Targeted delivery to PEPT1-overexpressing cells: acidic, basic, and secondary floxuridine amino acid ester prodrugs.

abstract：:STAT3 has been recognized for its key role in the progression of cancer, where it is frequently upregulated or constitutively hyperactivated, contributing to tumor cell proliferation, survival, and migration, as well as angiogenesis and suppression of antitumor immunity. Given the ubiquity of dysregulated STAT3 activi...

journal_title：Molecular cancer therapeutics

authors： Shiah JV,Grandis JR,Johnson DE

更新日期：2020-11-17 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：:Expression of fatty acid synthase (FASN), the key enzyme in de novo synthesis of long-chain fatty acids, is normally low but increases in cancer. Consequently, FASN is a novel target for cancer therapy. However, because FASN inhibitors can lead to tumor stasis rather than shrinkage, noninvasive methods for assessing F...

journal_title：Molecular cancer therapeutics

authors： Ross J,Najjar AM,Sankaranarayanapillai M,Tong WP,Kaluarachchi K,Ronen SM

更新日期：2008-08-01 00:00:00

abstract：:Met-amplified EGFR-tyrosine kinase inhibitor (TKI)-resistant non-small cell lung cancer (NSCLC) harboring an activating EGFR mutation is responsive to concurrent EGFR-TKI and Met-TKI treatment in a preclinical model. Here, we determined that Met-amplified gefitinib-resistant cells acquire dual resistance to inhibition...

journal_title：Molecular cancer therapeutics

authors： Yamaoka T,Ohmori T,Ohba M,Arata S,Kishino Y,Murata Y,Kusumoto S,Ishida H,Shirai T,Hirose T,Ohnishi T,Sasaki Y

更新日期：2016-12-01 00:00:00

abstract：:Metastatic castration-resistant prostate cancer (CRPC) is currently incurable. Cancer growth and progression is intimately affected by its interaction with host microenvironment. Cotargeting of the stroma and prostate cancer is therefore an emerging therapeutic strategy for metastatic CRPC. Cancer-induced osteoclastog...

journal_title：Molecular cancer therapeutics

authors： Hsieh CL,Huang HS,Chen KC,Saka T,Chiang CY,Chung LWK,Sung SY

更新日期：2020-01-01 00:00:00

abstract：:Ligation of OX40 (CD134, TNFRSF4) on activated T cells by its natural ligand (OX40L, CD252, TNFSF4) enhances cellular survival, proliferation, and effector functions such as cytokine release and cellular cytotoxicity. We engineered a recombinant human OX40L IgG4P Fc fusion protein termed MEDI6383 that assembles into a...

journal_title：Molecular cancer therapeutics

authors： Oberst MD,Augé C,Morris C,Kentner S,Mulgrew K,McGlinchey K,Hair J,Hanabuchi S,Du Q,Damschroder M,Feng H,Eck S,Buss N,de Haan L,Pierce AJ,Park H,Sylwester A,Axthelm MK,Picker L,Morris NP,Weinberg A,Hammond SA

更新日期：2018-05-01 00:00:00

abstract：:HER2-positive breast cancer is currently managed with chemotherapy in combination with specific anti-HER2 therapies, including trastuzumab. However, a high percentage of patients with HER2-positive tumors do not respond to trastuzumab (primary resistance) or either recur (acquired resistance), mostly due to molecular ...

journal_title：Molecular cancer therapeutics

authors： Zazo S,González-Alonso P,Martín-Aparicio E,Chamizo C,Luque M,Sanz-Álvarez M,Mínguez P,Gómez-López G,Cristóbal I,Caramés C,García-Foncillas J,Eroles P,Lluch A,Arpí O,Rovira A,Albanell J,Madoz-Gúrpide J,Rojo F

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

abstract：:With current techniques, it remains a challenge to assess coregulator binding of nuclear receptors, for example, the estrogen receptor alpha (ERα). ERα is critical in many breast tumors and is inhibited by antiestrogens such as tamoxifen in cancer therapy. ERα is also modified by acetylation and phosphorylation that a...

journal_title：Molecular cancer therapeutics

authors： Houtman R,de Leeuw R,Rondaij M,Melchers D,Verwoerd D,Ruijtenbeek R,Martens JW,Neefjes J,Michalides R

更新日期：2012-04-01 00:00:00

abstract：:Uveal melanoma is a rare and aggressive cancer that originates in the eye. Currently, there are no approved targeted therapies and very few effective treatments for this cancer. Although activating mutations in the G protein alpha subunits, GNAQ and GNA11, are key genetic drivers of the disease, few additional drug ta...

journal_title：Molecular cancer therapeutics

authors： Rago F,Elliott G,Li A,Sprouffske K,Kerr G,Desplat A,Abramowski D,Chen JT,Farsidjani A,Xiang KX,Bushold G,Feng Y,Shirley MD,Bric A,Vattay A,Möbitz H,Nakajima K,Adair CD,Mathieu S,Ntaganda R,Smith T,Papillon JPN,

更新日期：2020-10-01 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 study aims to explore whether E545K, the most common hotspot mutation of PIK3CA in cervical cancer, confers radioresistance to cervical cancer cells, to demonstrate the underling mechanism, and to develop the effective targets. SiHa and MS751 cells with PIK3CA-WT and PIK3CA-E545K were established by lentiviral tr...

journal_title：Molecular cancer therapeutics

authors： Jiang W,Wu Y,He T,Zhu H,Ke G,Xiang L,Yang H

更新日期：2020-02-01 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：:Vascular endothelial growth factor (VEGF) is a primary stimulant of angiogenesis and is a macrophage chemotactic protein. Inhibition of VEGF is beneficial in combination with chemotherapy for some breast cancer patients. However, the mechanism by which inhibition of VEGF affects tumor growth seems to involve more than...

journal_title：Molecular cancer therapeutics

authors： Roland CL,Dineen SP,Lynn KD,Sullivan LA,Dellinger MT,Sadegh L,Sullivan JP,Shames DS,Brekken RA

更新日期：2009-07-01 00:00:00

abstract：:The phosphatidylinositol 3-kinase (PI3K)/Akt pathway is known to be activated by radiation. The mammalian target of rapamycin (mTOR) is downstream of Akt, and we investigated the effects of radiation on Akt/mTOR signaling in breast cancer cell models. RAD001 (everolimus), a potent derivative of the mTOR inhibitor rapa...

journal_title：Molecular cancer therapeutics

authors： Albert JM,Kim KW,Cao C,Lu B

更新日期：2006-05-01 00:00:00

abstract：:Antiangiogenic therapies targeting VEGFA have been commonly used in clinics to treat cancers over the past decade. However, their clinical efficacy has been limited, with drawbacks including acquisition of resistance and activation of compensatory pathways resulting from elevated circulating VEGFB and placental growth...

journal_title：Molecular cancer therapeutics

authors： Lee JE,Kim C,Yang H,Park I,Oh N,Hua S,Jeong H,An HJ,Kim SC,Lee GM,Koh GY,Kim HM

更新日期：2015-02-01 00:00:00

abstract：:RAD51 is a key protein in the homologous recombination (HR) pathway of DNA double-strand break repair, and HR represents a novel target for cancer therapy. Because imatinib (Gleevec) has been reported to reduce RAD51 protein levels, we tested the clonogenic survival for RT112, H1299, PANC1, and PC3 tumor cell lines of...

journal_title：Molecular cancer therapeutics

authors： Choudhury A,Zhao H,Jalali F,Al Rashid S,Ran J,Supiot S,Kiltie AE,Bristow RG

更新日期：2009-01-01 00:00:00

abstract：:In recent years, HER3 has increasingly been implicated in the progression of a variety of tumor types and in acquired resistance to EGFR and HER2 therapies. Whereas EGFR and HER2 primarily signal through the MAPK pathway, HER3, as a heterodimer with EGFR or HER2, potently activates the PI3K pathway. Despite its critic...

journal_title：Molecular cancer therapeutics

authors： Thakkar D,Sancenon V,Taguiam MM,Guan S,Wu Z,Ng E,Paszkiewicz KH,Ingram PJ,Boyd-Kirkup JD

更新日期：2020-02-01 00:00:00

abstract：:C-phycocyanin, which is a major biliprotein of the blue-green algae, has been shown to possess cyclooxygenase-2 inhibitory activity. We have studied the effect of phycocyanin on a rat histiocytic tumor line. AK-5 cells are induced into apoptotic death program when treated with phycocyanin, which involves the activatio...

journal_title：Molecular cancer therapeutics

authors： Pardhasaradhi BV,Ali AM,Kumari AL,Reddanna P,Khar A

更新日期：2003-11-01 00:00:00

abstract：:Malignant ascitis (MA) is a highly intractable and immunotherapy-resistant state of advanced gastrointestinal and ovarian cancers. Using a murine model of MA with CT26 colon cancer cells, we here determined that the imbalance between the VEGF-A/vascular permeability factor and its decoy receptor, soluble fms-like tryr...

journal_title：Molecular cancer therapeutics

authors： Sugiyama M,Kakeji Y,Tsujitani S,Harada Y,Onimaru M,Yoshida K,Tanaka S,Emi Y,Morita M,Morodomi Y,Hasegawa M,Maehara Y,Yonemitsu Y

更新日期：2011-03-01 00:00:00

abstract：:Radiotherapy, a frequent mode of cancer treatment, is often restricted by dose-related toxicity and development of therapeutic resistance. To develop a novel and selective radiosensitizer, we studied the radiosensitizing effects and associated mechanisms of silibinin in prostate cancer. The radiosensitizing effect of ...

journal_title：Molecular cancer therapeutics

authors： Nambiar DK,Rajamani P,Deep G,Jain AK,Agarwal R,Singh RP

更新日期：2015-12-01 00:00:00

abstract：:The endothelin (ET) axis, often deregulated in cancers, is a promising target for anticancer strategies. Whereas previous investigations have focused mostly on ET action in malignant cells, we chose a model allowing separate assessment of the effects of ETs and their receptors ET(A)R and ET(B)R in the tumor cells and ...

journal_title：Molecular cancer therapeutics

authors： Binder C,Hagemann T,Sperling S,Schulz M,Pukrop T,Grimshaw MJ,Ehrenreich H

更新日期：2009-08-01 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：: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：:Zoledronic acid, a third-generation bisphosphonate, has been shown to reduce cell migration, invasion, and metastasis. However, the effects of zoledronic acid on the epithelial-mesenchymal transition (EMT), a cellular process essential to the metastatic cascade, remain unclear. Therefore, the effects of zoledronic aci...

journal_title：Molecular cancer therapeutics

authors： Schech AJ,Kazi AA,Gilani RA,Brodie AH

更新日期：2013-07-01 00:00:00

abstract：:Tyrosine kinase inhibitors exhibit impressive activity against advanced renal cell carcinoma. However, recent clinical studies have shown an equivocal response to sunitinib in patients with castration-resistant prostate cancer. The tumor suppressor PTEN acts as a gatekeeper of the phosphoinositide 3-kinase (PI3K)/Akt/...

journal_title：Molecular cancer therapeutics

authors： Makhov PB,Golovine K,Kutikov A,Teper E,Canter DJ,Simhan J,Uzzo RG,Kolenko VM

更新日期：2012-07-01 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：: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：:Castration-resistant prostate cancer (CRPC) remains dependent on androgen receptor (AR) signaling. Alternative splicing of the AR to generate constitutively active, ligand-independent variants is one of the principal mechanisms that promote the development of resistance to next-generation antiandrogens such as enzalut...

journal_title：Molecular cancer therapeutics

authors： Nadiminty N,Tummala R,Liu C,Lou W,Evans CP,Gao AC

更新日期：2015-08-01 00:00:00

abstract：:Novel therapeutic approaches are urgently needed for high-stage neuroblastoma, a major therapeutic challenge in pediatric oncology. The majority of neuroblastoma tumors are p53 wild type with intact downstream p53 signaling pathways. We hypothesize that stabilization of p53 would sensitize this aggressive tumor to gen...

journal_title：Molecular cancer therapeutics

authors： Barbieri E,Mehta P,Chen Z,Zhang L,Slack A,Berg S,Shohet JM

更新日期：2006-09-01 00:00:00