Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation.

abstract：:Acute myeloid leukemia (AML) with Fms-related tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutation is notoriously hard to treat. We identified two drugs that together form an effective combination therapy against FLT3-ITD AML. One of the drugs, Sorafenib, an inhibitor of FLT3-ITD and other kinase activity...

journal_title：Molecular cancer therapeutics

authors： Wang R,Li Y,Gong P,Gabrilove J,Waxman S,Jing Y

更新日期：2018-09-01 00:00:00

abstract：:Metastatic castration-resistant prostate cancer (CRPC) is currently incurable. Cancer growth and progression is intimately affected by its interaction with host microenvironment. Cotargeting of the stroma and prostate cancer is therefore an emerging therapeutic strategy for metastatic CRPC. Cancer-induced osteoclastog...

journal_title：Molecular cancer therapeutics

authors： Hsieh CL,Huang HS,Chen KC,Saka T,Chiang CY,Chung LWK,Sung SY

更新日期：2020-01-01 00:00:00

abstract：:Ascofuranone has been shown to have antitumor activity, but the precise molecular mechanism by which it inhibits the proliferation of cancer cells remains unclear. Here, we study the effects of ascofuranone on cell cycle progression in human cancer cells and find that ascofuranone induces G(1) arrest without cytoxicit...

journal_title：Molecular cancer therapeutics

authors： Jeong JH,Kang SS,Park KK,Chang HW,Magae J,Chang YC

更新日期：2010-07-01 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：: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：:The FGF receptors (FGFR) are tyrosine kinases that are constitutively activated in a subset of tumors by genetic alterations such as gene amplifications, point mutations, or chromosomal translocations/rearrangements. Recently, small-molecule inhibitors that can inhibit the FGFR family as well as the VEGF receptor (VEG...

journal_title：Molecular cancer therapeutics

authors： Nakanishi Y,Akiyama N,Tsukaguchi T,Fujii T,Sakata K,Sase H,Isobe T,Morikami K,Shindoh H,Mio T,Ebiike H,Taka N,Aoki Y,Ishii N

更新日期：2014-11-01 00:00:00

abstract：:G-protein mutations are one of the most common mutations occurring in uveal melanoma activating the protein kinase C (PKC)/mitogen-activated protein kinase and phosphoinositide 3-kinase (PI3K)/AKT pathways. In this study, we described the effect of dual pathway inhibition in uveal melanoma harboring GNAQ and GNA11 mut...

journal_title：Molecular cancer therapeutics

authors： Musi E,Ambrosini G,de Stanchina E,Schwartz GK

更新日期：2014-05-01 00:00:00

abstract：:Notch signaling is aberrantly activated in approximately one third of non-small cell lung cancers (NSCLC). We characterized the interaction between BMS-906024, a clinically relevant Notch gamma secretase inhibitor, and front-line chemotherapy in preclinical models of NSCLC. Chemosensitivity assays were performed on 14...

journal_title：Molecular cancer therapeutics

authors： Morgan KM,Fischer BS,Lee FY,Shah JJ,Bertino JR,Rosenfeld J,Singh A,Khiabanian H,Pine SR

更新日期：2017-12-01 00:00:00

abstract：:Uveal melanoma is a rare and aggressive cancer that originates in the eye. Currently, there are no approved targeted therapies and very few effective treatments for this cancer. Although activating mutations in the G protein alpha subunits, GNAQ and GNA11, are key genetic drivers of the disease, few additional drug ta...

journal_title：Molecular cancer therapeutics

authors： Rago F,Elliott G,Li A,Sprouffske K,Kerr G,Desplat A,Abramowski D,Chen JT,Farsidjani A,Xiang KX,Bushold G,Feng Y,Shirley MD,Bric A,Vattay A,Möbitz H,Nakajima K,Adair CD,Mathieu S,Ntaganda R,Smith T,Papillon JPN,

更新日期：2020-10-01 00:00:00

abstract：:Prostate-specific membrane antigen (PSMA) is a protein up-regulated in the vast majority of prostate cancers. Antibodies to PSMA have proved highly specific for prostate cancer cells, and the therapeutic potential of such antibodies is currently being assessed in clinical trials. We have previously shown that PSMA at ...

journal_title：Molecular cancer therapeutics

authors： Christiansen JJ,Weimbs T,Bander N,Rajasekaran AK

更新日期：2006-10-01 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：:Neuroblastoma is the most common extracranial solid malignancy in the pediatric population, accounting for over 9% of all cancer-related deaths in children. Autophagy is a cell self-protective mechanism that promotes tumor cell growth and survival, making it an attractive target for treating cancer. However, the role ...

journal_title：Molecular cancer therapeutics

authors： Dower CM,Bhat N,Gebru MT,Chen L,Wills CA,Miller BA,Wang HG

更新日期：2018-11-01 00:00:00

abstract：:TAS-121 is a novel orally active selective covalent inhibitor of the mutant EGFR. We performed preclinical characterization of TAS-121 and compared its efficacy and selectivity for common EGFR mutations (Ex19del and L858R), first- and second- generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) resistance mutation (T7...

journal_title：Molecular cancer therapeutics

authors： Ito K,Nishio M,Kato M,Murakami H,Aoyagi Y,Ohe Y,Okayama T,Hashimoto A,Ohsawa H,Tanaka G,Nonoshita K,Ito S,Matsuo K,Miyadera K

更新日期：2019-05-01 00:00:00

abstract：:The efficacy of photodynamic therapy (PDT) for epithelial cancers is increased when PDT is combined with calcitriol (Vit D), a form of differentiation therapy (DT). Here, we describe an underlying mechanism for this effect. Differentiation-promoting agents are known to upregulate CCAAT/enhancer-binding proteins (C/EBP...

journal_title：Molecular cancer therapeutics

authors： Anand S,Hasan T,Maytin EV

更新日期：2013-08-01 00:00:00

abstract：:Both human epidermal growth factor receptor 2 (HER-2/neu) and VEGF overexpression correlate with aggressive phenotypes and decreased survival among breast cancer patients. Concordantly, the combination of trastuzumab (anti-HER2) with bevacizumab (anti-VEGF) has shown promising results in preclinical xenograft studies ...

journal_title：Molecular cancer therapeutics

authors： Pastuskovas CV,Mundo EE,Williams SP,Nayak TK,Ho J,Ulufatu S,Clark S,Ross S,Cheng E,Parsons-Reponte K,Cain G,Van Hoy M,Majidy N,Bheddah S,dela Cruz Chuh J,Kozak KR,Lewin-Koh N,Nauka P,Bumbaca D,Sliwkowski M,Tibbitt

更新日期：2012-03-01 00:00:00

abstract：:Phosphatidylinositol 3-kinase/phosphatidylinositide-dependent protein kinase 1 (PDPK1)/Akt signaling plays a critical role in activating proliferation and survival pathways within cancer cells. We report the molecular pharmacology and antitumor activity of PHT-427, a compound designed to bind to the pleckstrin homolog...

journal_title：Molecular cancer therapeutics

authors： Meuillet EJ,Zuohe S,Lemos R,Ihle N,Kingston J,Watkins R,Moses SA,Zhang S,Du-Cuny L,Herbst R,Jacoby JJ,Zhou LL,Ahad AM,Mash EA,Kirkpatrick DL,Powis G

更新日期：2010-03-01 00:00:00

abstract：:The therapeutic efficiency of anticancer nucleoside analogues (NA) strongly depends on their intracellular accumulation and conversion into 5'-triphosphates. Because active NATP cannot be directly administrated due to instability, we present here a strategy of nanoencapsulation of these active drugs for efficient deli...

journal_title：Molecular cancer therapeutics

authors： Galmarini CM,Warren G,Kohli E,Zeman A,Mitin A,Vinogradov SV

更新日期：2008-10-01 00:00:00

abstract：:Our previous studies and those of others have indicated that X-linked inhibitor of apoptosis protein (XIAP) holds promise as a target gene in colon cancer gene therapy. In this study, we constructed an adenoviral vector to deliver small hairpin RNA (shRNA) against XIAP (XIAP-shRNA) into colon cancer cells and tested i...

journal_title：Molecular cancer therapeutics

authors： Dai Y,Qiao L,Chan KW,Yang M,Ye J,Zhang R,Ma J,Zou B,Lam CS,Wang J,Pang R,Tan VP,Lan HY,Wong BC

更新日期：2009-09-01 00:00:00

abstract：:Despite significant advances in combinations of radiotherapy and chemotherapy, altered fractionation schedules and image-guided radiotherapy, many cancer patients fail to benefit from radiation. A prevailing hypothesis is that targeting repair of DNA double strand breaks (DSB) can enhance radiation effects in the tumo...

journal_title：Molecular cancer therapeutics

authors： Efimova EV,Ricco N,Labay E,Mauceri HJ,Flor AC,Ramamurthy A,Sutton HG,Weichselbaum RR,Kron SJ

更新日期：2018-02-01 00:00:00

abstract：:Zoledronic acid (ZOL) has been shown to reduce osteolysis in bone metastasis. Its efficacy in osteosarcoma has not been convincingly proved in a clinically relevant model for the disease. In vitro, ZOL decreased osteosarcoma cell proliferation, mainly due to an increase in apoptosis in a dose-dependent fashion. There ...

journal_title：Molecular cancer therapeutics

authors： Dass CR,Choong PF

更新日期：2007-12-01 00:00:00

abstract：:Nucleoside phosphonates are widely used therapeutic agents with a broad spectrum of antiviral activity. However, only a few of them are reported to have antitumor activity. In this study, we show that a tetrahydrofuran phosphonate analogue of guanosine, (-)-2-R-dihydroxyphosphinoyl-5-(S)-(guanin-9'-ylmethyl) tetrahydr...

journal_title：Molecular cancer therapeutics

authors： Leblond L,Attardo G,Hamelin B,Bouffard DY,Nguyen-Ba N,Gourdeau H

更新日期：2002-07-01 00:00:00

abstract：:Bortezomib combination with gemcitabine/cisplatin in patients with advanced tumors, predominantly non-small cell lung cancer (NSCLC), showed an unexpected transient drop in the deoxycytidine plasma levels, a marker for gemcitabine activity. This study investigates the pharmacokinetic/pharmacodynamic effect of bortezom...

journal_title：Molecular cancer therapeutics

authors： Ceresa C,Giovannetti E,Voortman J,Laan AC,Honeywell R,Giaccone G,Peters GJ

更新日期：2009-05-01 00:00:00

abstract：:Met-amplified EGFR-tyrosine kinase inhibitor (TKI)-resistant non-small cell lung cancer (NSCLC) harboring an activating EGFR mutation is responsive to concurrent EGFR-TKI and Met-TKI treatment in a preclinical model. Here, we determined that Met-amplified gefitinib-resistant cells acquire dual resistance to inhibition...

journal_title：Molecular cancer therapeutics

authors： Yamaoka T,Ohmori T,Ohba M,Arata S,Kishino Y,Murata Y,Kusumoto S,Ishida H,Shirai T,Hirose T,Ohnishi T,Sasaki Y

更新日期：2016-12-01 00:00:00

abstract：:DNA repair mechanisms are crucial for cell survival. It increases the cancer cell's ability to resist DNA damage. FEN1 is involved in DNA replication and repair, specifically long-patch base excision repair. Although the gene function and post-translational modification of FEN1 are well studied, the regulatory mechani...

journal_title：Molecular cancer therapeutics

authors： Zhu H,Wu C,Wu T,Xia W,Ci S,He W,Zhang Y,Li L,Zhou S,Zhang J,Edick AM,Zhang A,Pan FY,Hu Z,He L,Guo Z

更新日期：2019-12-01 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：: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：:As the population ages, more elderly patients require radiotherapy-based treatment for their pelvic malignancies, including muscle-invasive bladder cancer, as they are unfit for major surgery. Therefore, there is an urgent need to find radiosensitizing agents minimally toxic to normal tissues, including bowel and blad...

journal_title：Molecular cancer therapeutics

authors： Groselj B,Ruan JL,Scott H,Gorrill J,Nicholson J,Kelly J,Anbalagan S,Thompson J,Stratford MRL,Jevons SJ,Hammond EM,Scudamore CL,Kerr M,Kiltie AE

更新日期：2018-02-01 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：:Tumor-associated urokinase plasminogen activator (uPA) is a critical marker of invasion and metastasis, has strong prognostic relevance, and is thus a potential therapeutic target. Experimental data published to date has established the proof-of-principle of uPA targeting by (213)Bi-labeled plasminogen activator inhib...

journal_title：Molecular cancer therapeutics

authors： Stutchbury TK,Al-Ejeh F,Stillfried GE,Croucher DR,Andrews J,Irving D,Links M,Ranson M

更新日期：2007-01-01 00:00:00

abstract：:GA101 is a novel glycoengineered Type II CD20 monoclonal antibody. When compared with rituximab, it mediates less complement-dependent cytotoxicity (CDC). As expected for a Type II antibody, GA101 appears not to act through CDC and is more potent than the Type I antibody rituximab in inducing cell death via nonclassic...

journal_title：Molecular cancer therapeutics

authors： Dalle S,Reslan L,Besseyre de Horts T,Herveau S,Herting F,Plesa A,Friess T,Umana P,Klein C,Dumontet C

更新日期：2011-01-01 00:00:00