A comprehensive evaluation of biomarkers predictive of response to PI3K inhibitors and of resistance mechanisms in head and neck squamous cell carcinoma.

abstract：:Activation of beta-catenin is a critical step in the pathogenesis of many common human cancers and is the initiating event in adenocarcinoma of the colon. Because activation of beta-catenin provides a gain-of-function, it is tempting to speculate that specific pharmacological inhibition of activated beta-catenin might...

journal_title：Molecular cancer therapeutics

authors： Kim JS,Crooks H,Foxworth A,Waldman T

更新日期：2002-12-01 00:00:00

abstract：:This study aimed to investigate the antitumor and antiangiogenic effects utilizing a novel therapy regimen of metronomic topotecan and pazopanib, a multireceptor tyrosine kinase inhibitor. In vitro (Western blot) and in vivo dose-finding experiments were done following pazopanib therapy in ovarian cancer models. Pazop...

journal_title：Molecular cancer therapeutics

authors： Merritt WM,Nick AM,Carroll AR,Lu C,Matsuo K,Dumble M,Jennings N,Zhang S,Lin YG,Spannuth WA,Kamat AA,Stone RL,Shahzad MM,Coleman RL,Kumar R,Sood AK

更新日期：2010-04-01 00:00:00

abstract：:The PI3K/AKT/mTOR pathway, which is aberrantly stimulated in many cancer cells, has emerged as a target for therapy. However, mTORC1/S6K also mediates negative feedback loops that attenuate upstream signaling. Suppression of these feedback loops opposes the growth-suppressive effects of mTOR inhibitors and leads to dr...

journal_title：Molecular cancer therapeutics

authors： Soares HP,Ming M,Mellon M,Young SH,Han L,Sinnet-Smith J,Rozengurt E

更新日期：2015-04-01 00:00:00

abstract：:Expression of the proto-oncogene Bcl-2 is associated with tumor progression. Bcl-2's broad expression in tumors, coupled with its role in resistance to chemotherapy and radiation therapy-induced apoptosis, makes it a rational target for anticancer therapy. Antisense Bcl-2 oligodeoxynucleotide (ODN) reagents have been ...

journal_title：Molecular cancer therapeutics

authors： Anai S,Goodison S,Shiverick K,Hirao Y,Brown BD,Rosser CJ

更新日期：2007-01-01 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：:R-roscovitine (seliciclib, CYC202) is a cyclin-dependent kinase inhibitor currently in phase II clinical trials in patients with cancer. Here, we describe its mouse metabolism and pharmacokinetics as well as the identification of the principal metabolites in hepatic microsomes, plasma, and urine. Following microsomal ...

journal_title：Molecular cancer therapeutics

authors： Nutley BP,Raynaud FI,Wilson SC,Fischer PM,Hayes A,Goddard PM,McClue SJ,Jarman M,Lane DP,Workman P

更新日期：2005-01-01 00:00:00

abstract：:Clinical decision making for human papillomavirus (HPV)-negative head and neck squamous cell carcinoma (HNSCC) is predominantly guided by disease stage and anatomic location, with few validated biomarkers. The epidermal growth factor receptor (EGFR) is an important therapeutic target, but its value in guiding therapeu...

journal_title：Molecular cancer therapeutics

authors： Beck TN,Georgopoulos R,Shagisultanova EI,Sarcu D,Handorf EA,Dubyk C,Lango MN,Ridge JA,Astsaturov I,Serebriiskii IG,Burtness BA,Mehra R,Golemis EA

更新日期：2016-10-01 00:00:00

abstract：:This study aims to explore whether E545K, the most common hotspot mutation of PIK3CA in cervical cancer, confers radioresistance to cervical cancer cells, to demonstrate the underling mechanism, and to develop the effective targets. SiHa and MS751 cells with PIK3CA-WT and PIK3CA-E545K were established by lentiviral tr...

journal_title：Molecular cancer therapeutics

authors： Jiang W,Wu Y,He T,Zhu H,Ke G,Xiang L,Yang H

更新日期：2020-02-01 00:00:00

abstract：:Radiotherapy can be synergistically combined with immunotherapy in mouse models, extending its efficacious effects outside of the irradiated field (abscopal effects). We previously reported that a regimen encompassing local radiotherapy in combination with anti-CD137 plus anti-PD-1 mAbs achieves potent abscopal effect...

journal_title：Molecular cancer therapeutics

authors： Rodríguez-Ruiz ME,Rodríguez I,Mayorga L,Labiano T,Barbes B,Etxeberria I,Ponz-Sarvise M,Azpilikueta A,Bolaños E,Sanmamed MF,Berraondo P,Calvo FA,Barcelos-Hoff MH,Perez-Gracia JL,Melero I

更新日期：2019-03-01 00:00:00

abstract：:Several studies have identified silibinin as an anticarcinogenic agent. Recently, we showed that silibinin inhibits cell growth via G1 arrest, leading to differentiation of androgen-dependent human prostate carcinoma LNCaP cells (X. Zi and R. Agarwal, Proc. Natl. Acad. Sci. USA, 96: 7490-7495,1999). Here, we extend th...

journal_title：Molecular cancer therapeutics

authors： Tyagi A,Agarwal C,Agarwal R

更新日期：2002-05-01 00:00:00

abstract：:TNF-like weak inducer of apoptosis (TWEAK) and fibroblast growth factor (FGF)-inducible 14 (Fn14) are a TNF superfamily ligand-receptor pair involved in many cellular processes including proliferation, migration, differentiation, inflammation, and angiogenesis. The Fn14 receptor is expressed at relatively low levels i...

journal_title：Molecular cancer therapeutics

authors： Zhou H,Marks JW,Hittelman WN,Yagita H,Cheung LH,Rosenblum MG,Winkles JA

更新日期：2011-07-01 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：:Artesunate, the active agent from Artemisia annua L. used in the traditional Chinese medicine, is being applied as a first-line drug for malaria treatment, and trials are ongoing that include this drug in cancer therapy. Despite increasing interest in its therapeutic application, the mode of cell killing provoked by a...

journal_title：Molecular cancer therapeutics

authors： Berdelle N,Nikolova T,Quiros S,Efferth T,Kaina B

更新日期：2011-12-01 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：:Recently there have been explosive discoveries of new long noncoding RNAs (lncRNA) obtained by progress in the technology of second-generation sequencing. Genome scale analysis of transcriptome, in conjunction with studies on chromatin modifications at the epigenetic level, identified lncRNAs as a novel type of noncod...

journal_title：Molecular cancer therapeutics

authors： Zhang L,Peng D,Sood AK,Dang CV,Zhong X

更新日期：2018-09-01 00:00:00

abstract：:5'-Fluorouracil (5-FU), used in the treatment of colon and breast cancers, is converted intracellularly to 5'-fluoro-2'-deoxyuridine (5-FUdR) by thymidine phosphorylase and is subsequently phosphorylated by thymidine kinase to 5'-fluoro-2'-dUMP (5-FdUMP). This active metabolite, along with the reduced folate cofactor,...

journal_title：Molecular cancer therapeutics

authors： Pratt S,Shepard RL,Kandasamy RA,Johnston PA,Perry W 3rd,Dantzig AH

更新日期：2005-05-01 00:00:00

abstract：:Chemoresistance is a major hurdle in the management of patients with epithelial ovarian cancer and is responsible for its high mortality. Studies have shown that chemoresistance is due to the presence of a subgroup of cancer cells with stemness properties and a high capacity for tumor repair. We have developed a libra...

journal_title：Molecular cancer therapeutics

authors： Alvero AB,Heaton A,Lima E,Pitruzzello M,Sumi N,Yang-Hartwich Y,Cardenas C,Steinmacher S,Silasi DA,Brown D,Mor G

更新日期：2016-06-01 00:00:00

abstract：:The extracellular pH of tumor tissue is significantly lower than the extracellular pH of normal tissue, whereas the intracellular pH of both tissues is similar. In principle, extracellular acidity may be expected to enhance the intracellular uptake and cytotoxicity of weak acid chemotherapeutics that are membrane perm...

journal_title：Molecular cancer therapeutics

authors： Gerweck LE,Vijayappa S,Kozin S

更新日期：2006-05-01 00:00:00

abstract：:The goal of this study was to investigate the activity of the selective MEK1/2 inhibitor TAK-733 in both melanoma cell lines and patient-derived melanoma xenograft models. In vitro cell proliferation assays using the sulforhodamine B assay were conducted to determine TAK-733 potency and melanoma responsiveness. In viv...

journal_title：Molecular cancer therapeutics

authors： Micel LN,Tentler JJ,Tan AC,Selby HM,Brunkow KL,Robertson KM,Davis SL,Klauck PJ,Pitts TM,Gangolli E,Fabrey R,O'Connell SM,Vincent PW,Eckhardt SG

更新日期：2015-02-01 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：: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：: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：: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：:The covalent attachment of palmitate to specific proteins by the action of palmitoyl acyltransferases (PAT) plays critical roles in the biological activities of several oncoproteins. Two PAT activities are expressed by human cells: type 1 PATs that modify the farnesyl-dependent palmitoylation motif found in H- and N-R...

journal_title：Molecular cancer therapeutics

authors： Ducker CE,Griffel LK,Smith RA,Keller SN,Zhuang Y,Xia Z,Diller JD,Smith CD

更新日期：2006-07-01 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：UNLABELLED:Multiple myeloma (MM) is a malignancy of clonal B-cells that accounts for 10% of all hematologic malignancies. We have shown previously that a novel purine analogue, 8-chloro-adenosine, has significant activity for MM in preclinical studies. OBJECTIVE:Using MM cell lines, we investigated the molecular mecha...

journal_title：Molecular cancer therapeutics

authors： Krett NL,Davies KM,Ayres M,Ma C,Nabhan C,Gandhi V,Rosen ST

更新日期：2004-11-01 00:00:00

abstract：:We have developed a near-infrared (NIR) probe that targets cells overexpressing the EGF receptor (EGFR) for imaging glioblastoma brain tumors in live subjects. A peptide specific for the EGFR was modified with various lengths of monodiscrete polyethylene glycol (PEG) units and a NIR Cy5.5 fluorescence dye. The lead co...

journal_title：Molecular cancer therapeutics

authors： Agnes RS,Broome AM,Wang J,Verma A,Lavik K,Basilion JP

更新日期：2012-10-01 00:00:00

abstract：:Hepatocellular carcinoma (HCC) can arise from chronic inflammation due to viral infection, organ damage, drug toxicity, or alcohol abuse. Moreover, gene desensitization via aberrant CpG island methylation is a frequent epigenetic defect in HCC. However, the details of how inflammation is linked with epigenetic-mediate...

journal_title：Molecular cancer therapeutics

authors： Li CF,Tsai HH,Ko CY,Pan YC,Yen CJ,Lai HY,Yuh CH,Wu WC,Wang JM

更新日期：2015-11-01 00:00:00

abstract：:Ewing's sarcoma is a pediatric cancer of the bone that is characterized by the expression of the chimeric transcription factor EWS-FLI1 that confers a highly malignant phenotype and results from the chromosomal translocation t(11;22)(q24;q12). Poor overall survival and pronounced long-term side effects associated with...

journal_title：Molecular cancer therapeutics

authors： Winter GE,Rix U,Lissat A,Stukalov A,Müllner MK,Bennett KL,Colinge J,Nijman SM,Kubicek S,Kovar H,Kontny U,Superti-Furga G

更新日期：2011-10-01 00:00:00

abstract：:Microtubule-targeting cancer drugs such as paclitaxel block cell-cycle progression at mitosis by prolonged activation of the mitotic checkpoint. Cells can spontaneously escape mitotic arrest and enter interphase without chromosome segregation by a process termed mitotic slippage that involves the degradation of cyclin...

journal_title：Molecular cancer therapeutics

authors： Riffell JL,Jänicke RU,Roberge M

更新日期：2011-05-01 00:00:00