Blockade of Rac1 activity induces G1 cell cycle arrest or apoptosis in breast cancer cells through downregulation of cyclin D1, survivin, and X-linked inhibitor of apoptosis protein.

abstract：:Sulfonylurea receptor 1 (SUR1) is the regulatory subunit of ATP-sensitive potassium channels (KATP channels) and the receptor of antidiabetic drugs, such as glibenclamide, which induce insulin secretion in pancreatic β cells. However, the expression and role of SUR1 in cancer are unknown. In this study, we found that ...

journal_title：Molecular cancer therapeutics

authors： Xu K,Sun G,Li M,Chen H,Zhang Z,Qian X,Li P,Xu L,Huang W,Wang X

更新日期：2019-11-01 00:00:00

abstract：:Overexpression of Notch receptors and ligands has been associated with various cancers and developmental disorders, making Notch a potential therapeutic target. Here, we report characterization of Notch1 monoclonal antibodies (mAb) with therapeutic potential. The mAbs generated against epidermal growth factor (EGF) re...

journal_title：Molecular cancer therapeutics

authors： Sharma A,Paranjape AN,Rangarajan A,Dighe RR

更新日期：2012-01-01 00:00:00

abstract：:Accumulated evidence indicates that CCAT1 functions as an oncogene in the progression of a variety of tumors. However, little is known as to how CCAT1 impacts tumorigenesis in human prostate cancer. In this study, we found from The Cancer Genome Atlas and Memorial Sloan Kettering Cancer Center database that CCAT1 is h...

journal_title：Molecular cancer therapeutics

authors： You Z,Liu C,Wang C,Ling Z,Wang Y,Wang Y,Zhang M,Chen S,Xu B,Guan H,Chen M

更新日期：2019-12-01 00:00:00

abstract：:Anti-HER2 monoclonal antibodies (mAb) have been shown to reduce tumor size and increase survival in patients with breast cancer, but they are ineffective against brain metastases due to poor brain penetration. In previous studies, we identified a peptide, known as Angiopep-2 (An2), which crosses the blood-brain barrie...

journal_title：Molecular cancer therapeutics

authors： Regina A,Demeule M,Tripathy S,Lord-Dufour S,Currie JC,Iddir M,Annabi B,Castaigne JP,Lachowicz JE

更新日期：2015-01-01 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：:The entry of calcium into the mammary epithelial cell from the maternal plasma (i.e., calcium influx mechanisms) during lactation is poorly understood. As alterations in calcium channels and pumps are a key feature of some cancers, including breast cancer, understanding these calcium influx pathways may have significa...

journal_title：Molecular cancer therapeutics

authors： McAndrew D,Grice DM,Peters AA,Davis FM,Stewart T,Rice M,Smart CE,Brown MA,Kenny PA,Roberts-Thomson SJ,Monteith GR

更新日期：2011-03-01 00:00:00

abstract：:The anticancer actions of vitamin D and its hormonally active form, calcitriol, have been extensively documented in clinical and preclinical studies. However, the mechanisms underlying these actions have not been completely elucidated. Here, we examined the effect of dietary vitamin D and calcitriol on mouse breast tu...

journal_title：Molecular cancer therapeutics

authors： Jeong Y,Swami S,Krishnan AV,Williams JD,Martin S,Horst RL,Albertelli MA,Feldman BJ,Feldman D,Diehn M

更新日期：2015-08-01 00:00:00

abstract：:Controversy exists surrounding whether heterogeneous disruption of the blood-brain barrier (BBB), as seen in glioblastoma (GBM), leads to adequate drug delivery sufficient for efficacy in GBM. This question is especially important when using potent, targeted agents that have a poor penetration across an intact BBB. Ef...

journal_title：Molecular cancer therapeutics

authors： Kim M,Ma DJ,Calligaris D,Zhang S,Feathers RW,Vaubel RA,Meaux I,Mladek AC,Parrish KE,Jin F,Barriere C,Debussche L,Watters J,Tian S,Decker PA,Eckel-Passow JE,Kitange GJ,Johnson AJ,Parney IF,Anastasiadis PZ,Agar NYR

更新日期：2018-09-01 00:00:00

abstract：:miR34a is a tumor-suppressor miRNA that functions within the p53 pathway to regulate cell-cycle progression and apoptosis. With apparent roles in metastasis and cancer stem cell development, miR34a provides an interesting opportunity for therapeutic development. A mimic of miR34a was complexed with an amphoteric lipos...

journal_title：Molecular cancer therapeutics

authors： Daige CL,Wiggins JF,Priddy L,Nelligan-Davis T,Zhao J,Brown D

更新日期：2014-10-01 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：:Chemoresistance is a major reason that patients with osteosarcoma fail to achieve a lasting chemotherapy response, and it contributes to disease relapse, progression, and death. Human glutathione S-transferase P1 (GSTP1), a phase II detoxification enzyme, contributes to chemoresistance in many cancers. However, the ro...

journal_title：Molecular cancer therapeutics

authors： Huang G,Mills L,Worth LL

更新日期：2007-05-01 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 ductal adenocarcinoma (PDAC) is the fourth leading cause of cancer-related mortality in the United States. Aggressive treatment regimens have not changed the disease course, and the median survival has just recently reached a year. Several mechanisms are proposed to play a role in PDAC therapeutic resistanc...

journal_title：Molecular cancer therapeutics

authors： Logsdon DP,Grimard M,Luo M,Shahda S,Jiang Y,Tong Y,Yu Z,Zyromski N,Schipani E,Carta F,Supuran CT,Korc M,Ivan M,Kelley MR,Fishel ML

更新日期：2016-11-01 00:00:00

abstract：:Aberrant activation of Notch and Ras pathways has been detected in breast cancers. A synergy between these two pathways has also been shown in breast cell transformation in culture. Yet, the clinical relevance of Notch-Ras cooperation in breast cancer progression remains unexplored. In this study, we show that coordin...

journal_title：Molecular cancer therapeutics

authors： Mittal S,Sharma A,Balaji SA,Gowda MC,Dighe RR,Kumar RV,Rangarajan A

更新日期：2014-12-01 00:00:00

abstract：:STAT3 is an important transcriptional factor for cell growth, differentiation, and apoptosis. Although evidence suggests a positive role for STAT3 in cancer, the inhibitory effects of tumor STAT3 on natural killer (NK) cell functions in human hepatocellular carcinoma are unclear. In this study, we found that blocking ...

journal_title：Molecular cancer therapeutics

authors： Sun X,Sui Q,Zhang C,Tian Z,Zhang J

更新日期：2013-12-01 00:00:00

abstract：:Endocrine therapy has been highly effective for the treatment of estrogen receptor-positive breast cancer, but endocrine resistance develops in a significant proportion of patients. In an effort to develop novel therapeutic strategies for the treatment of endocrine-resistant breast cancer, we have evaluated a potent a...

journal_title：Molecular cancer therapeutics

authors： Lu J,McEachern D,Li S,Ellis MJ,Wang S

更新日期：2016-12-01 00:00:00

abstract：:Isodon diterpenoids have received considerable phytochemical and biological attention for their strong antitumor activity with low toxicity. In this study, ExcisaninA, a diterpenoid compound purified from Isodon MacrocalyxinD, was tested on human Hep3B and MDA-MB-453 cell lines and Hep3B xenograft models. The results ...

journal_title：Molecular cancer therapeutics

authors： Deng R,Tang J,Xia LP,Li DD,Zhou WJ,Wang LL,Feng GK,Zeng YX,Gao YH,Zhu XF

更新日期：2009-04-01 00:00:00

abstract：:Antiestrogens are effective therapies for the management of many estrogen receptor-alpha (ER)-positive breast cancers. Nonetheless, both de novo and acquired resistance occur and remain major problems in the clinical setting. IFNgamma is an inflammatory cytokine that induces the expression and function of IFN regulato...

journal_title：Molecular cancer therapeutics

authors： Ning Y,Riggins RB,Mulla JE,Chung H,Zwart A,Clarke R

更新日期：2010-05-01 00:00:00

abstract：:G-protein-coupled receptors (GPCR) activate the epidermal growth factor receptor (EGFR) and mediate EGFR-independent signaling pathways to promote the growth of a variety of cancers, including head and neck squamous cell carcinoma (HNSCC). Identification of the common signaling mechanisms involved in GPCR-induced EGFR...

journal_title：Molecular cancer therapeutics

authors： Bhola NE,Freilino ML,Joyce SC,Sen M,Thomas SM,Sahu A,Cassell A,Chen CS,Grandis JR

更新日期：2012-06-01 00:00:00

abstract：:Barasertib (AZD1152), a highly potent and selective aurora kinase B inhibitor, gave promising clinical activity in elderly acute myeloid leukemia (AML) patients. However, clinical utility was limited by the requirement for a 7-day infusion. Here we assessed the potential of a nanoparticle formulation of the selective ...

journal_title：Molecular cancer therapeutics

authors： Floc'h N,Ashton S,Taylor P,Trueman D,Harris E,Odedra R,Maratea K,Derbyshire N,Caddy J,Jacobs VN,Hattersley M,Wen S,Curtis NJ,Pilling JE,Pease EJ,Barry ST

更新日期：2017-06-01 00:00:00

abstract：:Aminoflavone (AF), a clinically investigational novel anticancer agent, requires sequential metabolic activation by CYP1A1 and SULT1A1 to exert its antitumor activities. The purpose of this study was to determine the functional significance of common polymorphisms of human CYP1A1 and SULT1A1 on the metabolism and cyto...

journal_title：Molecular cancer therapeutics

authors： Zheng Q,Sha X,Liu J,Heath E,Lorusso P,Li J

更新日期：2010-10-01 00:00:00

abstract：:Checkpoint kinase 1 (ChK1) is a serine/threonine kinase that functions as a central mediator of the intra-S and G2-M cell-cycle checkpoints. Following DNA damage or replication stress, ChK1-mediated phosphorylation of downstream effectors delays cell-cycle progression so that the damaged genome can be repaired. As a t...

journal_title：Molecular cancer therapeutics

authors： Blackwood E,Epler J,Yen I,Flagella M,O'Brien T,Evangelista M,Schmidt S,Xiao Y,Choi J,Kowanetz K,Ramiscal J,Wong K,Jakubiak D,Yee S,Cain G,Gazzard L,Williams K,Halladay J,Jackson PK,Malek S

更新日期：2013-10-01 00:00:00

abstract：:A novel series of 3,5-diaryl-oxadiazoles was identified as apoptosis-inducing agents through our cell and chemical genetics-based screening assay for compounds that induce apoptosis using a chemical genetics approach. Several analogues from this series including MX-74420 and MX-126374 were further characterized. MX-12...

journal_title：Molecular cancer therapeutics

authors： Jessen KA,English NM,Yu Wang J,Maliartchouk S,Archer SP,Qiu L,Brand R,Kuemmerle J,Zhang HZ,Gehlsen K,Drewe J,Tseng B,Cai SX,Kasibhatla S

更新日期：2005-05-01 00:00:00

abstract：:eIF4E is the key regulator of protein translation and critical for translation. The oncogenic potential of tumorigenesis, which is highly contingent on cap-dependent eIF4E, also arises from the critical role in the nuclear export and cytosolic translation of oncogenic transcripts. Inhibition of Exportin1 (XPO1), which...

journal_title：Molecular cancer therapeutics

authors： Li S,Fu J,Lu C,Mapara MY,Raza S,Hengst U,Lentzsch S

更新日期：2016-04-01 00:00:00

abstract：:Bortezomib is highly effective in the treatment of multiple myeloma; however, emergent drug resistance is common. Consequently, we employed CRISPR targeting 19,052 human genes to identify unbiased targets that contribute to bortezomib resistance. Specifically, we engineered an RPMI8226 multiple myeloma cell line to ex...

journal_title：Molecular cancer therapeutics

authors： Shi CX,Kortüm KM,Zhu YX,Bruins LA,Jedlowski P,Votruba PG,Luo M,Stewart RA,Ahmann J,Braggio E,Stewart AK

更新日期：2017-12-01 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：:Neuroblastoma is the most common extracranial solid tumor of childhood. The activity of J1 (l-melphalanyl-p-l-fluorophenylalanine ethyl ester), an enzymatically activated melphalan prodrug, was evaluated in neuroblastoma models in vitro and in vivo. Seven neuroblastoma cell lines with various levels of drug resistance...

journal_title：Molecular cancer therapeutics

authors： Wickström M,Johnsen JI,Ponthan F,Segerström L,Sveinbjörnsson B,Lindskog M,Lövborg H,Viktorsson K,Lewensohn R,Kogner P,Larsson R,Gullbo J

更新日期：2007-09-01 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：:In the present work, we have investigated the antitumor activity of 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol (NBDHEX) on aggressive small cell lung cancer. NBDHEX not only is cytotoxic toward the parental small cell lung cancer H69 cell line (LC(50) of 2.3 +/- 0.6 micromol/L) but also overcomes the multidrug re...

journal_title：Molecular cancer therapeutics

authors： Filomeni G,Turella P,Dupuis ML,Forini O,Ciriolo MR,Cianfriglia M,Pezzola S,Federici G,Caccuri AM

更新日期：2008-02-01 00:00:00

abstract：:Epigenetic abnormalities are common in hematologic malignancies, including multiple myeloma, and their effects can be efficiently counteracted by a class of tumor suppressor miRNAs, named epi-miRNAs. Given the oncogenic role of histone deacetylases (HDAC) in multiple myeloma, we investigated whether their activity cou...

journal_title：Molecular cancer therapeutics

authors： Amodio N,Stamato MA,Gullà AM,Morelli E,Romeo E,Raimondi L,Pitari MR,Ferrandino I,Misso G,Caraglia M,Perrotta I,Neri A,Fulciniti M,Rolfo C,Anderson KC,Munshi NC,Tagliaferri P,Tassone P

更新日期：2016-06-01 00:00:00