An integrated chemical biology approach identifies specific vulnerability of Ewing's sarcoma to combined inhibition of Aurora kinases A and B.

abstract：:Recently, pancreatic ductal adenocarcinoma (PDAC) has emerged as one of the most aggressive malignant tumors with the worst prognosis. Previous studies have demonstrated that long noncoding RNA metastasis-associated lung adenocarcinoma transcript 1 (MALAT1) is increased in pancreatic cancer and is identified as a diag...

journal_title：Molecular cancer therapeutics

authors： Li L,Chen H,Gao Y,Wang YW,Zhang GQ,Pan SH,Ji L,Kong R,Wang G,Jia YH,Bai XW,Sun B

更新日期：2016-09-01 00:00:00

abstract：:Castration-resistant prostate cancer (CRPC) remains dependent on androgen receptor (AR) signaling. Alternative splicing of the AR to generate constitutively active, ligand-independent variants is one of the principal mechanisms that promote the development of resistance to next-generation antiandrogens such as enzalut...

journal_title：Molecular cancer therapeutics

authors： Nadiminty N,Tummala R,Liu C,Lou W,Evans CP,Gao AC

更新日期：2015-08-01 00:00:00

abstract：:Malignant mesothelioma is an aggressive tumor of the serosal surfaces of the lungs, heart, and abdomen. Survival rates are poor and effective treatments are not available. However, recent therapeutic regimens targeting thymidylate synthase (TS) in malignant mesothelioma patients have shown promise. We have reported th...

journal_title：Molecular cancer therapeutics

authors： Flynn J,Berg RW,Wong T,van Aken M,Vincent MD,Fukushima M,Koropatnick J

更新日期：2006-06-01 00:00:00

abstract：:A novel oral Hsp90 inhibitor, NVP-HSP990, has been developed and characterized in vitro and in vivo. In vitro, NVP-HSP990 exhibits single digit nanomolar IC(50) values on three of the Hsp90 isoforms (Hsp90α, Hsp90β, and GRP94) and 320 nanomolar IC(50) value on the fourth (TRAP-1), with selectivity against unrelated en...

journal_title：Molecular cancer therapeutics

authors： Menezes DL,Taverna P,Jensen MR,Abrams T,Stuart D,Yu GK,Duhl D,Machajewski T,Sellers WR,Pryer NK,Gao Z

更新日期：2012-03-01 00:00:00

abstract：:Soft-tissue sarcomas (STS) represent a heterogeneous group of rare, malignant tumors of mesenchymal origin. Reliable in vivo sarcoma research models are scarce. We aimed to establish and characterize histologically and molecularly stable patient-derived xenograft (PDX) models from a broad variety of STS subtypes. A to...

journal_title：Molecular cancer therapeutics

authors： Cornillie J,Wozniak A,Li H,Wang Y,Boeckx B,Gebreyohannes YK,Wellens J,Vanleeuw U,Hompes D,Stas M,Sinnaeve F,Wafa H,Lambrechts D,Debiec-Rychter M,Sciot R,Schöffski P

更新日期：2019-06-01 00:00:00

abstract：:With current techniques, it remains a challenge to assess coregulator binding of nuclear receptors, for example, the estrogen receptor alpha (ERα). ERα is critical in many breast tumors and is inhibited by antiestrogens such as tamoxifen in cancer therapy. ERα is also modified by acetylation and phosphorylation that a...

journal_title：Molecular cancer therapeutics

authors： Houtman R,de Leeuw R,Rondaij M,Melchers D,Verwoerd D,Ruijtenbeek R,Martens JW,Neefjes J,Michalides R

更新日期：2012-04-01 00:00:00

abstract：:The androgen receptor (AR) is a key driver and therapeutic target in androgen-sensitive prostate cancer, castration-resistant prostate cancer (CRPC), and CRPC resistant to abiraterone and enzalutamide, two second-generation inhibitors of AR signaling. Because current AR inhibitors target a functioning C-terminal ligan...

journal_title：Molecular cancer therapeutics

authors： Dong J,Wu Z,Wang D,Pascal LE,Nelson JB,Wipf P,Wang Z

更新日期：2019-01-01 00:00:00

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：:Tamoxifen, a selective estrogen receptor (ER) modulator, is the most widely prescribed hormonal therapy treatment for breast cancer. Despite the benefits of tamoxifen therapy, almost all tamoxifen-responsive breast cancer patients develop resistance to therapy. In addition, tamoxifen displays estrogen-like effects in ...

journal_title：Molecular cancer therapeutics

authors： Shah YM,Al-Dhaheri M,Dong Y,Ip C,Jones FE,Rowan BG

更新日期：2005-08-01 00:00:00

abstract：:The treatment of breast cancer cells obtained by blocking the aberrant activation of the proliferation signaling pathways PI3K/Akt/mTOR and MEK/ERK has received considerable attention in recent years. Previous studies showed that Taiwanin A inhibited the proliferation of several types of cancer cells. In this study, w...

journal_title：Molecular cancer therapeutics

authors： Kuo YH,Chiang EI,Chao CY,Rodriguez RL,Chou PY,Tsai SY,Pai MH,Tang FY

更新日期：2017-03-01 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：:Crizotinib (PF02341066) is a tyrosine kinase inhibitor of anaplastic lymphoma kinase (ALK) that has been shown to selectively inhibit growth of cancer cells that harbor the EML4-ALK fusion found in a subset of patients with non-small cell lung cancer (NSCLC). While in clinical trials, PF02341066 has shown a significan...

journal_title：Molecular cancer therapeutics

authors： Sun Y,Nowak KA,Zaorsky NG,Winchester CL,Dalal K,Giacalone NJ,Liu N,Werner-Wasik M,Wasik MA,Dicker AP,Lu B

更新日期：2013-05-01 00:00:00

abstract：:Antibody-drug conjugates (ADC), potent cytotoxic drugs linked to antibodies via chemical linkers, allow specific targeting of drugs to neoplastic cells. We have used this technology to develop the ADC DCDT2980S that targets CD22, an antigen with expression limited to B cells and the vast majority of non-Hodgkin lympho...

journal_title：Molecular cancer therapeutics

authors： Li D,Poon KA,Yu SF,Dere R,Go M,Lau J,Zheng B,Elkins K,Danilenko D,Kozak KR,Chan P,Chuh J,Shi X,Nazzal D,Fuh F,McBride J,Ramakrishnan V,de Tute R,Rawstron A,Jack AS,Deng R,Chu YW,Dornan D,Williams M,Ho W,

更新日期：2013-07-01 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：:Pancreatic cancer is the fifth leading cause of cancer death in North America. Gemcitabine improves the quality of life of patients but fails to significantly reduce mortality. Our laboratory has demonstrated previously that the phosphatidylinositol 3'-kinase inhibitor wortmannin promotes gemcitabine antitumor activit...

journal_title：Molecular cancer therapeutics

authors： Ng SS,Tsao MS,Nicklee T,Hedley DW

更新日期：2002-08-01 00:00:00

abstract：:An ideal therapeutic for cancer would be one that selectively targets to tumor cells, is nontoxic to normal cells, and that could be systemically delivered, thereby reaching metastases as well as primary tumor. Immunoliposomes directed by monoclonal antibody or its fragments are promising vehicles for tumor-targeted d...

journal_title：Molecular cancer therapeutics

authors： Xu L,Huang CC,Huang W,Tang WH,Rait A,Yin YZ,Cruz I,Xiang LM,Pirollo KF,Chang EH

更新日期：2002-03-01 00:00:00

abstract：:Novel molecules are constantly being discovered and developed to find better means of managing debilitating and fatal diseases, which include cancer in its multiple forms. Among these molecules, and as a direct consequence of a better understanding of the molecular basis of diseases, are those falling within the class...

journal_title：Molecular cancer therapeutics

authors： Dass CR,Choong PF,Khachigian LM

更新日期：2008-02-01 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：:DNA damaging agents such as cisplatin arrest cell cycle progression at either G1, S, or G2 phase, although the G1 arrest is only seen in cells expressing the wild-type p53 tumor suppressor protein. We have reported that 7-hydroxystaurosporine (UCN-01) overcomes S and G2 phase arrest and enhances the cytotoxicity of ci...

journal_title：Molecular cancer therapeutics

authors： Eastman A,Kohn EA,Brown MK,Rathman J,Livingstone M,Blank DH,Gribble GW

更新日期：2002-10-01 00:00:00

abstract：:Constitutively activated STAT3 and STAT5 are expressed in a wide variety of human malignancies including solid and hematopoietic cancers and often correlate with a poor prognosis and resistance to multiple therapies. Given the well established role of STAT3 in tumorigenesis, inhibition of Janus-activated kinase 2 (JAK...

journal_title：Molecular cancer therapeutics

authors： Seavey MM,Lu LD,Stump KL,Wallace NH,Hockeimer W,O'Kane TM,Ruggeri BA,Dobrzanski P

更新日期：2012-04-01 00:00:00

abstract：:The inverse association between a high enterolactone (ENL) concentration in both urine and serum, and the risk of breast cancer found in epidemiological studies suggests a chemopreventive action for ENL. However, no causal relationship has been established in clinical studies or in experimental models for breast cance...

journal_title：Molecular cancer therapeutics

authors： Saarinen NM,Huovinen R,Wärri A,Mäkelä SI,Valentín-Blasini L,Sjöholm R,Ammälä J,Lehtilä R,Eckerman C,Collan YU,Santti RS

更新日期：2002-08-01 00:00:00

abstract：:p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is...

journal_title：Molecular cancer therapeutics

authors： Canon J,Osgood T,Olson SH,Saiki AY,Robertson R,Yu D,Eksterowicz J,Ye Q,Jin L,Chen A,Zhou J,Cordover D,Kaufman S,Kendall R,Oliner JD,Coxon A,Radinsky R

更新日期：2015-03-01 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：:Hepatocyte growth factor/scatter factor (HGF/SF) and its receptor, c-Met, have been implicated in the growth and progression of a variety of solid human tumors. Thus, inhibiting HGF/SF:c-Met signaling may provide a novel therapeutic approach for treating human tumors. We have generated and characterized fully human mo...

journal_title：Molecular cancer therapeutics

authors： Gao CF,Xie Q,Zhang YW,Su Y,Zhao P,Cao B,Furge K,Sun J,Rex K,Osgood T,Coxon A,Burgess TL,Vande Woude GF

更新日期：2009-10-01 00:00:00

abstract：:Urokinase plasminogen activator (uPA) is a tumor-specific protease highly expressed in several types of solid tumors and rarely present on normal cells under physiologic conditions. Due to its high expression on metastatic tumors, several different strategies have been used to target the urokinase system. These have m...

journal_title：Molecular cancer therapeutics

authors： Abi-Habib RJ,Singh R,Liu S,Bugge TH,Leppla SH,Frankel AE

更新日期：2006-10-01 00:00:00

abstract：:In patients with advanced bladder cancer, glucocorticoids are frequently given to reduce acute toxicity, particularly hyperemesis, during chemotherapy, as well as to improve cachectic conditions. However, it remains unclear whether glucocorticoids directly affect the development and progression of bladder cancer throu...

journal_title：Molecular cancer therapeutics

authors： Zheng Y,Izumi K,Li Y,Ishiguro H,Miyamoto H

更新日期：2012-12-01 00:00:00

abstract：:The MET receptor tyrosine kinase, the receptor for hepatocyte growth factor (HGF), has been implicated in cancer growth, invasion, migration, angiogenesis, and metastasis in a broad variety of human cancers, including human hepatocellular carcinoma (HCC). Recently, MET was suggested to be a potential target for the pe...

journal_title：Molecular cancer therapeutics

authors： Jo JC,Choi EK,Shin JS,Moon JH,Hong SW,Lee HR,Kim SM,Jung SA,Lee DH,Jung SH,Lee SH,Kim JE,Kim KP,Hong YS,Suh YA,Jang SJ,Choi EK,Lee JS,Jin DH,Kim TW

更新日期：2015-11-01 00:00:00

abstract：:Cytochrome P450 1B1 (CYP1B1) is found in tumor tissue and is suspected to play a role in oncogenesis and drug resistance. CYP1B1 gene polymorphisms have been associated with the risk of developing lung and other cancers. They may be associated with tumor response to anticancer drugs. We have determined 4 frequent nons...

journal_title：Molecular cancer therapeutics

authors： Laroche-Clary A,Le Morvan V,Yamori T,Robert J

更新日期：2010-12-01 00:00:00

abstract：:During camptothecin- and etoposide (VP-16)-induced apoptosis in HL-60 cells, the expression level of cell death receptor-3 (DR3), cell death receptor-4 (DR4), and FAS remained mostly unchanged, whereas the expression of silencers of death domain (SODD) and FLICE inhibitory proteins, inhibitors of the cell death recept...

journal_title：Molecular cancer therapeutics

authors： Bergeron S,Beauchemin M,Bertrand R

更新日期：2004-12-01 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