Novel inhibitors of Rad6 ubiquitin conjugating enzyme: design, synthesis, identification, and functional characterization.

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：:Using a luciferase reporter-based high-throughput chemical library screen and topological data analysis, we identified N-acridine-9-yl-N',N'-dimethylpropane-1,3-diamine (DAPA) as an inhibitor of the inositol requiring kinase 1α (IRE1α)-X-box binding protein-1 (XBP1) pathway of the unfolded protein response. We designe...

journal_title：Molecular cancer therapeutics

authors： Jiang D,Tam AB,Alagappan M,Hay MP,Gupta A,Kozak MM,Solow-Cordero DE,Lum PY,Denko NC,Giaccia AJ,Le QT,Niwa M,Koong AC

更新日期：2016-09-01 00:00:00

abstract：:Activin receptor-like kinase-1 (ALK1) is a type I, endothelial cell-specific member of the transforming growth factor-beta superfamily of receptors known to play an essential role in modulating angiogenesis and vessel maintenance. In the present study, we sought to examine the angiogenic and tumorigenic effects mediat...

journal_title：Molecular cancer therapeutics

authors： Mitchell D,Pobre EG,Mulivor AW,Grinberg AV,Castonguay R,Monnell TE,Solban N,Ucran JA,Pearsall RS,Underwood KW,Seehra J,Kumar R

更新日期：2010-02-01 00:00:00

abstract：:Resistance to antiandrogen drugs, like MDV3100, occurs in patients with castration-resistant prostate cancer (CRPC). Thus, preventing or treating antiandrogen resistance is a major clinical challenge. We identified a novel antiandrogen, Compound 30, and compared its efficacy with MDV3100. We found that Compound 30 inh...

journal_title：Molecular cancer therapeutics

authors： Kuruma H,Matsumoto H,Shiota M,Bishop J,Lamoureux F,Thomas C,Briere D,Los G,Gleave M,Fanjul A,Zoubeidi A

更新日期：2013-05-01 00:00:00

abstract：:The development of new drugs against cancer requires established cell lines. They are needed for in vitro studies to identify candidate drugs and in xenograft models to measure drug efficacy in vivo. Specific criteria need to be fulfilled by cell lines used in the evaluation of potential novel therapeutic agents. It i...

journal_title：Molecular cancer therapeutics

authors： Kees UR,Ford J,Watson M,Murch A,Ringńer M,Walker RL,Meltzer P

更新日期：2003-07-01 00:00:00

abstract：:Patients with non-small cell lung carcinoma (NSCLC) with activating mutations in epidermal growth factor receptor (EGFR) initially respond well to the EGFR inhibitors erlotinib and gefitinib. However, all patients relapse because of the emergence of drug-resistant mutations, with T790M mutations accounting for approxi...

journal_title：Molecular cancer therapeutics

authors： Tjin Tham Sjin R,Lee K,Walter AO,Dubrovskiy A,Sheets M,Martin TS,Labenski MT,Zhu Z,Tester R,Karp R,Medikonda A,Chaturvedi P,Ren Y,Haringsma H,Etter J,Raponi M,Simmons AD,Harding TC,Niu D,Nacht M,Westlin WF,Pette

更新日期：2014-06-01 00:00:00

abstract：:Acquired resistance to cancer drugs is common, also for modern targeted drugs like the Bruton tyrosine kinase (BTK) inhibitor ibrutinib, a new drug approved for the treatment of the highly aggressive and relapsing mantle cell lymphoma (MCL). The tumor microenvironment often impacts negatively on drug response. Here, w...

journal_title：Molecular cancer therapeutics

authors： Guan J,Huang D,Yakimchuk K,Okret S

更新日期：2018-05-01 00:00:00

abstract：:TIGIT is an immune checkpoint inhibitor expressed by effector CD4+ and CD8+ T cells, NK cells, and regulatory T cells (Tregs). Inhibition of TIGIT-ligand binding using antagonistic anti-TIGIT mAbs has shown in vitro potential to restore T-cell function and therapeutic efficacy in murine tumor models when combined with...

journal_title：Molecular cancer therapeutics

authors： Preillon J,Cuende J,Rabolli V,Garnero L,Mercier M,Wald N,Pappalardo A,Denies S,Jamart D,Michaux AC,Pirson R,Pitard V,Bagot M,Prasad S,Houthuys E,Brouwer M,Marillier R,Lambolez F,Marchante JR,Nyawouame F,Carter MJ

更新日期：2021-01-01 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：: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：:Prostate-specific membrane antigen (PSMA) is a membrane protein that is overexpressed manifold in prostate cancer and provides an attractive target for therapy. PSMA ADC is an antibody-drug conjugate (ADC) that consists of a fully human anti-PSMA monoclonal antibody conjugated to monomethylauristatin E through a valin...

journal_title：Molecular cancer therapeutics

authors： Wang X,Ma D,Olson WC,Heston WD

更新日期：2011-09-01 00:00:00

abstract：:The two-step transcriptional activation (TSTA) mechanism in gene therapy amplifies cell type-specific promoter activity, allowing for increased levels of gene expression in target tissues. In this system, the specific promoter drives expression of a strong transcriptional activator that binds to DNA target sequences l...

journal_title：Molecular cancer therapeutics

authors： Arendt ML,Nasir L,Morgan IM

更新日期：2009-12-01 00:00:00

abstract：:Gefitinib (Iressa, ZD1839), a quinazoline tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR), is approved for patients with advanced non-small cell lung cancer (NSCLC) in several countries including Japan. However, the mechanism of drug sensitivity to gefitinib is not fully understood. ...

journal_title：Molecular cancer therapeutics

authors： Ono M,Hirata A,Kometani T,Miyagawa M,Ueda S,Kinoshita H,Fujii T,Kuwano M

更新日期：2004-04-01 00:00:00

abstract：:Upregulation of HER2 is a hallmark of 20% to 30% of invasive breast cancers, rendering this receptor an attractive target for cancer therapy. Although HER2-targeting agents have provided substantial clinical benefit as cancer therapeutics, there is a need for the development of new agents aiming at circumventing anti-...

journal_title：Molecular cancer therapeutics

authors： Brack S,Attinger-Toller I,Schade B,Mourlane F,Klupsch K,Woods R,Hachemi H,von der Bey U,Koenig-Friedrich S,Bertschinger J,Grabulovski D

更新日期：2014-08-01 00:00:00

abstract：:Barasertib (AZD1152), a highly potent and selective aurora kinase B inhibitor, gave promising clinical activity in elderly acute myeloid leukemia (AML) patients. However, clinical utility was limited by the requirement for a 7-day infusion. Here we assessed the potential of a nanoparticle formulation of the selective ...

journal_title：Molecular cancer therapeutics

authors： Floc'h N,Ashton S,Taylor P,Trueman D,Harris E,Odedra R,Maratea K,Derbyshire N,Caddy J,Jacobs VN,Hattersley M,Wen S,Curtis NJ,Pilling JE,Pease EJ,Barry ST

更新日期：2017-06-01 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：:Melanoma is a highly drug-resistant cancer with resistance developing to agents targeting single proteins. To circumvent this problem, a new class of agent inhibiting multiple key pathways important in this disease is being developed to reduce the likelihood of developing resistant disease. The phosphoinositide 3-kina...

journal_title：Molecular cancer therapeutics

authors： Gowda R,Madhunapantula SV,Kuzu OF,Sharma A,Robertson GP

更新日期：2014-07-01 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：: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：:Current treatments for castration resistant prostate cancer (CRPC) largely fall into two classes: androgen receptor (AR)-targeted therapies such as the next-generation antiandrogen therapies (NGAT), enzalutamide and abiraterone, and taxanes such as docetaxel and cabazitaxel. Despite improvements in outcomes, patients ...

journal_title：Molecular cancer therapeutics

authors： Lombard AP,Liu L,Cucchiara V,Liu C,Armstrong CM,Zhao R,Yang JC,Lou W,Evans CP,Gao AC

更新日期：2018-10-01 00:00:00

abstract：:Mithramycin A is a DNA-binding antitumor agent, which has been clinically used in the therapies of several types of cancer and Paget's disease. In this study, we investigated the combined effect of mithramycin A and tumor necrosis factor-alpha-related apoptosis-inducing ligand (TRAIL) on apoptosis of cancer cells. In ...

journal_title：Molecular cancer therapeutics

authors： Lee TJ,Jung EM,Lee JT,Kim S,Park JW,Choi KS,Kwon TK

更新日期：2006-11-01 00:00:00

abstract：:The mammalian target of rapamycin (mTOR) is a serine/threonine protein kinase that exists in two complexes (mTORC1 and mTORC2) and integrates extracellular and intracellular signals to act as a master regulator of cell growth, survival, and metabolism. The PI3K/AKT/mTOR prosurvival pathway is often dysregulated in mul...

journal_title：Molecular cancer therapeutics

authors： Slotkin EK,Patwardhan PP,Vasudeva SD,de Stanchina E,Tap WD,Schwartz GK

更新日期：2015-02-01 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：: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：: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：:Gallium nitrate is a metallodrug with clinical efficacy in non-Hodgkin's lymphoma. Its mechanisms of antineoplastic action are not fully understood. In the present study, we investigated the roles of transferrin receptor (TfR) targeting and apoptotic pathways in gallium-induced cell death. Although DoHH2 lymphoma cell...

journal_title：Molecular cancer therapeutics

authors： Chitambar CR,Wereley JP,Matsuyama S

更新日期：2006-11-01 00:00:00

abstract：:Ras signaling can be modulated by the scaffolding activity of kinase suppressor of Ras-1 (KSR-1) and by the hKSR-2 protein, resulting in diverse phenotypic outcomes. The mitogen-activated protein kinase cascade downstream from Ras and KSRs includes Raf-1 and extracellular signal-regulated kinase 1/2 kinases, known to ...

journal_title：Molecular cancer therapeutics

authors： Wang X,Patel R,Studzinski GP

更新日期：2008-09-01 00:00:00

abstract：:The functional and therapeutic importance of the Warburg effect is increasingly recognized, and glycolysis has become a target of anticancer strategies. We recently reported the identification of a group of novel small compounds that inhibit basal glucose transport and reduce cancer cell growth by a glucose deprivatio...

journal_title：Molecular cancer therapeutics

authors： Liu Y,Cao Y,Zhang W,Bergmeier S,Qian Y,Akbar H,Colvin R,Ding J,Tong L,Wu S,Hines J,Chen X

更新日期：2012-08-01 00:00:00

abstract：:To isolate circulating tumor cells (CTC) from women with advanced cervical cancer and estimate the impact of CTCs and treatment on overall survival and progression-free survival (PFS). A total of 7.5 mL of whole blood was drawn pre-cycle 1 and 36 days post-cycle 1 from patients enrolled on Gynecologic Oncology Group 0...

journal_title：Molecular cancer therapeutics

authors： Tewari KS,Sill MW,Monk BJ,Penson RT,Moore DH,Lankes HA,Ramondetta LM,Landrum LM,Randall LM,Oaknin A,Leitao MM,Eisenhauer EL,DiSilvestro P,Van Le L,Pearl ML,Burke JJ,Salani R,Richardson DL,Michael HE,Kindelberger DW

更新日期：2020-08-26 00:00:00