ANG4043, a novel brain-penetrant peptide-mAb conjugate, is efficacious against HER2-positive intracranial tumors in mice.

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：: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：:The standard treatment for most advanced cancers is multidrug therapy. Unfortunately, combinations in the clinic often do not perform as predicted. Therefore, to complement identifying rational drug combinations based on biological assumptions, we hypothesized that a functional screen of drug combinations, without lim...

journal_title：Molecular cancer therapeutics

authors： Zinner RG,Barrett BL,Popova E,Damien P,Volgin AY,Gelovani JG,Lotan R,Tran HT,Pisano C,Mills GB,Mao L,Hong WK,Lippman SM,Miller JH

更新日期：2009-03-01 00:00:00

abstract：:Sulfonylurea receptor 1 (SUR1) is the regulatory subunit of ATP-sensitive potassium channels (KATP channels) and the receptor of antidiabetic drugs, such as glibenclamide, which induce insulin secretion in pancreatic β cells. However, the expression and role of SUR1 in cancer are unknown. In this study, we found that ...

journal_title：Molecular cancer therapeutics

authors： Xu K,Sun G,Li M,Chen H,Zhang Z,Qian X,Li P,Xu L,Huang W,Wang X

更新日期：2019-11-01 00:00:00

abstract：:The phosphatidylinositol 3-kinase (PI3K)/Akt pathway is known to be activated by radiation. The mammalian target of rapamycin (mTOR) is downstream of Akt, and we investigated the effects of radiation on Akt/mTOR signaling in breast cancer cell models. RAD001 (everolimus), a potent derivative of the mTOR inhibitor rapa...

journal_title：Molecular cancer therapeutics

authors： Albert JM,Kim KW,Cao C,Lu B

更新日期：2006-05-01 00:00:00

abstract：:The PI3K-AKT pathway has pleiotropic effects and its inhibition has long been of interest in the management of prostate cancer, where a compensatory increase in PI3K signaling has been reported following androgen receptor (AR) blockade. Prostate cancer cells can also bypass AR blockade through induction of other hormo...

journal_title：Molecular cancer therapeutics

authors： Adelaiye-Ogala R,Gryder BE,Nguyen YTM,Alilin AN,Grayson AR,Bajwa W,Jansson KH,Beshiri ML,Agarwal S,Rodriguez-Nieves JA,Capaldo B,Kelly K,VanderWeele DJ

更新日期：2020-07-01 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：:Many genes, with products involved in the protection of cells against carcinogens, oxidants, and other toxic chemicals, are under the transcriptional control of a simple DNA regulatory element [i.e., the antioxidant response element (ARE)]. One or more functional AREs have been confirmed or are believed to exist in th...

journal_title：Molecular cancer therapeutics

authors： Zhang Y,Gordon GB

更新日期：2004-07-01 00:00:00

abstract：:Enhancer of zester homolog 2 (EZH2), a histone lysine methyltransferase and the catalytic component of polycomb repressive complex 2, has been extensively investigated as a chromatin regulator and a transcriptional suppressor by methylating H3 at lysine 27 (H3K27). EZH2 is upregulated or mutated in most cancers, and i...

journal_title：Molecular cancer therapeutics

authors： Li Q,Liu KY,Liu Q,Wang G,Jiang W,Meng Q,Yi Y,Yang Y,Wang R,Zhu S,Li C,Wu L,Zhao D,Yan L,Zhang L,Kim JS,Zu X,Kozielski AJ,Qian W,Chang JC,Patnaik A,Chen K,Cao Q

更新日期：2020-10-01 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：:R-roscovitine (seliciclib, CYC202) is a cyclin-dependent kinase inhibitor currently in phase II clinical trials in patients with cancer. Here, we describe its mouse metabolism and pharmacokinetics as well as the identification of the principal metabolites in hepatic microsomes, plasma, and urine. Following microsomal ...

journal_title：Molecular cancer therapeutics

authors： Nutley BP,Raynaud FI,Wilson SC,Fischer PM,Hayes A,Goddard PM,McClue SJ,Jarman M,Lane DP,Workman P

更新日期：2005-01-01 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：: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：: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：:Overexpression of Notch receptors and ligands has been associated with various cancers and developmental disorders, making Notch a potential therapeutic target. Here, we report characterization of Notch1 monoclonal antibodies (mAb) with therapeutic potential. The mAbs generated against epidermal growth factor (EGF) re...

journal_title：Molecular cancer therapeutics

authors： Sharma A,Paranjape AN,Rangarajan A,Dighe RR

更新日期：2012-01-01 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：:Streptozotocin-based chemotherapy is the first-line chemotherapy recommended for advanced pancreatic neuroendocrine tumors (pNETs), whereas targeted therapies, including mTOR inhibitors, are available in second-line treatment. Unfortunately, objective response rates to both treatments are limited. Because mTOR pathway...

journal_title：Molecular cancer therapeutics

authors： Bollard J,Patte C,Massoma P,Goddard I,Gadot N,Benslama N,Hervieu V,Ferraro-Peyret C,Cordier-Bussat M,Scoazec JY,Roche C,Walter T,Vercherat C

更新日期：2018-01-01 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：: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：: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：:Targeting of epigenetic regulators as the chromatin remodeler SWI/SNF is proving to be a promising therapeutic strategy for individualized treatment of cancer patients. Here, we tested whether targeting one of the two mutually exclusive subdomains of the SWI/SNF complex BRM/SMARCA2 can sensitize specifically non-small...

journal_title：Molecular cancer therapeutics

authors： Zernickel E,Sak A,Riaz A,Klein D,Groneberg M,Stuschke M

更新日期：2019-03-01 00:00:00

abstract：:Prostate-specific membrane antigen (PSMA) is a protein up-regulated in the vast majority of prostate cancers. Antibodies to PSMA have proved highly specific for prostate cancer cells, and the therapeutic potential of such antibodies is currently being assessed in clinical trials. We have previously shown that PSMA at ...

journal_title：Molecular cancer therapeutics

authors： Christiansen JJ,Weimbs T,Bander N,Rajasekaran AK

更新日期：2006-10-01 00:00:00

abstract：:The humanized anti-HER2 monoclonal antibody (mAb) trastuzumab (Herceptin; Genentech) effectively inhibits human epidermal growth factor receptor 2 (HER2)-positive breast tumors. However, many patients responding to treatment often develop resistance. Cross-talk between type I insulin-like growth factor receptor (IGF-I...

journal_title：Molecular cancer therapeutics

authors： Chen C,Zhang Y,Zhang Y,Li J,Tsao SW,Zhang MY

更新日期：2014-01-01 00:00:00

abstract：:Cyclin-dependent kinases 4 and 6 (CDK4/6) have emerged as important therapeutic targets. Pharmacologic inhibitors of these kinases function to inhibit cell-cycle progression and exert other important effects on the tumor and host environment. Because of their impact on the cell cycle, CDK4/6 inhibitors (CDK4/6i) have ...

journal_title：Molecular cancer therapeutics

authors： Roberts PJ,Kumarasamy V,Witkiewicz AK,Knudsen ES

更新日期：2020-08-01 00:00:00

abstract：:Conditionally replicating adenoviruses (CRAd) can replicate specifically in cancer cells and lyse them. The CRAds were widely used in the preclinical and clinical studies of cancer therapy. We hypothesize that more precisely regulated replication of CRAds may further improve the vector safety profile and enhance its a...

journal_title：Molecular cancer therapeutics

authors： Wang X,Su C,Cao H,Li K,Chen J,Jiang L,Zhang Q,Wu X,Jia X,Liu Y,Wang W,Liu X,Wu M,Qian Q

更新日期：2008-06-01 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：: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：:Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) selectively kills tumor cells. However, its short half-life, poor delivery, and TRAIL-resistant tumor cells have diminished its clinical efficacy. In this study, we explored whether novel delivery methods will represent new and effective ways to treat gli...

journal_title：Molecular cancer therapeutics

authors： Hingtgen S,Ren X,Terwilliger E,Classon M,Weissleder R,Shah K

更新日期：2008-11-01 00:00:00

abstract：:The serine protease granzyme B (GrB; 25 kDa) is capable of inducing apoptosis through both caspase-dependent and caspase-independent mechanisms. We designed a novel vascular-targeting fusion construct designated as GrB/vascular endothelial growth factor (VEGF)121, which is composed of a non-heparin-binding isoform of ...

journal_title：Molecular cancer therapeutics

authors： Liu Y,Cheung LH,Thorpe P,Rosenblum MG

更新日期：2003-10-01 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