Mechanism of drug efficacy within the EGF receptor revealed by microsecond molecular dynamics simulation.

abstract：:Invasive ductal carcinomas (IDC) of the breast are associated with altered expression of hormone receptors (HR), amplification or overexpression of HER2, or a triple-negative phenotype. The most aggressive cases of IDC are characterized by a high proliferation rate, a great propensity to metastasize, and their ability...

journal_title：Molecular cancer therapeutics

authors： Borges S,Perez EA,Thompson EA,Radisky DC,Geiger XJ,Storz P

更新日期：2015-06-01 00:00:00

abstract：:Antibody-drug conjugates (ADC) represent a promising therapeutic modality for managing cancer. Here, we report a novel humanized ADC that targets the tetraspanin-like protein TM4SF1. TM4SF1 is highly expressed on the plasma membranes of many human cancer cells and also on the endothelial cells lining tumor blood vesse...

journal_title：Molecular cancer therapeutics

authors： Visintin A,Knowlton K,Tyminski E,Lin CI,Zheng X,Marquette K,Jain S,Tchistiakova L,Li D,O'Donnell CJ,Maderna A,Cao X,Dunn R,Snyder WB,Abraham AK,Leal M,Shetty S,Barry A,Zawel L,Coyle AJ,Dvorak HF,Jaminet SC

更新日期：2015-08-01 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：:Transforming growth factor (TGF)-β contributes to the malignant phenotype of glioblastoma by promoting invasiveness and angiogenesis and creating an immunosuppressive microenvironment. So far, TGF-β1 and TGF-β2 isoforms have been considered to act in a similar fashion without isoform-specific function in glioblastoma....

journal_title：Molecular cancer therapeutics

authors： Seystahl K,Papachristodoulou A,Burghardt I,Schneider H,Hasenbach K,Janicot M,Roth P,Weller M

更新日期：2017-06-01 00:00:00

abstract：:We discovered a thalidomide analogue [5-hydroxy-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33)] with antiproliferative activity against nine cancer cell lines in vitro. Flow cytometric analyses showed that the compound caused G2-M arrest, which occurred mainly at the mitotic phase. In addition, immunofluores...

journal_title：Molecular cancer therapeutics

authors： Li PK,Pandit B,Sackett DL,Hu Z,Zink J,Zhi J,Freeman D,Robey RW,Werbovetz K,Lewis A,Li C

更新日期：2006-02-01 00:00:00

abstract：:Advanced and hormone-refractory prostate cancer has long been considered as a chemoresistant disease. Recently, it was found that 14-3-3sigma expression increases as prostate tumor progresses, and that 14-3-3sigma contributes significantly to drug resistance in breast cancers. We, thus, hypothesized that advanced and ...

journal_title：Molecular cancer therapeutics

authors： Han B,Xie H,Chen Q,Zhang JT

更新日期：2006-04-01 00:00:00

abstract：:Amplification of human epidermal growth factor receptor 2 (HER2) has been detected in 20% to 30% of gastric cancers and is associated with a poor outcome. Combination therapies with HER2-targeting agents and cytotoxic agents are considered a potential therapeutic option for gastric cancer with HER2 amplification. We h...

journal_title：Molecular cancer therapeutics

authors： Tanizaki J,Okamoto I,Takezawa K,Tsukioka S,Uchida J,Kiniwa M,Fukuoka M,Nakagawa K

更新日期：2010-05-01 00:00:00

abstract：:Treatment options for hepatocellular carcinoma using chemotherapeutics at intermediate and advanced stages of disease are limited as patients most rapidly escape from therapy and succumb to disease progression. Mechanisms of the hepatic xenobiotic metabolism are mostly involved in providing chemoresistance to therapeu...

journal_title：Molecular cancer therapeutics

authors： Haider C,Grubinger M,Řezníčková E,Weiss TS,Rotheneder H,Miklos W,Berger W,Jorda R,Zatloukal M,Gucky T,Strnad M,Kryštof V,Mikulits W

更新日期：2013-10-01 00:00:00

abstract：:Anti-HER2 monoclonal antibodies (mAb) have been shown to reduce tumor size and increase survival in patients with breast cancer, but they are ineffective against brain metastases due to poor brain penetration. In previous studies, we identified a peptide, known as Angiopep-2 (An2), which crosses the blood-brain barrie...

journal_title：Molecular cancer therapeutics

authors： Regina A,Demeule M,Tripathy S,Lord-Dufour S,Currie JC,Iddir M,Annabi B,Castaigne JP,Lachowicz JE

更新日期：2015-01-01 00:00:00

abstract：:Zoledronic acid, a third-generation bisphosphonate, has been shown to reduce cell migration, invasion, and metastasis. However, the effects of zoledronic acid on the epithelial-mesenchymal transition (EMT), a cellular process essential to the metastatic cascade, remain unclear. Therefore, the effects of zoledronic aci...

journal_title：Molecular cancer therapeutics

authors： Schech AJ,Kazi AA,Gilani RA,Brodie AH

更新日期：2013-07-01 00:00:00

abstract：:The KiSS-1 gene has been reported to be a metastasis suppressor gene in human melanoma. The gene product was isolated from human placenta as the ligand of GPR54, a G protein-coupled receptor, and the C-terminally amidated peptide of 54 amino acids is called metastin. The binding of metastin to GPR54 has been shown to ...

journal_title：Molecular cancer therapeutics

authors： Takeda T,Kikuchi E,Mikami S,Suzuki E,Matsumoto K,Miyajima A,Okada Y,Oya M

更新日期：2012-04-01 00:00:00

abstract：:Gemcitabine shows a marked antitumor effect as a result of its cytotoxic action toward proliferative cells. In this article, we aim to investigate the potential antitumor and antiangiogenic effect of gemcitabine following a metronomic schedule that involves the regular administration of cytotoxic drugs at doses lower ...

journal_title：Molecular cancer therapeutics

authors： Laquente B,Lacasa C,Ginestà MM,Casanovas O,Figueras A,Galán M,Ribas IG,Germà JR,Capellà G,Viñals F

更新日期：2008-03-01 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：: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

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal cancer due in part to a lack of highly robust cytotoxic or molecular-based therapies. Recent studies investigating ligand-mediated Wnt/β-catenin signaling have highlighted its importance in pancreatic cancer initiation and progression, as well as its potential...

journal_title：Molecular cancer therapeutics

authors： Arensman MD,Telesca D,Lay AR,Kershaw KM,Wu N,Donahue TR,Dawson DW

更新日期：2014-10-01 00:00:00

abstract：:Enhancer of zester homolog 2 (EZH2), a histone lysine methyltransferase and the catalytic component of polycomb repressive complex 2, has been extensively investigated as a chromatin regulator and a transcriptional suppressor by methylating H3 at lysine 27 (H3K27). EZH2 is upregulated or mutated in most cancers, and i...

journal_title：Molecular cancer therapeutics

authors： Li Q,Liu KY,Liu Q,Wang G,Jiang W,Meng Q,Yi Y,Yang Y,Wang R,Zhu S,Li C,Wu L,Zhao D,Yan L,Zhang L,Kim JS,Zu X,Kozielski AJ,Qian W,Chang JC,Patnaik A,Chen K,Cao Q

更新日期：2020-10-01 00:00:00

abstract：:Although both erlotinib and gefitinib target the EGF receptor (EGFR), erlotinib is effective in patients with EGFR wild-type or mutated tumors, whereas gefitinib is only beneficial for patients with activating mutations. To determine whether these differences in clinical outcomes can be attributed to their respective ...

journal_title：Molecular cancer therapeutics

authors： Augustin A,Lamerz J,Meistermann H,Golling S,Scheiblich S,Hermann JC,Duchateau-Nguyen G,Tzouros M,Avila DW,Langen H,Essioux L,Klughammer B

更新日期：2013-04-01 00:00:00

abstract：:Multitargeted kinase inhibitors have shown clinical efficacy in a range of cancer types. However, two major problems associated with these drugs are the low fraction of patients for which these treatments provide initial clinical benefit and the occurrence of resistance during prolonged therapy. Several types of predi...

journal_title：Molecular cancer therapeutics

authors： Versele M,Talloen W,Rockx C,Geerts T,Janssen B,Lavrijssen T,King P,Göhlmann HW,Page M,Perera T

更新日期：2009-07-01 00:00:00

abstract：:Interference with endothelial cell metabolism is a promising, yet unexploited strategy for angiogenesis inhibition. We reported that the glucose analogue 2-deoxy-D-glucose (2-DG) inhibits angiogenesis at significantly lower concentrations than those required for tumor cytotoxicity. Here, we found that hypersensitivity...

journal_title：Molecular cancer therapeutics

authors： Kovács K,Decatur C,Toro M,Pham DG,Liu H,Jing Y,Murray TG,Lampidis TJ,Merchan JR

更新日期：2016-02-01 00:00:00

abstract：:Chemopreventive agents in colorectal cancer possess either antiproliferative or anti-inflammatory actions. Nonsteroidal anti-inflammatory drugs (NSAID) and cyclooxygenase-2 inhibitors have shown promise, but are compromised by side effects. Nitric oxide donor NSAIDs are organic nitrates conjugated via a labile linker ...

journal_title：Molecular cancer therapeutics

authors： Hagos GK,Carroll RE,Kouznetsova T,Li Q,Toader V,Fernandez PA,Swanson SM,Thatcher GR

更新日期：2007-08-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor γ (PPARγ) is an important transcription factor that modulates lipid metabolism and inflammation. However, it remains unclear whether PPARγ is involved in modulation of estrogen (E2)-induced inflammation, thus affecting apoptosis of E2-deprived breast cancer cells, MCF-7:5C an...

journal_title：Molecular cancer therapeutics

authors： Fan P,Abderrahman B,Chai TS,Yerrum S,Jordan VC

更新日期：2018-12-01 00:00:00

abstract：:Trabectedin (ET-743) is a marine alkaloid isolated from the Caribbean tunicate Ecteinascidia turbinata, with a chemical structure characterized by three fused tetrahydroisoquinoline rings. Two of these rings (subunits A and B) provide the framework for covalent interaction with the minor groove of the DNA double helix...

journal_title：Molecular cancer therapeutics

authors： D'Incalci M,Galmarini CM

更新日期：2010-08-01 00:00:00

abstract：:TIGIT is an immune checkpoint inhibitor expressed by effector CD4+ and CD8+ T cells, NK cells, and regulatory T cells (Tregs). Inhibition of TIGIT-ligand binding using antagonistic anti-TIGIT mAbs has shown in vitro potential to restore T-cell function and therapeutic efficacy in murine tumor models when combined with...

journal_title：Molecular cancer therapeutics

authors： Preillon J,Cuende J,Rabolli V,Garnero L,Mercier M,Wald N,Pappalardo A,Denies S,Jamart D,Michaux AC,Pirson R,Pitard V,Bagot M,Prasad S,Houthuys E,Brouwer M,Marillier R,Lambolez F,Marchante JR,Nyawouame F,Carter MJ

更新日期：2021-01-01 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：:The PI3K pathway is considered a master regulator for cancer due to its frequent activation, making it an attractive target for pharmacologic intervention. While substantial efforts have been made to develop drugs targeting PI3K signaling, few drugs have been able to achieve the inhibition necessary for effective tumo...

journal_title：Molecular cancer therapeutics

authors： Perino S,Moreau B,Freda J,Cirello A,White BH,Quinn JM,Kriksciukaite K,Someshwar A,Romagnoli J,Robinson M,Movassaghian S,Cipriani T,Wooster R,Bilodeau MT,Whalen KA

更新日期：2020-08-01 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：:Malignant ascitis (MA) is a highly intractable and immunotherapy-resistant state of advanced gastrointestinal and ovarian cancers. Using a murine model of MA with CT26 colon cancer cells, we here determined that the imbalance between the VEGF-A/vascular permeability factor and its decoy receptor, soluble fms-like tryr...

journal_title：Molecular cancer therapeutics

authors： Sugiyama M,Kakeji Y,Tsujitani S,Harada Y,Onimaru M,Yoshida K,Tanaka S,Emi Y,Morita M,Morodomi Y,Hasegawa M,Maehara Y,Yonemitsu Y

更新日期：2011-03-01 00:00:00

abstract：:Tumor recurrence after curative resection remains a major problem in patients with locally advanced colorectal cancer treated with adjuvant chemotherapy. Genetic single-nucleotide polymorphisms (SNP) may serve as useful molecular markers to predict clinical outcomes in these patients and identify targets for future dr...

journal_title：Molecular cancer therapeutics

authors： Ning Y,Gerger A,Zhang W,Hanna DL,Yang D,Winder T,Wakatsuki T,Labonte MJ,Stintzing S,Volz N,Sunakawa Y,Stremitzer S,El-Khoueiry R,Lenz HJ

更新日期：2014-02-01 00:00:00

abstract：:Notch signaling regulates cell-fate decisions during development and postnatal life. Little is known, however, about the role of Delta-like-4 (Dll4)-Notch signaling between cancer cells, or how this signaling affects cancer metastasis. We, therefore, assessed the role of Dll4-Notch signaling in cancer metastasis. We g...

journal_title：Molecular cancer therapeutics

authors： Kuramoto T,Goto H,Mitsuhashi A,Tabata S,Ogawa H,Uehara H,Saijo A,Kakiuchi S,Maekawa Y,Yasutomo K,Hanibuchi M,Akiyama S,Sone S,Nishioka Y

更新日期：2012-12-01 00:00:00

abstract：:The present studies have determined whether interactions between the cyclin-dependent kinase inhibitor flavopiridol and the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA; vorinostat; Zolinza) occur in breast cancer cells. MDA-MB-231 and MCF7 cells were treated with flavopiridol (25-100 nmol/L) an...

journal_title：Molecular cancer therapeutics

authors： Mitchell C,Park MA,Zhang G,Yacoub A,Curiel DT,Fisher PB,Roberts JD,Grant S,Dent P

更新日期：2007-12-01 00:00:00