abstract：:2-Amino-4,4alpha-dihydro-4alpha,7-dimethyl-3H-phenoxazine-3-one (Phx-1) has been developed as a novel phenoxazine derivative having an anticancer activity on a variety of cancer cell lines as well as transplanted tumors in mice with minimal toxicity to normal cells. We examined the effects of Phx-1 on Jurkat cells, a ...

journal_title：Molecular cancer therapeutics

authors： Hara K,Okamoto M,Aki T,Yagita H,Tanaka H,Mizukami Y,Nakamura H,Tomoda A,Hamasaki N,Kang D

更新日期：2005-07-01 00:00:00

abstract：:Antibodies conjugated to radionuclides emitting low-energy electrons, which include Auger electrons and some conversion electrons, were recently shown to efficiently kill cells bearing a high density of the antigen recognized. The primary purpose of this study was to determine if such killing could be obtained with an...

journal_title：Molecular cancer therapeutics

authors： Michel RB,Andrews PM,Castillo ME,Mattes MJ

更新日期：2005-06-01 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：: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：:5'-Fluorouracil (5-FU), used in the treatment of colon and breast cancers, is converted intracellularly to 5'-fluoro-2'-deoxyuridine (5-FUdR) by thymidine phosphorylase and is subsequently phosphorylated by thymidine kinase to 5'-fluoro-2'-dUMP (5-FdUMP). This active metabolite, along with the reduced folate cofactor,...

journal_title：Molecular cancer therapeutics

authors： Pratt S,Shepard RL,Kandasamy RA,Johnston PA,Perry W 3rd,Dantzig AH

更新日期：2005-05-01 00:00:00

abstract：:Multiple myeloma is a slowly proliferating B-cell malignancy that accumulates apoptosis-resistant and replication-quiescent cell populations, posing a challenge for current chemotherapeutics that target rapidly replicating cells. Multiple myeloma remains an incurable disease in need of new therapeutic approaches. The ...

journal_title：Molecular cancer therapeutics

authors： Ghias K,Ma C,Gandhi V,Platanias LC,Krett NL,Rosen ST

更新日期：2005-04-01 00:00:00

abstract：:Floxuridine is a clinically proven anticancer agent in the treatment of metastatic colon carcinomas and hepatic metastases. However, prodrug strategies may be necessary to improve its physiochemical properties and selectivity and to reduce undesirable toxicity effects. Previous studies with amino acid ester prodrugs o...

journal_title：Molecular cancer therapeutics

authors： Landowski CP,Vig BS,Song X,Amidon GL

更新日期：2005-04-01 00:00:00

abstract：:Extensive efforts are under way to identify antiangiogenic therapies for the treatment of human cancers. Many proposed therapeutics target vascular endothelial growth factor (VEGF) or the kinase insert domain receptor (KDR/VEGF receptor-2/FLK-1), the mitogenic VEGF receptor tyrosine kinase expressed by endothelial cel...

journal_title：Molecular cancer therapeutics

authors： Hardwick JS,Yang Y,Zhang C,Shi B,McFall R,Koury EJ,Hill SL,Dai H,Wasserman R,Phillips RL,Weinstein EJ,Kohl NE,Severino ME,Lamb JR,Sepp-Lorenzino L

更新日期：2005-03-01 00:00:00

abstract：:Our recent studies showed that antisense oligodeoxynucleotide targeting antiapoptotic gene, clusterin, enhanced apoptosis induced by conventional therapeutic modalities using several prostate cancer models. In this study, to establish a more effective therapeutic strategy against prostate cancer, we investigated the e...

journal_title：Molecular cancer therapeutics

authors： Yamanaka K,Gleave ME,Hara I,Muramaki M,Miyake H

更新日期：2005-02-01 00:00:00

abstract：:Several studies have shown antitumor activities of the melanoma differentiation-associated gene 7 (mda-7) and the nonsteroidal anti-inflammatory drug sulindac when used as a monotherapies against a wide variety of human cancers. However, the combined effects of mda-7 and sulindac have not previously been tested. There...

journal_title：Molecular cancer therapeutics

authors： Oida Y,Gopalan B,Miyahara R,Inoue S,Branch CD,Mhashilkar AM,Lin E,Bekele BN,Roth JA,Chada S,Ramesh R

更新日期：2005-02-01 00:00:00

abstract：:Aberrant overexpression of antiapoptotic members of the Bcl-2 protein family, including Bcl-2 and Bcl-X(L), contributes to malignant transformation and subsequent resistance to traditional chemotherapeutics. Thus, these proteins represent attractive targets for novel anticancer agents. The small molecule, gossypol, wa...

journal_title：Molecular cancer therapeutics

authors： Oliver CL,Miranda MB,Shangary S,Land S,Wang S,Johnson DE

更新日期：2005-01-01 00:00:00

abstract：:R-roscovitine (seliciclib, CYC202) is a cyclin-dependent kinase inhibitor currently in phase II clinical trials in patients with cancer. Here, we describe its mouse metabolism and pharmacokinetics as well as the identification of the principal metabolites in hepatic microsomes, plasma, and urine. Following microsomal ...

journal_title：Molecular cancer therapeutics

authors： Nutley BP,Raynaud FI,Wilson SC,Fischer PM,Hayes A,Goddard PM,McClue SJ,Jarman M,Lane DP,Workman P

更新日期：2005-01-01 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：:During camptothecin- and etoposide (VP-16)-induced apoptosis in HL-60 cells, the expression level of cell death receptor-3 (DR3), cell death receptor-4 (DR4), and FAS remained mostly unchanged, whereas the expression of silencers of death domain (SODD) and FLICE inhibitory proteins, inhibitors of the cell death recept...

journal_title：Molecular cancer therapeutics

authors： Bergeron S,Beauchemin M,Bertrand R

更新日期：2004-12-01 00:00:00

abstract：UNLABELLED:Multiple myeloma (MM) is a malignancy of clonal B-cells that accounts for 10% of all hematologic malignancies. We have shown previously that a novel purine analogue, 8-chloro-adenosine, has significant activity for MM in preclinical studies. OBJECTIVE:Using MM cell lines, we investigated the molecular mecha...

journal_title：Molecular cancer therapeutics

authors： Krett NL,Davies KM,Ayres M,Ma C,Nabhan C,Gandhi V,Rosen ST

更新日期：2004-11-01 00:00:00

abstract：:Because proliferation of eukaryotic cells requires cell cycle-regulated chromatid separation by the mitotic spindle, it is subject to regulation by mitotic checkpoints. To determine the mechanism of the antiproliferative activity of the flavoprotein-specific inhibitor diphenyleneiodonium (DPI), I have examined its eff...

journal_title：Molecular cancer therapeutics

authors： Scaife RM

更新日期：2004-10-01 00:00:00

abstract：:Using the "one-bead one-peptide" combinatorial technology, a library of random cyclic octapeptides and nonapeptides, consisting of natural and unnatural amino acids, was synthesized on polystyrene beads. This library was used to screen for peptides that promoted attachment and proliferation of bronchioloalveolar carci...

journal_title：Molecular cancer therapeutics

authors： Mikawa M,Wang H,Guo L,Liu R,Marik J,Takada Y,Lam K,Lau D

更新日期：2004-10-01 00:00:00

abstract：:Cryptophycin 52 (LY355703) is a potent antiproliferative analogue of the marine natural product cryptophycin 1. It has been shown to have a broad range of antitumor activity against human tumor xenografts and murine tumors including tumors resistant to Taxol and Adriamycin. Its mechanism of action involves arresting c...

journal_title：Molecular cancer therapeutics

authors： Al-Awar RS,Corbett TH,Ray JE,Polin L,Kennedy JH,Wagner MM,Williams DC

更新日期：2004-09-01 00:00:00

abstract：OBJECTIVES:Emerging evidence implicates the SNAIL family of transcriptional repressors in cancer development; however, the role of SNAIL in colorectal cancer has not been established. To investigate the importance of SNAIL in colorectal carcinogenesis, we examined the phenotypic and cellular consequences of SNAIL down-...

journal_title：Molecular cancer therapeutics

authors： Roy HK,Iversen P,Hart J,Liu Y,Koetsier JL,Kim Y,Kunte DP,Madugula M,Backman V,Wali RK

更新日期：2004-09-01 00:00:00

abstract：OBJECTIVE:Targeting the tumor vasculature may offer an alternative or complementary therapeutic approach to targeting growth factor signaling in lung cancer. The aim of these studies was to evaluate the antitumor effects in vivo of the combination of ZD6126, a tumor-selective vascular-targeting agent; ZD1839 (gefitinib...

journal_title：Molecular cancer therapeutics

authors： Raben D,Bianco C,Damiano V,Bianco R,Melisi D,Mignogna C,D'Armiento FP,Cionini L,Bianco AR,Tortora G,Ciardiello F,Bunn P

更新日期：2004-08-01 00:00:00

abstract：:Targeted thrombotic eradication of solid tumors is a novel therapeutic strategy. The feasibility, efficacy, selectivity, and safety are dependent on multiple variables of protein design, molecular assembly, vascular target, and exclusive restriction of function to the tumor vasculature. To advance this strategy, we de...

journal_title：Molecular cancer therapeutics

authors： Liu C,Dickinson C,Shobe J,Doñate F,Ruf W,Edgington T

更新日期：2004-07-01 00:00:00

abstract：:Many genes, with products involved in the protection of cells against carcinogens, oxidants, and other toxic chemicals, are under the transcriptional control of a simple DNA regulatory element [i.e., the antioxidant response element (ARE)]. One or more functional AREs have been confirmed or are believed to exist in th...

journal_title：Molecular cancer therapeutics

authors： Zhang Y,Gordon GB

更新日期：2004-07-01 00:00:00

abstract：:Gene therapy is a promising approach for the treatment of cancers. Strategies for gene vector delivery include systemic and local-regional approaches. Intratumoral delivery of vectors has generally employed direct injections into single or multiple locations throughout the tumor volume. However, this approach leads to...

journal_title：Molecular cancer therapeutics

authors： Jung M,Zhang Y,Dimtchev A,Subramanian MR,Suthanthiran K,Dritschilo A

更新日期：2004-06-01 00:00:00

abstract：:Transforming growth factor-beta (TGF-beta) is a multifunctional cytokine that promotes malignant glioma invasion, angiogenesis, and immunosuppression. Antisense oligonucleotide suppression of TGF-beta(2) ligand expression has shown promise in preclinical and clinical studies but at least two ligands mediate the effect...

journal_title：Molecular cancer therapeutics

authors： Hjelmeland MD,Hjelmeland AB,Sathornsumetee S,Reese ED,Herbstreith MH,Laping NJ,Friedman HS,Bigner DD,Wang XF,Rich JN

更新日期：2004-06-01 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：:Camptothecin and Adriamycin are clinically important inhibitors for topoisomerase (Topo) I and Topo II, respectively. The ataxia-telangiectasia mutated (ATM) product is essential for ionizing radiation-induced DNA damage responses, but the role of ATM in Topo poisons-induced checkpoints remains unresolved. We found th...

journal_title：Molecular cancer therapeutics

authors： Siu WY,Lau A,Arooz T,Chow JP,Ho HT,Poon RY

更新日期：2004-05-01 00:00:00

abstract：:Gefitinib (Iressa, ZD1839), a quinazoline tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR), is approved for patients with advanced non-small cell lung cancer (NSCLC) in several countries including Japan. However, the mechanism of drug sensitivity to gefitinib is not fully understood. ...

journal_title：Molecular cancer therapeutics

authors： Ono M,Hirata A,Kometani T,Miyagawa M,Ueda S,Kinoshita H,Fujii T,Kuwano M

更新日期：2004-04-01 00:00:00

abstract：:The expression of cyclooxygenase (COX)-2 is increased in human cancers including cholangiocarcinoma. This study was designed to evaluate the effect and mechanisms of the selective COX-2 inhibitor celecoxib in the growth control of human cholangiocarcinoma cells. Immunohistochemical analysis using human cholangiocarcin...

journal_title：Molecular cancer therapeutics

authors： Wu T,Leng J,Han C,Demetris AJ

更新日期：2004-03-01 00:00:00

abstract：:Programmed cell death 4 (Pdcd4), originally identified as an inhibitor of murine cellular transformation, inhibits protein synthesis by directly interacting with eukaryotic initiation factor 4A (eIF4A) of the translation initiation complex. The relevance of Pdcd4 to a broad range of human cancers derived from multiple...

journal_title：Molecular cancer therapeutics

authors： Jansen AP,Camalier CE,Stark C,Colburn NH

更新日期：2004-02-01 00:00:00

abstract：:Cadmium (Cd) is an ubiquitous environmental carcinogen. Membrane phospholipids as well as fatty acid profile of membrane phospholipids are known to be altered in tumorigenicity and malignancy. Synthesis of cellular phosphatidylcholine (PC) has been used as a marker for membrane proliferation in the neoplastic mammary ...

journal_title：Molecular cancer therapeutics

authors： Sinha Roy S,Mukherjee S,Mukhopadhyay S,Das SK

更新日期：2004-02-01 00:00:00

abstract：:The protein kinase family represents an enormous opportunity for drug development. However, the current limitation in structural diversity of kinase inhibitors has complicated efforts to identify effective treatments of diseases that involve protein kinase signaling pathways. We have identified a new structural class ...

journal_title：Molecular cancer therapeutics

authors： Hamdouchi C,Keyser H,Collins E,Jaramillo C,De Diego JE,Spencer CD,Dempsey JA,Anderson BD,Leggett T,Stamm NB,Schultz RM,Watkins SA,Cocke K,Lemke S,Burke TF,Beckmann RP,Dixon JT,Gurganus TM,Rankl NB,Houck KA,Zhang F

更新日期：2004-01-01 00:00:00

abstract：:Allicin (diallyl thiosulfinate), a highly active component in extracts of freshly crushed garlic, is the interaction product of non-protein amino acid alliin (S-allyl-L-cysteine sulfoxide) with the enzyme alliinase (alliin lyase; EC 4.4.1.4). Allicin was shown to be toxic in various mammalian cells in a dose-dependent...

journal_title：Molecular cancer therapeutics

authors： Miron T,Mironchik M,Mirelman D,Wilchek M,Rabinkov A

更新日期：2003-12-01 00:00:00

abstract：:C-phycocyanin, which is a major biliprotein of the blue-green algae, has been shown to possess cyclooxygenase-2 inhibitory activity. We have studied the effect of phycocyanin on a rat histiocytic tumor line. AK-5 cells are induced into apoptotic death program when treated with phycocyanin, which involves the activatio...

journal_title：Molecular cancer therapeutics

authors： Pardhasaradhi BV,Ali AM,Kumari AL,Reddanna P,Khar A

更新日期：2003-11-01 00:00:00

abstract：:The serine protease granzyme B (GrB; 25 kDa) is capable of inducing apoptosis through both caspase-dependent and caspase-independent mechanisms. We designed a novel vascular-targeting fusion construct designated as GrB/vascular endothelial growth factor (VEGF)121, which is composed of a non-heparin-binding isoform of ...

journal_title：Molecular cancer therapeutics

authors： Liu Y,Cheung LH,Thorpe P,Rosenblum MG

更新日期：2003-10-01 00:00:00

abstract：:Bisperoxovanadium (bpV) compounds are irreversible protein tyrosine phosphatase (PTP) inhibitors with a spectrum of activity distinct from that of vanadium salts. We studied the efficacy of a panel of bpVs as antineoplastic agents in vitro and in vivo with a view to investigating phosphatases as potential antineoplast...

journal_title：Molecular cancer therapeutics

authors： Scrivens PJ,Alaoui-Jamali MA,Giannini G,Wang T,Loignon M,Batist G,Sandor VA

更新日期：2003-10-01 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：: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：:Antioxidants, such as vitamin E, are being investigated for efficacy in prostate cancer prevention. In this study, we show that the antioxidant moiety of vitamin E, 2,2,5,7,8-pentamethyl-6-chromanol (PMCol), has antiandrogen activity in prostate carcinoma cells. In the presence of PMCol, the androgen-stimulated biphas...

journal_title：Molecular cancer therapeutics

authors： Thompson TA,Wilding G

更新日期：2003-08-01 00:00:00

abstract：:The development of new drugs against cancer requires established cell lines. They are needed for in vitro studies to identify candidate drugs and in xenograft models to measure drug efficacy in vivo. Specific criteria need to be fulfilled by cell lines used in the evaluation of potential novel therapeutic agents. It i...

journal_title：Molecular cancer therapeutics

authors： Kees UR,Ford J,Watson M,Murch A,Ringńer M,Walker RL,Meltzer P

更新日期：2003-07-01 00:00:00

abstract：:Lavendamycin is a bacterially derived quinolinedione that displays significant antimicrobial and antitumor activities. However, preclinical development of lavendamycin as an anticancer agent was halted due to the poor aqueous solubility and relatively nonspecific cytotoxic activity of this compound. In this report, we...

journal_title：Molecular cancer therapeutics

authors： Fang Y,Linardic CM,Richardson DA,Cai W,Behforouz M,Abraham RT

更新日期：2003-06-01 00:00:00