Effective Concentration of a Multikinase Inhibitor within Bone Marrow Correlates with In Vitro Cell Killing in Therapy-Resistant Chronic Myeloid Leukemia.

abstract：:Alpha-emitters can be pharmacologically delivered for irradiation of single cancer cells, but cellular lethality could be further enhanced by targeting alpha-emitters directly to the nucleus. PARP-1 is a druggable protein in the nucleus that is overexpressed in neuroblastoma compared with normal tissues and is associa...

journal_title：Molecular cancer therapeutics

authors： Makvandi M,Lee H,Puentes LN,Reilly SW,Rathi KS,Weng CC,Chan HS,Hou C,Raman P,Martinez D,Xu K,Carlin SD,Greenberg RA,Pawel BR,Mach RH,Maris JM,Pryma DA

更新日期：2019-07-01 00:00:00

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：:Multiple roles within mitosis have been assigned to Polo-like kinase 1 (Plk1), making it an attractive candidate for mitotic targeting of cancer cells. We have employed chimeric antisense oligonucleotides to investigate the molecular alterations after targeted interference with Plk1 in RKO human colon adenocarcinoma a...

journal_title：Molecular cancer therapeutics

authors： Schmidt M,Hofmann HP,Sanders K,Sczakiel G,Beckers TL,Gekeler V

更新日期：2006-04-01 00:00:00

abstract：:Epidermal growth factor receptor (EGFR) vIII is a mutated EGFR that is frequently overexpressed in glioblastomas and implicated in response to receptor tyrosine kinase inhibitors. In this study, we investigate the effect of ZD6474 (ZACTIMA, vandetanib), a dual inhibitor for vascular endothelial growth factor receptor ...

journal_title：Molecular cancer therapeutics

authors： Yiin JJ,Hu B,Schornack PA,Sengar RS,Liu KW,Feng H,Lieberman FS,Chiou SH,Sarkaria JN,Wiener EC,Ma HI,Cheng SY

更新日期：2010-04-01 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal cancer due in part to a lack of highly robust cytotoxic or molecular-based therapies. Recent studies investigating ligand-mediated Wnt/β-catenin signaling have highlighted its importance in pancreatic cancer initiation and progression, as well as its potential...

journal_title：Molecular cancer therapeutics

authors： Arensman MD,Telesca D,Lay AR,Kershaw KM,Wu N,Donahue TR,Dawson DW

更新日期：2014-10-01 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：:Neuroblastoma is the most common extracranial solid malignancy in the pediatric population, accounting for over 9% of all cancer-related deaths in children. Autophagy is a cell self-protective mechanism that promotes tumor cell growth and survival, making it an attractive target for treating cancer. However, the role ...

journal_title：Molecular cancer therapeutics

authors： Dower CM,Bhat N,Gebru MT,Chen L,Wills CA,Miller BA,Wang HG

更新日期：2018-11-01 00:00:00

abstract：:Phospho-sulindac is a sulindac derivative with promising anticancer activity in lung cancer, but its limited metabolic stability presents a major challenge for systemic therapy. We reasoned that inhalation delivery of phospho-sulindac might overcome first-pass metabolism and produce high levels of intact drug in lung ...

journal_title：Molecular cancer therapeutics

authors： Cheng KW,Wong CC,Alston N,Mackenzie GG,Huang L,Ouyang N,Xie G,Wiedmann T,Rigas B

更新日期：2013-08-01 00:00:00

abstract：:Insulin-like growth factor-I receptor (IGF-IR) is an important mediator of tumor cell survival and shows prognostic significance in sarcoma. To explore potential therapeutic strategies for interrupting signaling through this pathway, we assessed the ability of cyclolignan picropodophyllin (PPP), a member of the cyclol...

journal_title：Molecular cancer therapeutics

authors： Duan Z,Choy E,Harmon D,Yang C,Ryu K,Schwab J,Mankin H,Hornicek FJ

更新日期：2009-08-01 00:00:00

abstract：:Notch signaling regulates cell-fate decisions during development and postnatal life. Little is known, however, about the role of Delta-like-4 (Dll4)-Notch signaling between cancer cells, or how this signaling affects cancer metastasis. We, therefore, assessed the role of Dll4-Notch signaling in cancer metastasis. We g...

journal_title：Molecular cancer therapeutics

authors： Kuramoto T,Goto H,Mitsuhashi A,Tabata S,Ogawa H,Uehara H,Saijo A,Kakiuchi S,Maekawa Y,Yasutomo K,Hanibuchi M,Akiyama S,Sone S,Nishioka Y

更新日期：2012-12-01 00:00:00

abstract：:Notch signaling is aberrantly activated in approximately one third of non-small cell lung cancers (NSCLC). We characterized the interaction between BMS-906024, a clinically relevant Notch gamma secretase inhibitor, and front-line chemotherapy in preclinical models of NSCLC. Chemosensitivity assays were performed on 14...

journal_title：Molecular cancer therapeutics

authors： Morgan KM,Fischer BS,Lee FY,Shah JJ,Bertino JR,Rosenfeld J,Singh A,Khiabanian H,Pine SR

更新日期：2017-12-01 00:00:00

abstract：:Invasion into deep myometrium and/or lymphovascular space is a well-known risk factor for endometrial cancer metastasis, resulting in poor prognosis. It is therefore clinically important to identify novel molecules that suppress tumor invasion. Reduced expression of the metastasis suppressor, kisspeptin (KISS1), and i...

journal_title：Molecular cancer therapeutics

authors： Kang HS,Baba T,Mandai M,Matsumura N,Hamanishi J,Kharma B,Kondoh E,Yoshioka Y,Oishi S,Fujii N,Murphy SK,Konishi I

更新日期：2011-04-01 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：:Breast cancer resistance to the antiestrogens tamoxifen (OHT) and fulvestrant is accompanied by alterations in both estrogen-dependent and estrogen-independent signaling pathways. Consequently, effective inhibition of both pathways may be necessary to block proliferation of antiestrogen-resistant breast cancer cells. ...

journal_title：Molecular cancer therapeutics

authors： Long X,Fan M,Bigsby RM,Nephew KP

更新日期：2008-07-01 00:00:00

abstract：:Replication protein A (RPA) is a single-strand DNA-binding protein with essential roles in DNA replication, recombination, and repair. It is necessary for the formation of the preincision complex that is required for proper incision of damaged DNA nucleotides during DNA repair. We have previously identified small mole...

journal_title：Molecular cancer therapeutics

authors： Neher TM,Bodenmiller D,Fitch RW,Jalal SI,Turchi JJ

更新日期：2011-10-01 00:00:00

abstract：:Breast cancer exhibits a propensity to metastasize to bone, resulting in debilitating skeletal complications associated with significant morbidity and poor prognosis. The cross-talk between metastatic cancer cells and bone is critical to the development and progression of bone metastases. We have shown the involvement...

journal_title：Molecular cancer therapeutics

authors： Previdi S,Abbadessa G,Dalò F,France DS,Broggini M

更新日期：2012-01-01 00:00:00

abstract：:Tumor cells are efficiently killed after incubation with alpha-emitter immunoconjugates targeting tumor-specific antigens. Therefore, application of alpha-emitter immunoconjugates is a promising therapeutic option for treatment of carcinomas that are characterized by dissemination of single tumor cells in the peritone...

journal_title：Molecular cancer therapeutics

authors： Seidl C,Port M,Gilbertz KP,Morgenstern A,Bruchertseifer F,Schwaiger M,Röper B,Senekowitsch-Schmidtke R,Abend M

更新日期：2007-08-01 00:00:00

abstract：:Soluble copolymers of camptothecin (CPT), based on poly[N-(2-hydroxypropyl) methacrylamide] (pHPMA), were obtained by conjugation through the degradable spacers -Gly-Phe-Leu-Gly- or -Gly-6-aminohexanoyl-Gly-. We investigated to what extent passive accumulation and retention of hydroxypropyl methacrylamide copolymer of...

journal_title：Molecular cancer therapeutics

authors： Zamai M,VandeVen M,Farao M,Gratton E,Ghiglieri A,Castelli MG,Fontana E,D'Argy R,Fiorino A,Pesenti E,Suarato A,Caiolfa VR

更新日期：2003-01-01 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：:TAS-121 is a novel orally active selective covalent inhibitor of the mutant EGFR. We performed preclinical characterization of TAS-121 and compared its efficacy and selectivity for common EGFR mutations (Ex19del and L858R), first- and second- generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) resistance mutation (T7...

journal_title：Molecular cancer therapeutics

authors： Ito K,Nishio M,Kato M,Murakami H,Aoyagi Y,Ohe Y,Okayama T,Hashimoto A,Ohsawa H,Tanaka G,Nonoshita K,Ito S,Matsuo K,Miyadera K

更新日期：2019-05-01 00:00:00

abstract：:Melanoma is a highly metastatic and deadly disease. An agent simultaneously targeting the COX-2, PI3K/Akt, and mitogen-activated protein kinase (MAPK) signaling pathways that are deregulated in up to 70% of sporadic melanomas might be an effective treatment, but no agent of this type exists. To develop a single drug i...

journal_title：Molecular cancer therapeutics

authors： Gowda R,Madhunapantula SV,Desai D,Amin S,Robertson GP

更新日期：2013-01-01 00:00:00

abstract：:We discovered a thalidomide analogue [5-hydroxy-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33)] with antiproliferative activity against nine cancer cell lines in vitro. Flow cytometric analyses showed that the compound caused G2-M arrest, which occurred mainly at the mitotic phase. In addition, immunofluores...

journal_title：Molecular cancer therapeutics

authors： Li PK,Pandit B,Sackett DL,Hu Z,Zink J,Zhi J,Freeman D,Robey RW,Werbovetz K,Lewis A,Li C

更新日期：2006-02-01 00:00:00

abstract：:The TGFβ-mediated alteration of the tumor microenvironment plays a crucial role in tumor progression. Mesothelial cells are the primary components of the tumor microenvironment for ovarian cancer cells; however, the exact role of TGFβ-stimulated mesothelial cells in ovarian cancer progression remains uncertain. In thi...

journal_title：Molecular cancer therapeutics

authors： Sugiyama K,Kajiyama H,Shibata K,Yuan H,Kikkawa F,Senga T

更新日期：2014-08-01 00:00:00

abstract：:Genital human papillomavirus (HPV) infection is the primary cause of cervical cancer in women. Although the HPV recombinant L1 protein was recently licensed as an available vaccine, it has numerous shortcomings. New vaccination strategies should be considered. To enable the design of a prophylactic and therapeutic low...

journal_title：Molecular cancer therapeutics

authors： Bian T,Wang Y,Lu Z,Ye Z,Zhao L,Ren J,Zhang H,Ruan L,Tian H

更新日期：2008-05-01 00:00:00

abstract：:In the current study, we examined a panel of serially passaged glioblastoma xenografts, in the context of an intracranial tumor therapy response model, to identify associations between glioblastoma molecular characteristics and tumor sensitivity to the epidermal growth factor receptor (EGFR) kinase inhibitor erlotinib...

journal_title：Molecular cancer therapeutics

authors： Sarkaria JN,Yang L,Grogan PT,Kitange GJ,Carlson BL,Schroeder MA,Galanis E,Giannini C,Wu W,Dinca EB,James CD

更新日期：2007-03-01 00:00:00

abstract：:The epithelial-mesenchymal transition (EMT) is a process associated with the metastasis of solid tumors as well as with the acquisition of resistance to standard anticancer modalities. A major initiator of EMT in carcinoma cells is TGF-β, which has been shown to induce the expression of several transcription factors u...

journal_title：Molecular cancer therapeutics

authors： Larocca C,Cohen JR,Fernando RI,Huang B,Hamilton DH,Palena C

更新日期：2013-09-01 00:00:00

abstract：:Antioxidants, such as vitamin E, are being investigated for efficacy in prostate cancer prevention. In this study, we show that the antioxidant moiety of vitamin E, 2,2,5,7,8-pentamethyl-6-chromanol (PMCol), has antiandrogen activity in prostate carcinoma cells. In the presence of PMCol, the androgen-stimulated biphas...

journal_title：Molecular cancer therapeutics

authors： Thompson TA,Wilding G

更新日期：2003-08-01 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：:The anticancer actions of vitamin D and its hormonally active form, calcitriol, have been extensively documented in clinical and preclinical studies. However, the mechanisms underlying these actions have not been completely elucidated. Here, we examined the effect of dietary vitamin D and calcitriol on mouse breast tu...

journal_title：Molecular cancer therapeutics

authors： Jeong Y,Swami S,Krishnan AV,Williams JD,Martin S,Horst RL,Albertelli MA,Feldman BJ,Feldman D,Diehn M

更新日期：2015-08-01 00:00:00

abstract：:Antibody-drug conjugates (ADC) represent a promising therapeutic modality for managing cancer. Here, we report a novel humanized ADC that targets the tetraspanin-like protein TM4SF1. TM4SF1 is highly expressed on the plasma membranes of many human cancer cells and also on the endothelial cells lining tumor blood vesse...

journal_title：Molecular cancer therapeutics

authors： Visintin A,Knowlton K,Tyminski E,Lin CI,Zheng X,Marquette K,Jain S,Tchistiakova L,Li D,O'Donnell CJ,Maderna A,Cao X,Dunn R,Snyder WB,Abraham AK,Leal M,Shetty S,Barry A,Zawel L,Coyle AJ,Dvorak HF,Jaminet SC

更新日期：2015-08-01 00:00:00