A novel antiandrogen, Compound 30, suppresses castration-resistant and MDV3100-resistant prostate cancer growth in vitro and in vivo.

abstract：:EP-100 is a synthetic lytic peptide that specifically targets the gonadotropin-releasing hormone receptor on cancer cells. To extend the utility of EP-100, we aimed to identify effective combination therapies with EP-100 for ovarian cancer and explore potential mechanisms of this combination. A series of in vitro (MTT...

journal_title：Molecular cancer therapeutics

authors： Ma S,Pradeep S,Villar-Prados A,Wen Y,Bayraktar E,Mangala LS,Kim MS,Wu SY,Hu W,Rodriguez-Aguayo C,Leuschner C,Liang X,Ram PT,Schlacher K,Coleman RL,Sood AK

更新日期：2019-05-01 00:00:00

abstract：:Aberrant overexpression of antiapoptotic members of the Bcl-2 protein family, including Bcl-2 and Bcl-X(L), contributes to malignant transformation and subsequent resistance to traditional chemotherapeutics. Thus, these proteins represent attractive targets for novel anticancer agents. The small molecule, gossypol, wa...

journal_title：Molecular cancer therapeutics

authors： Oliver CL,Miranda MB,Shangary S,Land S,Wang S,Johnson DE

更新日期：2005-01-01 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDA) is an aggressive malignancy with one of the worst outcomes among all cancers. PDA often recurs after initial treatment to result in patient death despite the use of chemotherapy or radiation therapy. PDA contains a subset of tumor-initiating cells capable of extensive self-renewa...

journal_title：Molecular cancer therapeutics

authors： Rajeshkumar NV,Rasheed ZA,García-García E,López-Ríos F,Fujiwara K,Matsui WH,Hidalgo M

更新日期：2010-09-01 00:00:00

abstract：:Molecular mechanisms underlying epothilone-induced apoptotic cell death were investigated in SW620 human colon cancer cells. Treatment with epothilone B and D at different concentrations (1-100 nmol/L) dose-dependently inhibited cell growth and caused cell cycle arrest at G2-M, which was followed by apoptosis. Consist...

journal_title：Molecular cancer therapeutics

authors： Lee SH,Son SM,Son DJ,Kim SM,Kim TJ,Song S,Moon DC,Lee HW,Ryu JC,Yoon DY,Hong JT

更新日期：2007-10-01 00:00:00

abstract：:Histone deacetylase inhibitors represent a promising new class of anticancer agents. In the current investigation, we examined the activity of PXD101, a potent histone deacetylase inhibitor, used alone or in combination with clinically relevant chemotherapeutics (docetaxel, paclitaxel, and carboplatin), in preclinical...

journal_title：Molecular cancer therapeutics

authors： Qian X,LaRochelle WJ,Ara G,Wu F,Petersen KD,Thougaard A,Sehested M,Lichenstein HS,Jeffers M

更新日期：2006-08-01 00:00:00

abstract：:Tumors can exploit the indoleamine 2,3-dioxygenase 1 (IDO1) pathway to create an immunosuppressive microenvironment. Activated IDO1 metabolizes tryptophan into immunosuppressive kynurenine, leading to suppressed effector T-cell (Teff) proliferation, allowing for tumor escape from host immune surveillance. IDO1 inhibit...

journal_title：Molecular cancer therapeutics

authors： Balog A,Lin TA,Maley D,Gullo-Brown J,Kandoussi EH,Zeng J,Hunt JT

更新日期：2020-12-09 00:00:00

abstract：:The challenge of developing effective pharmacodynamic biomarkers for preclinical and clinical testing of FGFR signaling inhibition is significant. Assays that rely on the measurement of phospho-protein epitopes can be limited by the availability of effective antibody detection reagents. Transcript profiling enables ac...

journal_title：Molecular cancer therapeutics

authors： Delpuech O,Rooney C,Mooney L,Baker D,Shaw R,Dymond M,Wang D,Zhang P,Cross S,Veldman-Jones M,Wilson J,Davies BR,Dry JR,Kilgour E,Smith PD

更新日期：2016-11-01 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：:Glycosylation is a complex multienzyme-related process that is frequently deregulated in cancer. Aberrant glycosylation can lead to the generation of novel tumor surface-specific glycotopes that can be targeted by antibodies. Murine DS6 mAb (muDS6) was generated from serous ovary adenocarcinoma immunization. It recogn...

journal_title：Molecular cancer therapeutics

authors： Nicolazzi C,Caron A,Tellier A,Trombe M,Pinkas J,Payne G,Carrez C,Guérif S,Maguin M,Baffa R,Fassan M,Adam J,Mangatal-Wade L,Blanc V

更新日期：2020-08-01 00:00:00

abstract：:Previous studies from our laboratory have identified several endothelial cell-associated marker genes implicated in human melanoma metastasis via tumor vasculogenic mimicry. In this study, we used dual model systems composed of melanoma cell lines and clinical melanoma samples to validate the importance of insulin-lik...

journal_title：Molecular cancer therapeutics

authors： Xi Y,Nakajima G,Hamil T,Fodstad O,Riker A,Ju J

更新日期：2006-12-01 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：:DNA damage repair capacity is required for cells to survive catastrophic DNA damage and proliferate under conditions of intratumoral stress. The ability of the minor histone protein H2AX to serve as a hub for the assembly of a productive DNA damage repair complex is a necessary step in preventing DNA damage-induced ce...

journal_title：Molecular cancer therapeutics

authors： Wang Y,Pandey RN,Riffle S,Chintala H,Wikenheiser-Brokamp KA,Hegde RS

更新日期：2018-08-01 00:00:00

abstract：:Malignant mesothelioma is an aggressive tumor of the serosal surfaces of the lungs, heart, and abdomen. Survival rates are poor and effective treatments are not available. However, recent therapeutic regimens targeting thymidylate synthase (TS) in malignant mesothelioma patients have shown promise. We have reported th...

journal_title：Molecular cancer therapeutics

authors： Flynn J,Berg RW,Wong T,van Aken M,Vincent MD,Fukushima M,Koropatnick J

更新日期：2006-06-01 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：:There is an urgent need for the development of novel therapies to treat pancreatic cancer, which is among the most lethal of all cancers. KRAS-activating mutations, which are found in more than 90% of pancreatic adenocarcinomas, drive tumor dependency on the Ras/MAPK and Akt signaling pathways. Radiation is currently ...

journal_title：Molecular cancer therapeutics

authors： Williams TM,Flecha AR,Keller P,Ram A,Karnak D,Galbán S,Galbán CJ,Ross BD,Lawrence TS,Rehemtulla A,Sebolt-Leopold J

更新日期：2012-05-01 00:00:00

abstract：:Small cell lung cancer (SCLC) has a poor prognosis. Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase regulating cell proliferation, survival, migration, and invasion, which is overexpressed and/or activated in several cancers, including SCLC. We wanted to determine whether FAK contributes to SCLC aggressi...

journal_title：Molecular cancer therapeutics

authors： Aboubakar Nana F,Lecocq M,Ladjemi MZ,Detry B,Dupasquier S,Feron O,Massion PP,Sibille Y,Pilette C,Ocak S

更新日期：2019-01-01 00:00:00

abstract：:RX-5902 is a first-in-class anticancer agent targeting phosphorylated-p68 and attenuating nuclear shuttling of β-catenin. The purpose of this study was to evaluate the efficacy of RX-5902 in preclinical models of triple-negative breast cancer (TNBC) and to explore effects on β-catenin expression. A panel of 18 TNBC ce...

journal_title：Molecular cancer therapeutics

authors： Capasso A,Bagby SM,Dailey KL,Currimjee N,Yacob BW,Ionkina A,Frank JG,Kim DJ,George C,Lee YB,Benaim E,Gittleman B,Hartman SJ,Tan AC,Kim J,Pitts TM,Eckhardt SG,Tentler JJ,Diamond JR

更新日期：2019-11-01 00:00:00

abstract：:Using a luciferase reporter-based high-throughput chemical library screen and topological data analysis, we identified N-acridine-9-yl-N',N'-dimethylpropane-1,3-diamine (DAPA) as an inhibitor of the inositol requiring kinase 1α (IRE1α)-X-box binding protein-1 (XBP1) pathway of the unfolded protein response. We designe...

journal_title：Molecular cancer therapeutics

authors： Jiang D,Tam AB,Alagappan M,Hay MP,Gupta A,Kozak MM,Solow-Cordero DE,Lum PY,Denko NC,Giaccia AJ,Le QT,Niwa M,Koong AC

更新日期：2016-09-01 00:00:00

abstract：OBJECTIVE:Targeting the tumor vasculature may offer an alternative or complementary therapeutic approach to targeting growth factor signaling in lung cancer. The aim of these studies was to evaluate the antitumor effects in vivo of the combination of ZD6126, a tumor-selective vascular-targeting agent; ZD1839 (gefitinib...

journal_title：Molecular cancer therapeutics

authors： Raben D,Bianco C,Damiano V,Bianco R,Melisi D,Mignogna C,D'Armiento FP,Cionini L,Bianco AR,Tortora G,Ciardiello F,Bunn P

更新日期：2004-08-01 00:00:00

abstract：:Antibody-drug conjugates (ADC), potent cytotoxic drugs linked to antibodies via chemical linkers, allow specific targeting of drugs to neoplastic cells. We have used this technology to develop the ADC DCDT2980S that targets CD22, an antigen with expression limited to B cells and the vast majority of non-Hodgkin lympho...

journal_title：Molecular cancer therapeutics

authors： Li D,Poon KA,Yu SF,Dere R,Go M,Lau J,Zheng B,Elkins K,Danilenko D,Kozak KR,Chan P,Chuh J,Shi X,Nazzal D,Fuh F,McBride J,Ramakrishnan V,de Tute R,Rawstron A,Jack AS,Deng R,Chu YW,Dornan D,Williams M,Ho W,

更新日期：2013-07-01 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 oncoprotein Eps8 facilitates proliferation in fibroblasts and colon cancer cells. However, its role in human cervical cancer is unclear. By immunohistochemical staining and Western blotting, aberrant Eps8 expression was observed in cervical carcinoma compared with normal cervical epithelial cells. Clinicopathologi...

journal_title：Molecular cancer therapeutics

authors： Chen YJ,Shen MR,Chen YJ,Maa MC,Leu TH

更新日期：2008-06-01 00:00:00

abstract：:This study aimed to investigate the antitumor and antiangiogenic effects utilizing a novel therapy regimen of metronomic topotecan and pazopanib, a multireceptor tyrosine kinase inhibitor. In vitro (Western blot) and in vivo dose-finding experiments were done following pazopanib therapy in ovarian cancer models. Pazop...

journal_title：Molecular cancer therapeutics

authors： Merritt WM,Nick AM,Carroll AR,Lu C,Matsuo K,Dumble M,Jennings N,Zhang S,Lin YG,Spannuth WA,Kamat AA,Stone RL,Shahzad MM,Coleman RL,Kumar R,Sood AK

更新日期：2010-04-01 00:00:00

abstract：:Breast cancer is a major public health problem all over the world, and the current treatment strategies are not potent enough for some patients, especially those with triple-negative breast cancer (TNBC). Recent studies have demonstrated that microRNAs (miRNA) play vital roles in the development of TNBC. In this study...

journal_title：Molecular cancer therapeutics

authors： Tang H,Liu P,Yang L,Xie X,Ye F,Wu M,Liu X,Chen B,Zhang L,Xie X

更新日期：2014-12-01 00:00:00

abstract：:We reported previously a significant increase in survival of nude rats harboring orthotopic A549 human non-small cell lung cancer tumors after treatment with a combination of exisulind (Sulindac Sulfone) and docetaxel (D. C. Chan, Clin. Cancer Res., 8: 904-912, 2002). The purpose of the current study was to determine ...

journal_title：Molecular cancer therapeutics

authors： Whitehead CM,Earle KA,Fetter J,Xu S,Hartman T,Chan DC,Zhao TL,Piazza G,Klein-Szanto AJ,Pamukcu R,Alila H,Bunn PA Jr,Thompson WJ

更新日期：2003-05-01 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：: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：:Protein tyrosine kinases of the Janus kinase (JAK) family are associated with many cytokine receptors, which, on ligand binding, regulate important cellular functions such as proliferation, survival, and differentiation. In multiple myeloma, JAKs may be persistently activated due to a constant stimulation by interleuk...

journal_title：Molecular cancer therapeutics

authors： Burger R,Le Gouill S,Tai YT,Shringarpure R,Tassone P,Neri P,Podar K,Catley L,Hideshima T,Chauhan D,Caulder E,Neilan CL,Vaddi K,Li J,Gramatzki M,Fridman JS,Anderson KC

更新日期：2009-01-01 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：:HER2-targeted therapies, such as trastuzumab, have increased the survival rates of HER2+ breast cancer patients. However, despite these therapies, many tumors eventually develop resistance to these therapies. Our lab previously reported an unexpected sensitivity of HER2+ breast cancer cells to poly (ADP-ribose) polyme...

journal_title：Molecular cancer therapeutics

authors： Wielgos ME,Zhang Z,Rajbhandari R,Cooper TS,Zeng L,Forero A,Esteva FJ,Osborne CK,Schiff R,LoBuglio AF,Nozell SE,Yang ES

更新日期：2018-05-01 00:00:00