abstract：:Urokinase plasminogen activator (uPA) is a tumor-specific protease highly expressed in several types of solid tumors and rarely present on normal cells under physiologic conditions. Due to its high expression on metastatic tumors, several different strategies have been used to target the urokinase system. These have m...

journal_title：Molecular cancer therapeutics

authors： Abi-Habib RJ,Singh R,Liu S,Bugge TH,Leppla SH,Frankel AE

更新日期：2006-10-01 00:00:00

abstract：:Rapamycin and its analogues are being tested as new antitumor agents. Rapamycin binds to FKBP-12 and this complex inhibits the activity of FRAP/mammalian target of rapamycin, which leads to dephosphorylation of 4EBP1 and p70 S6 kinase, resulting in blockade of translation initiation. We have found that RAP inhibits th...

journal_title：Molecular cancer therapeutics

authors： García-Morales P,Hernando E,Carrasco-García E,Menéndez-Gutierrez MP,Saceda M,Martínez-Lacaci I

更新日期：2006-09-01 00:00:00

abstract：:The present study aimed to investigate the therapeutic efficacy of combining vascular endothelial growth factor (VEGF) receptor blockade using tyrosine kinase inhibitor PTK787 with hypoxia for the treatment of hepatocellular carcinoma (HCC). The in vivo effects of the treatments were determined in a rat orthotopic HCC...

journal_title：Molecular cancer therapeutics

authors： Yang ZF,Poon RT,Liu Y,Lau CK,Ho DW,Tam KH,Lam CT,Fan ST

更新日期：2006-09-01 00:00:00

abstract：:Novel therapeutic approaches are urgently needed for high-stage neuroblastoma, a major therapeutic challenge in pediatric oncology. The majority of neuroblastoma tumors are p53 wild type with intact downstream p53 signaling pathways. We hypothesize that stabilization of p53 would sensitize this aggressive tumor to gen...

journal_title：Molecular cancer therapeutics

authors： Barbieri E,Mehta P,Chen Z,Zhang L,Slack A,Berg S,Shohet JM

更新日期：2006-09-01 00:00:00

abstract：:Nanotechnology refers to the interactions of cellular and molecular components and engineered materials-typically, clusters of atoms, molecules, and molecular fragments into incredibly small particles-between 1 and 100 nm. Nanometer-sized particles have novel optical, electronic, and structural properties that are not...

journal_title：Molecular cancer therapeutics

authors： Sinha R,Kim GJ,Nie S,Shin DM

更新日期：2006-08-01 00:00:00

abstract：:Curcumin (curcumin I), demethoxycurcumin (curcumin II), and bisdemethoxycurcumin (curcumin III) are the major forms of curcuminoids found in the turmeric powder, which exhibit anticancer, antioxidant, and anti-inflammatory activities. In this study, we evaluated the ability of purified curcuminoids to modulate the fun...

journal_title：Molecular cancer therapeutics

authors： Chearwae W,Shukla S,Limtrakul P,Ambudkar SV

更新日期：2006-08-01 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：:The covalent attachment of palmitate to specific proteins by the action of palmitoyl acyltransferases (PAT) plays critical roles in the biological activities of several oncoproteins. Two PAT activities are expressed by human cells: type 1 PATs that modify the farnesyl-dependent palmitoylation motif found in H- and N-R...

journal_title：Molecular cancer therapeutics

authors： Ducker CE,Griffel LK,Smith RA,Keller SN,Zhuang Y,Xia Z,Diller JD,Smith CD

更新日期：2006-07-01 00:00:00

abstract：:CEP-7055, a fully synthetic, orally active N,N-dimethylglycine ester of CEP-5214, a C3-(isopropylmethoxy)-fused pyrrolocarbazole with potent pan-vascular endothelial growth factor receptor (VEGFR) kinase inhibitory activity, has recently completed phase I clinical trials in cancer patients. These studies evaluated the...

journal_title：Molecular cancer therapeutics

authors： Jones-Bolin S,Zhao H,Hunter K,Klein-Szanto A,Ruggeri B

更新日期：2006-07-01 00:00:00

abstract：:Proteasome inhibitors are potent inducers of apoptosis in isolated lymphocytes from patients with chronic lymphocytic leukemia (CLL). However, the reversible proteasome inhibitor bortezomib (PS-341; Velcade) did not display substantial antitumor activity in CLL patients. Here, we compared the effects of bortezomib and...

journal_title：Molecular cancer therapeutics

authors： Ruiz S,Krupnik Y,Keating M,Chandra J,Palladino M,McConkey D

更新日期：2006-07-01 00:00:00

abstract：:Malignant mesothelioma is an aggressive tumor of the serosal surfaces of the lungs, heart, and abdomen. Survival rates are poor and effective treatments are not available. However, recent therapeutic regimens targeting thymidylate synthase (TS) in malignant mesothelioma patients have shown promise. We have reported th...

journal_title：Molecular cancer therapeutics

authors： Flynn J,Berg RW,Wong T,van Aken M,Vincent MD,Fukushima M,Koropatnick J

更新日期：2006-06-01 00:00:00

abstract：:We have synthesized several new phenyl maleimide compounds, which are potent growth inhibitors of several human tumor cell lines. Among these, PM-20 was the most potent with an IC50 of 700 nmol/L for Hep3B human hepatoma cell growth. Two other derivatives, PM-26 and PM-38, did not inhibit Hep3B cell growth even at 100...

journal_title：Molecular cancer therapeutics

authors： Kar S,Wang M,Yao W,Michejda CJ,Carr BI

更新日期：2006-06-01 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：:Survivin, an inhibitor of apoptosis protein, is highly expressed in most cancers and associated with chemotherapy resistance, increased tumor recurrence, and shorter patient survival, making antisurvivin therapy an attractive cancer treatment strategy. However, growing evidence indicates that survivin is expressed in ...

journal_title：Molecular cancer therapeutics

authors： Fukuda S,Pelus LM

更新日期：2006-05-01 00:00:00

abstract：:The phosphatidylinositol 3-kinase (PI3K)/Akt pathway is known to be activated by radiation. The mammalian target of rapamycin (mTOR) is downstream of Akt, and we investigated the effects of radiation on Akt/mTOR signaling in breast cancer cell models. RAD001 (everolimus), a potent derivative of the mTOR inhibitor rapa...

journal_title：Molecular cancer therapeutics

authors： Albert JM,Kim KW,Cao C,Lu B

更新日期：2006-05-01 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：: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：:Multiple roles within mitosis have been assigned to Polo-like kinase 1 (Plk1), making it an attractive candidate for mitotic targeting of cancer cells. We have employed chimeric antisense oligonucleotides to investigate the molecular alterations after targeted interference with Plk1 in RKO human colon adenocarcinoma a...

journal_title：Molecular cancer therapeutics

authors： Schmidt M,Hofmann HP,Sanders K,Sczakiel G,Beckers TL,Gekeler V

更新日期：2006-04-01 00:00:00

abstract：:Advanced and hormone-refractory prostate cancer has long been considered as a chemoresistant disease. Recently, it was found that 14-3-3sigma expression increases as prostate tumor progresses, and that 14-3-3sigma contributes significantly to drug resistance in breast cancers. We, thus, hypothesized that advanced and ...

journal_title：Molecular cancer therapeutics

authors： Han B,Xie H,Chen Q,Zhang JT

更新日期：2006-04-01 00:00:00

abstract：:The oncogenic beta-catenin/T-cell factor (TCF) signal is a common trigger inducing expressions of various cancer-related genes and is activated in various types of human malignancy. The aim of this study was to create an effective double-stranded DNA decoy that would interfere with endogenous TCF hyperactivity in tumo...

journal_title：Molecular cancer therapeutics

authors： Seki Y,Yamamoto H,Ngan CY,Yasui M,Tomita N,Kitani K,Takemasa I,Ikeda M,Sekimoto M,Matsuura N,Albanese C,Kaneda Y,Pestell RG,Monden M

更新日期：2006-04-01 00:00:00

abstract：:In breast and certain other cancers, receptor tyrosine kinases, including the insulin-like growth factor I receptor (IGF-IR), play an important role in promoting the oncogenic process. The IGF-IR is therefore an important target for developing new anti-breast cancer therapies. An initial screening of a chemical librar...

journal_title：Molecular cancer therapeutics

authors： Gable KL,Maddux BA,Penaranda C,Zavodovskaya M,Campbell MJ,Lobo M,Robinson L,Schow S,Kerner JA,Goldfine ID,Youngren JF

更新日期：2006-04-01 00:00:00

abstract：:Radiosensitization caused by the poly(ADP-ribose) polymerase (PARP) inhibitor 4-amino-1,8-naphthalimide (ANI) was investigated in 10 asynchronously growing rodent (V79, CHO-Xrs6, CHO-K1, PARP-1+/+ 3T3, and PARP-1-/- 3T3) or human (HeLa, MRC5VI, IMR90, M059J, and M059K) cell lines, either repair proficient or defective...

journal_title：Molecular cancer therapeutics

authors： Noël G,Godon C,Fernet M,Giocanti N,Mégnin-Chanet F,Favaudon V

更新日期：2006-03-01 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：:Colorectal cancer is the second leading cause of cancer mortality in the United States. Substantial human and animal data support the ability of nonsteroidal anti-inflammatory drugs to cause regression of existing colon tumors and prevent new tumor formation. The mechanism by which the nonsteroidal anti-inflammatory d...

journal_title：Molecular cancer therapeutics

authors： Rice PL,Peters SL,Beard KS,Ahnen DJ

更新日期：2006-03-01 00:00:00

abstract：:Resistance to paclitaxel-based therapy is frequently encountered in the clinic. The mechanisms of intrinsic or acquired paclitaxel resistance are not well understood. We sought to characterize the resistance mechanisms that develop upon chronic exposure of a cancer cell line to paclitaxel in the presence of the P-glyc...

journal_title：Molecular cancer therapeutics

authors： Hari M,Loganzo F,Annable T,Tan X,Musto S,Morilla DB,Nettles JH,Snyder JP,Greenberger LM

更新日期：2006-02-01 00:00:00

abstract：:Recent studies have shown that up to 90% of viral vectors could disseminate to normal organs following intratumoral infusion. The amount of dissemination might be dependent on the infusion conditions. Therefore, we investigated the effects of infusion rate, volume, and dose on transgene expression in liver and tumor t...

journal_title：Molecular cancer therapeutics

authors： Wang Y,Wang H,Li CY,Yuan F

更新日期：2006-02-01 00:00:00

abstract：:We discovered a thalidomide analogue [5-hydroxy-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33)] with antiproliferative activity against nine cancer cell lines in vitro. Flow cytometric analyses showed that the compound caused G2-M arrest, which occurred mainly at the mitotic phase. In addition, immunofluores...

journal_title：Molecular cancer therapeutics

authors： Li PK,Pandit B,Sackett DL,Hu Z,Zink J,Zhi J,Freeman D,Robey RW,Werbovetz K,Lewis A,Li C

更新日期：2006-02-01 00:00:00

abstract：:Mitotic spindle poisons (e.g., Taxol and vinblastine), used as chemotherapy drugs, inhibit mitotic spindle function, activate the mitotic spindle checkpoint, arrest cells in mitosis, and then cause cell death by mechanisms that are poorly understood. By expression cloning, we identified a truncated version of human TR...

journal_title：Molecular cancer therapeutics

authors： Yamada HY,Gorbsky GJ

更新日期：2006-01-01 00:00:00

abstract：:P140K-MGMT and G156A-MGMT genes encode two O(6)-benzylguanine-resistant O(6)-alkylguanine DNA alkyltransferase proteins that confer a high degree of O(6)-benzylguanine and 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) or O(6)-benzylguanine and temozolomide resistance to primary hematopoietic cells. In this study, we dir...

journal_title：Molecular cancer therapeutics

authors： Fontes AM,Davis BM,Encell LP,Lingas K,Covas DT,Zago MA,Loeb LA,Pegg AE,Gerson SL

更新日期：2006-01-01 00:00:00

abstract：:The breast-specific antigen alpha-lactalbumin is expressed in >60% of breast cancer tissues. To evaluate the effect of gene therapy for breast cancer by controlling adenovirus replication with human alpha-lactalbumin promoter, we investigated the activity of a 762-bp human alpha-lactalbumin promoter. Alpha-lactalbumin...

journal_title：Molecular cancer therapeutics

authors： Li X,Zhang J,Gao H,Vieth E,Bae KH,Zhang YP,Lee SJ,Raikwar S,Gardner TA,Hutchins GD,VanderPutten D,Kao C,Jeng MH

更新日期：2005-12-01 00:00:00

abstract：:Histone modification has emerged as a promising approach to cancer therapy. We explored the efficacy of a novel class of histone deacetylase inhibitors in the treatment of malignant gliomas. Treatment of glioma cell lines with two butyric acid derivatives, pivaloylomethyl butyrate (AN-9) and butyroyloxymethyl butyrate...

journal_title：Molecular cancer therapeutics

authors： Entin-Meer M,Rephaeli A,Yang X,Nudelman A,VandenBerg SR,Haas-Kogan DA

更新日期：2005-12-01 00:00:00

abstract：:Bcl-2 and Bcl-xL are associated with treatment resistance and progression in many cancers, including prostate cancer. The objective of this study was to determine whether a novel bispecific antisense oligonucleotide targeting both Bcl-2 and Bcl-xL induces apoptosis and enhances chemosensitivity in androgen-independent...

journal_title：Molecular cancer therapeutics

authors： Yamanaka K,Rocchi P,Miyake H,Fazli L,Vessella B,Zangemeister-Wittke U,Gleave ME

更新日期：2005-11-01 00:00:00

abstract：:Localized activation of the prodrug ifosfamide in or close to tumors by implanting encapsulated ifosfamide-activating cells is an efficacious strategy for tumor therapy. The aim of this study was to evaluate the feasibility of subsieve-size agarose capsules for enclosing the cells in this application. Compared with ma...

journal_title：Molecular cancer therapeutics

authors： Sakai S,Kawabata K,Tanaka S,Harimoto N,Hashimoto I,Mu C,Salmons B,Ijima H,Kawakami K

更新日期：2005-11-01 00:00:00

abstract：:DNA cytosine methylation plays a considerable role in normal development, gene regulation, and carcinogenesis. Hypermethylation of the promoters of some tumor suppressor genes and the associated silencing of these genes often occur in certain cancer types. The reversal of this process by DNA methylation inhibitors is ...

journal_title：Molecular cancer therapeutics

authors： Chuang JC,Yoo CB,Kwan JM,Li TW,Liang G,Yang AS,Jones PA

更新日期：2005-10-01 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：: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：: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：:We investigated integrin-linked kinase (ILK), a focal adhesion serine-threonine protein kinase, as a new molecular target for treating anaplastic thyroid cancer. ILK mediates cell growth and survival signals and is overexpressed in a number of cancers. Therefore, we hypothesized that inhibition of ILK leads to growth ...

journal_title：Molecular cancer therapeutics

authors： Younes MN,Kim S,Yigitbasi OG,Mandal M,Jasser SA,Dakak Yazici Y,Schiff BA,El-Naggar A,Bekele BN,Mills GB,Myers JN

更新日期：2005-08-01 00:00:00

abstract：:Tamoxifen, a selective estrogen receptor (ER) modulator, is the most widely prescribed hormonal therapy treatment for breast cancer. Despite the benefits of tamoxifen therapy, almost all tamoxifen-responsive breast cancer patients develop resistance to therapy. In addition, tamoxifen displays estrogen-like effects in ...

journal_title：Molecular cancer therapeutics

authors： Shah YM,Al-Dhaheri M,Dong Y,Ip C,Jones FE,Rowan BG

更新日期：2005-08-01 00:00:00

abstract：:Previous studies have shown a statistically significant correlation between human carcinomas and monoclonal antibody detection of a Mycoplasma hyorhinis-encoded protein known as p37. A potential mechanism of p37 is that it might promote invasion and metastasis. Recombinant p37 enhanced the invasiveness of two prostate...

journal_title：Molecular cancer therapeutics

authors： Ketcham CM,Anai S,Reutzel R,Sheng S,Schuster SM,Brenes RB,Agbandje-McKenna M,McKenna R,Rosser CJ,Boehlein SK

更新日期：2005-07-01 00:00:00