MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo.

abstract：:While epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors improve the prognosis of patients with EGFR mutant lung cancer, the prognosis of patients with nonmutant EGFR lung cancer, especially those with metastases, is still extremely poor. We have assessed the therapeutic efficacy of E7080, an orally av...

journal_title：Molecular cancer therapeutics

authors： Ogino H,Hanibuchi M,Kakiuchi S,Trung VT,Goto H,Ikuta K,Yamada T,Uehara H,Tsuruoka A,Uenaka T,Wang W,Li Q,Takeuchi S,Yano S,Nishioka Y,Sone S

更新日期：2011-07-01 00:00:00

abstract：:The protein kinase family represents an enormous opportunity for drug development. However, the current limitation in structural diversity of kinase inhibitors has complicated efforts to identify effective treatments of diseases that involve protein kinase signaling pathways. We have identified a new structural class ...

journal_title：Molecular cancer therapeutics

authors： Hamdouchi C,Keyser H,Collins E,Jaramillo C,De Diego JE,Spencer CD,Dempsey JA,Anderson BD,Leggett T,Stamm NB,Schultz RM,Watkins SA,Cocke K,Lemke S,Burke TF,Beckmann RP,Dixon JT,Gurganus TM,Rankl NB,Houck KA,Zhang F

更新日期：2004-01-01 00:00:00

abstract：:For a subpopulation of acute myeloid leukemia (AML) patients, the constitutively activated tyrosine kinase, mutant FLT3, has emerged as a promising target for therapy. The development of drug resistance, however, is a growing concern for mutant FLT3 inhibitors, such as PKC412. Potential therapeutic benefit can arise f...

journal_title：Molecular cancer therapeutics

authors： Weisberg E,Choi HG,Barrett R,Zhou W,Zhang J,Ray A,Nelson EA,Jiang J,Moreno D,Stone R,Galinsky I,Fox E,Adamia S,Kung AL,Gray NS,Griffin JD

更新日期：2010-09-01 00:00:00

abstract：:Transforming growth factor (TGF)-β contributes to the malignant phenotype of glioblastoma by promoting invasiveness and angiogenesis and creating an immunosuppressive microenvironment. So far, TGF-β1 and TGF-β2 isoforms have been considered to act in a similar fashion without isoform-specific function in glioblastoma....

journal_title：Molecular cancer therapeutics

authors： Seystahl K,Papachristodoulou A,Burghardt I,Schneider H,Hasenbach K,Janicot M,Roth P,Weller M

更新日期：2017-06-01 00:00:00

abstract：:The covalent attachment of palmitate to specific proteins by the action of palmitoyl acyltransferases (PAT) plays critical roles in the biological activities of several oncoproteins. Two PAT activities are expressed by human cells: type 1 PATs that modify the farnesyl-dependent palmitoylation motif found in H- and N-R...

journal_title：Molecular cancer therapeutics

authors： Ducker CE,Griffel LK,Smith RA,Keller SN,Zhuang Y,Xia Z,Diller JD,Smith CD

更新日期：2006-07-01 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：:In 2017, an estimated 17,000 individuals were diagnosed with esophageal adenocarcinoma (EAC), and less than 20% will survive 5 years. Positron emission tomography avidity is indicative of high glucose utilization and is nearly universal in EAC. TXNIP blocks glucose uptake and exhibits proapoptotic functions. Higher ex...

journal_title：Molecular cancer therapeutics

authors： Feingold PL,Surman DR,Brown K,Xu Y,McDuffie LA,Shukla V,Reardon ES,Crooks DR,Trepel JB,Lee S,Lee MJ,Gao S,Xi S,McLoughlin KC,Diggs LP,Beer DG,Nancarrow DJ,Neckers LM,Davis JL,Hoang CD,Hernandez JM,Schrump DS,R

更新日期：2018-09-01 00:00:00

abstract：:Multiple myeloma is a slowly proliferating B-cell malignancy that accumulates apoptosis-resistant and replication-quiescent cell populations, posing a challenge for current chemotherapeutics that target rapidly replicating cells. Multiple myeloma remains an incurable disease in need of new therapeutic approaches. The ...

journal_title：Molecular cancer therapeutics

authors： Ghias K,Ma C,Gandhi V,Platanias LC,Krett NL,Rosen ST

更新日期：2005-04-01 00:00:00

abstract：:Repurposing cationic amphiphilic drugs (CAD) for cancer treatment is emerging as an attractive means to enhance the efficacy of chemotherapy. Many commonly used CADs, including several cation amphiphilic antihistamines and antidepressants, induce cancer-specific, lysosome-dependent cell death and sensitize cancer cell...

journal_title：Molecular cancer therapeutics

authors： Anand A,Liu B,Dicroce Giacobini J,Maeda K,Rohde M,Jäättelä M

更新日期：2019-09-01 00:00:00

abstract：:Cadmium (Cd) is an ubiquitous environmental carcinogen. Membrane phospholipids as well as fatty acid profile of membrane phospholipids are known to be altered in tumorigenicity and malignancy. Synthesis of cellular phosphatidylcholine (PC) has been used as a marker for membrane proliferation in the neoplastic mammary ...

journal_title：Molecular cancer therapeutics

authors： Sinha Roy S,Mukherjee S,Mukhopadhyay S,Das SK

更新日期：2004-02-01 00:00:00

abstract：:AMAD, an emodin azide methyl anthraquinone derivative, was extracted from the nature giant knotweed rhizome of traditional Chinese herbs. Here, we investigated the anticancer activities and signaling pathways implicated in AMAD-induced apoptosis in human breast cancer cell lines MDA-MB-453 and human lung adenocarcinom...

journal_title：Molecular cancer therapeutics

authors： Yan Y,Su X,Liang Y,Zhang J,Shi C,Lu Y,Gu L,Fu L

更新日期：2008-06-01 00:00:00

abstract：:The breast-specific antigen alpha-lactalbumin is expressed in >60% of breast cancer tissues. To evaluate the effect of gene therapy for breast cancer by controlling adenovirus replication with human alpha-lactalbumin promoter, we investigated the activity of a 762-bp human alpha-lactalbumin promoter. Alpha-lactalbumin...

journal_title：Molecular cancer therapeutics

authors： Li X,Zhang J,Gao H,Vieth E,Bae KH,Zhang YP,Lee SJ,Raikwar S,Gardner TA,Hutchins GD,VanderPutten D,Kao C,Jeng MH

更新日期：2005-12-01 00:00:00

abstract：:eIF4E is the key regulator of protein translation and critical for translation. The oncogenic potential of tumorigenesis, which is highly contingent on cap-dependent eIF4E, also arises from the critical role in the nuclear export and cytosolic translation of oncogenic transcripts. Inhibition of Exportin1 (XPO1), which...

journal_title：Molecular cancer therapeutics

authors： Li S,Fu J,Lu C,Mapara MY,Raza S,Hengst U,Lentzsch S

更新日期：2016-04-01 00:00:00

abstract：:Current treatments for castration resistant prostate cancer (CRPC) largely fall into two classes: androgen receptor (AR)-targeted therapies such as the next-generation antiandrogen therapies (NGAT), enzalutamide and abiraterone, and taxanes such as docetaxel and cabazitaxel. Despite improvements in outcomes, patients ...

journal_title：Molecular cancer therapeutics

authors： Lombard AP,Liu L,Cucchiara V,Liu C,Armstrong CM,Zhao R,Yang JC,Lou W,Evans CP,Gao AC

更新日期：2018-10-01 00:00:00

abstract：:The entry of calcium into the mammary epithelial cell from the maternal plasma (i.e., calcium influx mechanisms) during lactation is poorly understood. As alterations in calcium channels and pumps are a key feature of some cancers, including breast cancer, understanding these calcium influx pathways may have significa...

journal_title：Molecular cancer therapeutics

authors： McAndrew D,Grice DM,Peters AA,Davis FM,Stewart T,Rice M,Smart CE,Brown MA,Kenny PA,Roberts-Thomson SJ,Monteith GR

更新日期：2011-03-01 00:00:00

abstract：:Although proteasome inhibitors such as bortezomib had significant therapeutic effects in multiple myeloma and mantel cell lymphoma, they exhibited minimal clinical activity as a monotherapy for solid tumors, including colorectal cancer. We found in this study that proteasome inhibition induced a remarkable nuclear exp...

journal_title：Molecular cancer therapeutics

authors： Wu T,Chen W,Zhong Y,Hou X,Fang S,Liu CY,Wang G,Yu T,Huang YY,Ouyang X,Li HQ,Cui L,Yang Y

更新日期：2017-04-01 00:00:00

abstract：:Vascular endothelial growth factor (VEGF)-induced endothelial cell migration is an important component of tumor angiogenesis. Rho and Rho-associated kinase (ROCK) are key regulators of focal adhesion, stress fiber formation, and thus cell motility. Inhibitors of this pathway have been shown to inhibit endothelial cell...

journal_title：Molecular cancer therapeutics

authors： Yin L,Morishige K,Takahashi T,Hashimoto K,Ogata S,Tsutsumi S,Takata K,Ohta T,Kawagoe J,Takahashi K,Kurachi H

更新日期：2007-05-01 00:00:00

abstract：:Previous studies from our laboratory have identified several endothelial cell-associated marker genes implicated in human melanoma metastasis via tumor vasculogenic mimicry. In this study, we used dual model systems composed of melanoma cell lines and clinical melanoma samples to validate the importance of insulin-lik...

journal_title：Molecular cancer therapeutics

authors： Xi Y,Nakajima G,Hamil T,Fodstad O,Riker A,Ju J

更新日期：2006-12-01 00:00:00

abstract：:There is considerable interest in the clinical development of inhibitors of mTOR complexes mTORC1 and 2. Because mTORC1 and its downstream mRNA translation effectors may protect against genotoxic DNA damage, we investigated the inhibition of mTORC1 and mTORC1/2 in the ability to reverse platinum resistance in tissue c...

journal_title：Molecular cancer therapeutics

authors： Musa F,Alard A,David-West G,Curtin JP,Blank SV,Schneider RJ

更新日期：2016-07-01 00:00:00

abstract：:Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and for maintaining the spindle assembly checkpoint until all chromosomes are properly attached. Mps1 is expressed at high levels during mitosis and is abundantly expressed in cancer cells. Disr...

journal_title：Molecular cancer therapeutics

authors： Tardif KD,Rogers A,Cassiano J,Roth BL,Cimbora DM,McKinnon R,Peterson A,Douce TB,Robinson R,Dorweiler I,Davis T,Hess MA,Ostanin K,Papac DI,Baichwal V,McAlexander I,Willardsen JA,Saunders M,Christophe H,Kumar DV,Wet

更新日期：2011-12-01 00:00:00

abstract：:Proteasome inhibitors are potent inducers of apoptosis in isolated lymphocytes from patients with chronic lymphocytic leukemia (CLL). However, the reversible proteasome inhibitor bortezomib (PS-341; Velcade) did not display substantial antitumor activity in CLL patients. Here, we compared the effects of bortezomib and...

journal_title：Molecular cancer therapeutics

authors： Ruiz S,Krupnik Y,Keating M,Chandra J,Palladino M,McConkey D

更新日期：2006-07-01 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：:Multiple myeloma remains incurable and the majority of patients die within 5 years of diagnosis. Reolysin, the infusible form of human reovirus (RV), is a novel viral oncolytic therapy associated with antitumor activity likely resulting from direct oncolysis and a virus-mediated antitumor immune response. Results from...

journal_title：Molecular cancer therapeutics

authors： Stiff A,Caserta E,Sborov DW,Nuovo GJ,Mo X,Schlotter SY,Canella A,Smith E,Badway J,Old M,Jaime-Ramirez AC,Yan P,Benson DM,Byrd JC,Baiocchi R,Kaur B,Hofmeister CC,Pichiorri F

更新日期：2016-05-01 00:00:00

abstract：:Checkpoint kinase 1 (ChK1) is a serine/threonine kinase that functions as a central mediator of the intra-S and G2-M cell-cycle checkpoints. Following DNA damage or replication stress, ChK1-mediated phosphorylation of downstream effectors delays cell-cycle progression so that the damaged genome can be repaired. As a t...

journal_title：Molecular cancer therapeutics

authors： Blackwood E,Epler J,Yen I,Flagella M,O'Brien T,Evangelista M,Schmidt S,Xiao Y,Choi J,Kowanetz K,Ramiscal J,Wong K,Jakubiak D,Yee S,Cain G,Gazzard L,Williams K,Halladay J,Jackson PK,Malek S

更新日期：2013-10-01 00:00:00

abstract：:Histone deacetylase inhibitors represent a promising new class of anticancer agents. In the current investigation, we examined the activity of PXD101, a potent histone deacetylase inhibitor, used alone or in combination with clinically relevant chemotherapeutics (docetaxel, paclitaxel, and carboplatin), in preclinical...

journal_title：Molecular cancer therapeutics

authors： Qian X,LaRochelle WJ,Ara G,Wu F,Petersen KD,Thougaard A,Sehested M,Lichenstein HS,Jeffers M

更新日期：2006-08-01 00:00:00

abstract：:Soft-tissue sarcomas (STS) represent a heterogeneous group of rare, malignant tumors of mesenchymal origin. Reliable in vivo sarcoma research models are scarce. We aimed to establish and characterize histologically and molecularly stable patient-derived xenograft (PDX) models from a broad variety of STS subtypes. A to...

journal_title：Molecular cancer therapeutics

authors： Cornillie J,Wozniak A,Li H,Wang Y,Boeckx B,Gebreyohannes YK,Wellens J,Vanleeuw U,Hompes D,Stas M,Sinnaeve F,Wafa H,Lambrechts D,Debiec-Rychter M,Sciot R,Schöffski P

更新日期：2019-06-01 00:00:00

abstract：:The emergence of drug resistance is often an inevitable obstacle that limits the long-term effectiveness of clinical cancer chemotherapeutics. Although various forms of cancer cell-intrinsic mechanisms of drug resistance have been experimentally revealed, the role and the underlying mechanism of tumor microenvironment...

journal_title：Molecular cancer therapeutics

authors： Zheng Y,Bao J,Zhao Q,Zhou T,Sun X

更新日期：2018-04-01 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：:Disruption of Cyclin-Dependent Kinase 12 (CDK12) is known to lead to defects in DNA repair and sensitivity to platinum salts and PARP1/2 inhibitors. However, CDK12 has also been proposed as an oncogene in breast cancer. We therefore aimed to assess the frequency and distribution of CDK12 protein expression by IHC in i...

journal_title：Molecular cancer therapeutics

authors： Naidoo K,Wai PT,Maguire SL,Daley F,Haider S,Kriplani D,Campbell J,Mirza H,Grigoriadis A,Tutt A,Moseley PM,Abdel-Fatah TMA,Chan SYT,Madhusudan S,Rhaka EA,Ellis IO,Lord CJ,Yuan Y,Green AR,Natrajan R

更新日期：2018-01-01 00:00:00

abstract：:Staphylococcal nuclease domain-containing protein 1 (SND1) is a multifunctional oncoprotein overexpressed in breast cancer. Binding of metadherin (MTDH) to SND1 results in the stabilization of SND1 and is important in the initiation and progression of breast cancer. Disruption of such interaction is a potential therap...

journal_title：Molecular cancer therapeutics

authors： Li P,He Y,Chen T,Choy KY,Chow TS,Wong ILK,Yang X,Sun W,Su X,Chan TH,Chow LMC

更新日期：2021-01-01 00:00:00