TTK Inhibitors as a Targeted Therapy for CTNNB1 (β-catenin) Mutant Cancers.

abstract：:The cytotoxicity of 5-aza-2'-deoxycytidine (DAC) has been linked to demethylation of the INK4a/ARF tumor suppressor gene locus in various cell systems, but the causality of this association remains unproven. To test this assumption, we have examined the effects of DAC in two human cancer cell lines of differing INK4a/...

journal_title：Molecular cancer therapeutics

authors： Xiong J,Epstein RJ

更新日期：2009-04-01 00:00:00

abstract：:Because the majority of cancers exhibit direct or indirect deregulation of cyclin-dependent kinase (CDK) function, members of the CDK family are attractive targets for the development of anticancer agents. As part of an ongoing program, novel imidazopyridines were identified and developed as potent and selective CDK i...

journal_title：Molecular cancer therapeutics

authors： Byth KF,Geh C,Forder CL,Oakes SE,Thomas AP

更新日期：2006-03-01 00:00:00

abstract：:Imatinib mesylate is a potent, molecularly targeted therapy against the oncogenic tyrosine kinase BCR-ABL. Although imatinib mesylate has considerable efficacy against chronic myeloid leukemia (CML), advanced-stage CML patients frequently become refractory to this agent. The bone marrow is the predominant microenviron...

journal_title：Molecular cancer therapeutics

authors： Bewry NN,Nair RR,Emmons MF,Boulware D,Pinilla-Ibarz J,Hazlehurst LA

更新日期：2008-10-01 00:00:00

abstract：:DNA topoisomerase I (Top1) inhibition by camptothecin derivatives can impair the hypoxia-induced cell transcriptional response. In the present work, we determined molecular aspects of the mechanism of camptothecin's effects on hypoxia-inducible factor-1α (HIF-1α) activity in human cancer cells. In particular, we provi...

journal_title：Molecular cancer therapeutics

authors： Bertozzi D,Marinello J,Manzo SG,Fornari F,Gramantieri L,Capranico G

更新日期：2014-01-01 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：:Spongistatin 1, a marine experimental substance with chemotherapeutic potential, induces apoptosis and inhibits clonogenic survival of MCF-7 cells. Regarding the apoptotic signaling pathways of spongistatin 1, we present two major facts. Firstly, spongistatin 1-induced cell death, mainly caspase-independent, involves ...

journal_title：Molecular cancer therapeutics

authors： Schneiders UM,Schyschka L,Rudy A,Vollmar AM

更新日期：2009-10-01 00:00:00

abstract：:Tumor cells are efficiently killed after incubation with alpha-emitter immunoconjugates targeting tumor-specific antigens. Therefore, application of alpha-emitter immunoconjugates is a promising therapeutic option for treatment of carcinomas that are characterized by dissemination of single tumor cells in the peritone...

journal_title：Molecular cancer therapeutics

authors： Seidl C,Port M,Gilbertz KP,Morgenstern A,Bruchertseifer F,Schwaiger M,Röper B,Senekowitsch-Schmidtke R,Abend M

更新日期：2007-08-01 00:00:00

abstract：:Several clinical trials have shown gallium nitrate to be an active agent in the treatment of lymphoma. Whereas gallium is known to target cellular iron homeostasis, the basis for lymphoma cell resistance to gallium is not known. Understanding mechanisms of resistance may suggest strategies to enhance the clinical effi...

journal_title：Molecular cancer therapeutics

authors： Yang M,Kroft SH,Chitambar CR

更新日期：2007-02-01 00:00:00

abstract：:At later stages of tumor progression, epithelial carcinogenesis is associated with transition to a mesenchymal phenotype, which may contribute to the more aggressive properties of cancer cells and may be stimulated by growth factors such as epidermal growth factor and transforming growth factor-beta. Previously, we fo...

journal_title：Molecular cancer therapeutics

authors： Paccione RJ,Miyazaki H,Patel V,Waseem A,Gutkind JS,Zehner ZE,Yeudall WA

更新日期：2008-09-01 00:00:00

abstract：:STAT3 has been recognized for its key role in the progression of cancer, where it is frequently upregulated or constitutively hyperactivated, contributing to tumor cell proliferation, survival, and migration, as well as angiogenesis and suppression of antitumor immunity. Given the ubiquity of dysregulated STAT3 activi...

journal_title：Molecular cancer therapeutics

authors： Shiah JV,Grandis JR,Johnson DE

更新日期：2020-11-17 00:00:00

abstract：:Given the bulky nature of nanotherapeutics relative to small molecules, it is hypothesized that effective tumor delivery and penetration are critical barriers to their clinical activity. HER2-targeted PEGylated liposomal doxorubicin (MM-302, HER2-tPLD) is an antibody-liposomal drug conjugate designed to deliver doxoru...

journal_title：Molecular cancer therapeutics

authors： Geretti E,Leonard SC,Dumont N,Lee H,Zheng J,De Souza R,Gaddy DF,Espelin CW,Jaffray DA,Moyo V,Nielsen UB,Wickham TJ,Hendriks BS

更新日期：2015-09-01 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：: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：:Several studies have shown antitumor activities of the melanoma differentiation-associated gene 7 (mda-7) and the nonsteroidal anti-inflammatory drug sulindac when used as a monotherapies against a wide variety of human cancers. However, the combined effects of mda-7 and sulindac have not previously been tested. There...

journal_title：Molecular cancer therapeutics

authors： Oida Y,Gopalan B,Miyahara R,Inoue S,Branch CD,Mhashilkar AM,Lin E,Bekele BN,Roth JA,Chada S,Ramesh R

更新日期：2005-02-01 00:00:00

abstract：:Overexpression or hyperactivation of MDM2 contributes to functional inactivation of wild-type p53 in nearly 50% of tumors. Inhibition of p53 by MDM2 depends on binding between an NH(2)-terminal (residues 16-28) p53 alpha-helical peptide and a hydrophobic pocket on MDM2, presenting an attractive target for development ...

journal_title：Molecular cancer therapeutics

authors： Chen L,Yin H,Farooqi B,Sebti S,Hamilton AD,Chen J

更新日期：2005-06-01 00:00:00

abstract：:Allicin (diallyl thiosulfinate), a highly active component in extracts of freshly crushed garlic, is the interaction product of non-protein amino acid alliin (S-allyl-L-cysteine sulfoxide) with the enzyme alliinase (alliin lyase; EC 4.4.1.4). Allicin was shown to be toxic in various mammalian cells in a dose-dependent...

journal_title：Molecular cancer therapeutics

authors： Miron T,Mironchik M,Mirelman D,Wilchek M,Rabinkov A

更新日期：2003-12-01 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：: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：:Melanoma is a highly metastatic and deadly disease. An agent simultaneously targeting the COX-2, PI3K/Akt, and mitogen-activated protein kinase (MAPK) signaling pathways that are deregulated in up to 70% of sporadic melanomas might be an effective treatment, but no agent of this type exists. To develop a single drug i...

journal_title：Molecular cancer therapeutics

authors： Gowda R,Madhunapantula SV,Desai D,Amin S,Robertson GP

更新日期：2013-01-01 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：: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：: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：:Pulmonary metastasis is the most significant prognostic determinant for osteosarcoma, but methods for its prediction and treatment have not been established. Using oligonucleotide microarrays, we compared the global gene expression of biopsy samples between seven osteosarcoma patients who developed pulmonary metastasi...

journal_title：Molecular cancer therapeutics

authors： Kobayashi E,Masuda M,Nakayama R,Ichikawa H,Satow R,Shitashige M,Honda K,Yamaguchi U,Shoji A,Tochigi N,Morioka H,Toyama Y,Hirohashi S,Kawai A,Yamada T

更新日期：2010-03-01 00:00:00

abstract：:Activation of anaplastic lymphoma receptor tyrosine kinase (ALK) is involved in the pathogenesis of several carcinomas, including non-small cell lung cancer (NSCLC). Echinoderm microtubule-associated protein like 4 (EML4)-ALK, which is derived from the rearrangement of ALK and EML4 genes, has been validated as a thera...

journal_title：Molecular cancer therapeutics

authors： Mori M,Ueno Y,Konagai S,Fushiki H,Shimada I,Kondoh Y,Saito R,Mori K,Shindou N,Soga T,Sakagami H,Furutani T,Doihara H,Kudoh M,Kuromitsu S

更新日期：2014-02-01 00:00:00

abstract：:Mis-expression of microRNAs (miRNA) is widespread in human cancers, including in pancreatic cancer. Aberrations of miRNA include overexpression of oncogenic miRs (Onco-miRs) or downregulation of so-called tumor suppressor TSG-miRs. Restitution of TSG-miRs in cancer cells through systemic delivery is a promising avenue...

journal_title：Molecular cancer therapeutics

authors： Pramanik D,Campbell NR,Karikari C,Chivukula R,Kent OA,Mendell JT,Maitra A

更新日期：2011-08-01 00:00:00

abstract：:Breast cancer exhibits a propensity to metastasize to bone, resulting in debilitating skeletal complications associated with significant morbidity and poor prognosis. The cross-talk between metastatic cancer cells and bone is critical to the development and progression of bone metastases. We have shown the involvement...

journal_title：Molecular cancer therapeutics

authors： Previdi S,Abbadessa G,Dalò F,France DS,Broggini M

更新日期：2012-01-01 00:00:00

abstract：:Transforming growth factor-beta (TGF-beta) is a multifunctional cytokine that promotes malignant glioma invasion, angiogenesis, and immunosuppression. Antisense oligonucleotide suppression of TGF-beta(2) ligand expression has shown promise in preclinical and clinical studies but at least two ligands mediate the effect...

journal_title：Molecular cancer therapeutics

authors： Hjelmeland MD,Hjelmeland AB,Sathornsumetee S,Reese ED,Herbstreith MH,Laping NJ,Friedman HS,Bigner DD,Wang XF,Rich JN

更新日期：2004-06-01 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 ability of the epidermal growth factor receptor inhibitor gefitinib (Iressa) to prevent/treat methylnitrosourea (MNU)-induced mammary cancers and to modulate biomarkers in female Sprague-Dawley rats was examined. Rats were given a single dose of MNU (75 mg/kg body weight) at 50 days of age. In the prevention studi...

journal_title：Molecular cancer therapeutics

authors： Lubet RA,Szabo E,Christov K,Bode AM,Ericson ME,Steele VE,Juliana MM,Grubbs CJ

更新日期：2008-04-01 00:00:00

abstract：:Leukemia cells escape BCR-ABL-targeted therapy by developing mutations, such as T315I, in the p210(BCR-ABL) fusion protein in Philadelphia chromosome-positive chronic myeloid leukemia (CML). Although most effort has been focused on development of new tyrosine kinase inhibitors, enrichment of these small-molecule inhib...

journal_title：Molecular cancer therapeutics

authors： Mu C,Wu X,Ma H,Tao W,Zhang G,Xia X,Shen J,Mai J,Sun T,Sun X,Arlinghaus RB,Shen H

更新日期：2016-05-01 00:00:00