Camptothecin poly[n-(2-hydroxypropyl) methacrylamide] copolymers in antitopoisomerase-I tumor therapy: intratumor release and antitumor efficacy.

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：: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：:Ascofuranone has been shown to have antitumor activity, but the precise molecular mechanism by which it inhibits the proliferation of cancer cells remains unclear. Here, we study the effects of ascofuranone on cell cycle progression in human cancer cells and find that ascofuranone induces G(1) arrest without cytoxicit...

journal_title：Molecular cancer therapeutics

authors： Jeong JH,Kang SS,Park KK,Chang HW,Magae J,Chang YC

更新日期：2010-07-01 00:00:00

abstract：:The primary mechanism of antibody-drug conjugates (ADC) is targeted delivery of a cytotoxic payload to tumor cells via cancer-associated membrane receptors. However, the tumor microenvironment likely plays a role in ADC penetration, distribution, and processing and thus impacts the overall antitumor activity. Here, we...

journal_title：Molecular cancer therapeutics

authors： Li F,Ulrich M,Jonas M,Stone IJ,Linares G,Zhang X,Westendorf L,Benjamin DR,Law CL

更新日期：2017-07-01 00:00:00

abstract：:DNA repair mechanisms are crucial for cell survival. It increases the cancer cell's ability to resist DNA damage. FEN1 is involved in DNA replication and repair, specifically long-patch base excision repair. Although the gene function and post-translational modification of FEN1 are well studied, the regulatory mechani...

journal_title：Molecular cancer therapeutics

authors： Zhu H,Wu C,Wu T,Xia W,Ci S,He W,Zhang Y,Li L,Zhou S,Zhang J,Edick AM,Zhang A,Pan FY,Hu Z,He L,Guo Z

更新日期：2019-12-01 00:00:00

abstract：:Lavendamycin is a bacterially derived quinolinedione that displays significant antimicrobial and antitumor activities. However, preclinical development of lavendamycin as an anticancer agent was halted due to the poor aqueous solubility and relatively nonspecific cytotoxic activity of this compound. In this report, we...

journal_title：Molecular cancer therapeutics

authors： Fang Y,Linardic CM,Richardson DA,Cai W,Behforouz M,Abraham RT

更新日期：2003-06-01 00:00:00

abstract：:Allicin (diallyl thiosulfinate), a highly active component in extracts of freshly crushed garlic, is the interaction product of non-protein amino acid alliin (S-allyl-L-cysteine sulfoxide) with the enzyme alliinase (alliin lyase; EC 4.4.1.4). Allicin was shown to be toxic in various mammalian cells in a dose-dependent...

journal_title：Molecular cancer therapeutics

authors： Miron T,Mironchik M,Mirelman D,Wilchek M,Rabinkov A

更新日期：2003-12-01 00:00:00

abstract：:Ewing's sarcoma is a pediatric cancer of the bone that is characterized by the expression of the chimeric transcription factor EWS-FLI1 that confers a highly malignant phenotype and results from the chromosomal translocation t(11;22)(q24;q12). Poor overall survival and pronounced long-term side effects associated with...

journal_title：Molecular cancer therapeutics

authors： Winter GE,Rix U,Lissat A,Stukalov A,Müllner MK,Bennett KL,Colinge J,Nijman SM,Kubicek S,Kovar H,Kontny U,Superti-Furga G

更新日期：2011-10-01 00:00:00

abstract：:Phortress is a novel, potent, and selective experimental antitumor agent. Its mechanism of action involves induction of CYP1A1-catalyzed biotransformation of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203) to generate electrophilic species, which covalently bind to DNA, exacting lethal damage to sensitive tu...

journal_title：Molecular cancer therapeutics

authors： Leong CO,Suggitt M,Swaine DJ,Bibby MC,Stevens MF,Bradshaw TD

更新日期：2004-12-01 00:00:00

abstract：:The spindle assembly checkpoint kinase TTK (Mps1) is a key regulator of chromosome segregation and is the subject of novel targeted therapy approaches by small-molecule inhibitors. Although the first TTK inhibitors have entered phase I dose escalating studies in combination with taxane chemotherapy, a patient stratifi...

journal_title：Molecular cancer therapeutics

authors： Zaman GJR,de Roos JADM,Libouban MAA,Prinsen MBW,de Man J,Buijsman RC,Uitdehaag JCM

更新日期：2017-11-01 00:00:00

abstract：:Stem cell factor (SCF)/Kit and insulin-like growth factor-I (IGF-I)/IGF-I receptor (IGF-IR) autocrine loops play a prominent role in the growth of small cell lung cancer (SCLC). Previous data suggested that IGF-I protects cells from apoptosis induced by STI571, an efficient inhibitor of Kit signal transduction, by act...

journal_title：Molecular cancer therapeutics

authors： Warshamana-Greene GS,Litz J,Buchdunger E,Hofmann F,García-Echeverría C,Krystal GW

更新日期：2004-05-01 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：: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：:Nasopharyngeal carcinoma (NPC) is relatively rare in Western countries but is a common cancer in southern Asia. Many differentially expressed genes have been linked to NPC; however, how to prioritize therapeutic targets and potential drugs from unsorted gene lists remains largely unknown. We first collected 558 upregu...

journal_title：Molecular cancer therapeutics

authors： Lan MY,Chen CL,Lin KT,Lee SA,Yang WL,Hsu CN,Wu JC,Ho CY,Lin JC,Huang CY

更新日期：2010-09-01 00:00:00

abstract：:Multiple myeloma remains incurable and the majority of patients die within 5 years of diagnosis. Reolysin, the infusible form of human reovirus (RV), is a novel viral oncolytic therapy associated with antitumor activity likely resulting from direct oncolysis and a virus-mediated antitumor immune response. Results from...

journal_title：Molecular cancer therapeutics

authors： Stiff A,Caserta E,Sborov DW,Nuovo GJ,Mo X,Schlotter SY,Canella A,Smith E,Badway J,Old M,Jaime-Ramirez AC,Yan P,Benson DM,Byrd JC,Baiocchi R,Kaur B,Hofmeister CC,Pichiorri F

更新日期：2016-05-01 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：: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：: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：:We discovered a thalidomide analogue [5-hydroxy-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33)] with antiproliferative activity against nine cancer cell lines in vitro. Flow cytometric analyses showed that the compound caused G2-M arrest, which occurred mainly at the mitotic phase. In addition, immunofluores...

journal_title：Molecular cancer therapeutics

authors： Li PK,Pandit B,Sackett DL,Hu Z,Zink J,Zhi J,Freeman D,Robey RW,Werbovetz K,Lewis A,Li C

更新日期：2006-02-01 00:00:00

abstract：:Several studies have shown antitumor activities of the melanoma differentiation-associated gene 7 (mda-7) and the nonsteroidal anti-inflammatory drug sulindac when used as a monotherapies against a wide variety of human cancers. However, the combined effects of mda-7 and sulindac have not previously been tested. There...

journal_title：Molecular cancer therapeutics

authors： Oida Y,Gopalan B,Miyahara R,Inoue S,Branch CD,Mhashilkar AM,Lin E,Bekele BN,Roth JA,Chada S,Ramesh R

更新日期：2005-02-01 00:00:00

abstract：:2-Amino-4,4alpha-dihydro-4alpha,7-dimethyl-3H-phenoxazine-3-one (Phx-1) has been developed as a novel phenoxazine derivative having an anticancer activity on a variety of cancer cell lines as well as transplanted tumors in mice with minimal toxicity to normal cells. We examined the effects of Phx-1 on Jurkat cells, a ...

journal_title：Molecular cancer therapeutics

authors： Hara K,Okamoto M,Aki T,Yagita H,Tanaka H,Mizukami Y,Nakamura H,Tomoda A,Hamasaki N,Kang D

更新日期：2005-07-01 00:00:00

abstract：:Activin receptor-like kinase-1 (ALK1) is a type I, endothelial cell-specific member of the transforming growth factor-beta superfamily of receptors known to play an essential role in modulating angiogenesis and vessel maintenance. In the present study, we sought to examine the angiogenic and tumorigenic effects mediat...

journal_title：Molecular cancer therapeutics

authors： Mitchell D,Pobre EG,Mulivor AW,Grinberg AV,Castonguay R,Monnell TE,Solban N,Ucran JA,Pearsall RS,Underwood KW,Seehra J,Kumar R

更新日期：2010-02-01 00:00:00

abstract：:Gallium nitrate is a metallodrug with clinical efficacy in non-Hodgkin's lymphoma. Its mechanisms of antineoplastic action are not fully understood. In the present study, we investigated the roles of transferrin receptor (TfR) targeting and apoptotic pathways in gallium-induced cell death. Although DoHH2 lymphoma cell...

journal_title：Molecular cancer therapeutics

authors： Chitambar CR,Wereley JP,Matsuyama S

更新日期：2006-11-01 00:00:00

abstract：:Targeting death receptor-mediated apoptosis has emerged as an effective strategy for cancer therapy. However, certain types of cancer cells are intrinsically resistant to death receptor-mediated apoptosis. In an effort to identify agents that can sensitize cancer cells to death receptor-induced apoptosis, we have iden...

journal_title：Molecular cancer therapeutics

authors： Raja SM,Chen S,Yue P,Acker TM,Lefkove B,Arbiser JL,Khuri FR,Sun SY

更新日期：2008-07-01 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：:Melanoma is a highly drug-resistant cancer with resistance developing to agents targeting single proteins. To circumvent this problem, a new class of agent inhibiting multiple key pathways important in this disease is being developed to reduce the likelihood of developing resistant disease. The phosphoinositide 3-kina...

journal_title：Molecular cancer therapeutics

authors： Gowda R,Madhunapantula SV,Kuzu OF,Sharma A,Robertson GP

更新日期：2014-07-01 00:00:00

abstract：:Replication protein A (RPA) is a single-strand DNA-binding protein with essential roles in DNA replication, recombination, and repair. It is necessary for the formation of the preincision complex that is required for proper incision of damaged DNA nucleotides during DNA repair. We have previously identified small mole...

journal_title：Molecular cancer therapeutics

authors： Neher TM,Bodenmiller D,Fitch RW,Jalal SI,Turchi JJ

更新日期：2011-10-01 00:00:00

abstract：:Hepatocyte growth factor/scatter factor (HGF/SF) and its receptor, c-Met, have been implicated in the growth and progression of a variety of solid human tumors. Thus, inhibiting HGF/SF:c-Met signaling may provide a novel therapeutic approach for treating human tumors. We have generated and characterized fully human mo...

journal_title：Molecular cancer therapeutics

authors： Gao CF,Xie Q,Zhang YW,Su Y,Zhao P,Cao B,Furge K,Sun J,Rex K,Osgood T,Coxon A,Burgess TL,Vande Woude GF

更新日期：2009-10-01 00:00:00

abstract：:Transforming growth factor (TGF)-β contributes to the malignant phenotype of glioblastoma by promoting invasiveness and angiogenesis and creating an immunosuppressive microenvironment. So far, TGF-β1 and TGF-β2 isoforms have been considered to act in a similar fashion without isoform-specific function in glioblastoma....

journal_title：Molecular cancer therapeutics

authors： Seystahl K,Papachristodoulou A,Burghardt I,Schneider H,Hasenbach K,Janicot M,Roth P,Weller M

更新日期：2017-06-01 00:00:00

abstract：:Histone deacetylase inhibitors have emerged as promising anticancer drugs. Using an unbiased ultrahigh throughput screening system, a novel mercaptoketone-based histone deacetylase inhibitor series was identified that was optimized to the lead compound, KD5170. KD5170 inhibited the proliferation of myeloma cell lines ...

journal_title：Molecular cancer therapeutics

authors： Feng R,Ma H,Hassig CA,Payne JE,Smith ND,Mapara MY,Hager JH,Lentzsch S

更新日期：2008-06-01 00:00:00