2-Deoxy-Glucose Downregulates Endothelial AKT and ERK via Interference with N-Linked Glycosylation, Induction of Endoplasmic Reticulum Stress, and GSK3β Activation.

abstract：:Clear cell renal cell carcinoma (CC-RCC) is a devastating disease with limited therapeutic options available for advanced stages. The objective of this study was to investigate HMG-CoA reductase inhibitors, also known as statins, as potential therapeutics for CC-RCC. Importantly, treatment with statins was found to be...

journal_title：Molecular cancer therapeutics

authors： Thompson JM,Alvarez A,Singha MK,Pavesic MW,Nguyen QH,Nelson LJ,Fruman DA,Razorenova OV

更新日期：2018-08-01 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：: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：:The tyrosine kinase receptor c-Met and its ligand hepatocyte growth factor (HGF) are frequently overexpressed and the tumor suppressor PTEN is often mutated in glioblastoma. Because PTEN can interact with c-Met-dependent signaling, we studied the effects of PTEN on c-Met-induced malignancy and associated molecular eve...

journal_title：Molecular cancer therapeutics

authors： Li Y,Guessous F,DiPierro C,Zhang Y,Mudrick T,Fuller L,Johnson E,Marcinkiewicz L,Engelhardt M,Kefas B,Schiff D,Kim J,Abounader R

更新日期：2009-02-01 00:00:00

abstract：:There is a growing recognition that current preclinical models do not reflect the tumor microenvironment in cellular, biological, and biophysical content and this may have a profound effect on drug efficacy testing, especially in the era of molecular-targeted agents. Here, we describe a method to directly embed low-pa...

journal_title：Molecular cancer therapeutics

authors： Onion D,Argent RH,Reece-Smith AM,Craze ML,Pineda RG,Clarke PA,Ratan HL,Parsons SL,Lobo DN,Duffy JP,Atherton JC,McKenzie AJ,Kumari R,King P,Hall BM,Grabowska AM

更新日期：2016-04-01 00:00:00

abstract：:ErbB2 tyrosine kinase inhibitors (TKI) block tyrosine autophosphorylation and activation of the full-length transmembrane ErbB2 receptor (p185(ErbB2)). In addition to p185(ErbB2), truncated forms of ErbB2 exist in breast cancer cell lines and clinical tumors. The contribution of these truncated forms, specifically tho...

journal_title：Molecular cancer therapeutics

authors： Xia W,Liu Z,Zong R,Liu L,Zhao S,Bacus SS,Mao Y,He J,Wulfkuhle JD,Petricoin EF 3rd,Osada T,Yang XY,Hartman ZC,Clay TM,Blackwell KL,Lyerly HK,Spector NL

更新日期：2011-08-01 00:00:00

abstract：:Crizotinib (PF02341066) is a tyrosine kinase inhibitor of anaplastic lymphoma kinase (ALK) that has been shown to selectively inhibit growth of cancer cells that harbor the EML4-ALK fusion found in a subset of patients with non-small cell lung cancer (NSCLC). While in clinical trials, PF02341066 has shown a significan...

journal_title：Molecular cancer therapeutics

authors： Sun Y,Nowak KA,Zaorsky NG,Winchester CL,Dalal K,Giacalone NJ,Liu N,Werner-Wasik M,Wasik MA,Dicker AP,Lu B

更新日期：2013-05-01 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is a deadly malignancy that frequently metastasizes and that overexpresses transforming growth factor-beta s (TGF-beta s). To determine whether TGF-beta s can act to enhance the metastatic potential of PDAC, PANC-1 human pancreatic cancer cells were transfected with an expressio...

journal_title：Molecular cancer therapeutics

authors： Rowland-Goldsmith MA,Maruyama H,Matsuda K,Idezawa T,Ralli M,Ralli S,Korc M

更新日期：2002-01-01 00:00:00

abstract：:Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), a member of the tumor necrosis factor superfamily, is in clinical trials for cancer therapy, but its anticancer potential is limited by the development of resistance. We investigated the ability of tocotrienol (T3), an unsaturated vitamin E present in pa...

journal_title：Molecular cancer therapeutics

authors： Kannappan R,Ravindran J,Prasad S,Sung B,Yadav VR,Reuter S,Chaturvedi MM,Aggarwal BB

更新日期：2010-08-01 00:00:00

abstract：:STAT3 has been recognized for its key role in the progression of cancer, where it is frequently upregulated or constitutively hyperactivated, contributing to tumor cell proliferation, survival, and migration, as well as angiogenesis and suppression of antitumor immunity. Given the ubiquity of dysregulated STAT3 activi...

journal_title：Molecular cancer therapeutics

authors： Shiah JV,Grandis JR,Johnson DE

更新日期：2020-11-17 00:00:00

abstract：:Neuroblastoma is the most common extracranial solid tumor of childhood. The activity of J1 (l-melphalanyl-p-l-fluorophenylalanine ethyl ester), an enzymatically activated melphalan prodrug, was evaluated in neuroblastoma models in vitro and in vivo. Seven neuroblastoma cell lines with various levels of drug resistance...

journal_title：Molecular cancer therapeutics

authors： Wickström M,Johnsen JI,Ponthan F,Segerström L,Sveinbjörnsson B,Lindskog M,Lövborg H,Viktorsson K,Lewensohn R,Kogner P,Larsson R,Gullbo J

更新日期：2007-09-01 00:00:00

abstract：:Angiogenesis is required for tumor growth and metastasis, and targeting angiogenesis is a novel anticancer strategy. However, cancer development is a complex multistep process, and single antiangiogenic agents have limited therapeutic efficacy. Here, we report a triple fusion protein, namely CTT peptide-endostatin mim...

journal_title：Molecular cancer therapeutics

authors： Wang H,Yang Z,Gu J

更新日期：2014-11-01 00:00:00

abstract：:Imatinib mesylate is a potent, molecularly targeted therapy against the oncogenic tyrosine kinase BCR-ABL. Although imatinib mesylate has considerable efficacy against chronic myeloid leukemia (CML), advanced-stage CML patients frequently become refractory to this agent. The bone marrow is the predominant microenviron...

journal_title：Molecular cancer therapeutics

authors： Bewry NN,Nair RR,Emmons MF,Boulware D,Pinilla-Ibarz J,Hazlehurst LA

更新日期：2008-10-01 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：: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：:Luteolin, a common dietary flavonoid, has been found to have antitumor properties and therefore poses special interest for the development of preventive and/or therapeutic agent for cancers. E-cadherin, a marker of epithelial cells, mediates cell-cell adhesion. Decreased expression of E-cadherin results in a loss of c...

journal_title：Molecular cancer therapeutics

authors： Zhou Q,Yan B,Hu X,Li XB,Zhang J,Fang J

更新日期：2009-06-01 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：: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：:Deregulation of the cell cycle has long been recognized as an essential driver of tumorigenesis, and agents that selectively target key cell cycle components continue to hold promise as potential therapeutics. We have developed AZD5438, a 4-(1-isopropyl-2-methylimidazol-5-yl)-2-(4-methylsulphonylanilino) pyrimidine, a...

journal_title：Molecular cancer therapeutics

authors： Byth KF,Thomas A,Hughes G,Forder C,McGregor A,Geh C,Oakes S,Green C,Walker M,Newcombe N,Green S,Growcott J,Barker A,Wilkinson RW

更新日期：2009-07-01 00:00:00

abstract：:Controversy exists surrounding whether heterogeneous disruption of the blood-brain barrier (BBB), as seen in glioblastoma (GBM), leads to adequate drug delivery sufficient for efficacy in GBM. This question is especially important when using potent, targeted agents that have a poor penetration across an intact BBB. Ef...

journal_title：Molecular cancer therapeutics

authors： Kim M,Ma DJ,Calligaris D,Zhang S,Feathers RW,Vaubel RA,Meaux I,Mladek AC,Parrish KE,Jin F,Barriere C,Debussche L,Watters J,Tian S,Decker PA,Eckel-Passow JE,Kitange GJ,Johnson AJ,Parney IF,Anastasiadis PZ,Agar NYR

更新日期：2018-09-01 00:00:00

abstract：:In 2017, an estimated 17,000 individuals were diagnosed with esophageal adenocarcinoma (EAC), and less than 20% will survive 5 years. Positron emission tomography avidity is indicative of high glucose utilization and is nearly universal in EAC. TXNIP blocks glucose uptake and exhibits proapoptotic functions. Higher ex...

journal_title：Molecular cancer therapeutics

authors： Feingold PL,Surman DR,Brown K,Xu Y,McDuffie LA,Shukla V,Reardon ES,Crooks DR,Trepel JB,Lee S,Lee MJ,Gao S,Xi S,McLoughlin KC,Diggs LP,Beer DG,Nancarrow DJ,Neckers LM,Davis JL,Hoang CD,Hernandez JM,Schrump DS,R

更新日期：2018-09-01 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：: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：:While epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors improve the prognosis of patients with EGFR mutant lung cancer, the prognosis of patients with nonmutant EGFR lung cancer, especially those with metastases, is still extremely poor. We have assessed the therapeutic efficacy of E7080, an orally av...

journal_title：Molecular cancer therapeutics

authors： Ogino H,Hanibuchi M,Kakiuchi S,Trung VT,Goto H,Ikuta K,Yamada T,Uehara H,Tsuruoka A,Uenaka T,Wang W,Li Q,Takeuchi S,Yano S,Nishioka Y,Sone S

更新日期：2011-07-01 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：: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：:Our previous studies have shown that z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. We now report a novel response to z-guggulsterone involving the inhibition of angiogenesis in vitro and in vivo. The z-guggu...

journal_title：Molecular cancer therapeutics

authors： Xiao D,Singh SV

更新日期：2008-01-01 00:00:00

abstract：:The primary mechanism of antibody-drug conjugates (ADC) is targeted delivery of a cytotoxic payload to tumor cells via cancer-associated membrane receptors. However, the tumor microenvironment likely plays a role in ADC penetration, distribution, and processing and thus impacts the overall antitumor activity. Here, we...

journal_title：Molecular cancer therapeutics

authors： Li F,Ulrich M,Jonas M,Stone IJ,Linares G,Zhang X,Westendorf L,Benjamin DR,Law CL

更新日期：2017-07-01 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：:Elevated levels of Src kinase expression have been found in a variety of human epithelial cancers. Most notably in colon cancer, elevated Src expression correlates with malignant potential and is also associated with metastatic disease. Dasatinib (BMS-354825) is a novel, orally active, multi-targeted kinase inhibitor ...

journal_title：Molecular cancer therapeutics

authors： Serrels A,Macpherson IR,Evans TR,Lee FY,Clark EA,Sansom OJ,Ashton GH,Frame MC,Brunton VG

更新日期：2006-12-01 00:00:00