Discovery and characterization of inhibitors of human palmitoyl acyltransferases.

abstract：:RAV12 is a chimeric antibody that recognizes an N-linked carbohydrate antigen (RAAG12) strongly expressed on multiple solid organ cancers. More than 90% of tumors of colorectal, gastric, and pancreatic origin express RAAG12, and a majority of these tumors exhibit uniform RAAG12 expression. RAV12 exhibits potent cytoto...

journal_title：Molecular cancer therapeutics

authors： Loo D,Pryer N,Young P,Liang T,Coberly S,King KL,Kang K,Roberts P,Tsao M,Xu X,Potts B,Mather JP

更新日期：2007-03-01 00:00:00

abstract：:Chemoresistance is a major hurdle in the management of patients with epithelial ovarian cancer and is responsible for its high mortality. Studies have shown that chemoresistance is due to the presence of a subgroup of cancer cells with stemness properties and a high capacity for tumor repair. We have developed a libra...

journal_title：Molecular cancer therapeutics

authors： Alvero AB,Heaton A,Lima E,Pitruzzello M,Sumi N,Yang-Hartwich Y,Cardenas C,Steinmacher S,Silasi DA,Brown D,Mor G

更新日期：2016-06-01 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：:The advent of multikinase inhibitors targeting the vascular endothelial growth factor (VEGF) receptor has revolutionized the treatment of highly angiogenic malignancies such as renal cell carcinoma. Interestingly, several such inhibitors are commercially available, and they each possess diverse specific beneficial and...

journal_title：Molecular cancer therapeutics

authors： Liu JY,Park SH,Morisseau C,Hwang SH,Hammock BD,Weiss RH

更新日期：2009-08-01 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：: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：: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：: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：:Tyrosine kinase inhibitors exhibit impressive activity against advanced renal cell carcinoma. However, recent clinical studies have shown an equivocal response to sunitinib in patients with castration-resistant prostate cancer. The tumor suppressor PTEN acts as a gatekeeper of the phosphoinositide 3-kinase (PI3K)/Akt/...

journal_title：Molecular cancer therapeutics

authors： Makhov PB,Golovine K,Kutikov A,Teper E,Canter DJ,Simhan J,Uzzo RG,Kolenko VM

更新日期：2012-07-01 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal cancer due in part to a lack of highly robust cytotoxic or molecular-based therapies. Recent studies investigating ligand-mediated Wnt/β-catenin signaling have highlighted its importance in pancreatic cancer initiation and progression, as well as its potential...

journal_title：Molecular cancer therapeutics

authors： Arensman MD,Telesca D,Lay AR,Kershaw KM,Wu N,Donahue TR,Dawson DW

更新日期：2014-10-01 00:00:00

abstract：:Floxuridine is a clinically proven anticancer agent in the treatment of metastatic colon carcinomas and hepatic metastases. However, prodrug strategies may be necessary to improve its physiochemical properties and selectivity and to reduce undesirable toxicity effects. Previous studies with amino acid ester prodrugs o...

journal_title：Molecular cancer therapeutics

authors： Landowski CP,Vig BS,Song X,Amidon GL

更新日期：2005-04-01 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：:Resistance to radiotherapy due to insufficient cancer cell death is a significant cause of treatment failure in non-small cell lung cancer (NSCLC). The endogenous caspase-8 inhibitor FLIP is a critical regulator of cell death that is frequently overexpressed in NSCLC and is an established inhibitor of apoptotic cell d...

journal_title：Molecular cancer therapeutics

authors： McLaughlin KA,Nemeth Z,Bradley CA,Humphreys L,Stasik I,Fenning C,Majkut J,Higgins C,Crawford N,Holohan C,Johnston PG,Harrison T,Hanna GG,Butterworth KT,Prise KM,Longley DB

更新日期：2016-10-01 00:00:00

abstract：:Myeloid-derived suppressor cells (MDSC) are innate immune cells that potently inhibit T cells. In cancer, novel therapies aimed to activate T cells can be rendered ineffective due to the activity of MDSCs. Thus, targeted inhibition of MDSCs may greatly enhance T-cell-mediated antitumor immunity, but mechanisms remain ...

journal_title：Molecular cancer therapeutics

authors： Plebanek MP,Bhaumik D,Bryce PJ,Thaxton CS

更新日期：2018-03-01 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：:Novel therapeutic approaches are urgently needed for high-stage neuroblastoma, a major therapeutic challenge in pediatric oncology. The majority of neuroblastoma tumors are p53 wild type with intact downstream p53 signaling pathways. We hypothesize that stabilization of p53 would sensitize this aggressive tumor to gen...

journal_title：Molecular cancer therapeutics

authors： Barbieri E,Mehta P,Chen Z,Zhang L,Slack A,Berg S,Shohet JM

更新日期：2006-09-01 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：:Activation of translation initiation is essential for the malignant phenotype and is emerging as a potential therapeutic target. Translation is regulated by the expression of translation initiation factor 4E (eIF4E) as well as the interaction of eIF4E with eIF4E-binding proteins (e.g., 4E-BP1). Rapamycin inhibits tran...

journal_title：Molecular cancer therapeutics

authors： Soni A,Akcakanat A,Singh G,Luyimbazi D,Zheng Y,Kim D,Gonzalez-Angulo A,Meric-Bernstam F

更新日期：2008-07-01 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：: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

abstract：:Met-amplified EGFR-tyrosine kinase inhibitor (TKI)-resistant non-small cell lung cancer (NSCLC) harboring an activating EGFR mutation is responsive to concurrent EGFR-TKI and Met-TKI treatment in a preclinical model. Here, we determined that Met-amplified gefitinib-resistant cells acquire dual resistance to inhibition...

journal_title：Molecular cancer therapeutics

authors： Yamaoka T,Ohmori T,Ohba M,Arata S,Kishino Y,Murata Y,Kusumoto S,Ishida H,Shirai T,Hirose T,Ohnishi T,Sasaki Y

更新日期：2016-12-01 00:00:00

abstract：:GA101 is a novel glycoengineered Type II CD20 monoclonal antibody. When compared with rituximab, it mediates less complement-dependent cytotoxicity (CDC). As expected for a Type II antibody, GA101 appears not to act through CDC and is more potent than the Type I antibody rituximab in inducing cell death via nonclassic...

journal_title：Molecular cancer therapeutics

authors： Dalle S,Reslan L,Besseyre de Horts T,Herveau S,Herting F,Plesa A,Friess T,Umana P,Klein C,Dumontet C

更新日期：2011-01-01 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：: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：:Cryptophycin 52 (LY355703) is a potent antiproliferative analogue of the marine natural product cryptophycin 1. It has been shown to have a broad range of antitumor activity against human tumor xenografts and murine tumors including tumors resistant to Taxol and Adriamycin. Its mechanism of action involves arresting c...

journal_title：Molecular cancer therapeutics

authors： Al-Awar RS,Corbett TH,Ray JE,Polin L,Kennedy JH,Wagner MM,Williams DC

更新日期：2004-09-01 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：:The standard treatment for most advanced cancers is multidrug therapy. Unfortunately, combinations in the clinic often do not perform as predicted. Therefore, to complement identifying rational drug combinations based on biological assumptions, we hypothesized that a functional screen of drug combinations, without lim...

journal_title：Molecular cancer therapeutics

authors： Zinner RG,Barrett BL,Popova E,Damien P,Volgin AY,Gelovani JG,Lotan R,Tran HT,Pisano C,Mills GB,Mao L,Hong WK,Lippman SM,Miller JH

更新日期：2009-03-01 00:00:00

abstract：:Soluble copolymers of camptothecin (CPT), based on poly[N-(2-hydroxypropyl) methacrylamide] (pHPMA), were obtained by conjugation through the degradable spacers -Gly-Phe-Leu-Gly- or -Gly-6-aminohexanoyl-Gly-. We investigated to what extent passive accumulation and retention of hydroxypropyl methacrylamide copolymer of...

journal_title：Molecular cancer therapeutics

authors： Zamai M,VandeVen M,Farao M,Gratton E,Ghiglieri A,Castelli MG,Fontana E,D'Argy R,Fiorino A,Pesenti E,Suarato A,Caiolfa VR

更新日期：2003-01-01 00:00:00

abstract：:Tumor recurrence after curative resection remains a major problem in patients with locally advanced colorectal cancer treated with adjuvant chemotherapy. Genetic single-nucleotide polymorphisms (SNP) may serve as useful molecular markers to predict clinical outcomes in these patients and identify targets for future dr...

journal_title：Molecular cancer therapeutics

authors： Ning Y,Gerger A,Zhang W,Hanna DL,Yang D,Winder T,Wakatsuki T,Labonte MJ,Stintzing S,Volz N,Sunakawa Y,Stremitzer S,El-Khoueiry R,Lenz HJ

更新日期：2014-02-01 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