Trastuzumab-Resistant HER2+ Breast Cancer Cells Retain Sensitivity to Poly (ADP-Ribose) Polymerase (PARP) Inhibition.

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：:Stromal myofibroblasts play an important role in tumor progression. The transition of fibroblasts to myofibroblasts is characterized by expression of smooth muscle genes and profuse synthesis of extracellular matrix proteins. We evaluated the efficacy of targeting fibroblast-to-myofibroblast transition with halofugino...

journal_title：Molecular cancer therapeutics

authors： Sheffer Y,Leon O,Pinthus JH,Nagler A,Mor Y,Genin O,Iluz M,Kawada N,Yoshizato K,Pines M

更新日期：2007-02-01 00:00:00

abstract：:Epidermal growth factor receptor (EGFR) vIII is a mutated EGFR that is frequently overexpressed in glioblastomas and implicated in response to receptor tyrosine kinase inhibitors. In this study, we investigate the effect of ZD6474 (ZACTIMA, vandetanib), a dual inhibitor for vascular endothelial growth factor receptor ...

journal_title：Molecular cancer therapeutics

authors： Yiin JJ,Hu B,Schornack PA,Sengar RS,Liu KW,Feng H,Lieberman FS,Chiou SH,Sarkaria JN,Wiener EC,Ma HI,Cheng SY

更新日期：2010-04-01 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：:This conference opened with Franco Muggia, host and principal organizer, thanking Joseph Landolph, co-Chair of the International Scientific Organizing Committee and its members (Franco Muggia, co-Chair, Max Costa, Steven Burakoff, Howard Hochster, Eliezer Huberman, John Bertram, Peter Danenberg, and Richard Moran); th...

journal_title：Molecular cancer therapeutics

authors： Muggia FM,Peters GJ,Landolph JR Jr

更新日期：2009-05-01 00:00:00

abstract：:Activation of translation initiation is essential for the malignant phenotype and is emerging as a potential therapeutic target. Translation is regulated by the expression of translation initiation factor 4E (eIF4E) as well as the interaction of eIF4E with eIF4E-binding proteins (e.g., 4E-BP1). Rapamycin inhibits tran...

journal_title：Molecular cancer therapeutics

authors： Soni A,Akcakanat A,Singh G,Luyimbazi D,Zheng Y,Kim D,Gonzalez-Angulo A,Meric-Bernstam F

更新日期：2008-07-01 00:00:00

abstract：:Raf inhibitors are under clinical investigation, specifically in patients with tumor types harboring frequent activating mutations in B-Raf. Here, we show that cell lines and tumors harboring mutant B-Raf were sensitive to a novel series of Raf inhibitors (e.g., (V600E)B-Raf A375, IC(50) on cells = 2 nmol/L; ED(50) on...

journal_title：Molecular cancer therapeutics

authors： Carnahan J,Beltran PJ,Babij C,Le Q,Rose MJ,Vonderfecht S,Kim JL,Smith AL,Nagapudi K,Broome MA,Fernando M,Kha H,Belmontes B,Radinsky R,Kendall R,Burgess TL

更新日期：2010-08-01 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：: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：:The serine/threonine kinase AKT/PKB plays a critical role in cancer and represents a rational target for therapy. Although efforts in targeting AKT pathway have accelerated in recent years, relatively few small molecule inhibitors of AKT have been reported. The development of selective AKT inhibitors is further challe...

journal_title：Molecular cancer therapeutics

authors： Toral-Barza L,Zhang WG,Huang X,McDonald LA,Salaski EJ,Barbieri LR,Ding WD,Krishnamurthy G,Hu YB,Lucas J,Bernan VS,Cai P,Levin JI,Mansour TS,Gibbons JJ,Abraham RT,Yu K

更新日期：2007-11-01 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：: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：:Etoposide (VP-16), a topoisomerase II inhibitor, is an effective anticancer drug currently used for the treatment of a wide range of cancers. Excision repair cross-complementary 1 (ERCC1) is a key protein involved in the process of nucleotide excision repair. High level of ERCC1 expression in cancers is associated wit...

journal_title：Molecular cancer therapeutics

authors： Tsai MS,Weng SH,Chen HJ,Chiu YF,Huang YC,Tseng SC,Kuo YH,Lin YW

更新日期：2012-03-01 00:00:00

abstract：:Antioxidants, such as vitamin E, are being investigated for efficacy in prostate cancer prevention. In this study, we show that the antioxidant moiety of vitamin E, 2,2,5,7,8-pentamethyl-6-chromanol (PMCol), has antiandrogen activity in prostate carcinoma cells. In the presence of PMCol, the androgen-stimulated biphas...

journal_title：Molecular cancer therapeutics

authors： Thompson TA,Wilding G

更新日期：2003-08-01 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：:Constitutive activation of Janus kinases (JAKs) and signal transducers and activators of transcription (STAT) occurs at very high frequency in various hematopoietic malignancies and solid tumors. It has been demonstrated that the tyrosine kinase inhibitor, AG-490, selectively blocks JAK activity and completely elimina...

journal_title：Molecular cancer therapeutics

authors： Burdelya L,Catlett-Falcone R,Levitzki A,Cheng F,Mora LB,Sotomayor E,Coppola D,Sun J,Sebti S,Dalton WS,Jove R,Yu H

更新日期：2002-09-01 00:00:00

abstract：:Phortress is a novel, potent, and selective experimental antitumor agent. Its mechanism of action involves induction of CYP1A1-catalyzed biotransformation of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203) to generate electrophilic species, which covalently bind to DNA, exacting lethal damage to sensitive tu...

journal_title：Molecular cancer therapeutics

authors： Leong CO,Suggitt M,Swaine DJ,Bibby MC,Stevens MF,Bradshaw TD

更新日期：2004-12-01 00:00:00

abstract：:Radiotherapy, a frequent mode of cancer treatment, is often restricted by dose-related toxicity and development of therapeutic resistance. To develop a novel and selective radiosensitizer, we studied the radiosensitizing effects and associated mechanisms of silibinin in prostate cancer. The radiosensitizing effect of ...

journal_title：Molecular cancer therapeutics

authors： Nambiar DK,Rajamani P,Deep G,Jain AK,Agarwal R,Singh RP

更新日期：2015-12-01 00:00:00

abstract：:The difficulties associated with treatment of malignant brain tumors are well documented. For example, local infiltration of high-grade astrocytomas prevents the complete resection of all malignant cells. It is, therefore, critical to develop delivery systems for chemotherapeutic agents that ablate individual cancer c...

journal_title：Molecular cancer therapeutics

authors： Madhankumar AB,Slagle-Webb B,Mintz A,Sheehan JM,Connor JR

更新日期：2006-12-01 00:00:00

abstract：:Targeting inhibitor of apoptosis proteins (IAP) with second mitochondria-derived activator of caspase (SMAC) mimetics may promote cancer cell death. We tested whether cIAP1 predicts poor prognosis in head and neck squamous cell carcinoma (HNSCC) and whether a novel Smac-mimetic, LCL161, could radiosensitize human papi...

journal_title：Molecular cancer therapeutics

authors： Yang L,Kumar B,Shen C,Zhao S,Blakaj D,Li T,Romito M,Teknos TN,Williams TM

更新日期：2019-06-01 00:00:00

abstract：:Antiangiogenic therapies targeting VEGFA have been commonly used in clinics to treat cancers over the past decade. However, their clinical efficacy has been limited, with drawbacks including acquisition of resistance and activation of compensatory pathways resulting from elevated circulating VEGFB and placental growth...

journal_title：Molecular cancer therapeutics

authors： Lee JE,Kim C,Yang H,Park I,Oh N,Hua S,Jeong H,An HJ,Kim SC,Lee GM,Koh GY,Kim HM

更新日期：2015-02-01 00:00:00

abstract：:PTTG1 protein, the human securin, has a central role in sister chromatid separation during mitosis, and its altered expression has been reported in many tumor types. Paclitaxel is a widely used chemotherapeutic drug, whose mechanism of action is related to its ability to arrest cells in mitosis and the subsequent indu...

journal_title：Molecular cancer therapeutics

authors： Castilla C,Flores ML,Medina R,Pérez-Valderrama B,Romero F,Tortolero M,Japón MA,Sáez C

更新日期：2014-10-01 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：: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：:Nasopharyngeal carcinoma (NPC) is relatively rare in Western countries but is a common cancer in southern Asia. Many differentially expressed genes have been linked to NPC; however, how to prioritize therapeutic targets and potential drugs from unsorted gene lists remains largely unknown. We first collected 558 upregu...

journal_title：Molecular cancer therapeutics

authors： Lan MY,Chen CL,Lin KT,Lee SA,Yang WL,Hsu CN,Wu JC,Ho CY,Lin JC,Huang CY

更新日期：2010-09-01 00:00:00

abstract：:Imatinib mesylate has shown remarkable efficacy in the treatment of patients in the chronic phase of chronic myeloid leukemia. However, despite an overall significant hematological and cytogenetic response, imatinib therapy may favor the emergence of drug-resistant clones, ultimately leading to relapse. Some imatinib ...

journal_title：Molecular cancer therapeutics

authors： Deville L,Hillion J,Pendino F,Samy M,Nguyen E,Ségal-Bendirdjian E

更新日期：2011-05-01 00:00:00

abstract：:Survivin, an inhibitor of apoptosis protein, is highly expressed in most cancers and associated with chemotherapy resistance, increased tumor recurrence, and shorter patient survival, making antisurvivin therapy an attractive cancer treatment strategy. However, growing evidence indicates that survivin is expressed in ...

journal_title：Molecular cancer therapeutics

authors： Fukuda S,Pelus LM

更新日期：2006-05-01 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：:Cationic liposomes have been used for targeted drug delivery to tumor blood vessels, via mechanisms that are not fully elucidated. Doxorubicin (Dox)-loaded liposomes were prepared that incorporate a cationic lipid; 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), along with a small amount of porphyrin-phospholipid (P...

journal_title：Molecular cancer therapeutics

authors： Luo D,Geng J,Li N,Carter KA,Shao S,Atilla-Gokcumen GE,Lovell JF

更新日期：2017-11-01 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