(-)-Gossypol acts directly on the mitochondria to overcome Bcl-2- and Bcl-X(L)-mediated apoptosis resistance.

abstract：:The cytotoxicity of 5-aza-2'-deoxycytidine (DAC) has been linked to demethylation of the INK4a/ARF tumor suppressor gene locus in various cell systems, but the causality of this association remains unproven. To test this assumption, we have examined the effects of DAC in two human cancer cell lines of differing INK4a/...

journal_title：Molecular cancer therapeutics

authors： Xiong J,Epstein RJ

更新日期：2009-04-01 00:00:00

abstract：:Tumor-associated urokinase plasminogen activator (uPA) is a critical marker of invasion and metastasis, has strong prognostic relevance, and is thus a potential therapeutic target. Experimental data published to date has established the proof-of-principle of uPA targeting by (213)Bi-labeled plasminogen activator inhib...

journal_title：Molecular cancer therapeutics

authors： Stutchbury TK,Al-Ejeh F,Stillfried GE,Croucher DR,Andrews J,Irving D,Links M,Ranson M

更新日期：2007-01-01 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：: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：:Small cell lung cancer (SCLC) has a poor prognosis. Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase regulating cell proliferation, survival, migration, and invasion, which is overexpressed and/or activated in several cancers, including SCLC. We wanted to determine whether FAK contributes to SCLC aggressi...

journal_title：Molecular cancer therapeutics

authors： Aboubakar Nana F,Lecocq M,Ladjemi MZ,Detry B,Dupasquier S,Feron O,Massion PP,Sibille Y,Pilette C,Ocak S

更新日期：2019-01-01 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is one of the most chemotherapy- and radiotherapy-resistant tumors. The c-Met and Hedgehog (Hh) pathways have been shown previously by our group to be key regulatory pathways in the primary tumor growth and metastases formation. Targeting both the HGF/c-Met and Hh pathways has s...

journal_title：Molecular cancer therapeutics

authors： Rucki AA,Xiao Q,Muth S,Chen J,Che X,Kleponis J,Sharma R,Anders RA,Jaffee EM,Zheng L

更新日期：2017-11-01 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：: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：: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

abstract：:Luteolin, a common dietary flavonoid, has been found to have antitumor properties and therefore poses special interest for the development of preventive and/or therapeutic agent for cancers. E-cadherin, a marker of epithelial cells, mediates cell-cell adhesion. Decreased expression of E-cadherin results in a loss of c...

journal_title：Molecular cancer therapeutics

authors： Zhou Q,Yan B,Hu X,Li XB,Zhang J,Fang J

更新日期：2009-06-01 00:00:00

abstract：:The two-step transcriptional activation (TSTA) mechanism in gene therapy amplifies cell type-specific promoter activity, allowing for increased levels of gene expression in target tissues. In this system, the specific promoter drives expression of a strong transcriptional activator that binds to DNA target sequences l...

journal_title：Molecular cancer therapeutics

authors： Arendt ML,Nasir L,Morgan IM

更新日期：2009-12-01 00:00:00

abstract：UNLABELLED:Multiple myeloma (MM) is a malignancy of clonal B-cells that accounts for 10% of all hematologic malignancies. We have shown previously that a novel purine analogue, 8-chloro-adenosine, has significant activity for MM in preclinical studies. OBJECTIVE:Using MM cell lines, we investigated the molecular mecha...

journal_title：Molecular cancer therapeutics

authors： Krett NL,Davies KM,Ayres M,Ma C,Nabhan C,Gandhi V,Rosen ST

更新日期：2004-11-01 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：:To investigate the mechanism by which 5-aminoimidazole-4-carboxamide-1-β-riboside (AICAr) induces apoptosis in multiple myeloma cells, we conducted an unbiased metabolomics screen. AICAr had selective effects on nucleotide metabolism, resulting in an increase in purine metabolites and a decrease in pyrimidine metaboli...

journal_title：Molecular cancer therapeutics

authors： Bardeleben C,Sharma S,Reeve JR,Bassilian S,Frost P,Hoang B,Shi Y,Lichtenstein A

更新日期：2013-07-01 00:00:00

abstract：:Many malignant human tumors, including melanomas, are auxotrophic for arginine due to reduced expression of argininosuccinate synthetase-1 (ASS1), the rate-limiting enzyme for arginine biosynthesis. Pegylated arginine deiminase (ADI-PEG20), which degrades extracellular arginine, resulting in arginine deprivation, has ...

journal_title：Molecular cancer therapeutics

authors： Long Y,Tsai WB,Wangpaichitr M,Tsukamoto T,Savaraj N,Feun LG,Kuo MT

更新日期：2013-11-01 00:00:00

abstract：:Preclinical data suggest that combined EGF receptor (EGFR) targeting with an EGFR tyrosine kinase inhibitor and an anti-EGFR monoclonal antibody may be superior over single-agent targeting. Therefore, as part of a phase I study, we analyzed the outcome of 20 patients with non-small cell lung cancer treated with the co...

journal_title：Molecular cancer therapeutics

authors： Wheler JJ,Tsimberidou AM,Falchook GS,Zinner RG,Hong DS,Fok JY,Fu S,Piha-Paul SA,Naing A,Kurzrock R

更新日期：2013-10-01 00:00:00

abstract：:The CDC25 cell cycle regulators are promising targets for new pharmacologic approaches in cancer therapy. Inhibitory compounds such as BN82685 have proven to be effective in specifically targeting CDC25 in cultured cells and in inhibiting tumor cell growth. Here, we report that BN82685 impairs microtubule dynamic inst...

journal_title：Molecular cancer therapeutics

authors： Cazales M,Boutros R,Brezak MC,Chaumeron S,Prevost G,Ducommun B

更新日期：2007-01-01 00:00:00

abstract：:1,1-Bis(3'-indolyl)-1-(p-substituted phenyl)methanes containing p-trifluoromethyl, t-butyl, and phenyl [1,1-bis(3'-indolyl)-1-(p-phenyl)methane (DIM-C-pPhC(6)H(5))] substituents induce peroxisome proliferator-activated receptor gamma (PPARgamma)-mediated transactivation in SW480 colon cancer cells. These PPARgamma-act...

journal_title：Molecular cancer therapeutics

authors： Chintharlapalli S,Papineni S,Safe S

更新日期：2006-05-01 00:00:00

abstract：:Novel molecules are constantly being discovered and developed to find better means of managing debilitating and fatal diseases, which include cancer in its multiple forms. Among these molecules, and as a direct consequence of a better understanding of the molecular basis of diseases, are those falling within the class...

journal_title：Molecular cancer therapeutics

authors： Dass CR,Choong PF,Khachigian LM

更新日期：2008-02-01 00:00:00

abstract：:In patients with advanced bladder cancer, glucocorticoids are frequently given to reduce acute toxicity, particularly hyperemesis, during chemotherapy, as well as to improve cachectic conditions. However, it remains unclear whether glucocorticoids directly affect the development and progression of bladder cancer throu...

journal_title：Molecular cancer therapeutics

authors： Zheng Y,Izumi K,Li Y,Ishiguro H,Miyamoto H

更新日期：2012-12-01 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：: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：:Complexities in treating breast cancer with bone metastasis are enhanced by a vicious protumorigenic pathology, involving a shift in skeletal homeostasis toward aggressive osteoclast activity and polarization of immune cells supporting tumor growth and immunosuppression. Recent studies signify the role of receptor act...

journal_title：Molecular cancer therapeutics

authors： Wang H,Ashton R,Hensel JA,Lee JH,Khattar V,Wang Y,Deshane JS,Ponnazhagan S

更新日期：2020-12-01 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：:The serine/threonine kinase AKT/PKB plays a critical role in cancer and represents a rational target for therapy. Although efforts in targeting AKT pathway have accelerated in recent years, relatively few small molecule inhibitors of AKT have been reported. The development of selective AKT inhibitors is further challe...

journal_title：Molecular cancer therapeutics

authors： Toral-Barza L,Zhang WG,Huang X,McDonald LA,Salaski EJ,Barbieri LR,Ding WD,Krishnamurthy G,Hu YB,Lucas J,Bernan VS,Cai P,Levin JI,Mansour TS,Gibbons JJ,Abraham RT,Yu K

更新日期：2007-11-01 00:00:00

abstract：:Rac1 GTPase regulates a variety of signaling pathways that are implicated in malignant phenotypes. Here, we show that selective inhibition of Rac1 activity by the pharmacologic inhibitor NSC23766 suppressed cell growth in a panel of human breast cancer cell lines, whereas it had little toxicity to normal mammary epith...

journal_title：Molecular cancer therapeutics

authors： Yoshida T,Zhang Y,Rivera Rosado LA,Chen J,Khan T,Moon SY,Zhang B

更新日期：2010-06-01 00:00:00

abstract：:Trastuzumab and the related ADC, ado-trastuzumab emtansine (T-DM1), both target HER2-overexpressing cells. Together, these drugs have treatment indications in both early-stage and metastatic settings for HER2+ breast cancer. T-DM1 retains the antibody functionalities of trastuzumab and adds the potency of a cytotoxic ...

journal_title：Molecular cancer therapeutics

authors： Barfield RM,Kim YC,Chuprakov S,Zhang F,Bauzon M,Ogunkoya AO,Yeo D,Hickle C,Pegram MD,Rabuka D,Drake PM

更新日期：2020-09-01 00:00:00

abstract：:It is well recognized that nitric oxide (NO) is involved in tumor progression, including melanoma. Measurement of proliferative and metastatic capacity by MTS and Matrigel invasion assays, respectively, was done and showed that NO-treated melanoma cells exhibited a higher capacity compared with control, especially met...

journal_title：Molecular cancer therapeutics

authors： Yang Z,Yang S,Misner BJ,Chiu R,Liu F,Meyskens FL Jr

更新日期：2008-12-01 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：:The majority of patients with HER2-overexpressing metastatic breast cancer who initially respond to the HER2-targeted antibody trastuzumab show disease progression within 1 year. The identification of novel agents that effectively inhibit survival of cancer cells that have progressed on trastuzumab is critical for imp...

journal_title：Molecular cancer therapeutics

authors： Rowe DL,Ozbay T,Bender LM,Nahta R

更新日期：2008-07-01 00:00:00