Caspase-3-dependent mitotic checkpoint inactivation by the small-molecule inducers of mitotic slippage SU6656 and geraldol.

abstract：:Tumor resistance to antitubulin drugs resulting from P-glycoprotein (Pgp) drug-efflux activity, increased expression of the βIII tubulin isotype, and alterations in the drug-binding sites are major obstacles in cancer therapy. Consequently, novel antitubulin drugs that overcome these challenges are of substantial inte...

journal_title：Molecular cancer therapeutics

authors： Nguyen TL,Cera MR,Pinto A,Lo Presti L,Hamel E,Conti P,Gussio R,De Wulf P

更新日期：2012-05-01 00:00:00

abstract：:Epithelial ovarian cancer is characterized by a low recovery rate because the disease is typically diagnosed at an advanced stage, by which time most patients (80%) already exhibit disseminated neoplasia. The cytokine receptor CXCR4 has been implicated in the development of metastasis in various tumor types. Using a p...

journal_title：Molecular cancer therapeutics

authors： Figueras A,Alsina-Sanchís E,Lahiguera Á,Abreu M,Muinelo-Romay L,Moreno-Bueno G,Casanovas O,Graupera M,Matias-Guiu X,Vidal A,Villanueva A,Viñals F

更新日期：2018-02-01 00:00:00

abstract：:Hsp90 is widely overexpressed in cancer cells and believed to be essential for the maintenance of malignant phenotypes. Targeting Hsp90 by small molecules has shown promise in solid and hematologic malignancies, which likely involves degradation of client oncoproteins in a cell-type-specific manner. In this study, we ...

journal_title：Molecular cancer therapeutics

authors： He K,Zheng X,Zhang L,Yu J

更新日期：2013-11-01 00:00:00

abstract：:We have developed a near-infrared (NIR) probe that targets cells overexpressing the EGF receptor (EGFR) for imaging glioblastoma brain tumors in live subjects. A peptide specific for the EGFR was modified with various lengths of monodiscrete polyethylene glycol (PEG) units and a NIR Cy5.5 fluorescence dye. The lead co...

journal_title：Molecular cancer therapeutics

authors： Agnes RS,Broome AM,Wang J,Verma A,Lavik K,Basilion JP

更新日期：2012-10-01 00:00:00

abstract：:Aberrant DNA methylation patterns play an important role in the pathogenesis of hematologic malignancies. The DNA methyltransferase inhibitors azacytidine and decitabine have shown significant clinical benefits in the treatment of myelodysplastic syndrome (MDS), but their precise mode of action remains to be establish...

journal_title：Molecular cancer therapeutics

authors： Stresemann C,Bokelmann I,Mahlknecht U,Lyko F

更新日期：2008-09-01 00:00:00

abstract：:Curcumin (curcumin I), demethoxycurcumin (curcumin II), and bisdemethoxycurcumin (curcumin III) are the major forms of curcuminoids found in the turmeric powder, which exhibit anticancer, antioxidant, and anti-inflammatory activities. In this study, we evaluated the ability of purified curcuminoids to modulate the fun...

journal_title：Molecular cancer therapeutics

authors： Chearwae W,Shukla S,Limtrakul P,Ambudkar SV

更新日期：2006-08-01 00:00:00

abstract：:DNA repair mechanisms are crucial for cell survival. It increases the cancer cell's ability to resist DNA damage. FEN1 is involved in DNA replication and repair, specifically long-patch base excision repair. Although the gene function and post-translational modification of FEN1 are well studied, the regulatory mechani...

journal_title：Molecular cancer therapeutics

authors： Zhu H,Wu C,Wu T,Xia W,Ci S,He W,Zhang Y,Li L,Zhou S,Zhang J,Edick AM,Zhang A,Pan FY,Hu Z,He L,Guo Z

更新日期：2019-12-01 00:00:00

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：:Mutations in ERK signaling drive a significant percentage of malignancies. LY3009120, a pan-RAF and dimer inhibitor, has preclinical activity in RAS- and BRAF-mutated cell lines including BRAF-mutant melanoma resistant to BRAF inhibitors. This multicenter, open-label, phase I clinical trial (NCT02014116) consisted of ...

journal_title：Molecular cancer therapeutics

authors： Sullivan RJ,Hollebecque A,Flaherty KT,Shapiro GI,Rodon Ahnert J,Millward MJ,Zhang W,Gao L,Sykes A,Willard MD,Yu D,Schade AE,Crowe K,Flynn DL,Kaufman MD,Henry JR,Peng SB,Benhadji KA,Conti I,Gordon MS,Tiu RV,Hong

更新日期：2020-02-01 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：:We reported previously a significant increase in survival of nude rats harboring orthotopic A549 human non-small cell lung cancer tumors after treatment with a combination of exisulind (Sulindac Sulfone) and docetaxel (D. C. Chan, Clin. Cancer Res., 8: 904-912, 2002). The purpose of the current study was to determine ...

journal_title：Molecular cancer therapeutics

authors： Whitehead CM,Earle KA,Fetter J,Xu S,Hartman T,Chan DC,Zhao TL,Piazza G,Klein-Szanto AJ,Pamukcu R,Alila H,Bunn PA Jr,Thompson WJ

更新日期：2003-05-01 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

abstract：:Ovarian cancer is the leading cause of death from gynecologic cancer. Often, the disease has spread beyond the ovary to involve the peritoneal cavity and causes ascites. Whereas mammalian target of rapamycin (mTOR) functions to regulate protein translation, cell cycle progression, and metastasis, vascular endothelial ...

journal_title：Molecular cancer therapeutics

authors： Huynh H,Teo CC,Soo KC

更新日期：2007-11-01 00:00:00

abstract：:Acquired resistance severely hinders the application of small-molecule inhibitors. Our understanding of acquired resistance related to FGFRs is limited. Here, to explore the underlying mechanism of acquired resistance in FGFR-aberrant cancer cells, we generated cells resistant to multiple FGFR inhibitors (FGFRi) and i...

journal_title：Molecular cancer therapeutics

authors： Wang X,Ai J,Liu H,Peng X,Chen H,Chen Y,Su Y,Shen A,Huang X,Ding J,Geng M

更新日期：2019-03-01 00:00:00

abstract：:(18)F-Fluorodeoxyglucose ((18)F-FDG) is the most common molecular imaging agent in oncology, with a high sensitivity and specificity for detecting several cancers. Antibodies could enhance specificity; therefore, procedures were developed for radiolabeling a small ( approximately 1451 Da) hapten peptide with (68)Ga or...

journal_title：Molecular cancer therapeutics

authors： Schoffelen R,Sharkey RM,Goldenberg DM,Franssen G,McBride WJ,Rossi EA,Chang CH,Laverman P,Disselhorst JA,Eek A,van der Graaf WT,Oyen WJ,Boerman OC

更新日期：2010-04-01 00:00:00

abstract：:Etoposide (VP-16), a topoisomerase II inhibitor, is an effective anticancer drug currently used for the treatment of a wide range of cancers. Excision repair cross-complementary 1 (ERCC1) is a key protein involved in the process of nucleotide excision repair. High level of ERCC1 expression in cancers is associated wit...

journal_title：Molecular cancer therapeutics

authors： Tsai MS,Weng SH,Chen HJ,Chiu YF,Huang YC,Tseng SC,Kuo YH,Lin YW

更新日期：2012-03-01 00:00:00

abstract：:Androgen deprivation therapy and second-generation androgen receptor signaling inhibitors such as enzalutamide are standard treatments for advanced/metastatic prostate cancer. Unfortunately, most men develop resistance and relapse; signaling via insulin-like growth factor (IGF) has been implicated in castration-resist...

journal_title：Molecular cancer therapeutics

authors： Weyer-Czernilofsky U,Hofmann MH,Friedbichler K,Baumgartinger R,Adam PJ,Solca F,Kraut N,Nguyen HM,Corey E,Liu G,Sprenger CC,Plymate SR,Bogenrieder T

更新日期：2020-04-01 00:00:00

abstract：:Improved survival for patients with head and neck cancers (HNC) with recurrent and metastatic disease warrants that cancer therapy is specific, with protected delivery of the therapeutic agent to primary and metastatic cancer cells. A further objective should be that downregulation of the intracellular therapy target ...

journal_title：Molecular cancer therapeutics

authors： Unger GM,Kren BT,Korman VL,Kimbrough TG,Vogel RI,Ondrey FG,Trembley JH,Ahmed K

更新日期：2014-08-01 00:00:00

abstract：:Molecular profiling of markers involved in the activity of chemotherapeutic agents can shed light on the successes and failures of treatment in patients and can also provide a basis for individualization of therapy. Toward those ends, we have used reverse-phase protein lysate microarrays to evaluate expression of prot...

journal_title：Molecular cancer therapeutics

authors： Stevens EV,Nishizuka S,Antony S,Reimers M,Varma S,Young L,Munson PJ,Weinstein JN,Kohn EC,Pommier Y

更新日期：2008-01-01 00:00:00

abstract：:Human epidermal growth factor receptor-2 (HER2) and epidermal growth factor receptor (EGFR) heterodimerize to activate mitogenic signaling pathways. We have shown previously, using MCF7 subcloned cell lines with graded levels of HER2 expression, that responsiveness to trastuzumab and AG1478 (an anti-EGFR agent), varie...

journal_title：Molecular cancer therapeutics

authors： Emlet DR,Brown KA,Kociban DL,Pollice AA,Smith CA,Ong BB,Shackney SE

更新日期：2007-10-01 00:00:00

abstract：:Radiosensitization caused by the poly(ADP-ribose) polymerase (PARP) inhibitor 4-amino-1,8-naphthalimide (ANI) was investigated in 10 asynchronously growing rodent (V79, CHO-Xrs6, CHO-K1, PARP-1+/+ 3T3, and PARP-1-/- 3T3) or human (HeLa, MRC5VI, IMR90, M059J, and M059K) cell lines, either repair proficient or defective...

journal_title：Molecular cancer therapeutics

authors： Noël G,Godon C,Fernet M,Giocanti N,Mégnin-Chanet F,Favaudon V

更新日期：2006-03-01 00:00:00

abstract：:HA14-1 is a small molecular compound that was identified based on the structure of Bcl-2. HA14-1 interacts with Bcl-2 and inhibits the antiapoptotic effect of Bcl-2. We investigated the mechanism of HA14-1-induced apoptosis and found that HA14-1 induces translocation of Bax from cytosols to the mitochondria. Cells def...

journal_title：Molecular cancer therapeutics

authors： Chen J,Freeman A,Liu J,Dai Q,Lee RM

更新日期：2002-10-01 00:00:00

abstract：:Passive immunotherapy with monoclonal antibodies represents a cornerstone of human anticancer therapies, but has not been established in veterinary medicine yet. As the tumor-associated antigen EGFR (ErbB-1) is highly conserved between humans and dogs, and considering the effectiveness of the anti-EGFR antibody cetuxi...

journal_title：Molecular cancer therapeutics

authors： Singer J,Fazekas J,Wang W,Weichselbaumer M,Matz M,Mader A,Steinfellner W,Meitz S,Mechtcheriakova D,Sobanov Y,Willmann M,Stockner T,Spillner E,Kunert R,Jensen-Jarolim E

更新日期：2014-07-01 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：: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：: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：:Chronic myelogenous leukemia is characterized by the presence of the chimeric BCR-ABL gene, which is expressed as the constitutively active Bcr-Abl kinase. Although kinase activity is directly responsible for the clinical phenotype, current diagnostic and prognostic methods focus on a genetic classification system in ...

journal_title：Molecular cancer therapeutics

authors： Sylvester JE,Kron SJ

更新日期：2010-05-01 00:00:00

abstract：:The FGF receptors (FGFR) are tyrosine kinases that are constitutively activated in a subset of tumors by genetic alterations such as gene amplifications, point mutations, or chromosomal translocations/rearrangements. Recently, small-molecule inhibitors that can inhibit the FGFR family as well as the VEGF receptor (VEG...

journal_title：Molecular cancer therapeutics

authors： Nakanishi Y,Akiyama N,Tsukaguchi T,Fujii T,Sakata K,Sase H,Isobe T,Morikami K,Shindoh H,Mio T,Ebiike H,Taka N,Aoki Y,Ishii N

更新日期：2014-11-01 00:00:00

abstract：:Crizotinib (PF02341066) is a tyrosine kinase inhibitor of anaplastic lymphoma kinase (ALK) that has been shown to selectively inhibit growth of cancer cells that harbor the EML4-ALK fusion found in a subset of patients with non-small cell lung cancer (NSCLC). While in clinical trials, PF02341066 has shown a significan...

journal_title：Molecular cancer therapeutics

authors： Sun Y,Nowak KA,Zaorsky NG,Winchester CL,Dalal K,Giacalone NJ,Liu N,Werner-Wasik M,Wasik MA,Dicker AP,Lu B

更新日期：2013-05-01 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