TACIMA-218: A Novel Pro-Oxidant Agent Exhibiting Selective Antitumoral Activity.

abstract：:Labetuzumab govitecan (IMMU-130), an antibody-drug conjugate (ADC) with an average of 7.6 SN-38/IgG, was evaluated for its potential to enhance delivery of SN-38 to human colonic tumor xenografts. Mice bearing LS174T or GW-39 human colonic tumor xenografts were injected with irinotecan or IMMU-130 (SN-38 equivalents ∼...

journal_title：Molecular cancer therapeutics

authors： Sharkey RM,Govindan SV,Cardillo TM,Donnell J,Xia J,Rossi EA,Chang CH,Goldenberg DM

更新日期：2018-01-01 00:00:00

abstract：:Cells contain a large number of antioxidants to prevent or repair the damage caused by reactive oxygen species. One component of the antioxidant system, manganese superoxide dismutase (MnSOD), is localized in the mitochondria, and the levels of this protein have been previously shown to inversely correlate with pancre...

journal_title：Molecular cancer therapeutics

authors： Weydert C,Roling B,Liu J,Hinkhouse MM,Ritchie JM,Oberley LW,Cullen JJ

更新日期：2003-04-01 00:00:00

abstract：:Glioblastoma is the most frequent brain tumor of glial origin in adults. With the best available standard-of-care, patients with this disease have a life expectancy of only approximately 15 months after diagnosis. Because the EGF receptor (HER1/EGFR) is one of the most commonly dysregulated oncogenes in glioblastoma, ...

journal_title：Molecular cancer therapeutics

authors： Karpel-Massler G,Westhoff MA,Zhou S,Nonnenmacher L,Dwucet A,Kast RE,Bachem MG,Wirtz CR,Debatin KM,Halatsch ME

更新日期：2013-09-01 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：:The tumor-associated Tn antigen has been investigated extensively as a biomarker and therapeutic target. Cancer vaccines containing the Tn antigen as a single tumor antigen or as a component of a polyvalent vaccine have progressed into phase I and II clinical trials. One major focus of Tn-based vaccines is the treatme...

journal_title：Molecular cancer therapeutics

authors： Li Q,Anver MR,Butcher DO,Gildersleeve JC

更新日期：2009-04-01 00:00:00

abstract：:DNA damage repair capacity is required for cells to survive catastrophic DNA damage and proliferate under conditions of intratumoral stress. The ability of the minor histone protein H2AX to serve as a hub for the assembly of a productive DNA damage repair complex is a necessary step in preventing DNA damage-induced ce...

journal_title：Molecular cancer therapeutics

authors： Wang Y,Pandey RN,Riffle S,Chintala H,Wikenheiser-Brokamp KA,Hegde RS

更新日期：2018-08-01 00:00:00

abstract：:Programmed cell death 4 (Pdcd4), originally identified as an inhibitor of murine cellular transformation, inhibits protein synthesis by directly interacting with eukaryotic initiation factor 4A (eIF4A) of the translation initiation complex. The relevance of Pdcd4 to a broad range of human cancers derived from multiple...

journal_title：Molecular cancer therapeutics

authors： Jansen AP,Camalier CE,Stark C,Colburn NH

更新日期：2004-02-01 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：:FOXO proteins are Akt-regulated transcription factors involved in the control of cell cycle, DNA repair, stress defense, apoptosis, and tumor suppression. We reported that plasmid-based overexpression of constitutively active FOXO3 in cells from chronic lymphocytic leukemia (CLL) reduced their survival, suggesting tha...

journal_title：Molecular cancer therapeutics

authors： Essafi M,Baudot AD,Mouska X,Cassuto JP,Ticchioni M,Deckert M

更新日期：2011-01-01 00:00:00

abstract：:Hodgkin-Reed/Sternberg (HRS) cells of classical Hodgkin lymphoma show aberrant expression and activation of several receptor tyrosine kinases (RTK) in the majority of cases. Therefore, we tested whether tyrosine kinase inhibitors (TKI) already in clinical use or late stages of clinical trials have antiproliferative ef...

journal_title：Molecular cancer therapeutics

authors： Holz MS,Janning A,Renné C,Gattenlöhner S,Spieker T,Bräuninger A

更新日期：2013-02-01 00:00:00

abstract：:Endocrine therapy has been highly effective for the treatment of estrogen receptor-positive breast cancer, but endocrine resistance develops in a significant proportion of patients. In an effort to develop novel therapeutic strategies for the treatment of endocrine-resistant breast cancer, we have evaluated a potent a...

journal_title：Molecular cancer therapeutics

authors： Lu J,McEachern D,Li S,Ellis MJ,Wang S

更新日期：2016-12-01 00:00:00

abstract：:PI3K is frequently mutated in cancer and plays an important role in cell growth and survival. Heregulin (HRG)-mediated autocrine or paracrine signaling through the receptor tyrosine kinase ErbB3 potently activates the PI3K/AKT pathway and has been shown to mediate resistance to a wide variety of anticancer agents. Alt...

journal_title：Molecular cancer therapeutics

authors： Yarar D,Lahdenranta J,Kubasek W,Nielsen UB,MacBeath G

更新日期：2015-09-01 00:00:00

abstract：:Rapamycin and its analogues are being tested as new antitumor agents. Rapamycin binds to FKBP-12 and this complex inhibits the activity of FRAP/mammalian target of rapamycin, which leads to dephosphorylation of 4EBP1 and p70 S6 kinase, resulting in blockade of translation initiation. We have found that RAP inhibits th...

journal_title：Molecular cancer therapeutics

authors： García-Morales P,Hernando E,Carrasco-García E,Menéndez-Gutierrez MP,Saceda M,Martínez-Lacaci I

更新日期：2006-09-01 00:00:00

abstract：:Elevated levels of Src kinase expression have been found in a variety of human epithelial cancers. Most notably in colon cancer, elevated Src expression correlates with malignant potential and is also associated with metastatic disease. Dasatinib (BMS-354825) is a novel, orally active, multi-targeted kinase inhibitor ...

journal_title：Molecular cancer therapeutics

authors： Serrels A,Macpherson IR,Evans TR,Lee FY,Clark EA,Sansom OJ,Ashton GH,Frame MC,Brunton VG

更新日期：2006-12-01 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：:A quaternary ammonium-based drug-linker has been developed to expand the scope of antibody-drug conjugate (ADC) payloads to include tertiary amines, a functional group commonly present in biologically active compounds. The linker strategy was exemplified with a β-glucuronidase-cleavable auristatin E construct. The dru...

journal_title：Molecular cancer therapeutics

authors： Burke PJ,Hamilton JZ,Pires TA,Setter JR,Hunter JH,Cochran JH,Waight AB,Gordon KA,Toki BE,Emmerton KK,Zeng W,Stone IJ,Senter PD,Lyon RP,Jeffrey SC

更新日期：2016-05-01 00:00:00

abstract：:Glioma is the most common type of primary malignant brain tumor in adults. Our previous work discovered that plasma miR-454-3p may have some advantages in glioma prognosis, but the clinical significance and the regulatory mechanism of miR-454-3p in glioma have not been systematically investigated, especially regarding...

journal_title：Molecular cancer therapeutics

authors： Shao N,Xue L,Wang R,Luo K,Zhi F,Lan Q

更新日期：2019-02-01 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：: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：:Oncostatin M (OSM), an interleukin 6-type cytokine, induces sustained up-regulation of CCAAT/enhancer-binding protein (C/EBP) delta mRNA and protein in nonneoplastic HC11 mouse mammary epithelial cells. This up-regulation is dependent on signaling by phospho-Stat3 (signal transducers and activators of transcription). ...

journal_title：Molecular cancer therapeutics

authors： Hutt JA,DeWille JW

更新日期：2002-06-01 00:00:00

abstract：:Endocrine therapy is important for management of patients with estrogen receptor (ER)-positive breast cancer; however, positive ER staining does not reliably predict therapy response. We assessed the potential to improve prediction of response to endocrine treatment of a novel test that quantifies functional ER pathwa...

journal_title：Molecular cancer therapeutics

authors： Inda MA,Blok EJ,Kuppen PJK,Charehbili A,den Biezen-Timmermans EC,van Brussel A,Fruytier SE,Meershoek-Klein Kranenbarg E,Kloet S,van der Burg B,Martens JWM,Sims AH,Turnbull AK,Dixon JM,Verhaegh W,Kroep JR,van de Velde CJH

更新日期：2020-02-01 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：:With the increase of treatment course, resistance to EGFR blockade is inevitable in patients with metastatic colorectal cancer (mCRC). KRAS mutations have been considered to be primary drivers of this resistance; however, the potential function of other genes has not been extensively investigated. This study collected...

journal_title：Molecular cancer therapeutics

authors： Ye S,Hu X,Ni C,Jin W,Xu Y,Chang L,Zhou H,Jiang J,Yang L

更新日期：2020-03-01 00:00:00

abstract：:Antibodies conjugated to radionuclides emitting low-energy electrons, which include Auger electrons and some conversion electrons, were recently shown to efficiently kill cells bearing a high density of the antigen recognized. The primary purpose of this study was to determine if such killing could be obtained with an...

journal_title：Molecular cancer therapeutics

authors： Michel RB,Andrews PM,Castillo ME,Mattes MJ

更新日期：2005-06-01 00:00:00

abstract：:Ovarian cancer is the leading cause of death from gynecologic cancer. Often, the disease has spread beyond the ovary to involve the peritoneal cavity and causes ascites. Whereas mammalian target of rapamycin (mTOR) functions to regulate protein translation, cell cycle progression, and metastasis, vascular endothelial ...

journal_title：Molecular cancer therapeutics

authors： Huynh H,Teo CC,Soo KC

更新日期：2007-11-01 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：: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：:Neuroblastoma is the most common extracranial solid malignancy in the pediatric population, accounting for over 9% of all cancer-related deaths in children. Autophagy is a cell self-protective mechanism that promotes tumor cell growth and survival, making it an attractive target for treating cancer. However, the role ...

journal_title：Molecular cancer therapeutics

authors： Dower CM,Bhat N,Gebru MT,Chen L,Wills CA,Miller BA,Wang HG

更新日期：2018-11-01 00:00:00

abstract：:Aminoflavone (AF), a clinically investigational novel anticancer agent, requires sequential metabolic activation by CYP1A1 and SULT1A1 to exert its antitumor activities. The purpose of this study was to determine the functional significance of common polymorphisms of human CYP1A1 and SULT1A1 on the metabolism and cyto...

journal_title：Molecular cancer therapeutics

authors： Zheng Q,Sha X,Liu J,Heath E,Lorusso P,Li J

更新日期：2010-10-01 00:00:00

abstract：:Tissue transglutaminase 2 belongs to a family of transglutaminase proteins that confers mechanical resistance from proteolysis and stabilizes proteins. Transglutaminase 2 promotes transamidation between glutamine and lysine residues with the formation of covalent linkages between proteins. Transglutaminase 2 also inte...

journal_title：Molecular cancer therapeutics

authors： Yuan L,Choi K,Khosla C,Zheng X,Higashikubo R,Chicoine MR,Rich KM

更新日期：2005-09-01 00:00:00