Characterization of the cytotoxic activities of novel analogues of the antitumor agent, lavendamycin.

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：: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：:Erlotinib is a tyrosine kinase inhibitor approved for the treatment of patients with advanced non-small cell lung cancer (NSCLC). In these patients, erlotinib prolongs survival but its benefit remains modest because many tumors express wild-type (wt) EGFR or develop a second-site EGFR mutation. To test drug combinatio...

journal_title：Molecular cancer therapeutics

authors： Dermawan JK,Gurova K,Pink J,Dowlati A,De S,Narla G,Sharma N,Stark GR

更新日期：2014-09-01 00:00:00

abstract：:Inhibition of both the de novo (DNP) and salvage (NSP) pathways of nucleoside synthesis has been demonstrated to impair leukemia cells. We endeavored to determine whether this approach would be efficacious in glioblastoma. To diminish nucleoside biosynthesis, we utilized compound DI-39, which selectively targets NSP, ...

journal_title：Molecular cancer therapeutics

authors： Laks DR,Ta L,Crisman TJ,Gao F,Coppola G,Radu CG,Nathanson DA,Kornblum HI

更新日期：2016-06-01 00:00:00

abstract：:Amplification of human epidermal growth factor receptor 2 (HER2) has been detected in 20% to 30% of gastric cancers and is associated with a poor outcome. Combination therapies with HER2-targeting agents and cytotoxic agents are considered a potential therapeutic option for gastric cancer with HER2 amplification. We h...

journal_title：Molecular cancer therapeutics

authors： Tanizaki J,Okamoto I,Takezawa K,Tsukioka S,Uchida J,Kiniwa M,Fukuoka M,Nakagawa K

更新日期：2010-05-01 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：: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：:Small cell lung cancer (SCLC) has a poor prognosis. Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase regulating cell proliferation, survival, migration, and invasion, which is overexpressed and/or activated in several cancers, including SCLC. We wanted to determine whether FAK contributes to SCLC aggressi...

journal_title：Molecular cancer therapeutics

authors： Aboubakar Nana F,Lecocq M,Ladjemi MZ,Detry B,Dupasquier S,Feron O,Massion PP,Sibille Y,Pilette C,Ocak S

更新日期：2019-01-01 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：:To investigate the mechanism by which 5-aminoimidazole-4-carboxamide-1-β-riboside (AICAr) induces apoptosis in multiple myeloma cells, we conducted an unbiased metabolomics screen. AICAr had selective effects on nucleotide metabolism, resulting in an increase in purine metabolites and a decrease in pyrimidine metaboli...

journal_title：Molecular cancer therapeutics

authors： Bardeleben C,Sharma S,Reeve JR,Bassilian S,Frost P,Hoang B,Shi Y,Lichtenstein A

更新日期：2013-07-01 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：:We previously showed that in innately resistant tumors, silencing of the estrogen receptor (ER) could be reversed by treatment with a histone deacetylase (HDAC) inhibitor, entinostat. Tumors were then responsive to aromatase inhibitor (AI) letrozole. Here, we investigated whether ER in the acquired letrozole-resistant...

journal_title：Molecular cancer therapeutics

authors： Sabnis GJ,Goloubeva OG,Kazi AA,Shah P,Brodie AH

更新日期：2013-12-01 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：:5'-Fluorouracil (5-FU), used in the treatment of colon and breast cancers, is converted intracellularly to 5'-fluoro-2'-deoxyuridine (5-FUdR) by thymidine phosphorylase and is subsequently phosphorylated by thymidine kinase to 5'-fluoro-2'-dUMP (5-FdUMP). This active metabolite, along with the reduced folate cofactor,...

journal_title：Molecular cancer therapeutics

authors： Pratt S,Shepard RL,Kandasamy RA,Johnston PA,Perry W 3rd,Dantzig AH

更新日期：2005-05-01 00:00:00

abstract：:Synthetic retinoid-related molecules (RRMs) have been described that show strong antiproliferative activity and induce apoptosis in cancer cells. These RRMs induce caspase activity independently of the retinoid receptors in Jurkat T cells. We observed that the inhibitor of cathepsins B and L Z-FA-fmk blocks the induct...

journal_title：Molecular cancer therapeutics

authors： Lopez-Hernandez FJ,Ortiz MA,Bayon Y,Piedrafita FJ

更新日期：2003-03-01 00:00:00

abstract：:Using the "one-bead one-peptide" combinatorial technology, a library of random cyclic octapeptides and nonapeptides, consisting of natural and unnatural amino acids, was synthesized on polystyrene beads. This library was used to screen for peptides that promoted attachment and proliferation of bronchioloalveolar carci...

journal_title：Molecular cancer therapeutics

authors： Mikawa M,Wang H,Guo L,Liu R,Marik J,Takada Y,Lam K,Lau D

更新日期：2004-10-01 00:00:00

abstract：:Involuntary weight loss, a part of the cachexia syndrome, is a debilitating comorbidity of cancer and currently has no treatment options. Results from a recent clinical trial at our institution showed that biliary tract cancer patients treated with a MEK inhibitor exhibited poor tumor responses but surprisingly gained...

journal_title：Molecular cancer therapeutics

authors： Talbert EE,Yang J,Mace TA,Farren MR,Farris AB,Young GS,Elnaggar O,Che Z,Timmers CD,Rajasekera P,Maskarinec JM,Bloomston M,Bekaii-Saab T,Guttridge DC,Lesinski GB

更新日期：2017-02-01 00:00:00

abstract：:Photodynamic therapy (PDT) induces the expression of the hypoxia-inducible factor 1alpha (HIF-1alpha) subunit of the HIF-1 transcription factor and its target genes in vitro and in vivo. PDT also induces the expression of the enzyme cyclooxygenase-2 and its metabolite, prostaglandin E2 (PGE2). PGE2 and hypoxia act ind...

journal_title：Molecular cancer therapeutics

authors： Mitra S,Cassar SE,Niles DJ,Puskas JA,Frelinger JG,Foster TH

更新日期：2006-12-01 00:00:00

abstract：:Clear cell renal cell carcinoma (CC-RCC) is a devastating disease with limited therapeutic options available for advanced stages. The objective of this study was to investigate HMG-CoA reductase inhibitors, also known as statins, as potential therapeutics for CC-RCC. Importantly, treatment with statins was found to be...

journal_title：Molecular cancer therapeutics

authors： Thompson JM,Alvarez A,Singha MK,Pavesic MW,Nguyen QH,Nelson LJ,Fruman DA,Razorenova OV

更新日期：2018-08-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor γ (PPARγ) is an important transcription factor that modulates lipid metabolism and inflammation. However, it remains unclear whether PPARγ is involved in modulation of estrogen (E2)-induced inflammation, thus affecting apoptosis of E2-deprived breast cancer cells, MCF-7:5C an...

journal_title：Molecular cancer therapeutics

authors： Fan P,Abderrahman B,Chai TS,Yerrum S,Jordan VC

更新日期：2018-12-01 00:00:00

abstract：:ABT-263 is a potent, orally bioavailable inhibitor of the antiapoptotic Bcl-2 family members Bcl-2, Bcl-x(L), and Bcl-w, which is currently in phase I clinical trials. Previous work has shown that this compound has low nanomolar cell-killing activity in a variety of lymphoma and leukemia cell lines, many of which over...

journal_title：Molecular cancer therapeutics

authors： Ackler S,Xiao Y,Mitten MJ,Foster K,Oleksijew A,Refici M,Schlessinger S,Wang B,Chemburkar SR,Bauch J,Tse C,Frost DJ,Fesik SW,Rosenberg SH,Elmore SW,Shoemaker AR

更新日期：2008-10-01 00:00:00

abstract：:B-Raf is an important mediator of cell proliferation and survival signals transduced via the Ras-Raf-MEK-ERK cascade. BRAF mutations have been detected in several tumors, including papillary thyroid carcinoma, but the precise role of B-Raf as a therapeutic target for thyroid carcinoma is still under investigation. We ...

journal_title：Molecular cancer therapeutics

authors： Mitsiades CS,Negri J,McMullan C,McMillin DW,Sozopoulos E,Fanourakis G,Voutsinas G,Tseleni-Balafouta S,Poulaki V,Batt D,Mitsiades N

更新日期：2007-03-01 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：:Glycosylation is a complex multienzyme-related process that is frequently deregulated in cancer. Aberrant glycosylation can lead to the generation of novel tumor surface-specific glycotopes that can be targeted by antibodies. Murine DS6 mAb (muDS6) was generated from serous ovary adenocarcinoma immunization. It recogn...

journal_title：Molecular cancer therapeutics

authors： Nicolazzi C,Caron A,Tellier A,Trombe M,Pinkas J,Payne G,Carrez C,Guérif S,Maguin M,Baffa R,Fassan M,Adam J,Mangatal-Wade L,Blanc V

更新日期：2020-08-01 00:00:00

abstract：:There is a growing recognition that current preclinical models do not reflect the tumor microenvironment in cellular, biological, and biophysical content and this may have a profound effect on drug efficacy testing, especially in the era of molecular-targeted agents. Here, we describe a method to directly embed low-pa...

journal_title：Molecular cancer therapeutics

authors： Onion D,Argent RH,Reece-Smith AM,Craze ML,Pineda RG,Clarke PA,Ratan HL,Parsons SL,Lobo DN,Duffy JP,Atherton JC,McKenzie AJ,Kumari R,King P,Hall BM,Grabowska AM

更新日期：2016-04-01 00:00:00

abstract：:Members of the signal transducer and activator of transcription (STAT) family of transcription factors are potential targets for the treatment and prevention of cancers including non-small-cell lung cancer. STAT proteins can be phosphorylated and activated by diverse upstream kinases including cytokine receptors and t...

journal_title：Molecular cancer therapeutics

authors： Song L,Rawal B,Nemeth JA,Haura EB

更新日期：2011-03-01 00:00:00

abstract：:Why does it seem that, repeatedly, when a new treatment with a striking effect is discovered in the cancer field, it is effective for a very rare cancer type? For example, groundbreaking therapeutic discoveries have been made for extremely uncommon malignancies such as hairy cell leukemia, chronic myelogenous leukemia...

journal_title：Molecular cancer therapeutics

authors： Braiteh F,Kurzrock R

更新日期：2007-04-01 00:00:00

abstract：:PTTG1 protein, the human securin, has a central role in sister chromatid separation during mitosis, and its altered expression has been reported in many tumor types. Paclitaxel is a widely used chemotherapeutic drug, whose mechanism of action is related to its ability to arrest cells in mitosis and the subsequent indu...

journal_title：Molecular cancer therapeutics

authors： Castilla C,Flores ML,Medina R,Pérez-Valderrama B,Romero F,Tortolero M,Japón MA,Sáez C

更新日期：2014-10-01 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：: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