Efficacy of the MDM2 Inhibitor SAR405838 in Glioblastoma Is Limited by Poor Distribution Across the Blood-Brain Barrier.

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：:We investigated integrin-linked kinase (ILK), a focal adhesion serine-threonine protein kinase, as a new molecular target for treating anaplastic thyroid cancer. ILK mediates cell growth and survival signals and is overexpressed in a number of cancers. Therefore, we hypothesized that inhibition of ILK leads to growth ...

journal_title：Molecular cancer therapeutics

authors： Younes MN,Kim S,Yigitbasi OG,Mandal M,Jasser SA,Dakak Yazici Y,Schiff BA,El-Naggar A,Bekele BN,Mills GB,Myers JN

更新日期：2005-08-01 00:00:00

abstract：:RX-5902 is a first-in-class anticancer agent targeting phosphorylated-p68 and attenuating nuclear shuttling of β-catenin. The purpose of this study was to evaluate the efficacy of RX-5902 in preclinical models of triple-negative breast cancer (TNBC) and to explore effects on β-catenin expression. A panel of 18 TNBC ce...

journal_title：Molecular cancer therapeutics

authors： Capasso A,Bagby SM,Dailey KL,Currimjee N,Yacob BW,Ionkina A,Frank JG,Kim DJ,George C,Lee YB,Benaim E,Gittleman B,Hartman SJ,Tan AC,Kim J,Pitts TM,Eckhardt SG,Tentler JJ,Diamond JR

更新日期：2019-11-01 00:00:00

abstract：:Advanced and hormone-refractory prostate cancer has long been considered as a chemoresistant disease. Recently, it was found that 14-3-3sigma expression increases as prostate tumor progresses, and that 14-3-3sigma contributes significantly to drug resistance in breast cancers. We, thus, hypothesized that advanced and ...

journal_title：Molecular cancer therapeutics

authors： Han B,Xie H,Chen Q,Zhang JT

更新日期：2006-04-01 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：:The efficacy of photodynamic therapy (PDT) for epithelial cancers is increased when PDT is combined with calcitriol (Vit D), a form of differentiation therapy (DT). Here, we describe an underlying mechanism for this effect. Differentiation-promoting agents are known to upregulate CCAAT/enhancer-binding proteins (C/EBP...

journal_title：Molecular cancer therapeutics

authors： Anand S,Hasan T,Maytin EV

更新日期：2013-08-01 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：:To determine the efficacy of a novel and safer (for gastrointestinal tract) aspirin (aspirin-PC) in preclinical models of ovarian cancer, in vitro dose-response studies were performed to compare the growth-inhibitory effect of aspirin-PC versus aspirin on three human (A2780, SKOV3ip1, and HeyA8) and a mouse (ID8) ovar...

journal_title：Molecular cancer therapeutics

authors： Huang Y,Lichtenberger LM,Taylor M,Bottsford-Miller JN,Haemmerle M,Wagner MJ,Lyons Y,Pradeep S,Hu W,Previs RA,Hansen JM,Fang D,Dorniak PL,Filant J,Dial EJ,Shen F,Hatakeyama H,Sood AK

更新日期：2016-12-01 00:00:00

abstract：:The cannabinoid 1 (CB(1)) and cannabinoid 2 (CB(2)) receptor agonist Delta(9)-tetrahydrocannabinol (THC) has been shown to be a broad-range inhibitor of cancer in culture and in vivo, and is currently being used in a clinical trial for the treatment of glioblastoma. It has been suggested that other plant-derived canna...

journal_title：Molecular cancer therapeutics

authors： Marcu JP,Christian RT,Lau D,Zielinski AJ,Horowitz MP,Lee J,Pakdel A,Allison J,Limbad C,Moore DH,Yount GL,Desprez PY,McAllister SD

更新日期：2010-01-01 00:00:00

abstract：:Hepatocyte growth factor/scatter factor (HGF/SF) and its receptor, c-Met, have been implicated in the growth and progression of a variety of solid human tumors. Thus, inhibiting HGF/SF:c-Met signaling may provide a novel therapeutic approach for treating human tumors. We have generated and characterized fully human mo...

journal_title：Molecular cancer therapeutics

authors： Gao CF,Xie Q,Zhang YW,Su Y,Zhao P,Cao B,Furge K,Sun J,Rex K,Osgood T,Coxon A,Burgess TL,Vande Woude GF

更新日期：2009-10-01 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDA) is an aggressive malignancy with one of the worst outcomes among all cancers. PDA often recurs after initial treatment to result in patient death despite the use of chemotherapy or radiation therapy. PDA contains a subset of tumor-initiating cells capable of extensive self-renewa...

journal_title：Molecular cancer therapeutics

authors： Rajeshkumar NV,Rasheed ZA,García-García E,López-Ríos F,Fujiwara K,Matsui WH,Hidalgo M

更新日期：2010-09-01 00:00:00

abstract：:Complexities in treating breast cancer with bone metastasis are enhanced by a vicious protumorigenic pathology, involving a shift in skeletal homeostasis toward aggressive osteoclast activity and polarization of immune cells supporting tumor growth and immunosuppression. Recent studies signify the role of receptor act...

journal_title：Molecular cancer therapeutics

authors： Wang H,Ashton R,Hensel JA,Lee JH,Khattar V,Wang Y,Deshane JS,Ponnazhagan S

更新日期：2020-12-01 00:00:00

abstract：:Endothelins (ETs) are a group of vasoactive peptides (ET-1, ET-2 and ET-3) produced by many cell types that bind to G-protein-linked transmembrane receptors, ET-A receptors (ET-RAs) and ET-B receptors (ET-RBs). These peptides are expressed in several human tumors, including carcinomas of the breast, and have a mitogen...

journal_title：Molecular cancer therapeutics

authors： Grimshaw MJ,Naylor S,Balkwill FR

更新日期：2002-12-01 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：:Activation of the epidermal growth factor receptor (EGFR) has been observed in many malignant tumors and its constitutive signal transduction facilitates the proliferation of tumors. EGFR-tyrosine kinase inhibitors, such as gefitinib, are widely used as a molecular-targeting agent for the inactivation of EGFR signalin...

journal_title：Molecular cancer therapeutics

authors： Saito K,Takigawa N,Ohtani N,Iioka H,Tomita Y,Ueda R,Fukuoka J,Kuwahara K,Ichihara E,Kiura K,Kondo E

更新日期：2013-08-01 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：: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：:Nanotechnology has enabled significant advances in the areas of cancer diagnosis and therapy. The field of drug delivery is a sterling example, with nanoparticles being increasingly used for generating therapeutic formulations of poorly water-soluble, yet potent anticancer drugs. Whereas a number of nanoparticle-drug ...

journal_title：Molecular cancer therapeutics

authors： Bisht S,Feldmann G,Koorstra JB,Mullendore M,Alvarez H,Karikari C,Rudek MA,Lee CK,Maitra A,Maitra A

更新日期：2008-12-01 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：:Most non-small cell lung cancer (NSCLC) tumors with activating mutations of the epidermal growth factor receptor (EGFR) are initially responsive to first-generation, reversible EGFR tyrosine kinase inhibitors (TKI) such as gefitinib, but they subsequently develop resistance to these drugs through either acquisition of...

journal_title：Molecular cancer therapeutics

authors： Takezawa K,Okamoto I,Tanizaki J,Kuwata K,Yamaguchi H,Fukuoka M,Nishio K,Nakagawa K

更新日期：2010-06-01 00:00:00

abstract：:G-protein-coupled receptors (GPCR) activate the epidermal growth factor receptor (EGFR) and mediate EGFR-independent signaling pathways to promote the growth of a variety of cancers, including head and neck squamous cell carcinoma (HNSCC). Identification of the common signaling mechanisms involved in GPCR-induced EGFR...

journal_title：Molecular cancer therapeutics

authors： Bhola NE,Freilino ML,Joyce SC,Sen M,Thomas SM,Sahu A,Cassell A,Chen CS,Grandis JR

更新日期：2012-06-01 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：:Despite frequent overexpression of numerous growth factor receptors by pancreatic ductal adenocarcinomas (PDAC), such as EGFR, therapeutic antibodies have not proven effective. Desmoplasia, hypovascularity, and hypoperfusion create a functional drug delivery barrier that contributes to treatment resistance. Drug combi...

journal_title：Molecular cancer therapeutics

authors： Wang J,Chan DKW,Sen A,Ma WW,Straubinger RM

更新日期：2019-11-01 00:00:00

abstract：:In the present work, we have investigated the antitumor activity of 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol (NBDHEX) on aggressive small cell lung cancer. NBDHEX not only is cytotoxic toward the parental small cell lung cancer H69 cell line (LC(50) of 2.3 +/- 0.6 micromol/L) but also overcomes the multidrug re...

journal_title：Molecular cancer therapeutics

authors： Filomeni G,Turella P,Dupuis ML,Forini O,Ciriolo MR,Cianfriglia M,Pezzola S,Federici G,Caccuri AM

更新日期：2008-02-01 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：:Deregulation of the cell cycle has long been recognized as an essential driver of tumorigenesis, and agents that selectively target key cell cycle components continue to hold promise as potential therapeutics. We have developed AZD5438, a 4-(1-isopropyl-2-methylimidazol-5-yl)-2-(4-methylsulphonylanilino) pyrimidine, a...

journal_title：Molecular cancer therapeutics

authors： Byth KF,Thomas A,Hughes G,Forder C,McGregor A,Geh C,Oakes S,Green C,Walker M,Newcombe N,Green S,Growcott J,Barker A,Wilkinson RW

更新日期：2009-07-01 00:00:00

abstract：:There is an urgent need for the development of novel therapies to treat pancreatic cancer, which is among the most lethal of all cancers. KRAS-activating mutations, which are found in more than 90% of pancreatic adenocarcinomas, drive tumor dependency on the Ras/MAPK and Akt signaling pathways. Radiation is currently ...

journal_title：Molecular cancer therapeutics

authors： Williams TM,Flecha AR,Keller P,Ram A,Karnak D,Galbán S,Galbán CJ,Ross BD,Lawrence TS,Rehemtulla A,Sebolt-Leopold J

更新日期：2012-05-01 00:00:00

abstract：:Normal tissue toxicity markedly reduces the therapeutic index of genotoxic anticancer agents, including ionizing radiation. Countermeasures against tissue damage caused by radiation are limited by their potential to also protect malignant cells and tissues. Here, we tested a panel of signal transduction modifiers for ...

journal_title：Molecular cancer therapeutics

authors： Alexeev V,Lash E,Aguillard A,Corsini L,Bitterman A,Ward K,Dicker AP,Linnenbach A,Rodeck U

更新日期：2014-12-01 00:00:00

abstract：:Increasing literature suggests that cell adhesion molecule alpha4beta1 integrin plays a pivotal role in autoimmune diseases and cancer development. Noninvasive visualization of alpha4beta1 integrin in vivo will facilitate the understanding of its involvement in disease progression and development of targeted therapies...

journal_title：Molecular cancer therapeutics

authors： Peng L,Liu R,Andrei M,Xiao W,Lam KS

更新日期：2008-02-01 00:00:00

abstract：:17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) converts estrone (E1) into estradiol (E2) and is expressed in many steroidogenic tissues and breast cancer cell lines. Because the potent estrogen E2 stimulates the growth and development of hormone-dependent diseases, inhibition of the final step of E2 synthesis is c...

journal_title：Molecular cancer therapeutics

authors： Ayan D,Maltais R,Roy J,Poirier D

更新日期：2012-10-01 00:00:00