The Indenoisoquinoline LMP517: A Novel Antitumor Agent Targeting both TOP1 and TOP2.

abstract：:Many malignant human tumors, including melanomas, are auxotrophic for arginine due to reduced expression of argininosuccinate synthetase-1 (ASS1), the rate-limiting enzyme for arginine biosynthesis. Pegylated arginine deiminase (ADI-PEG20), which degrades extracellular arginine, resulting in arginine deprivation, has ...

journal_title：Molecular cancer therapeutics

authors： Long Y,Tsai WB,Wangpaichitr M,Tsukamoto T,Savaraj N,Feun LG,Kuo MT

更新日期：2013-11-01 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：: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：:The serine/threonine kinase AKT/PKB plays a critical role in cancer and represents a rational target for therapy. Although efforts in targeting AKT pathway have accelerated in recent years, relatively few small molecule inhibitors of AKT have been reported. The development of selective AKT inhibitors is further challe...

journal_title：Molecular cancer therapeutics

authors： Toral-Barza L,Zhang WG,Huang X,McDonald LA,Salaski EJ,Barbieri LR,Ding WD,Krishnamurthy G,Hu YB,Lucas J,Bernan VS,Cai P,Levin JI,Mansour TS,Gibbons JJ,Abraham RT,Yu K

更新日期：2007-11-01 00:00:00

abstract：:Mithramycin A is a DNA-binding antitumor agent, which has been clinically used in the therapies of several types of cancer and Paget's disease. In this study, we investigated the combined effect of mithramycin A and tumor necrosis factor-alpha-related apoptosis-inducing ligand (TRAIL) on apoptosis of cancer cells. In ...

journal_title：Molecular cancer therapeutics

authors： Lee TJ,Jung EM,Lee JT,Kim S,Park JW,Choi KS,Kwon TK

更新日期：2006-11-01 00:00:00

abstract：:The endothelin (ET) axis, often deregulated in cancers, is a promising target for anticancer strategies. Whereas previous investigations have focused mostly on ET action in malignant cells, we chose a model allowing separate assessment of the effects of ETs and their receptors ET(A)R and ET(B)R in the tumor cells and ...

journal_title：Molecular cancer therapeutics

authors： Binder C,Hagemann T,Sperling S,Schulz M,Pukrop T,Grimshaw MJ,Ehrenreich H

更新日期：2009-08-01 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：:The PI3K/AKT/mTOR pathway is frequently activated in head and neck squamous cell carcinoma (HNSCC), but pathway inhibition has variable efficacy. Identification of predictive biomarkers and mechanisms of resistance would allow selection of patients most likely to respond and novel therapeutic combinations. The purpose...

journal_title：Molecular cancer therapeutics

authors： Mazumdar T,Byers LA,Ng PK,Mills GB,Peng S,Diao L,Fan YH,Stemke-Hale K,Heymach JV,Myers JN,Glisson BS,Johnson FM

更新日期：2014-11-01 00:00:00

abstract：:Heat shock protein 90 (Hsp90) is widely overexpressed in cancer cells and necessary for maintenance of malignant phenotypes. Hsp90 inhibition induces tumor cell death through degradation of its client oncoproteins and has shown promises in preclinical studies. However, the mechanism by which Hsp90 inhibitors kill tumo...

journal_title：Molecular cancer therapeutics

authors： Tong J,Tan S,Nikolovska-Coleska Z,Yu J,Zou F,Zhang L

更新日期：2017-09-01 00:00:00

abstract：:Betulinic acid (BA), a pentacyclic triterpene isolated from birch bark and other plants, selectively inhibits the growth of human cancer cell lines. However, the poor potency of BA hinders its clinical development, despite a lack of toxicity in animal studies even at high concentrations. Here, we describe six BA deriv...

journal_title：Molecular cancer therapeutics

authors： Liby K,Honda T,Williams CR,Risingsong R,Royce DB,Suh N,Dinkova-Kostova AT,Stephenson KK,Talalay P,Sundararajan C,Gribble GW,Sporn MB

更新日期：2007-07-01 00:00:00

abstract：:Labetuzumab govitecan (IMMU-130), an antibody-drug conjugate (ADC) with an average of 7.6 SN-38/IgG, was evaluated for its potential to enhance delivery of SN-38 to human colonic tumor xenografts. Mice bearing LS174T or GW-39 human colonic tumor xenografts were injected with irinotecan or IMMU-130 (SN-38 equivalents ∼...

journal_title：Molecular cancer therapeutics

authors： Sharkey RM,Govindan SV,Cardillo TM,Donnell J,Xia J,Rossi EA,Chang CH,Goldenberg DM

更新日期：2018-01-01 00:00:00

abstract：:We previously reported that the EGFR-targeted inhibitor erlotinib induces G1 arrest of squamous cell carcinoma of the head and neck (SCCHN) cell lines without inducing significant apoptosis. Large-scale genomic studies suggest that >50% of SCCHN cases have activation of PI3K pathways. This study investigated whether c...

journal_title：Molecular cancer therapeutics

authors： Anisuzzaman AS,Haque A,Wang D,Rahman MA,Zhang C,Chen Z,Chen ZG,Shin DM,Amin AR

更新日期：2017-04-01 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：:PHA-739358 is a small-molecule 3-aminopyrazole derivative with strong activity against Aurora kinases and cross-reactivities with some receptor tyrosine kinases relevant for cancer. PHA-739358 inhibits all Aurora kinase family members and shows a dominant Aurora B kinase inhibition-related cellular phenotype and mecha...

journal_title：Molecular cancer therapeutics

authors： Carpinelli P,Ceruti R,Giorgini ML,Cappella P,Gianellini L,Croci V,Degrassi A,Texido G,Rocchetti M,Vianello P,Rusconi L,Storici P,Zugnoni P,Arrigoni C,Soncini C,Alli C,Patton V,Marsiglio A,Ballinari D,Pesenti E,Fan

更新日期：2007-12-01 00:00:00

abstract：:We reported previously that 5-fluorouracil (FUra) efficacy could be enhanced by increasing tumoral thymidine phosphorylase (TP) activity. Potentiated TP yield was achieved by either transfecting cells with human TP gene (A. Evrard et al., Br. J. Cancer, 80: 1726-1733, 1999) or associating FUra with 2'-deoxyinosine (d-...

journal_title：Molecular cancer therapeutics

authors： Ciccolini J,Cuq P,Evrard A,Giacometti S,Pelegrin A,Aubert C,Cano JP,Iliadis A

更新日期：2001-12-01 00:00:00

abstract：:Hodgkin-Reed/Sternberg (HRS) cells of classical Hodgkin lymphoma show aberrant expression and activation of several receptor tyrosine kinases (RTK) in the majority of cases. Therefore, we tested whether tyrosine kinase inhibitors (TKI) already in clinical use or late stages of clinical trials have antiproliferative ef...

journal_title：Molecular cancer therapeutics

authors： Holz MS,Janning A,Renné C,Gattenlöhner S,Spieker T,Bräuninger A

更新日期：2013-02-01 00:00:00

abstract：:Molecular mechanisms underlying epothilone-induced apoptotic cell death were investigated in SW620 human colon cancer cells. Treatment with epothilone B and D at different concentrations (1-100 nmol/L) dose-dependently inhibited cell growth and caused cell cycle arrest at G2-M, which was followed by apoptosis. Consist...

journal_title：Molecular cancer therapeutics

authors： Lee SH,Son SM,Son DJ,Kim SM,Kim TJ,Song S,Moon DC,Lee HW,Ryu JC,Yoon DY,Hong JT

更新日期：2007-10-01 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：: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：:In the current study, we examined a panel of serially passaged glioblastoma xenografts, in the context of an intracranial tumor therapy response model, to identify associations between glioblastoma molecular characteristics and tumor sensitivity to the epidermal growth factor receptor (EGFR) kinase inhibitor erlotinib...

journal_title：Molecular cancer therapeutics

authors： Sarkaria JN,Yang L,Grogan PT,Kitange GJ,Carlson BL,Schroeder MA,Galanis E,Giannini C,Wu W,Dinca EB,James CD

更新日期：2007-03-01 00:00:00

abstract：:Several clinical trials have shown gallium nitrate to be an active agent in the treatment of lymphoma. Whereas gallium is known to target cellular iron homeostasis, the basis for lymphoma cell resistance to gallium is not known. Understanding mechanisms of resistance may suggest strategies to enhance the clinical effi...

journal_title：Molecular cancer therapeutics

authors： Yang M,Kroft SH,Chitambar CR

更新日期：2007-02-01 00:00:00

abstract：:Phospho-sulindac is a sulindac derivative with promising anticancer activity in lung cancer, but its limited metabolic stability presents a major challenge for systemic therapy. We reasoned that inhalation delivery of phospho-sulindac might overcome first-pass metabolism and produce high levels of intact drug in lung ...

journal_title：Molecular cancer therapeutics

authors： Cheng KW,Wong CC,Alston N,Mackenzie GG,Huang L,Ouyang N,Xie G,Wiedmann T,Rigas B

更新日期：2013-08-01 00:00:00

abstract：:FOXO proteins are Akt-regulated transcription factors involved in the control of cell cycle, DNA repair, stress defense, apoptosis, and tumor suppression. We reported that plasmid-based overexpression of constitutively active FOXO3 in cells from chronic lymphocytic leukemia (CLL) reduced their survival, suggesting tha...

journal_title：Molecular cancer therapeutics

authors： Essafi M,Baudot AD,Mouska X,Cassuto JP,Ticchioni M,Deckert M

更新日期：2011-01-01 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 PI3K-AKT pathway has pleiotropic effects and its inhibition has long been of interest in the management of prostate cancer, where a compensatory increase in PI3K signaling has been reported following androgen receptor (AR) blockade. Prostate cancer cells can also bypass AR blockade through induction of other hormo...

journal_title：Molecular cancer therapeutics

authors： Adelaiye-Ogala R,Gryder BE,Nguyen YTM,Alilin AN,Grayson AR,Bajwa W,Jansson KH,Beshiri ML,Agarwal S,Rodriguez-Nieves JA,Capaldo B,Kelly K,VanderWeele DJ

更新日期：2020-07-01 00:00:00

abstract：:Artesunate, the active agent from Artemisia annua L. used in the traditional Chinese medicine, is being applied as a first-line drug for malaria treatment, and trials are ongoing that include this drug in cancer therapy. Despite increasing interest in its therapeutic application, the mode of cell killing provoked by a...

journal_title：Molecular cancer therapeutics

authors： Berdelle N,Nikolova T,Quiros S,Efferth T,Kaina B

更新日期：2011-12-01 00:00:00

abstract：:Human epidermal growth factor receptor-2 (HER2) and epidermal growth factor receptor (EGFR) heterodimerize to activate mitogenic signaling pathways. We have shown previously, using MCF7 subcloned cell lines with graded levels of HER2 expression, that responsiveness to trastuzumab and AG1478 (an anti-EGFR agent), varie...

journal_title：Molecular cancer therapeutics

authors： Emlet DR,Brown KA,Kociban DL,Pollice AA,Smith CA,Ong BB,Shackney SE

更新日期：2007-10-01 00:00:00

abstract：:Endothelins (ETs) are a group of vasoactive peptides (ET-1, ET-2 and ET-3) produced by many cell types that bind to G-protein-linked transmembrane receptors, ET-A receptors (ET-RAs) and ET-B receptors (ET-RBs). These peptides are expressed in several human tumors, including carcinomas of the breast, and have a mitogen...

journal_title：Molecular cancer therapeutics

authors： Grimshaw MJ,Naylor S,Balkwill FR

更新日期：2002-12-01 00:00:00

abstract：:Viral-based chimeric antigen receptor-engineered T (CAR T)-cell manufacturing has potential safety risks and relatively high costs. The nonviral minicircle DNA (mcDNA) is safer for patients, cheaper to produce, and may be a more suitable technique to generate CAR T cells. In this study, we produced mcDNA-based CAR T c...

journal_title：Molecular cancer therapeutics

authors： Han J,Gao F,Geng S,Ye X,Wang T,Du P,Cai Z,Fu Z,Zhao Z,Shi L,Li Q,Cai J

更新日期：2020-01-01 00:00:00

abstract：:This study aimed to investigate the antitumor and antiangiogenic effects utilizing a novel therapy regimen of metronomic topotecan and pazopanib, a multireceptor tyrosine kinase inhibitor. In vitro (Western blot) and in vivo dose-finding experiments were done following pazopanib therapy in ovarian cancer models. Pazop...

journal_title：Molecular cancer therapeutics

authors： Merritt WM,Nick AM,Carroll AR,Lu C,Matsuo K,Dumble M,Jennings N,Zhang S,Lin YG,Spannuth WA,Kamat AA,Stone RL,Shahzad MM,Coleman RL,Kumar R,Sood AK

更新日期：2010-04-01 00:00:00