The TLR3 Agonist Inhibit Drug Efflux and Sequentially Consolidates Low-Dose Cisplatin-Based Chemoimmunotherapy while Reducing Side Effects.

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：:The majority of patients with HER2-overexpressing metastatic breast cancer who initially respond to the HER2-targeted antibody trastuzumab show disease progression within 1 year. The identification of novel agents that effectively inhibit survival of cancer cells that have progressed on trastuzumab is critical for imp...

journal_title：Molecular cancer therapeutics

authors： Rowe DL,Ozbay T,Bender LM,Nahta R

更新日期：2008-07-01 00:00:00

abstract：:Anti-HER2/CD3, a T-cell-dependent bispecific antibody (TDB) construct, induces T-cell-mediated cell death in cancer cells expressing HER2 by cross-linking tumor HER2 with CD3 on cytotoxic T cells, thereby creating a functional cytolytic synapse. TDB design is a very challenging process that requires consideration of m...

journal_title：Molecular cancer therapeutics

authors： Mandikian D,Takahashi N,Lo AA,Li J,Eastham-Anderson J,Slaga D,Ho J,Hristopoulos M,Clark R,Totpal K,Lin K,Joseph SB,Dennis MS,Prabhu S,Junttila TT,Boswell CA

更新日期：2018-04-01 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 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：:The epithelial-mesenchymal transition (EMT) is a process associated with the metastasis of solid tumors as well as with the acquisition of resistance to standard anticancer modalities. A major initiator of EMT in carcinoma cells is TGF-β, which has been shown to induce the expression of several transcription factors u...

journal_title：Molecular cancer therapeutics

authors： Larocca C,Cohen JR,Fernando RI,Huang B,Hamilton DH,Palena C

更新日期：2013-09-01 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：:Androgen deprivation therapy and second-generation androgen receptor signaling inhibitors such as enzalutamide are standard treatments for advanced/metastatic prostate cancer. Unfortunately, most men develop resistance and relapse; signaling via insulin-like growth factor (IGF) has been implicated in castration-resist...

journal_title：Molecular cancer therapeutics

authors： Weyer-Czernilofsky U,Hofmann MH,Friedbichler K,Baumgartinger R,Adam PJ,Solca F,Kraut N,Nguyen HM,Corey E,Liu G,Sprenger CC,Plymate SR,Bogenrieder T

更新日期：2020-04-01 00:00:00

abstract：:Bortezomib is highly effective in the treatment of multiple myeloma; however, emergent drug resistance is common. Consequently, we employed CRISPR targeting 19,052 human genes to identify unbiased targets that contribute to bortezomib resistance. Specifically, we engineered an RPMI8226 multiple myeloma cell line to ex...

journal_title：Molecular cancer therapeutics

authors： Shi CX,Kortüm KM,Zhu YX,Bruins LA,Jedlowski P,Votruba PG,Luo M,Stewart RA,Ahmann J,Braggio E,Stewart AK

更新日期：2017-12-01 00:00:00

abstract：:A novel oral Hsp90 inhibitor, NVP-HSP990, has been developed and characterized in vitro and in vivo. In vitro, NVP-HSP990 exhibits single digit nanomolar IC(50) values on three of the Hsp90 isoforms (Hsp90α, Hsp90β, and GRP94) and 320 nanomolar IC(50) value on the fourth (TRAP-1), with selectivity against unrelated en...

journal_title：Molecular cancer therapeutics

authors： Menezes DL,Taverna P,Jensen MR,Abrams T,Stuart D,Yu GK,Duhl D,Machajewski T,Sellers WR,Pryer NK,Gao Z

更新日期：2012-03-01 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：:IPI-504 is a novel, highly soluble small-molecule inhibitor of heat shock protein 90 (Hsp90), a protein chaperone essential for regulating homeostasis of oncoproteins and cell signaling proteins. Human epidermal growth factor receptor 2 (HER2; ErbB2) oncoprotein, expressed in a subset of metastatic breast cancers, is ...

journal_title：Molecular cancer therapeutics

authors： Leow CC,Chesebrough J,Coffman KT,Fazenbaker CA,Gooya J,Weng D,Coats S,Jackson D,Jallal B,Chang Y

更新日期：2009-08-01 00:00:00

abstract：:Barasertib (AZD1152), a highly potent and selective aurora kinase B inhibitor, gave promising clinical activity in elderly acute myeloid leukemia (AML) patients. However, clinical utility was limited by the requirement for a 7-day infusion. Here we assessed the potential of a nanoparticle formulation of the selective ...

journal_title：Molecular cancer therapeutics

authors： Floc'h N,Ashton S,Taylor P,Trueman D,Harris E,Odedra R,Maratea K,Derbyshire N,Caddy J,Jacobs VN,Hattersley M,Wen S,Curtis NJ,Pilling JE,Pease EJ,Barry ST

更新日期：2017-06-01 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：:Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and for maintaining the spindle assembly checkpoint until all chromosomes are properly attached. Mps1 is expressed at high levels during mitosis and is abundantly expressed in cancer cells. Disr...

journal_title：Molecular cancer therapeutics

authors： Tardif KD,Rogers A,Cassiano J,Roth BL,Cimbora DM,McKinnon R,Peterson A,Douce TB,Robinson R,Dorweiler I,Davis T,Hess MA,Ostanin K,Papac DI,Baichwal V,McAlexander I,Willardsen JA,Saunders M,Christophe H,Kumar DV,Wet

更新日期：2011-12-01 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：:Although proteasome inhibitors such as bortezomib had significant therapeutic effects in multiple myeloma and mantel cell lymphoma, they exhibited minimal clinical activity as a monotherapy for solid tumors, including colorectal cancer. We found in this study that proteasome inhibition induced a remarkable nuclear exp...

journal_title：Molecular cancer therapeutics

authors： Wu T,Chen W,Zhong Y,Hou X,Fang S,Liu CY,Wang G,Yu T,Huang YY,Ouyang X,Li HQ,Cui L,Yang Y

更新日期：2017-04-01 00:00:00

abstract：:RECQL1, a key member of the RecQ family of DNA helicases, is required for DNA replication and DNA repair. Two recent studies have shown that germline RECQL1 mutations are associated with increased breast cancer susceptibility. Whether altered RECQL1 expression has clinicopathologic significance in sporadic breast canc...

journal_title：Molecular cancer therapeutics

authors： Arora A,Parvathaneni S,Aleskandarany MA,Agarwal D,Ali R,Abdel-Fatah T,Green AR,Ball GR,Rakha EA,Ellis IO,Sharma S,Madhusudan S

更新日期：2017-01-01 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

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：:Nanotechnology has enabled significant advances in the areas of cancer diagnosis and therapy. The field of drug delivery is a sterling example, with nanoparticles being increasingly used for generating therapeutic formulations of poorly water-soluble, yet potent anticancer drugs. Whereas a number of nanoparticle-drug ...

journal_title：Molecular cancer therapeutics

authors： Bisht S,Feldmann G,Koorstra JB,Mullendore M,Alvarez H,Karikari C,Rudek MA,Lee CK,Maitra A,Maitra A

更新日期：2008-12-01 00:00:00

abstract：:STAT3 has been strongly implicated in human malignancies, and constitutive activation of STAT3 serves a crucial role in cell survival, angiogenesis, immune evasion, and inflammation. In this study, we showed that nitidine chloride, a natural phytochemical alkaloid derived from Zanthoxylum nitidum (Roxb) DC, exerts pot...

journal_title：Molecular cancer therapeutics

authors： Chen J,Wang J,Lin L,He L,Wu Y,Zhang L,Yi Z,Chen Y,Pang X,Liu M

更新日期：2012-02-01 00:00:00

abstract：:Aptamers, also termed as decoys or "chemical antibodies," represent an emerging class of therapeutics. They are short DNA or RNA oligonucleotides or peptides that assume a specific and stable three-dimensional shape in vivo, thereby providing specific tight binding to protein targets. In some cases and as opposed to a...

journal_title：Molecular cancer therapeutics

authors： Ireson CR,Kelland LR

更新日期：2006-12-01 00:00:00

abstract：:Streptozotocin-based chemotherapy is the first-line chemotherapy recommended for advanced pancreatic neuroendocrine tumors (pNETs), whereas targeted therapies, including mTOR inhibitors, are available in second-line treatment. Unfortunately, objective response rates to both treatments are limited. Because mTOR pathway...

journal_title：Molecular cancer therapeutics

authors： Bollard J,Patte C,Massoma P,Goddard I,Gadot N,Benslama N,Hervieu V,Ferraro-Peyret C,Cordier-Bussat M,Scoazec JY,Roche C,Walter T,Vercherat C

更新日期：2018-01-01 00:00:00

abstract：:Hsp90 is widely overexpressed in cancer cells and believed to be essential for the maintenance of malignant phenotypes. Targeting Hsp90 by small molecules has shown promise in solid and hematologic malignancies, which likely involves degradation of client oncoproteins in a cell-type-specific manner. In this study, we ...

journal_title：Molecular cancer therapeutics

authors： He K,Zheng X,Zhang L,Yu J

更新日期：2013-11-01 00:00:00

abstract：:Chemoresistance is a major reason that patients with osteosarcoma fail to achieve a lasting chemotherapy response, and it contributes to disease relapse, progression, and death. Human glutathione S-transferase P1 (GSTP1), a phase II detoxification enzyme, contributes to chemoresistance in many cancers. However, the ro...

journal_title：Molecular cancer therapeutics

authors： Huang G,Mills L,Worth LL

更新日期：2007-05-01 00:00:00

abstract：:Specific delivery to tumors and efficient cellular uptake of nucleic acids remain major challenges for gene-targeted cancer therapies. Here we report the use of a designed ankyrin repeat protein (DARPin) specific for the epithelial cell adhesion molecule (EpCAM) as a carrier for small interfering RNA (siRNA) complemen...

journal_title：Molecular cancer therapeutics

authors： Winkler J,Martin-Killias P,Plückthun A,Zangemeister-Wittke U

更新日期：2009-09-01 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：:The objective of this study was to evaluate circulating hepatocyte growth factor (cHGF) as a pharmacodynamic biomarker of Met inhibition for onartuzumab (MetMAb, OA5D5v2) in a phase I trial in patients with advanced cancers and a phase II trial in non-small cell lung cancer (NSCLC). The phase I study was a dose escala...

journal_title：Molecular cancer therapeutics

authors： Penuel E,Li C,Parab V,Burton L,Cowan KJ,Merchant M,Yauch RL,Patel P,Peterson A,Hampton GM,Lackner MR,Hegde PS

更新日期：2013-06-01 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