z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo.

abstract：:Genotoxic stress such as ionizing radiation halts entry into mitosis by activation of the G(2) DNA damage checkpoint. The CHK1 inhibitor 7-hydroxystaurosporine (UCN-01) can bypass the checkpoint and induce unscheduled mitosis in irradiated cells. Precisely, how cells behave following checkpoint abrogation remains to b...

journal_title：Molecular cancer therapeutics

authors： On KF,Chen Y,Ma HT,Chow JP,Poon RY

更新日期：2011-05-01 00:00:00

abstract：:Hodgkin-Reed/Sternberg (HRS) cells of classical Hodgkin lymphoma show aberrant expression and activation of several receptor tyrosine kinases (RTK) in the majority of cases. Therefore, we tested whether tyrosine kinase inhibitors (TKI) already in clinical use or late stages of clinical trials have antiproliferative ef...

journal_title：Molecular cancer therapeutics

authors： Holz MS,Janning A,Renné C,Gattenlöhner S,Spieker T,Bräuninger A

更新日期：2013-02-01 00:00:00

abstract：:Metastasis is the primary determinant of death in patients with diverse solid tumors and MDA-9/Syntenin (SDCBP), a pro-metastatic and pro-angiogenic gene, contributes to this process. Recently, we documented that by physically interacting with IGF-1R, MDA-9/Syntenin activates STAT3 and regulates prostate cancer pathog...

journal_title：Molecular cancer therapeutics

authors： Das SK,Kegelman TP,Pradhan AK,Shen XN,Bhoopathi P,Talukdar S,Maji S,Sarkar D,Emdad L,Fisher PB

更新日期：2019-11-01 00:00:00

abstract：:The increasing characterization of childhood acute lymphoblastic leukemia (ALL) has led to the identification of multiple molecular targets but has yet to translate into more effective targeted therapies, particularly for high-risk, relapsed T-cell ALL. Searching for master regulators controlling multiple signaling pa...

journal_title：Molecular cancer therapeutics

authors： Ding J,Fishel ML,Reed AM,McAdams E,Czader MB,Cardoso AA,Kelley MR

更新日期：2017-07-01 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：:Overexpression or hyperactivation of MDM2 contributes to functional inactivation of wild-type p53 in nearly 50% of tumors. Inhibition of p53 by MDM2 depends on binding between an NH(2)-terminal (residues 16-28) p53 alpha-helical peptide and a hydrophobic pocket on MDM2, presenting an attractive target for development ...

journal_title：Molecular cancer therapeutics

authors： Chen L,Yin H,Farooqi B,Sebti S,Hamilton AD,Chen J

更新日期：2005-06-01 00:00:00

abstract：:B-Raf is an important mediator of cell proliferation and survival signals transduced via the Ras-Raf-MEK-ERK cascade. BRAF mutations have been detected in several tumors, including papillary thyroid carcinoma, but the precise role of B-Raf as a therapeutic target for thyroid carcinoma is still under investigation. We ...

journal_title：Molecular cancer therapeutics

authors： Mitsiades CS,Negri J,McMullan C,McMillin DW,Sozopoulos E,Fanourakis G,Voutsinas G,Tseleni-Balafouta S,Poulaki V,Batt D,Mitsiades N

更新日期：2007-03-01 00:00:00

abstract：:A quaternary ammonium-based drug-linker has been developed to expand the scope of antibody-drug conjugate (ADC) payloads to include tertiary amines, a functional group commonly present in biologically active compounds. The linker strategy was exemplified with a β-glucuronidase-cleavable auristatin E construct. The dru...

journal_title：Molecular cancer therapeutics

authors： Burke PJ,Hamilton JZ,Pires TA,Setter JR,Hunter JH,Cochran JH,Waight AB,Gordon KA,Toki BE,Emmerton KK,Zeng W,Stone IJ,Senter PD,Lyon RP,Jeffrey SC

更新日期：2016-05-01 00:00:00

abstract：:p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is...

journal_title：Molecular cancer therapeutics

authors： Canon J,Osgood T,Olson SH,Saiki AY,Robertson R,Yu D,Eksterowicz J,Ye Q,Jin L,Chen A,Zhou J,Cordover D,Kaufman S,Kendall R,Oliner JD,Coxon A,Radinsky R

更新日期：2015-03-01 00:00:00

abstract：:Integrin-linked kinase (ILK) was assesed as a therapeutic target in glioblastoma xenograft models through multiple endpoints including treatment related changes in the tumor microenvironment. Glioblastoma cell lines were tested in vitro for sensitivity toward the small-molecule inhibitors QLT0254 and QLT0267. Cell via...

journal_title：Molecular cancer therapeutics

authors： Edwards LA,Woo J,Huxham LA,Verreault M,Dragowska WH,Chiu G,Rajput A,Kyle AH,Kalra J,Yapp D,Yan H,Minchinton AI,Huntsman D,Daynard T,Waterhouse DN,Thiessen B,Dedhar S,Bally MB

更新日期：2008-01-01 00:00:00

abstract：:The challenge of developing effective pharmacodynamic biomarkers for preclinical and clinical testing of FGFR signaling inhibition is significant. Assays that rely on the measurement of phospho-protein epitopes can be limited by the availability of effective antibody detection reagents. Transcript profiling enables ac...

journal_title：Molecular cancer therapeutics

authors： Delpuech O,Rooney C,Mooney L,Baker D,Shaw R,Dymond M,Wang D,Zhang P,Cross S,Veldman-Jones M,Wilson J,Davies BR,Dry JR,Kilgour E,Smith PD

更新日期：2016-11-01 00:00:00

abstract：:Targeting inhibitor of apoptosis proteins (IAP) with second mitochondria-derived activator of caspase (SMAC) mimetics may promote cancer cell death. We tested whether cIAP1 predicts poor prognosis in head and neck squamous cell carcinoma (HNSCC) and whether a novel Smac-mimetic, LCL161, could radiosensitize human papi...

journal_title：Molecular cancer therapeutics

authors： Yang L,Kumar B,Shen C,Zhao S,Blakaj D,Li T,Romito M,Teknos TN,Williams TM

更新日期：2019-06-01 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：:Interference with endothelial cell metabolism is a promising, yet unexploited strategy for angiogenesis inhibition. We reported that the glucose analogue 2-deoxy-D-glucose (2-DG) inhibits angiogenesis at significantly lower concentrations than those required for tumor cytotoxicity. Here, we found that hypersensitivity...

journal_title：Molecular cancer therapeutics

authors： Kovács K,Decatur C,Toro M,Pham DG,Liu H,Jing Y,Murray TG,Lampidis TJ,Merchan JR

更新日期：2016-02-01 00:00:00

abstract：:Microtubule-targeting cancer drugs such as paclitaxel block cell-cycle progression at mitosis by prolonged activation of the mitotic checkpoint. Cells can spontaneously escape mitotic arrest and enter interphase without chromosome segregation by a process termed mitotic slippage that involves the degradation of cyclin...

journal_title：Molecular cancer therapeutics

authors： Riffell JL,Jänicke RU,Roberge M

更新日期：2011-05-01 00:00:00

abstract：:Anti-HER2/CD3, a T-cell-dependent bispecific antibody (TDB) construct, induces T-cell-mediated cell death in cancer cells expressing HER2 by cross-linking tumor HER2 with CD3 on cytotoxic T cells, thereby creating a functional cytolytic synapse. TDB design is a very challenging process that requires consideration of m...

journal_title：Molecular cancer therapeutics

authors： Mandikian D,Takahashi N,Lo AA,Li J,Eastham-Anderson J,Slaga D,Ho J,Hristopoulos M,Clark R,Totpal K,Lin K,Joseph SB,Dennis MS,Prabhu S,Junttila TT,Boswell CA

更新日期：2018-04-01 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：:In breast and certain other cancers, receptor tyrosine kinases, including the insulin-like growth factor I receptor (IGF-IR), play an important role in promoting the oncogenic process. The IGF-IR is therefore an important target for developing new anti-breast cancer therapies. An initial screening of a chemical librar...

journal_title：Molecular cancer therapeutics

authors： Gable KL,Maddux BA,Penaranda C,Zavodovskaya M,Campbell MJ,Lobo M,Robinson L,Schow S,Kerner JA,Goldfine ID,Youngren JF

更新日期：2006-04-01 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：: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：:Transforming growth factor-beta (TGF-beta) is a multifunctional cytokine that promotes malignant glioma invasion, angiogenesis, and immunosuppression. Antisense oligonucleotide suppression of TGF-beta(2) ligand expression has shown promise in preclinical and clinical studies but at least two ligands mediate the effect...

journal_title：Molecular cancer therapeutics

authors： Hjelmeland MD,Hjelmeland AB,Sathornsumetee S,Reese ED,Herbstreith MH,Laping NJ,Friedman HS,Bigner DD,Wang XF,Rich JN

更新日期：2004-06-01 00:00:00

abstract：:The secondary T790M mutation in epidermal growth factor receptor (EGFR) is the major mechanism of acquired resistance to EGFR tyrosine kinase inhibitors (TKI) in non-small cell lung cancer (NSCLC). Although irreversible EGFR TKIs, such as afatinib or dacomitinib, have been introduced to overcome the acquired resistanc...

journal_title：Molecular cancer therapeutics

authors： Kim SM,Kwon OJ,Hong YK,Kim JH,Solca F,Ha SJ,Soo RA,Christensen JG,Lee JH,Cho BC

更新日期：2012-10-01 00:00:00

abstract：:The PI3K/AKT/mTOR pathway is frequently activated in head and neck squamous cell carcinoma (HNSCC), but pathway inhibition has variable efficacy. Identification of predictive biomarkers and mechanisms of resistance would allow selection of patients most likely to respond and novel therapeutic combinations. The purpose...

journal_title：Molecular cancer therapeutics

authors： Mazumdar T,Byers LA,Ng PK,Mills GB,Peng S,Diao L,Fan YH,Stemke-Hale K,Heymach JV,Myers JN,Glisson BS,Johnson FM

更新日期：2014-11-01 00:00:00

abstract：:Allicin (diallyl thiosulfinate), a highly active component in extracts of freshly crushed garlic, is the interaction product of non-protein amino acid alliin (S-allyl-L-cysteine sulfoxide) with the enzyme alliinase (alliin lyase; EC 4.4.1.4). Allicin was shown to be toxic in various mammalian cells in a dose-dependent...

journal_title：Molecular cancer therapeutics

authors： Miron T,Mironchik M,Mirelman D,Wilchek M,Rabinkov A

更新日期：2003-12-01 00:00:00

abstract：:The effect of vascular endothelial growth factor (VEGF) ligands and cediranib on tumor cell proliferation, migration, and invasion was determined. It has recently been suggested that autocrine signaling through the VEGF receptor (VEGFR) pathway may play a role in tumor cell survival, invasion, and migration. The purpo...

journal_title：Molecular cancer therapeutics

authors： Morelli MP,Brown AM,Pitts TM,Tentler JJ,Ciardiello F,Ryan A,Jürgensmeier JM,Eckhardt SG

更新日期：2009-09-01 00:00:00

abstract：:Treatment options for hepatocellular carcinoma using chemotherapeutics at intermediate and advanced stages of disease are limited as patients most rapidly escape from therapy and succumb to disease progression. Mechanisms of the hepatic xenobiotic metabolism are mostly involved in providing chemoresistance to therapeu...

journal_title：Molecular cancer therapeutics

authors： Haider C,Grubinger M,Řezníčková E,Weiss TS,Rotheneder H,Miklos W,Berger W,Jorda R,Zatloukal M,Gucky T,Strnad M,Kryštof V,Mikulits W

更新日期：2013-10-01 00:00:00

abstract：:Upregulation of HER2 is a hallmark of 20% to 30% of invasive breast cancers, rendering this receptor an attractive target for cancer therapy. Although HER2-targeting agents have provided substantial clinical benefit as cancer therapeutics, there is a need for the development of new agents aiming at circumventing anti-...

journal_title：Molecular cancer therapeutics

authors： Brack S,Attinger-Toller I,Schade B,Mourlane F,Klupsch K,Woods R,Hachemi H,von der Bey U,Koenig-Friedrich S,Bertschinger J,Grabulovski D

更新日期：2014-08-01 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：:Tamoxifen, a selective estrogen receptor (ER) modulator, is the most widely prescribed hormonal therapy treatment for breast cancer. Despite the benefits of tamoxifen therapy, almost all tamoxifen-responsive breast cancer patients develop resistance to therapy. In addition, tamoxifen displays estrogen-like effects in ...

journal_title：Molecular cancer therapeutics

authors： Shah YM,Al-Dhaheri M,Dong Y,Ip C,Jones FE,Rowan BG

更新日期：2005-08-01 00:00:00

abstract：:Pancreatic cancer is the fifth leading cause of cancer death in North America. Gemcitabine improves the quality of life of patients but fails to significantly reduce mortality. Our laboratory has demonstrated previously that the phosphatidylinositol 3'-kinase inhibitor wortmannin promotes gemcitabine antitumor activit...

journal_title：Molecular cancer therapeutics

authors： Ng SS,Tsao MS,Nicklee T,Hedley DW

更新日期：2002-08-01 00:00:00