A new nonestrogenic steroidal inhibitor of 17β-hydroxysteroid dehydrogenase type I blocks the estrogen-dependent breast cancer tumor growth induced by estrone.

abstract：:We report the discovery, via a unique high-throughput screening strategy, of a novel bioactive anticancer compound: Thiol Alkylating Compound Inducing Massive Apoptosis (TACIMA)-218. We demonstrate that this molecule engenders apoptotic cell death in genetically diverse murine and human cancer cell lines, irrespective...

journal_title：Molecular cancer therapeutics

authors： Abusarah J,Cui Y,El-Hachem N,El-Kadiry AE,Hammond-Martel I,Wurtele H,Beaudry A,Raynal NJ,Robert F,Pelletier J,Jankovic M,Mercier F,Kamyabiazar S,Annabi B,Rafei M

更新日期：2021-01-01 00:00:00

abstract：:Histone modification has emerged as a promising approach to cancer therapy. We explored the efficacy of a novel class of histone deacetylase inhibitors in the treatment of malignant gliomas. Treatment of glioma cell lines with two butyric acid derivatives, pivaloylomethyl butyrate (AN-9) and butyroyloxymethyl butyrate...

journal_title：Molecular cancer therapeutics

authors： Entin-Meer M,Rephaeli A,Yang X,Nudelman A,VandenBerg SR,Haas-Kogan DA

更新日期：2005-12-01 00:00:00

abstract：:Protein tyrosine kinases of the Janus kinase (JAK) family are associated with many cytokine receptors, which, on ligand binding, regulate important cellular functions such as proliferation, survival, and differentiation. In multiple myeloma, JAKs may be persistently activated due to a constant stimulation by interleuk...

journal_title：Molecular cancer therapeutics

authors： Burger R,Le Gouill S,Tai YT,Shringarpure R,Tassone P,Neri P,Podar K,Catley L,Hideshima T,Chauhan D,Caulder E,Neilan CL,Vaddi K,Li J,Gramatzki M,Fridman JS,Anderson KC

更新日期：2009-01-01 00:00:00

abstract：:To date, there is no effective therapy for hormone-independent prostate cancer. Therefore, as a new strategy for refractory cancer, gene therapy is showing increasing promise. In this study, we attempted to use a nonviral gene transfer system, in vivo electroporation, in prostate cancer cell PC-3 xenografts with the w...

journal_title：Molecular cancer therapeutics

authors： Mikata K,Uemura H,Ohuchi H,Ohta S,Nagashima Y,Kubota Y

更新日期：2002-02-01 00:00:00

abstract：:Aptamers, also termed as decoys or "chemical antibodies," represent an emerging class of therapeutics. They are short DNA or RNA oligonucleotides or peptides that assume a specific and stable three-dimensional shape in vivo, thereby providing specific tight binding to protein targets. In some cases and as opposed to a...

journal_title：Molecular cancer therapeutics

authors： Ireson CR,Kelland LR

更新日期：2006-12-01 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：:Nanotechnology refers to the interactions of cellular and molecular components and engineered materials-typically, clusters of atoms, molecules, and molecular fragments into incredibly small particles-between 1 and 100 nm. Nanometer-sized particles have novel optical, electronic, and structural properties that are not...

journal_title：Molecular cancer therapeutics

authors： Sinha R,Kim GJ,Nie S,Shin DM

更新日期：2006-08-01 00:00:00

abstract：UNLABELLED:Multiple myeloma (MM) is a malignancy of clonal B-cells that accounts for 10% of all hematologic malignancies. We have shown previously that a novel purine analogue, 8-chloro-adenosine, has significant activity for MM in preclinical studies. OBJECTIVE:Using MM cell lines, we investigated the molecular mecha...

journal_title：Molecular cancer therapeutics

authors： Krett NL,Davies KM,Ayres M,Ma C,Nabhan C,Gandhi V,Rosen ST

更新日期：2004-11-01 00:00:00

abstract：:This study aims to explore whether E545K, the most common hotspot mutation of PIK3CA in cervical cancer, confers radioresistance to cervical cancer cells, to demonstrate the underling mechanism, and to develop the effective targets. SiHa and MS751 cells with PIK3CA-WT and PIK3CA-E545K were established by lentiviral tr...

journal_title：Molecular cancer therapeutics

authors： Jiang W,Wu Y,He T,Zhu H,Ke G,Xiang L,Yang H

更新日期：2020-02-01 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：:Several antiangiogenic drugs targeting VEGF/VEGF receptor (VEGFR) that were approved by the Food and Drug Administration for many cancer types, including colorectal and lung cancer, can effectively reduce tumor growth. However, targeting the VEGF signaling pathway will probably influence the normal function of endothe...

journal_title：Molecular cancer therapeutics

authors： Chen CT,Yamaguchi H,Lee HJ,Du Y,Lee HH,Xia W,Yu WH,Hsu JL,Yen CJ,Sun HL,Wang Y,Yeh ET,Hortobagyi GN,Hung MC

更新日期：2011-08-01 00:00:00

abstract：:As the population ages, more elderly patients require radiotherapy-based treatment for their pelvic malignancies, including muscle-invasive bladder cancer, as they are unfit for major surgery. Therefore, there is an urgent need to find radiosensitizing agents minimally toxic to normal tissues, including bowel and blad...

journal_title：Molecular cancer therapeutics

authors： Groselj B,Ruan JL,Scott H,Gorrill J,Nicholson J,Kelly J,Anbalagan S,Thompson J,Stratford MRL,Jevons SJ,Hammond EM,Scudamore CL,Kerr M,Kiltie AE

更新日期：2018-02-01 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：: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：:Aberrant overexpression of antiapoptotic members of the Bcl-2 protein family, including Bcl-2 and Bcl-X(L), contributes to malignant transformation and subsequent resistance to traditional chemotherapeutics. Thus, these proteins represent attractive targets for novel anticancer agents. The small molecule, gossypol, wa...

journal_title：Molecular cancer therapeutics

authors： Oliver CL,Miranda MB,Shangary S,Land S,Wang S,Johnson DE

更新日期：2005-01-01 00:00:00

abstract：:Hepatocellular carcinoma is highly chemoresistant, and ATP-binding cassette subfamily G member 2 (ABCG2) is thought to play a critical role in this drug resistance. The present study aims to develop effective therapeutic strategies to decrease ABCG2 expression level and to surmount drug resistance in hepatocellular ca...

journal_title：Molecular cancer therapeutics

authors： Hou H,Sun H,Lu P,Ge C,Zhang L,Li H,Zhao F,Tian H,Zhang L,Chen T,Yao M,Li J

更新日期：2013-12-01 00:00:00

abstract：:Mitotic spindle poisons (e.g., Taxol and vinblastine), used as chemotherapy drugs, inhibit mitotic spindle function, activate the mitotic spindle checkpoint, arrest cells in mitosis, and then cause cell death by mechanisms that are poorly understood. By expression cloning, we identified a truncated version of human TR...

journal_title：Molecular cancer therapeutics

authors： Yamada HY,Gorbsky GJ

更新日期：2006-01-01 00:00:00

abstract：:Patients with non-small cell lung cancer (NSCLC) harboring activating mutations in the epidermal growth factor receptor (EGFR) kinase domain tend to respond well to the tyrosine kinase inhibitors, gefitinib and erlotinib. However, following clinical response, these patients typically relapse within a year of treatment...

journal_title：Molecular cancer therapeutics

authors： Godin-Heymann N,Ulkus L,Brannigan BW,McDermott U,Lamb J,Maheswaran S,Settleman J,Haber DA

更新日期：2008-04-01 00:00:00

abstract：:Nucleoside phosphonates are widely used therapeutic agents with a broad spectrum of antiviral activity. However, only a few of them are reported to have antitumor activity. In this study, we show that a tetrahydrofuran phosphonate analogue of guanosine, (-)-2-R-dihydroxyphosphinoyl-5-(S)-(guanin-9'-ylmethyl) tetrahydr...

journal_title：Molecular cancer therapeutics

authors： Leblond L,Attardo G,Hamelin B,Bouffard DY,Nguyen-Ba N,Gourdeau H

更新日期：2002-07-01 00:00:00

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：: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：: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：:The epithelial-mesenchymal transition (EMT) is an important mechanism of resistance to angiogenesis inhibition. The ability of EMT pathway genetic variants to predict the efficacy of antiangiogenic therapy is unknown. We analyzed associations between functional SNPs in EMT-related genes and outcomes in metastatic colo...

journal_title：Molecular cancer therapeutics

authors： Matsusaka S,Zhang W,Cao S,Hanna DL,Sunakawa Y,Sebio A,Ueno M,Yang D,Ning Y,Parekh A,Okazaki S,Berger MD,Ichikawa W,Mizunuma N,Lenz HJ

更新日期：2016-06-01 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：: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：:Despite the availability of several Food and Drug Administration-approved drugs, advanced inoperable colorectal cancer remains incurable. In this study, we focused on the development of combined molecular targeted therapies against colon cancer by testing the efficacy of the combination of the histone deacetylase inhi...

journal_title：Molecular cancer therapeutics

authors： Pitts TM,Morrow M,Kaufman SA,Tentler JJ,Eckhardt SG

更新日期：2009-02-01 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

abstract：:Genotoxic stress such as ionizing radiation halts entry into mitosis by activation of the G(2) DNA damage checkpoint. The CHK1 inhibitor 7-hydroxystaurosporine (UCN-01) can bypass the checkpoint and induce unscheduled mitosis in irradiated cells. Precisely, how cells behave following checkpoint abrogation remains to b...

journal_title：Molecular cancer therapeutics

authors： On KF,Chen Y,Ma HT,Chow JP,Poon RY

更新日期：2011-05-01 00:00:00

abstract：:Sorafenib is a second-generation, orally active multikinase inhibitor that is approved for the treatment of patients with advanced renal cell carcinoma and patients with unresectable hepatocellular carcinoma. We studied active transport of sorafenib in MDCK-II cells expressing human P-glycoprotein (P-gp/ABCB1) or ABCG...

journal_title：Molecular cancer therapeutics

authors： Lagas JS,van Waterschoot RA,Sparidans RW,Wagenaar E,Beijnen JH,Schinkel AH

更新日期：2010-02-01 00:00:00

abstract：:The oncoprotein Eps8 facilitates proliferation in fibroblasts and colon cancer cells. However, its role in human cervical cancer is unclear. By immunohistochemical staining and Western blotting, aberrant Eps8 expression was observed in cervical carcinoma compared with normal cervical epithelial cells. Clinicopathologi...

journal_title：Molecular cancer therapeutics

authors： Chen YJ,Shen MR,Chen YJ,Maa MC,Leu TH

更新日期：2008-06-01 00:00:00