The natural product honokiol preferentially inhibits cellular FLICE-inhibitory protein and augments death receptor-induced apoptosis.

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：:Squamous cell carcinoma (SCC) is one of the most common human cancers worldwide. Recent studies show that regulatory T cells (Treg) have a critical role in the modulation of an antitumor immune response, and consequently the SCC development. Because the accumulation of Tregs at the tumor site is, in part, due to selec...

journal_title：Molecular cancer therapeutics

authors： de Oliveira CE,Gasparoto TH,Pinheiro CR,Amôr NG,Nogueira MRS,Kaneno R,Garlet GP,Lara VS,Silva JS,Cavassani KA,Campanelli AP

更新日期：2017-12-01 00:00:00

abstract：:CEP-7055, a fully synthetic, orally active N,N-dimethylglycine ester of CEP-5214, a C3-(isopropylmethoxy)-fused pyrrolocarbazole with potent pan-vascular endothelial growth factor receptor (VEGFR) kinase inhibitory activity, has recently completed phase I clinical trials in cancer patients. These studies evaluated the...

journal_title：Molecular cancer therapeutics

authors： Jones-Bolin S,Zhao H,Hunter K,Klein-Szanto A,Ruggeri B

更新日期：2006-07-01 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：: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：: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：:Although gemcitabine is the standard chemotherapeutic drug for treatment of pancreatic cancer, almost all patients eventually develop resistance to this agent. Previous studies identified Polo-like kinase 1 (Plk1) as the mediator of gemcitabine resistance, but the molecular mechanism remains unknown. In this study, we...

journal_title：Molecular cancer therapeutics

authors： Song B,Liu XS,Rice SJ,Kuang S,Elzey BD,Konieczny SF,Ratliff TL,Hazbun T,Chiorean EG,Liu X

更新日期：2013-01-01 00:00:00

abstract：:Tumor-associated urokinase plasminogen activator (uPA) is a critical marker of invasion and metastasis, has strong prognostic relevance, and is thus a potential therapeutic target. Experimental data published to date has established the proof-of-principle of uPA targeting by (213)Bi-labeled plasminogen activator inhib...

journal_title：Molecular cancer therapeutics

authors： Stutchbury TK,Al-Ejeh F,Stillfried GE,Croucher DR,Andrews J,Irving D,Links M,Ranson M

更新日期：2007-01-01 00:00:00

abstract：:The CDC25 cell cycle regulators are promising targets for new pharmacologic approaches in cancer therapy. Inhibitory compounds such as BN82685 have proven to be effective in specifically targeting CDC25 in cultured cells and in inhibiting tumor cell growth. Here, we report that BN82685 impairs microtubule dynamic inst...

journal_title：Molecular cancer therapeutics

authors： Cazales M,Boutros R,Brezak MC,Chaumeron S,Prevost G,Ducommun B

更新日期：2007-01-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor γ (PPARγ) is an important transcription factor that modulates lipid metabolism and inflammation. However, it remains unclear whether PPARγ is involved in modulation of estrogen (E2)-induced inflammation, thus affecting apoptosis of E2-deprived breast cancer cells, MCF-7:5C an...

journal_title：Molecular cancer therapeutics

authors： Fan P,Abderrahman B,Chai TS,Yerrum S,Jordan VC

更新日期：2018-12-01 00:00:00

abstract：:Expression of the proto-oncogene Bcl-2 is associated with tumor progression. Bcl-2's broad expression in tumors, coupled with its role in resistance to chemotherapy and radiation therapy-induced apoptosis, makes it a rational target for anticancer therapy. Antisense Bcl-2 oligodeoxynucleotide (ODN) reagents have been ...

journal_title：Molecular cancer therapeutics

authors： Anai S,Goodison S,Shiverick K,Hirao Y,Brown BD,Rosser CJ

更新日期：2007-01-01 00:00:00

abstract：:D,L-Sulforaphane (SFN), a synthetic analogue of cruciferous vegetable-derived L-isomer, inhibits the growth of human prostate cancer cells in culture and in vivo and retards cancer development in a transgenic mouse model of prostate cancer. We now show that SFN treatment causes transcriptional repression of androgen r...

journal_title：Molecular cancer therapeutics

authors： Kim SH,Singh SV

更新日期：2009-07-01 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：: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：:The therapeutic efficiency of anticancer nucleoside analogues (NA) strongly depends on their intracellular accumulation and conversion into 5'-triphosphates. Because active NATP cannot be directly administrated due to instability, we present here a strategy of nanoencapsulation of these active drugs for efficient deli...

journal_title：Molecular cancer therapeutics

authors： Galmarini CM,Warren G,Kohli E,Zeman A,Mitin A,Vinogradov SV

更新日期：2008-10-01 00:00:00

abstract：:Because the majority of cancers exhibit direct or indirect deregulation of cyclin-dependent kinase (CDK) function, members of the CDK family are attractive targets for the development of anticancer agents. As part of an ongoing program, novel imidazopyridines were identified and developed as potent and selective CDK i...

journal_title：Molecular cancer therapeutics

authors： Byth KF,Geh C,Forder CL,Oakes SE,Thomas AP

更新日期：2006-03-01 00:00:00

abstract：:There is considerable interest in the clinical development of inhibitors of mTOR complexes mTORC1 and 2. Because mTORC1 and its downstream mRNA translation effectors may protect against genotoxic DNA damage, we investigated the inhibition of mTORC1 and mTORC1/2 in the ability to reverse platinum resistance in tissue c...

journal_title：Molecular cancer therapeutics

authors： Musa F,Alard A,David-West G,Curtin JP,Blank SV,Schneider RJ

更新日期：2016-07-01 00:00:00

abstract：:Gefitinib (Iressa, ZD1839), a quinazoline tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR), is approved for patients with advanced non-small cell lung cancer (NSCLC) in several countries including Japan. However, the mechanism of drug sensitivity to gefitinib is not fully understood. ...

journal_title：Molecular cancer therapeutics

authors： Ono M,Hirata A,Kometani T,Miyagawa M,Ueda S,Kinoshita H,Fujii T,Kuwano M

更新日期：2004-04-01 00:00:00

abstract：:Stromal myofibroblasts play an important role in tumor progression. The transition of fibroblasts to myofibroblasts is characterized by expression of smooth muscle genes and profuse synthesis of extracellular matrix proteins. We evaluated the efficacy of targeting fibroblast-to-myofibroblast transition with halofugino...

journal_title：Molecular cancer therapeutics

authors： Sheffer Y,Leon O,Pinthus JH,Nagler A,Mor Y,Genin O,Iluz M,Kawada N,Yoshizato K,Pines M

更新日期：2007-02-01 00:00:00

abstract：:Alpha-emitters can be pharmacologically delivered for irradiation of single cancer cells, but cellular lethality could be further enhanced by targeting alpha-emitters directly to the nucleus. PARP-1 is a druggable protein in the nucleus that is overexpressed in neuroblastoma compared with normal tissues and is associa...

journal_title：Molecular cancer therapeutics

authors： Makvandi M,Lee H,Puentes LN,Reilly SW,Rathi KS,Weng CC,Chan HS,Hou C,Raman P,Martinez D,Xu K,Carlin SD,Greenberg RA,Pawel BR,Mach RH,Maris JM,Pryma DA

更新日期：2019-07-01 00:00:00

abstract：:Human epidermal growth factor receptor-2 (HER2) and epidermal growth factor receptor (EGFR) heterodimerize to activate mitogenic signaling pathways. We have shown previously, using MCF7 subcloned cell lines with graded levels of HER2 expression, that responsiveness to trastuzumab and AG1478 (an anti-EGFR agent), varie...

journal_title：Molecular cancer therapeutics

authors： Emlet DR,Brown KA,Kociban DL,Pollice AA,Smith CA,Ong BB,Shackney SE

更新日期：2007-10-01 00:00:00

abstract：:Dietary phytochemicals exhibit chemopreventive potential in vivo through persistent low-dose exposures, whereas mechanistic in vitro studies with these agents generally use a high-dose single treatment. Because the latter approach is not representative of an in vivo steady state, we investigated antitumor activity of ...

journal_title：Molecular cancer therapeutics

authors： Moiseeva EP,Almeida GM,Jones GD,Manson MM

更新日期：2007-11-01 00:00:00

abstract：:Penta-1,2,3,4,6-O-galloyl-beta-D-glucose (PGG) is a naturally occurring gallotannin from some Oriental herbs. Several cell culture studies suggested a potential for PGG as a novel agent for the chemoprevention and treatment of cancer. Here, we investigated the cell death signaling mechanisms induced by PGG in human pr...

journal_title：Molecular cancer therapeutics

authors： Hu H,Lee HJ,Jiang C,Zhang J,Wang L,Zhao Y,Xiang Q,Lee EO,Kim SH,Lü J

更新日期：2008-09-01 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：:Near infrared photoimmunotherapy (NIR-PIT) is a new cancer treatment that combines the specificity of intravenously injected antibodies for targeting tumors with the toxicity induced by photosensitizers after exposure to near infrared (NIR) light. Herein, we evaluate the efficacy of NIR-PIT in a mouse model of dissemi...

journal_title：Molecular cancer therapeutics

authors： Sato K,Hanaoka H,Watanabe R,Nakajima T,Choyke PL,Kobayashi H

更新日期：2015-01-01 00:00:00

abstract：:Protein ubiquitination is important for cell signaling, DNA repair, and proteasomal degradation, and it is not surprising that alterations in ubiquitination occur frequently in cancer. Ubiquitin-conjugating enzymes (E2) mediate ubiquitination by selective interactions with ubiquitin-activating (E1) and ubiquitin ligas...

journal_title：Molecular cancer therapeutics

authors： Sanders MA,Brahemi G,Nangia-Makker P,Balan V,Morelli M,Kothayer H,Westwell AD,Shekhar MPV

更新日期：2013-04-01 00:00:00

abstract：:Chemoresistance of ovarian carcinoma has been associated previously to the absence of Bcl-x(L) expression downregulation in response to cisplatin. Among BH3-mimetic molecules constituting promising anticancer agents able to inhibit the activity of antiapoptotic Bcl-2 family proteins, we evaluated the effect of one of ...

journal_title：Molecular cancer therapeutics

authors： Simonin K,Brotin E,Dufort S,Dutoit S,Goux D,N'diaye M,Denoyelle C,Gauduchon P,Poulain L

更新日期：2009-11-01 00:00:00

abstract：:The NF-κB transcription factor functions as a crucial regulator of cell survival and chemoresistance in pancreatic cancer. Recent studies suggest that tocotrienols, which are the unsaturated forms of vitamin E, are a promising class of anticancer compounds that inhibit the growth and survival of many cancer cells, inc...

journal_title：Molecular cancer therapeutics

authors： Husain K,Francois RA,Yamauchi T,Perez M,Sebti SM,Malafa MP

更新日期：2011-12-01 00:00:00

abstract：:Flex-Het drugs induce apoptosis in multiple types of cancer cells, with little effect on normal cells. This apoptosis occurs through the intrinsic mitochondrial pathway accompanied by generation of reactive oxygen species (ROS). The objective of this study was to determine if direct or indirect targeting of mitochondr...

journal_title：Molecular cancer therapeutics

authors： Liu T,Hannafon B,Gill L,Kelly W,Benbrook D

更新日期：2007-06-01 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