Glibenclamide Targets Sulfonylurea Receptor 1 to Inhibit p70S6K Activity and Upregulate KLF4 Expression to Suppress Non-Small Cell Lung Carcinoma.

abstract：:Endocrine therapy is important for management of patients with estrogen receptor (ER)-positive breast cancer; however, positive ER staining does not reliably predict therapy response. We assessed the potential to improve prediction of response to endocrine treatment of a novel test that quantifies functional ER pathwa...

journal_title：Molecular cancer therapeutics

authors： Inda MA,Blok EJ,Kuppen PJK,Charehbili A,den Biezen-Timmermans EC,van Brussel A,Fruytier SE,Meershoek-Klein Kranenbarg E,Kloet S,van der Burg B,Martens JWM,Sims AH,Turnbull AK,Dixon JM,Verhaegh W,Kroep JR,van de Velde CJH

更新日期：2020-02-01 00:00:00

abstract：:Imatinib mesylate has shown remarkable efficacy in the treatment of patients in the chronic phase of chronic myeloid leukemia. However, despite an overall significant hematological and cytogenetic response, imatinib therapy may favor the emergence of drug-resistant clones, ultimately leading to relapse. Some imatinib ...

journal_title：Molecular cancer therapeutics

authors： Deville L,Hillion J,Pendino F,Samy M,Nguyen E,Ségal-Bendirdjian E

更新日期：2011-05-01 00:00:00

abstract：:One hallmark of cancer cells is their adaptation to rely upon an altered metabolic scheme that includes changes in the glycolytic pathway, known as the Warburg effect, and elevated glutamine metabolism. Glutaminase, a mitochondrial enzyme, plays a key role in the metabolism of glutamine in cancer cells, and its inhibi...

journal_title：Molecular cancer therapeutics

authors： Katt WP,Ramachandran S,Erickson JW,Cerione RA

更新日期：2012-06-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor γ (PPARγ) is an important transcription factor that modulates lipid metabolism and inflammation. However, it remains unclear whether PPARγ is involved in modulation of estrogen (E2)-induced inflammation, thus affecting apoptosis of E2-deprived breast cancer cells, MCF-7:5C an...

journal_title：Molecular cancer therapeutics

authors： Fan P,Abderrahman B,Chai TS,Yerrum S,Jordan VC

更新日期：2018-12-01 00:00:00

abstract：:Wee1 is a critical component of the G(2)-M cell-cycle checkpoint control and mediates cell-cycle arrest by regulating the phosphorylation of CDC2. Inhibition of Wee1 by a selective small molecule inhibitor MK1775 can abrogate G(2)-M checkpoint, resulting in premature mitotic entry and cell death. MK1775 has recently b...

journal_title：Molecular cancer therapeutics

authors： Kreahling JM,Gemmer JY,Reed D,Letson D,Bui M,Altiok S

更新日期：2012-01-01 00:00:00

abstract：:Clinical translation of intravenous therapies to treat disseminated or metastatic cancer is imperative. Comparative oncology, the evaluation of novel cancer therapies in animals with spontaneous cancer, can be utilized to inform and accelerate clinical translation. Preclinical murine studies demonstrate that single-sh...

journal_title：Molecular cancer therapeutics

authors： Naik S,Galyon GD,Jenks NJ,Steele MB,Miller AC,Allstadt SD,Suksanpaisan L,Peng KW,Federspiel MJ,Russell SJ,LeBlanc AK

更新日期：2018-01-01 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：:A number of cancer chemotherapeutic drugs designed to have cytotoxic actions on tumor cells have recently been shown to also have antiangiogenic activities. Endothelial cell migration and proliferation are key components of tumor angiogenesis, and agents that target the microtubule cytoskeleton can interfere with thes...

journal_title：Molecular cancer therapeutics

authors： Hotchkiss KA,Ashton AW,Mahmood R,Russell RG,Sparano JA,Schwartz EL

更新日期：2002-11-01 00:00:00

abstract：:The functional and therapeutic importance of the Warburg effect is increasingly recognized, and glycolysis has become a target of anticancer strategies. We recently reported the identification of a group of novel small compounds that inhibit basal glucose transport and reduce cancer cell growth by a glucose deprivatio...

journal_title：Molecular cancer therapeutics

authors： Liu Y,Cao Y,Zhang W,Bergmeier S,Qian Y,Akbar H,Colvin R,Ding J,Tong L,Wu S,Hines J,Chen X

更新日期：2012-08-01 00:00:00

abstract：:Our recent studies showed that antisense oligodeoxynucleotide targeting antiapoptotic gene, clusterin, enhanced apoptosis induced by conventional therapeutic modalities using several prostate cancer models. In this study, to establish a more effective therapeutic strategy against prostate cancer, we investigated the e...

journal_title：Molecular cancer therapeutics

authors： Yamanaka K,Gleave ME,Hara I,Muramaki M,Miyake H

更新日期：2005-02-01 00:00:00

abstract：:TRC105 is an anti-endoglin antibody currently being tested in combination with VEGF inhibitors. In the phase Ib trial, 38 patients were treated with both TRC105 and bevacizumab (BEV), and improved clinical outcomes were observed, despite the fact that 30 patients (79%) were refractory to prior anti-VEGF therapy. Plasm...

journal_title：Molecular cancer therapeutics

authors： Liu Y,Starr MD,Brady JC,Rushing C,Pang H,Adams B,Alvarez D,Theuer CP,Hurwitz HI,Nixon AB

更新日期：2018-10-01 00:00:00

abstract：:This meeting report on the fourth Fabisch Symposium for Cancer Research and Molecular Biology describes the aims of the international meeting, the main topics of the presentations, and the highlights of the conference. The fourth Fabisch Symposium was the second on Targeted Tumor Therapies and held from April 1-3, 200...

journal_title：Molecular cancer therapeutics

authors： Bachran C,Fuchs H

更新日期：2010-01-01 00:00:00

abstract：:STAT3 has been strongly implicated in human malignancies, and constitutive activation of STAT3 serves a crucial role in cell survival, angiogenesis, immune evasion, and inflammation. In this study, we showed that nitidine chloride, a natural phytochemical alkaloid derived from Zanthoxylum nitidum (Roxb) DC, exerts pot...

journal_title：Molecular cancer therapeutics

authors： Chen J,Wang J,Lin L,He L,Wu Y,Zhang L,Yi Z,Chen Y,Pang X,Liu M

更新日期：2012-02-01 00:00:00

abstract：:Bisperoxovanadium (bpV) compounds are irreversible protein tyrosine phosphatase (PTP) inhibitors with a spectrum of activity distinct from that of vanadium salts. We studied the efficacy of a panel of bpVs as antineoplastic agents in vitro and in vivo with a view to investigating phosphatases as potential antineoplast...

journal_title：Molecular cancer therapeutics

authors： Scrivens PJ,Alaoui-Jamali MA,Giannini G,Wang T,Loignon M,Batist G,Sandor VA

更新日期：2003-10-01 00:00:00

abstract：:The objective of this study was to evaluate circulating hepatocyte growth factor (cHGF) as a pharmacodynamic biomarker of Met inhibition for onartuzumab (MetMAb, OA5D5v2) in a phase I trial in patients with advanced cancers and a phase II trial in non-small cell lung cancer (NSCLC). The phase I study was a dose escala...

journal_title：Molecular cancer therapeutics

authors： Penuel E,Li C,Parab V,Burton L,Cowan KJ,Merchant M,Yauch RL,Patel P,Peterson A,Hampton GM,Lackner MR,Hegde PS

更新日期：2013-06-01 00:00:00

abstract：:The PI3K/AKT/mTOR pathway, which is aberrantly stimulated in many cancer cells, has emerged as a target for therapy. However, mTORC1/S6K also mediates negative feedback loops that attenuate upstream signaling. Suppression of these feedback loops opposes the growth-suppressive effects of mTOR inhibitors and leads to dr...

journal_title：Molecular cancer therapeutics

authors： Soares HP,Ming M,Mellon M,Young SH,Han L,Sinnet-Smith J,Rozengurt E

更新日期：2015-04-01 00:00:00

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：:Acquired resistance to cancer drugs is common, also for modern targeted drugs like the Bruton tyrosine kinase (BTK) inhibitor ibrutinib, a new drug approved for the treatment of the highly aggressive and relapsing mantle cell lymphoma (MCL). The tumor microenvironment often impacts negatively on drug response. Here, w...

journal_title：Molecular cancer therapeutics

authors： Guan J,Huang D,Yakimchuk K,Okret S

更新日期：2018-05-01 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：:Because proliferation of eukaryotic cells requires cell cycle-regulated chromatid separation by the mitotic spindle, it is subject to regulation by mitotic checkpoints. To determine the mechanism of the antiproliferative activity of the flavoprotein-specific inhibitor diphenyleneiodonium (DPI), I have examined its eff...

journal_title：Molecular cancer therapeutics

authors： Scaife RM

更新日期：2004-10-01 00:00:00

abstract：:Camptothecin and Adriamycin are clinically important inhibitors for topoisomerase (Topo) I and Topo II, respectively. The ataxia-telangiectasia mutated (ATM) product is essential for ionizing radiation-induced DNA damage responses, but the role of ATM in Topo poisons-induced checkpoints remains unresolved. We found th...

journal_title：Molecular cancer therapeutics

authors： Siu WY,Lau A,Arooz T,Chow JP,Ho HT,Poon RY

更新日期：2004-05-01 00:00:00

abstract：:Raf inhibitors are under clinical investigation, specifically in patients with tumor types harboring frequent activating mutations in B-Raf. Here, we show that cell lines and tumors harboring mutant B-Raf were sensitive to a novel series of Raf inhibitors (e.g., (V600E)B-Raf A375, IC(50) on cells = 2 nmol/L; ED(50) on...

journal_title：Molecular cancer therapeutics

authors： Carnahan J,Beltran PJ,Babij C,Le Q,Rose MJ,Vonderfecht S,Kim JL,Smith AL,Nagapudi K,Broome MA,Fernando M,Kha H,Belmontes B,Radinsky R,Kendall R,Burgess TL

更新日期：2010-08-01 00:00:00

abstract：:The present studies have determined whether interactions between the cyclin-dependent kinase inhibitor flavopiridol and the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA; vorinostat; Zolinza) occur in breast cancer cells. MDA-MB-231 and MCF7 cells were treated with flavopiridol (25-100 nmol/L) an...

journal_title：Molecular cancer therapeutics

authors： Mitchell C,Park MA,Zhang G,Yacoub A,Curiel DT,Fisher PB,Roberts JD,Grant S,Dent P

更新日期：2007-12-01 00:00:00

abstract：:The androgen receptor (AR) is a key driver and therapeutic target in androgen-sensitive prostate cancer, castration-resistant prostate cancer (CRPC), and CRPC resistant to abiraterone and enzalutamide, two second-generation inhibitors of AR signaling. Because current AR inhibitors target a functioning C-terminal ligan...

journal_title：Molecular cancer therapeutics

authors： Dong J,Wu Z,Wang D,Pascal LE,Nelson JB,Wipf P,Wang Z

更新日期：2019-01-01 00:00:00

abstract：:Dietary phytochemicals exhibit chemopreventive potential in vivo through persistent low-dose exposures, whereas mechanistic in vitro studies with these agents generally use a high-dose single treatment. Because the latter approach is not representative of an in vivo steady state, we investigated antitumor activity of ...

journal_title：Molecular cancer therapeutics

authors： Moiseeva EP,Almeida GM,Jones GD,Manson MM

更新日期：2007-11-01 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：: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：:To isolate circulating tumor cells (CTC) from women with advanced cervical cancer and estimate the impact of CTCs and treatment on overall survival and progression-free survival (PFS). A total of 7.5 mL of whole blood was drawn pre-cycle 1 and 36 days post-cycle 1 from patients enrolled on Gynecologic Oncology Group 0...

journal_title：Molecular cancer therapeutics

authors： Tewari KS,Sill MW,Monk BJ,Penson RT,Moore DH,Lankes HA,Ramondetta LM,Landrum LM,Randall LM,Oaknin A,Leitao MM,Eisenhauer EL,DiSilvestro P,Van Le L,Pearl ML,Burke JJ,Salani R,Richardson DL,Michael HE,Kindelberger DW

更新日期：2020-08-26 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：:Programmed cell death 4 (Pdcd4), originally identified as an inhibitor of murine cellular transformation, inhibits protein synthesis by directly interacting with eukaryotic initiation factor 4A (eIF4A) of the translation initiation complex. The relevance of Pdcd4 to a broad range of human cancers derived from multiple...

journal_title：Molecular cancer therapeutics

authors： Jansen AP,Camalier CE,Stark C,Colburn NH

更新日期：2004-02-01 00:00:00