Tivantinib (ARQ 197) exhibits antitumor activity by directly interacting with tubulin and overcomes ABC transporter-mediated drug resistance.

abstract：:Sulfonylurea receptor 1 (SUR1) is the regulatory subunit of ATP-sensitive potassium channels (KATP channels) and the receptor of antidiabetic drugs, such as glibenclamide, which induce insulin secretion in pancreatic β cells. However, the expression and role of SUR1 in cancer are unknown. In this study, we found that ...

journal_title：Molecular cancer therapeutics

authors： Xu K,Sun G,Li M,Chen H,Zhang Z,Qian X,Li P,Xu L,Huang W,Wang X

更新日期：2019-11-01 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：:Targeting of epigenetic regulators as the chromatin remodeler SWI/SNF is proving to be a promising therapeutic strategy for individualized treatment of cancer patients. Here, we tested whether targeting one of the two mutually exclusive subdomains of the SWI/SNF complex BRM/SMARCA2 can sensitize specifically non-small...

journal_title：Molecular cancer therapeutics

authors： Zernickel E,Sak A,Riaz A,Klein D,Groneberg M,Stuschke M

更新日期：2019-03-01 00:00:00

abstract：:DNA double-strand breaks (DSB) are the most cytotoxic lesions induced by topoisomerase II poisons. Nonhomologous end joining (NHEJ) is a major pathway for DSB repair and requires DNA-dependent protein kinase (DNA-PK) activity. DNA-PK catalytic subunit (DNA-PKcs) is structurally similar to PI-3K, which promotes cell su...

journal_title：Molecular cancer therapeutics

authors： Munck JM,Batey MA,Zhao Y,Jenkins H,Richardson CJ,Cano C,Tavecchio M,Barbeau J,Bardos J,Cornell L,Griffin RJ,Menear K,Slade A,Thommes P,Martin NM,Newell DR,Smith GC,Curtin NJ

更新日期：2012-08-01 00:00:00

abstract：:The type I EGF receptor (EGFR or ErbB1) and insulin-like growth factor-binding protein-3 (IGFBP-3) are highly expressed in triple-negative breast cancer (TNBC), a particularly aggressive disease that cannot be treated with conventional therapies targeting the estrogen or progesterone receptors (ER and PR), or HER2. We...

journal_title：Molecular cancer therapeutics

authors： Martin JL,de Silva HC,Lin MZ,Scott CD,Baxter RC

更新日期：2014-02-01 00:00:00

abstract：:Nanotechnology refers to the interactions of cellular and molecular components and engineered materials-typically, clusters of atoms, molecules, and molecular fragments into incredibly small particles-between 1 and 100 nm. Nanometer-sized particles have novel optical, electronic, and structural properties that are not...

journal_title：Molecular cancer therapeutics

authors： Sinha R,Kim GJ,Nie S,Shin DM

更新日期：2006-08-01 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：:The anticancer actions of vitamin D and its hormonally active form, calcitriol, have been extensively documented in clinical and preclinical studies. However, the mechanisms underlying these actions have not been completely elucidated. Here, we examined the effect of dietary vitamin D and calcitriol on mouse breast tu...

journal_title：Molecular cancer therapeutics

authors： Jeong Y,Swami S,Krishnan AV,Williams JD,Martin S,Horst RL,Albertelli MA,Feldman BJ,Feldman D,Diehn M

更新日期：2015-08-01 00:00:00

abstract：:The traditional maximum dose density chemotherapy renders the tumor patients not only the tumor remission but the chemotherapy resistance and more adverse side effects. According to the widely positive expression of Toll-like receptor (TLR)-3 in oral squamous cell carcinoma (OSCC) patients (n = 166), we here provided ...

journal_title：Molecular cancer therapeutics

authors： Ding L,Ren J,Zhang D,Li Y,Huang X,Ji J,Hu Q,Wang H,Ni Y,Hou Y

更新日期：2017-06-01 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：:A number of cancer chemotherapeutic drugs designed to have cytotoxic actions on tumor cells have recently been shown to also have antiangiogenic activities. Endothelial cell migration and proliferation are key components of tumor angiogenesis, and agents that target the microtubule cytoskeleton can interfere with thes...

journal_title：Molecular cancer therapeutics

authors： Hotchkiss KA,Ashton AW,Mahmood R,Russell RG,Sparano JA,Schwartz EL

更新日期：2002-11-01 00:00:00

abstract：:Small cell lung cancer (SCLC) easily acquires multidrug resistance after successful initial therapy. Overexpression of ATP-binding cassette (ABC) transporters is important for the multidrug resistance. Among them, ABCB1 and ABCG2 are known to be upregulated in chemoresistant SCLC cells. We found that human epidermal g...

journal_title：Molecular cancer therapeutics

authors： Minami T,Kijima T,Otani Y,Kohmo S,Takahashi R,Nagatomo I,Hirata H,Suzuki M,Inoue K,Takeda Y,Kida H,Tachibana I,Kumanogoh A

更新日期：2012-04-01 00:00:00

abstract：:The entry of calcium into the mammary epithelial cell from the maternal plasma (i.e., calcium influx mechanisms) during lactation is poorly understood. As alterations in calcium channels and pumps are a key feature of some cancers, including breast cancer, understanding these calcium influx pathways may have significa...

journal_title：Molecular cancer therapeutics

authors： McAndrew D,Grice DM,Peters AA,Davis FM,Stewart T,Rice M,Smart CE,Brown MA,Kenny PA,Roberts-Thomson SJ,Monteith GR

更新日期：2011-03-01 00:00:00

abstract：:At the present time, the optimal development of molecularly targeted anticancer agents is limited by the lack of clinically applicable tools to predict drug effects. This study aimed to develop methods that might be useful in predicting the efficacy of targeted agents in a novel model system of human pancreatic cancer...

journal_title：Molecular cancer therapeutics

authors： Rubio-Viqueira B,Mezzadra H,Nielsen ME,Jimeno A,Zhang X,Iacobuzio-Donahue C,Maitra A,Hidalgo M,Altiok S

更新日期：2007-02-01 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：:Acquired resistance severely hinders the application of small-molecule inhibitors. Our understanding of acquired resistance related to FGFRs is limited. Here, to explore the underlying mechanism of acquired resistance in FGFR-aberrant cancer cells, we generated cells resistant to multiple FGFR inhibitors (FGFRi) and i...

journal_title：Molecular cancer therapeutics

authors： Wang X,Ai J,Liu H,Peng X,Chen H,Chen Y,Su Y,Shen A,Huang X,Ding J,Geng M

更新日期：2019-03-01 00:00:00

abstract：:Hepatocellular carcinoma is highly chemoresistant, and ATP-binding cassette subfamily G member 2 (ABCG2) is thought to play a critical role in this drug resistance. The present study aims to develop effective therapeutic strategies to decrease ABCG2 expression level and to surmount drug resistance in hepatocellular ca...

journal_title：Molecular cancer therapeutics

authors： Hou H,Sun H,Lu P,Ge C,Zhang L,Li H,Zhao F,Tian H,Zhang L,Chen T,Yao M,Li J

更新日期：2013-12-01 00:00:00

abstract：:Chemoresistance of ovarian carcinoma has been associated previously to the absence of Bcl-x(L) expression downregulation in response to cisplatin. Among BH3-mimetic molecules constituting promising anticancer agents able to inhibit the activity of antiapoptotic Bcl-2 family proteins, we evaluated the effect of one of ...

journal_title：Molecular cancer therapeutics

authors： Simonin K,Brotin E,Dufort S,Dutoit S,Goux D,N'diaye M,Denoyelle C,Gauduchon P,Poulain L

更新日期：2009-11-01 00:00:00

abstract：:Bladder cancer is a common human malignancy. Conventional ultrasound and white-light cystoscopy are often used for bladder cancer diagnosis and resection, but insufficient specificity results in a high bladder cancer recurrence rate. New strategies for the diagnosis and resection of bladder cancer are needed. In this ...

journal_title：Molecular cancer therapeutics

authors： Peng L,Shang W,Guo P,He K,Wang H,Han Z,Jiang H,Tian J,Wang K,Xu W

更新日期：2018-10-01 00:00:00

abstract：:Expression of fatty acid synthase (FASN), the key enzyme in de novo synthesis of long-chain fatty acids, is normally low but increases in cancer. Consequently, FASN is a novel target for cancer therapy. However, because FASN inhibitors can lead to tumor stasis rather than shrinkage, noninvasive methods for assessing F...

journal_title：Molecular cancer therapeutics

authors： Ross J,Najjar AM,Sankaranarayanapillai M,Tong WP,Kaluarachchi K,Ronen SM

更新日期：2008-08-01 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：: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：: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：:Targeted thrombotic eradication of solid tumors is a novel therapeutic strategy. The feasibility, efficacy, selectivity, and safety are dependent on multiple variables of protein design, molecular assembly, vascular target, and exclusive restriction of function to the tumor vasculature. To advance this strategy, we de...

journal_title：Molecular cancer therapeutics

authors： Liu C,Dickinson C,Shobe J,Doñate F,Ruf W,Edgington T

更新日期：2004-07-01 00:00:00

abstract：:Histone modification has emerged as a promising approach to cancer therapy. We explored the efficacy of a novel class of histone deacetylase inhibitors in the treatment of malignant gliomas. Treatment of glioma cell lines with two butyric acid derivatives, pivaloylomethyl butyrate (AN-9) and butyroyloxymethyl butyrate...

journal_title：Molecular cancer therapeutics

authors： Entin-Meer M,Rephaeli A,Yang X,Nudelman A,VandenBerg SR,Haas-Kogan DA

更新日期：2005-12-01 00:00:00

abstract：:Signaling from the human hematopoietic stem cell (HSC) niche formed by osteoblastic cells regulates hematopoiesis. We previously found that retinoic acid receptor alpha (RARα), a transcription factor activated by retinoic acid (RA), mediates both granulocytic and osteoblastic differentiation. This effect depends on de...

journal_title：Molecular cancer therapeutics

authors： Chaudhry P,Yang X,Wagner M,Jong A,Wu L

更新日期：2012-02-01 00:00:00

abstract：:HER2-positive breast cancer is currently managed with chemotherapy in combination with specific anti-HER2 therapies, including trastuzumab. However, a high percentage of patients with HER2-positive tumors do not respond to trastuzumab (primary resistance) or either recur (acquired resistance), mostly due to molecular ...

journal_title：Molecular cancer therapeutics

authors： Zazo S,González-Alonso P,Martín-Aparicio E,Chamizo C,Luque M,Sanz-Álvarez M,Mínguez P,Gómez-López G,Cristóbal I,Caramés C,García-Foncillas J,Eroles P,Lluch A,Arpí O,Rovira A,Albanell J,Madoz-Gúrpide J,Rojo F

更新日期：2020-08-01 00:00:00

abstract：:For a subpopulation of acute myeloid leukemia (AML) patients, the constitutively activated tyrosine kinase, mutant FLT3, has emerged as a promising target for therapy. The development of drug resistance, however, is a growing concern for mutant FLT3 inhibitors, such as PKC412. Potential therapeutic benefit can arise f...

journal_title：Molecular cancer therapeutics

authors： Weisberg E,Choi HG,Barrett R,Zhou W,Zhang J,Ray A,Nelson EA,Jiang J,Moreno D,Stone R,Galinsky I,Fox E,Adamia S,Kung AL,Gray NS,Griffin JD

更新日期：2010-09-01 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：: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