Discovery and characterization of novel mutant FLT3 kinase inhibitors.

abstract：:Tumor-specific tissue-penetrating peptides deliver drugs into extravascular tumor tissue by increasing tumor vascular permeability through interaction with neuropilin (NRP). Here, we report that a prototypic tumor-penetrating peptide iRGD (amino acid sequence: CRGDKGPDC) potently inhibits spontaneous metastasis in mic...

journal_title：Molecular cancer therapeutics

authors： Sugahara KN,Braun GB,de Mendoza TH,Kotamraju VR,French RP,Lowy AM,Teesalu T,Ruoslahti E

更新日期：2015-01-01 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：:Histopathologic grading of astrocytic tumors based on current WHO criteria offers a valuable but simplified representation of oncologic reality and is often insufficient to predict clinical outcome. In this study, we report a new astrocytic tumor microarray gene expression data set (n = 65). We have used a simple arti...

journal_title：Molecular cancer therapeutics

authors： Petalidis LP,Oulas A,Backlund M,Wayland MT,Liu L,Plant K,Happerfield L,Freeman TC,Poirazi P,Collins VP

更新日期：2008-05-01 00:00:00

abstract：:Pulmonary metastasis is the most significant prognostic determinant for osteosarcoma, but methods for its prediction and treatment have not been established. Using oligonucleotide microarrays, we compared the global gene expression of biopsy samples between seven osteosarcoma patients who developed pulmonary metastasi...

journal_title：Molecular cancer therapeutics

authors： Kobayashi E,Masuda M,Nakayama R,Ichikawa H,Satow R,Shitashige M,Honda K,Yamaguchi U,Shoji A,Tochigi N,Morioka H,Toyama Y,Hirohashi S,Kawai A,Yamada T

更新日期：2010-03-01 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：:IPI-504 is a novel, highly soluble small-molecule inhibitor of heat shock protein 90 (Hsp90), a protein chaperone essential for regulating homeostasis of oncoproteins and cell signaling proteins. Human epidermal growth factor receptor 2 (HER2; ErbB2) oncoprotein, expressed in a subset of metastatic breast cancers, is ...

journal_title：Molecular cancer therapeutics

authors： Leow CC,Chesebrough J,Coffman KT,Fazenbaker CA,Gooya J,Weng D,Coats S,Jackson D,Jallal B,Chang Y

更新日期：2009-08-01 00:00:00

abstract：:R-roscovitine (seliciclib, CYC202) is a cyclin-dependent kinase inhibitor currently in phase II clinical trials in patients with cancer. Here, we describe its mouse metabolism and pharmacokinetics as well as the identification of the principal metabolites in hepatic microsomes, plasma, and urine. Following microsomal ...

journal_title：Molecular cancer therapeutics

authors： Nutley BP,Raynaud FI,Wilson SC,Fischer PM,Hayes A,Goddard PM,McClue SJ,Jarman M,Lane DP,Workman P

更新日期：2005-01-01 00:00:00

abstract：:Crizotinib (PF02341066) is a tyrosine kinase inhibitor of anaplastic lymphoma kinase (ALK) that has been shown to selectively inhibit growth of cancer cells that harbor the EML4-ALK fusion found in a subset of patients with non-small cell lung cancer (NSCLC). While in clinical trials, PF02341066 has shown a significan...

journal_title：Molecular cancer therapeutics

authors： Sun Y,Nowak KA,Zaorsky NG,Winchester CL,Dalal K,Giacalone NJ,Liu N,Werner-Wasik M,Wasik MA,Dicker AP,Lu B

更新日期：2013-05-01 00:00:00

abstract：:Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), a member of the tumor necrosis factor superfamily, is in clinical trials for cancer therapy, but its anticancer potential is limited by the development of resistance. We investigated the ability of tocotrienol (T3), an unsaturated vitamin E present in pa...

journal_title：Molecular cancer therapeutics

authors： Kannappan R,Ravindran J,Prasad S,Sung B,Yadav VR,Reuter S,Chaturvedi MM,Aggarwal BB

更新日期：2010-08-01 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：: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：:We investigated integrin-linked kinase (ILK), a focal adhesion serine-threonine protein kinase, as a new molecular target for treating anaplastic thyroid cancer. ILK mediates cell growth and survival signals and is overexpressed in a number of cancers. Therefore, we hypothesized that inhibition of ILK leads to growth ...

journal_title：Molecular cancer therapeutics

authors： Younes MN,Kim S,Yigitbasi OG,Mandal M,Jasser SA,Dakak Yazici Y,Schiff BA,El-Naggar A,Bekele BN,Mills GB,Myers JN

更新日期：2005-08-01 00:00:00

abstract：:The breast-specific antigen alpha-lactalbumin is expressed in >60% of breast cancer tissues. To evaluate the effect of gene therapy for breast cancer by controlling adenovirus replication with human alpha-lactalbumin promoter, we investigated the activity of a 762-bp human alpha-lactalbumin promoter. Alpha-lactalbumin...

journal_title：Molecular cancer therapeutics

authors： Li X,Zhang J,Gao H,Vieth E,Bae KH,Zhang YP,Lee SJ,Raikwar S,Gardner TA,Hutchins GD,VanderPutten D,Kao C,Jeng MH

更新日期：2005-12-01 00:00:00

abstract：:Invasion into deep myometrium and/or lymphovascular space is a well-known risk factor for endometrial cancer metastasis, resulting in poor prognosis. It is therefore clinically important to identify novel molecules that suppress tumor invasion. Reduced expression of the metastasis suppressor, kisspeptin (KISS1), and i...

journal_title：Molecular cancer therapeutics

authors： Kang HS,Baba T,Mandai M,Matsumura N,Hamanishi J,Kharma B,Kondoh E,Yoshioka Y,Oishi S,Fujii N,Murphy SK,Konishi I

更新日期：2011-04-01 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：: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

abstract：:Recombinant immunotoxins, consisting of single-chain variable fragments (scFv) genetically fused to polypeptide toxins, represent potentially effective candidates for cancer therapeutics. We evaluated the affinity of various anti-Her2/neu scFv fused to recombinant gelonin (rGel) and its effect on antitumor efficacy an...

journal_title：Molecular cancer therapeutics

authors： Cao Y,Marks JD,Huang Q,Rudnick SI,Xiong C,Hittelman WN,Wen X,Marks JW,Cheung LH,Boland K,Li C,Adams GP,Rosenblum MG

更新日期：2012-01-01 00:00:00

abstract：:Prostate-specific membrane antigen (PSMA) is a membrane protein that is overexpressed manifold in prostate cancer and provides an attractive target for therapy. PSMA ADC is an antibody-drug conjugate (ADC) that consists of a fully human anti-PSMA monoclonal antibody conjugated to monomethylauristatin E through a valin...

journal_title：Molecular cancer therapeutics

authors： Wang X,Ma D,Olson WC,Heston WD

更新日期：2011-09-01 00:00:00

abstract：:Tivantinib (ARQ197) was first reported as a highly selective inhibitor of c-MET and is currently being investigated in a phase III clinical trial. However, as recently reported by us and another group, tivantinib showed cytotoxic activity independent of cellular c-MET status and also disrupted microtubule dynamics. To...

journal_title：Molecular cancer therapeutics

authors： Aoyama A,Katayama R,Oh-Hara T,Sato S,Okuno Y,Fujita N

更新日期：2014-12-01 00:00:00

abstract：:Disruption of Cyclin-Dependent Kinase 12 (CDK12) is known to lead to defects in DNA repair and sensitivity to platinum salts and PARP1/2 inhibitors. However, CDK12 has also been proposed as an oncogene in breast cancer. We therefore aimed to assess the frequency and distribution of CDK12 protein expression by IHC in i...

journal_title：Molecular cancer therapeutics

authors： Naidoo K,Wai PT,Maguire SL,Daley F,Haider S,Kriplani D,Campbell J,Mirza H,Grigoriadis A,Tutt A,Moseley PM,Abdel-Fatah TMA,Chan SYT,Madhusudan S,Rhaka EA,Ellis IO,Lord CJ,Yuan Y,Green AR,Natrajan R

更新日期：2018-01-01 00:00:00

abstract：:Cadmium (Cd) is an ubiquitous environmental carcinogen. Membrane phospholipids as well as fatty acid profile of membrane phospholipids are known to be altered in tumorigenicity and malignancy. Synthesis of cellular phosphatidylcholine (PC) has been used as a marker for membrane proliferation in the neoplastic mammary ...

journal_title：Molecular cancer therapeutics

authors： Sinha Roy S,Mukherjee S,Mukhopadhyay S,Das SK

更新日期：2004-02-01 00:00:00

abstract：:The Notch signaling pathway has been implicated in cell fate determination and differentiation in many tissues. Accumulating evidence points toward a pivotal role in blood vessel formation, and the importance of the Delta-like ligand (Dll) 4-Notch1 ligand-receptor interaction has been shown in both physiological and t...

journal_title：Molecular cancer therapeutics

authors： Jenkins DW,Ross S,Veldman-Jones M,Foltz IN,Clavette BC,Manchulenko K,Eberlein C,Kendrew J,Petteruti P,Cho S,Damschroder M,Peng L,Baker D,Smith NR,Weir HM,Blakey DC,Bedian V,Barry ST

更新日期：2012-08-01 00:00:00

abstract：:Histone modification has emerged as a promising approach to cancer therapy. We explored the efficacy of a novel class of histone deacetylase inhibitors in the treatment of malignant gliomas. Treatment of glioma cell lines with two butyric acid derivatives, pivaloylomethyl butyrate (AN-9) and butyroyloxymethyl butyrate...

journal_title：Molecular cancer therapeutics

authors： Entin-Meer M,Rephaeli A,Yang X,Nudelman A,VandenBerg SR,Haas-Kogan DA

更新日期：2005-12-01 00:00:00

abstract：:Tumor-associated M2-macrophages are one of the most abundant immunosuppressive cell types in the pancreatic ductal adenocarcinoma (PDAC) tumor microenvironment (TME). However, the molecular mechanisms responsible for the generation of M2-macrophages are unclear. Here, we demonstrated that overexpression of DCLK1-isofo...

journal_title：Molecular cancer therapeutics

authors： Chandrakesan P,Panneerselvam J,May R,Weygant N,Qu D,Berry WR,Pitts K,Stanger BZ,Rao CV,Bronze MS,Houchen CW

更新日期：2020-07-01 00:00:00

abstract：:Previous studies have shown a statistically significant correlation between human carcinomas and monoclonal antibody detection of a Mycoplasma hyorhinis-encoded protein known as p37. A potential mechanism of p37 is that it might promote invasion and metastasis. Recombinant p37 enhanced the invasiveness of two prostate...

journal_title：Molecular cancer therapeutics

authors： Ketcham CM,Anai S,Reutzel R,Sheng S,Schuster SM,Brenes RB,Agbandje-McKenna M,McKenna R,Rosser CJ,Boehlein SK

更新日期：2005-07-01 00:00:00

abstract：:Multitargeted kinase inhibitors have shown clinical efficacy in a range of cancer types. However, two major problems associated with these drugs are the low fraction of patients for which these treatments provide initial clinical benefit and the occurrence of resistance during prolonged therapy. Several types of predi...

journal_title：Molecular cancer therapeutics

authors： Versele M,Talloen W,Rockx C,Geerts T,Janssen B,Lavrijssen T,King P,Göhlmann HW,Page M,Perera T

更新日期：2009-07-01 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：:The traditional maximum dose density chemotherapy renders the tumor patients not only the tumor remission but the chemotherapy resistance and more adverse side effects. According to the widely positive expression of Toll-like receptor (TLR)-3 in oral squamous cell carcinoma (OSCC) patients (n = 166), we here provided ...

journal_title：Molecular cancer therapeutics

authors： Ding L,Ren J,Zhang D,Li Y,Huang X,Ji J,Hu Q,Wang H,Ni Y,Hou Y

更新日期：2017-06-01 00:00:00

abstract：:Several studies have identified silibinin as an anticarcinogenic agent. Recently, we showed that silibinin inhibits cell growth via G1 arrest, leading to differentiation of androgen-dependent human prostate carcinoma LNCaP cells (X. Zi and R. Agarwal, Proc. Natl. Acad. Sci. USA, 96: 7490-7495,1999). Here, we extend th...

journal_title：Molecular cancer therapeutics

authors： Tyagi A,Agarwal C,Agarwal R

更新日期：2002-05-01 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