer cells, or how this signaling affects cancer metastasis. We, therefore, assessed the role of Dll4-Notch signaling in cancer metastasis. We g...

journal_title：Molecular cancer therapeutics

authors： Kuramoto T,Goto H,Mitsuhashi A,Tabata S,Ogawa H,Uehara H,Saijo A,Kakiuchi S,Maekawa Y,Yasutomo K,Hanibuchi M,Akiyama S,Sone S,Nishioka Y

更新日期：2012-12-01 00:00:00

abstract：:1,1-Bis(3'-indolyl)-1-(p-substituted phenyl)methanes containing p-trifluoromethyl, t-butyl, and phenyl [1,1-bis(3'-indolyl)-1-(p-phenyl)methane (DIM-C-pPhC(6)H(5))] substituents induce peroxisome proliferator-activated receptor gamma (PPARgamma)-mediated transactivation in SW480 colon cancer cells. These PPARgamma-act...

journal_title：Molecular cancer therapeutics

authors： Chintharlapalli S,Papineni S,Safe S

更新日期：2006-05-01 00:00:00

abstract：:Chemoresistance is a major hurdle in the management of patients with epithelial ovarian cancer and is responsible for its high mortality. Studies have shown that chemoresistance is due to the presence of a subgroup of cancer cells with stemness properties and a high capacity for tumor repair. We have developed a libra...

journal_title：Molecular cancer therapeutics

authors： Alvero AB,Heaton A,Lima E,Pitruzzello M,Sumi N,Yang-Hartwich Y,Cardenas C,Steinmacher S,Silasi DA,Brown D,Mor G

更新日期：2016-06-01 00:00:00

abstract：:Endocrine therapy is important for management of patients with estrogen receptor (ER)-positive breast cancer; however, positive ER staining does not reliably predict therapy response. We assessed the potential to improve prediction of response to endocrine treatment of a novel test that quantifies functional ER pathwa...

journal_title：Molecular cancer therapeutics

authors： Inda MA,Blok EJ,Kuppen PJK,Charehbili A,den Biezen-Timmermans EC,van Brussel A,Fruytier SE,Meershoek-Klein Kranenbarg E,Kloet S,van der Burg B,Martens JWM,Sims AH,Turnbull AK,Dixon JM,Verhaegh W,Kroep JR,van de Velde CJH

更新日期：2020-02-01 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：:DNA methylation, histone modifications, and nucleosomal occupancy collaborate to cause silencing of tumor-related genes in cancer. The development of drugs that target these processes is therefore important for cancer therapy. Inhibitors of DNA methylation and histone deacetylation have been approved by the Food and D...

journal_title：Molecular cancer therapeutics

authors： Miranda TB,Cortez CC,Yoo CB,Liang G,Abe M,Kelly TK,Marquez VE,Jones PA

更新日期：2009-06-01 00:00:00

abstract：:In patients with advanced bladder cancer, glucocorticoids are frequently given to reduce acute toxicity, particularly hyperemesis, during chemotherapy, as well as to improve cachectic conditions. However, it remains unclear whether glucocorticoids directly affect the development and progression of bladder cancer throu...

journal_title：Molecular cancer therapeutics

authors： Zheng Y,Izumi K,Li Y,Ishiguro H,Miyamoto H

更新日期：2012-12-01 00:00:00

abstract：:Green fluorescent protein (GFP) is employed as a selection marker for gene transduction and to track tumor cells. Transduction of enhanced GFP (eGFP) into human neuroblastoma cell lines via a lentiviral vector significantly sensitized CHLA-20 (wild-type and functional TP53), and to a lesser extent CHLA-90 cells (multi...

journal_title：Molecular cancer therapeutics

authors： Goto H,Yang B,Petersen D,Pepper KA,Alfaro PA,Kohn DB,Reynolds CP

更新日期：2003-09-01 00:00:00

abstract：:The autocrine endothelin (ET)-1/endothelin A receptor (ET(A)R) pathway is an important regulator of several processes involved in ovarian cancer progression, and its overexpression is associated with aggressive disease. These features have led to the proposal of the ET(A)R receptor as a potential target for improving ...

journal_title：Molecular cancer therapeutics

authors： Rosanò L,Di Castro V,Spinella F,Nicotra MR,Natali PG,Bagnato A

更新日期：2007-07-01 00:00:00

abstract：:Despite frequent overexpression of numerous growth factor receptors by pancreatic ductal adenocarcinomas (PDAC), such as EGFR, therapeutic antibodies have not proven effective. Desmoplasia, hypovascularity, and hypoperfusion create a functional drug delivery barrier that contributes to treatment resistance. Drug combi...

journal_title：Molecular cancer therapeutics

authors： Wang J,Chan DKW,Sen A,Ma WW,Straubinger RM

更新日期：2019-11-01 00:00:00

abstract：:An ideal therapeutic for cancer would be one that selectively targets to tumor cells, is nontoxic to normal cells, and that could be systemically delivered, thereby reaching metastases as well as primary tumor. Immunoliposomes directed by monoclonal antibody or its fragments are promising vehicles for tumor-targeted d...

journal_title：Molecular cancer therapeutics

authors： Xu L,Huang CC,Huang W,Tang WH,Rait A,Yin YZ,Cruz I,Xiang LM,Pirollo KF,Chang EH

更新日期：2002-03-01 00:00:00

abstract：:A quaternary ammonium-based drug-linker has been developed to expand the scope of antibody-drug conjugate (ADC) payloads to include tertiary amines, a functional group commonly present in biologically active compounds. The linker strategy was exemplified with a β-glucuronidase-cleavable auristatin E construct. The dru...

journal_title：Molecular cancer therapeutics

authors： Burke PJ,Hamilton JZ,Pires TA,Setter JR,Hunter JH,Cochran JH,Waight AB,Gordon KA,Toki BE,Emmerton KK,Zeng W,Stone IJ,Senter PD,Lyon RP,Jeffrey SC

更新日期：2016-05-01 00:00:00

abstract：:Head and neck squamous cell carcinoma (HNSCC) is characterized by epidermal growth factor receptor (EGFR) overexpression, where EGFR levels correlate with survival. To date, EGFR targeting has shown limited antitumor effects in head and neck cancer when administrated as monotherapy. We previously identified a gastrin-...

journal_title：Molecular cancer therapeutics

authors： Zhang Q,Bhola NE,Lui VW,Siwak DR,Thomas SM,Gubish CT,Siegfried JM,Mills GB,Shin D,Grandis JR

更新日期：2007-04-01 00:00:00

abstract：:Targeting inhibitor of apoptosis proteins (IAP) with second mitochondria-derived activator of caspase (SMAC) mimetics may promote cancer cell death. We tested whether cIAP1 predicts poor prognosis in head and neck squamous cell carcinoma (HNSCC) and whether a novel Smac-mimetic, LCL161, could radiosensitize human papi...

journal_title：Molecular cancer therapeutics

authors： Yang L,Kumar B,Shen C,Zhao S,Blakaj D,Li T,Romito M,Teknos TN,Williams TM

更新日期：2019-06-01 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is one of the most chemotherapy- and radiotherapy-resistant tumors. The c-Met and Hedgehog (Hh) pathways have been shown previously by our group to be key regulatory pathways in the primary tumor growth and metastases formation. Targeting both the HGF/c-Met and Hh pathways has s...

journal_title：Molecular cancer therapeutics

authors： Rucki AA,Xiao Q,Muth S,Chen J,Che X,Kleponis J,Sharma R,Anders RA,Jaffee EM,Zheng L

更新日期：2017-11-01 00:00:00

abstract：:Arsenic trioxide (As(2)O(3)) has been used successfully in the treatment of acute promyelocytic leukemia. However, effects of As(2)O(3) in normal peripheral blood T cells have not been studied in detail. The purpose of this study was to investigate whether As(2)O(3) would induce apoptosis in normal T cells and therefo...

journal_title：Molecular cancer therapeutics

authors： Gupta S,Yel L,Kim D,Kim C,Chiplunkar S,Gollapudi S

更新日期：2003-08-01 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：:In the present work, we have investigated the antitumor activity of 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol (NBDHEX) on aggressive small cell lung cancer. NBDHEX not only is cytotoxic toward the parental small cell lung cancer H69 cell line (LC(50) of 2.3 +/- 0.6 micromol/L) but also overcomes the multidrug re...

journal_title：Molecular cancer therapeutics

authors： Filomeni G,Turella P,Dupuis ML,Forini O,Ciriolo MR,Cianfriglia M,Pezzola S,Federici G,Caccuri AM

更新日期：2008-02-01 00:00:00

abstract：:SJG-136 is a new pyrrolobenzodiazepine dimer inducing time-dependent cytotoxicity. HCT 116 cells were exposed to 50 nmol/L of SJG-136 for 1 hour or 1 nmol/L of SJG-136 for 24 hours to achieve similar levels of interstrand cross-links (ICL). The short exposure led to a rapid formation of ICLs (1 hour), early H2AX foci ...

journal_title：Molecular cancer therapeutics

authors： Arnould S,Spanswick VJ,Macpherson JS,Hartley JA,Thurston DE,Jodrell DI,Guichard SM

更新日期：2006-06-01 00:00:00

abstract：:Alpha-emitters can be pharmacologically delivered for irradiation of single cancer cells, but cellular lethality could be further enhanced by targeting alpha-emitters directly to the nucleus. PARP-1 is a druggable protein in the nucleus that is overexpressed in neuroblastoma compared with normal tissues and is associa...

journal_title：Molecular cancer therapeutics

authors： Makvandi M,Lee H,Puentes LN,Reilly SW,Rathi KS,Weng CC,Chan HS,Hou C,Raman P,Martinez D,Xu K,Carlin SD,Greenberg RA,Pawel BR,Mach RH,Maris JM,Pryma DA

更新日期：2019-07-01 00:00:00

abstract：:Breast cancer exhibits a propensity to metastasize to bone, resulting in debilitating skeletal complications associated with significant morbidity and poor prognosis. The cross-talk between metastatic cancer cells and bone is critical to the development and progression of bone metastases. We have shown the involvement...

journal_title：Molecular cancer therapeutics

authors： Previdi S,Abbadessa G,Dalò F,France DS,Broggini M

更新日期：2012-01-01 00:00:00

abstract：:The standard treatment for most advanced cancers is multidrug therapy. Unfortunately, combinations in the clinic often do not perform as predicted. Therefore, to complement identifying rational drug combinations based on biological assumptions, we hypothesized that a functional screen of drug combinations, without lim...

journal_title：Molecular cancer therapeutics

authors： Zinner RG,Barrett BL,Popova E,Damien P,Volgin AY,Gelovani JG,Lotan R,Tran HT,Pisano C,Mills GB,Mao L,Hong WK,Lippman SM,Miller JH

更新日期：2009-03-01 00:00:00

abstract：:The mammalian target of rapamycin (mTOR) is a serine/threonine protein kinase that exists in two complexes (mTORC1 and mTORC2) and integrates extracellular and intracellular signals to act as a master regulator of cell growth, survival, and metabolism. The PI3K/AKT/mTOR prosurvival pathway is often dysregulated in mul...

journal_title：Molecular cancer therapeutics

authors： Slotkin EK,Patwardhan PP,Vasudeva SD,de Stanchina E,Tap WD,Schwartz GK

更新日期：2015-02-01 00:00:00

abstract：:Involuntary weight loss, a part of the cachexia syndrome, is a debilitating comorbidity of cancer and currently has no treatment options. Results from a recent clinical trial at our institution showed that biliary tract cancer patients treated with a MEK inhibitor exhibited poor tumor responses but surprisingly gained...

journal_title：Molecular cancer therapeutics

authors： Talbert EE,Yang J,Mace TA,Farren MR,Farris AB,Young GS,Elnaggar O,Che Z,Timmers CD,Rajasekera P,Maskarinec JM,Bloomston M,Bekaii-Saab T,Guttridge DC,Lesinski GB

更新日期：2017-02-01 00:00:00

abstract：:Overexpression or hyperactivation of MDM2 contributes to functional inactivation of wild-type p53 in nearly 50% of tumors. Inhibition of p53 by MDM2 depends on binding between an NH(2)-terminal (residues 16-28) p53 alpha-helical peptide and a hydrophobic pocket on MDM2, presenting an attractive target for development ...

journal_title：Molecular cancer therapeutics

authors： Chen L,Yin H,Farooqi B,Sebti S,Hamilton AD,Chen J

更新日期：2005-06-01 00:00:00

abstract：:Genomic analyses of squamous cell carcinoma (SCC) have yet to yield significant strategies against pathway activation to improve treatment. Platinum-based chemotherapy remains the mainstay of treatment for SCC of different histotypes either as a single-agent or alongside other chemotherapeutic drugs or radiotherapy; h...

journal_title：Molecular cancer therapeutics

authors： Kong LR,Chua KN,Sim WJ,Ng HC,Bi C,Ho J,Nga ME,Pang YH,Ong WR,Soo RA,Huynh H,Chng WJ,Thiery JP,Goh BC

更新日期：2015-07-01 00:00:00

abstract：:Met-amplified EGFR-tyrosine kinase inhibitor (TKI)-resistant non-small cell lung cancer (NSCLC) harboring an activating EGFR mutation is responsive to concurrent EGFR-TKI and Met-TKI treatment in a preclinical model. Here, we determined that Met-amplified gefitinib-resistant cells acquire dual resistance to inhibition...

journal_title：Molecular cancer therapeutics

authors： Yamaoka T,Ohmori T,Ohba M,Arata S,Kishino Y,Murata Y,Kusumoto S,Ishida H,Shirai T,Hirose T,Ohnishi T,Sasaki Y

更新日期：2016-12-01 00:00:00

abstract：:Genital human papillomavirus (HPV) infection is the primary cause of cervical cancer in women. Although the HPV recombinant L1 protein was recently licensed as an available vaccine, it has numerous shortcomings. New vaccination strategies should be considered. To enable the design of a prophylactic and therapeutic low...

journal_title：Molecular cancer therapeutics

authors： Bian T,Wang Y,Lu Z,Ye Z,Zhao L,Ren J,Zhang H,Ruan L,Tian H

更新日期：2008-05-01 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：:Antibody-drug conjugates (ADC) represent a promising therapeutic modality for the clinical management of cancer. We sought to develop a novel ADC that targets 5T4, an oncofetal antigen expressed on tumor-initiating cells (TIC), which comprise the most aggressive cell population in the tumor. We optimized an anti-5T4 A...

journal_title：Molecular cancer therapeutics

authors： Sapra P,Damelin M,Dijoseph J,Marquette K,Geles KG,Golas J,Dougher M,Narayanan B,Giannakou A,Khandke K,Dushin R,Ernstoff E,Lucas J,Leal M,Hu G,O'Donnell CJ,Tchistiakova L,Abraham RT,Gerber HP

更新日期：2013-01-01 00:00:00