Z-FA-fmk inhibits effector caspases but not initiator caspases 8 and 10, and demonstrates that novel anticancer retinoid-related molecules induce apoptosis via the intrinsic pathway.

abstract：:The tumor suppressor protein p53 is a potent inducer of apoptosis in transformed cells. Hdm2 is an ubiquitin ligase (E3) that acts as a major regulator of p53 by promoting its ubiquitylation and proteasomal degradation. For this reason, inhibiting the E3 activity of Hdm2 has been proposed as a therapeutic approach for...

journal_title：Molecular cancer therapeutics

authors： Kitagaki J,Agama KK,Pommier Y,Yang Y,Weissman AM

更新日期：2008-08-01 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：:A novel oral Hsp90 inhibitor, NVP-HSP990, has been developed and characterized in vitro and in vivo. In vitro, NVP-HSP990 exhibits single digit nanomolar IC(50) values on three of the Hsp90 isoforms (Hsp90α, Hsp90β, and GRP94) and 320 nanomolar IC(50) value on the fourth (TRAP-1), with selectivity against unrelated en...

journal_title：Molecular cancer therapeutics

authors： Menezes DL,Taverna P,Jensen MR,Abrams T,Stuart D,Yu GK,Duhl D,Machajewski T,Sellers WR,Pryer NK,Gao Z

更新日期：2012-03-01 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：:Antibody-drug conjugates (ADC) represent a promising therapeutic modality for the clinical management of cancer. We sought to develop a novel ADC that targets 5T4, an oncofetal antigen expressed on tumor-initiating cells (TIC), which comprise the most aggressive cell population in the tumor. We optimized an anti-5T4 A...

journal_title：Molecular cancer therapeutics

authors： Sapra P,Damelin M,Dijoseph J,Marquette K,Geles KG,Golas J,Dougher M,Narayanan B,Giannakou A,Khandke K,Dushin R,Ernstoff E,Lucas J,Leal M,Hu G,O'Donnell CJ,Tchistiakova L,Abraham RT,Gerber HP

更新日期：2013-01-01 00:00:00

abstract：:Thalidomide is considered to be a potent antiangiogenic and immunomodulatory drug for cancer therapy. Earlier clinical studies have found that patients responding to this drug often had high plasma levels of basic fibroblast growth factor (bFGF). This cytokine is a proangiogenic factor overexpressed in many tumors and...

journal_title：Molecular cancer therapeutics

authors： Mei SC,Wu RT

更新日期：2008-08-01 00:00:00

abstract：:Neuroblastoma is the most common extracranial solid malignancy in the pediatric population, accounting for over 9% of all cancer-related deaths in children. Autophagy is a cell self-protective mechanism that promotes tumor cell growth and survival, making it an attractive target for treating cancer. However, the role ...

journal_title：Molecular cancer therapeutics

authors： Dower CM,Bhat N,Gebru MT,Chen L,Wills CA,Miller BA,Wang HG

更新日期：2018-11-01 00:00:00

abstract：:Erlotinib is a tyrosine kinase inhibitor approved for the treatment of patients with advanced non-small cell lung cancer (NSCLC). In these patients, erlotinib prolongs survival but its benefit remains modest because many tumors express wild-type (wt) EGFR or develop a second-site EGFR mutation. To test drug combinatio...

journal_title：Molecular cancer therapeutics

authors： Dermawan JK,Gurova K,Pink J,Dowlati A,De S,Narla G,Sharma N,Stark GR

更新日期：2014-09-01 00:00:00

abstract：:Prostate-specific membrane antigen (PSMA) is a protein up-regulated in the vast majority of prostate cancers. Antibodies to PSMA have proved highly specific for prostate cancer cells, and the therapeutic potential of such antibodies is currently being assessed in clinical trials. We have previously shown that PSMA at ...

journal_title：Molecular cancer therapeutics

authors： Christiansen JJ,Weimbs T,Bander N,Rajasekaran AK

更新日期：2006-10-01 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：:Clinical translation of intravenous therapies to treat disseminated or metastatic cancer is imperative. Comparative oncology, the evaluation of novel cancer therapies in animals with spontaneous cancer, can be utilized to inform and accelerate clinical translation. Preclinical murine studies demonstrate that single-sh...

journal_title：Molecular cancer therapeutics

authors： Naik S,Galyon GD,Jenks NJ,Steele MB,Miller AC,Allstadt SD,Suksanpaisan L,Peng KW,Federspiel MJ,Russell SJ,LeBlanc AK

更新日期：2018-01-01 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：:Pancreatic ductal adenocarcinoma (PDAC) is the fourth leading cause of cancer-related mortality in the United States. Aggressive treatment regimens have not changed the disease course, and the median survival has just recently reached a year. Several mechanisms are proposed to play a role in PDAC therapeutic resistanc...

journal_title：Molecular cancer therapeutics

authors： Logsdon DP,Grimard M,Luo M,Shahda S,Jiang Y,Tong Y,Yu Z,Zyromski N,Schipani E,Carta F,Supuran CT,Korc M,Ivan M,Kelley MR,Fishel ML

更新日期：2016-11-01 00:00:00

abstract：:Melanoma is a highly metastatic and deadly disease. An agent simultaneously targeting the COX-2, PI3K/Akt, and mitogen-activated protein kinase (MAPK) signaling pathways that are deregulated in up to 70% of sporadic melanomas might be an effective treatment, but no agent of this type exists. To develop a single drug i...

journal_title：Molecular cancer therapeutics

authors： Gowda R,Madhunapantula SV,Desai D,Amin S,Robertson GP

更新日期：2013-01-01 00:00:00

abstract：:Bisperoxovanadium (bpV) compounds are irreversible protein tyrosine phosphatase (PTP) inhibitors with a spectrum of activity distinct from that of vanadium salts. We studied the efficacy of a panel of bpVs as antineoplastic agents in vitro and in vivo with a view to investigating phosphatases as potential antineoplast...

journal_title：Molecular cancer therapeutics

authors： Scrivens PJ,Alaoui-Jamali MA,Giannini G,Wang T,Loignon M,Batist G,Sandor VA

更新日期：2003-10-01 00:00:00

abstract：:Treatment options for hepatocellular carcinoma using chemotherapeutics at intermediate and advanced stages of disease are limited as patients most rapidly escape from therapy and succumb to disease progression. Mechanisms of the hepatic xenobiotic metabolism are mostly involved in providing chemoresistance to therapeu...

journal_title：Molecular cancer therapeutics

authors： Haider C,Grubinger M,Řezníčková E,Weiss TS,Rotheneder H,Miklos W,Berger W,Jorda R,Zatloukal M,Gucky T,Strnad M,Kryštof V,Mikulits W

更新日期：2013-10-01 00:00:00

abstract：:Staphylococcal nuclease domain-containing protein 1 (SND1) is a multifunctional oncoprotein overexpressed in breast cancer. Binding of metadherin (MTDH) to SND1 results in the stabilization of SND1 and is important in the initiation and progression of breast cancer. Disruption of such interaction is a potential therap...

journal_title：Molecular cancer therapeutics

authors： Li P,He Y,Chen T,Choy KY,Chow TS,Wong ILK,Yang X,Sun W,Su X,Chan TH,Chow LMC

更新日期：2021-01-01 00:00:00

abstract：:We previously showed that in innately resistant tumors, silencing of the estrogen receptor (ER) could be reversed by treatment with a histone deacetylase (HDAC) inhibitor, entinostat. Tumors were then responsive to aromatase inhibitor (AI) letrozole. Here, we investigated whether ER in the acquired letrozole-resistant...

journal_title：Molecular cancer therapeutics

authors： Sabnis GJ,Goloubeva OG,Kazi AA,Shah P,Brodie AH

更新日期：2013-12-01 00:00:00

abstract：:G-protein mutations are one of the most common mutations occurring in uveal melanoma activating the protein kinase C (PKC)/mitogen-activated protein kinase and phosphoinositide 3-kinase (PI3K)/AKT pathways. In this study, we described the effect of dual pathway inhibition in uveal melanoma harboring GNAQ and GNA11 mut...

journal_title：Molecular cancer therapeutics

authors： Musi E,Ambrosini G,de Stanchina E,Schwartz GK

更新日期：2014-05-01 00:00:00

abstract：:Anti-HER2 monoclonal antibodies (mAb) have been shown to reduce tumor size and increase survival in patients with breast cancer, but they are ineffective against brain metastases due to poor brain penetration. In previous studies, we identified a peptide, known as Angiopep-2 (An2), which crosses the blood-brain barrie...

journal_title：Molecular cancer therapeutics

authors： Regina A,Demeule M,Tripathy S,Lord-Dufour S,Currie JC,Iddir M,Annabi B,Castaigne JP,Lachowicz JE

更新日期：2015-01-01 00:00:00

abstract：:The increasing characterization of childhood acute lymphoblastic leukemia (ALL) has led to the identification of multiple molecular targets but has yet to translate into more effective targeted therapies, particularly for high-risk, relapsed T-cell ALL. Searching for master regulators controlling multiple signaling pa...

journal_title：Molecular cancer therapeutics

authors： Ding J,Fishel ML,Reed AM,McAdams E,Czader MB,Cardoso AA,Kelley MR

更新日期：2017-07-01 00:00:00

abstract：:Pancreatic carcinoma is one of the most aggressive tumor entities, and standard chemotherapy provides only modest benefit. Therefore, specific targeting of pancreatic cancer for early diagnosis and therapeutic intervention is of great interest. We have previously shown that the cellular receptor for Shiga toxin B (STx...

journal_title：Molecular cancer therapeutics

authors： Maak M,Nitsche U,Keller L,Wolf P,Sarr M,Thiebaud M,Rosenberg R,Langer R,Kleeff J,Friess H,Johannes L,Janssen KP

更新日期：2011-10-01 00:00:00

abstract：:Epigenetic abnormalities are common in hematologic malignancies, including multiple myeloma, and their effects can be efficiently counteracted by a class of tumor suppressor miRNAs, named epi-miRNAs. Given the oncogenic role of histone deacetylases (HDAC) in multiple myeloma, we investigated whether their activity cou...

journal_title：Molecular cancer therapeutics

authors： Amodio N,Stamato MA,Gullà AM,Morelli E,Romeo E,Raimondi L,Pitari MR,Ferrandino I,Misso G,Caraglia M,Perrotta I,Neri A,Fulciniti M,Rolfo C,Anderson KC,Munshi NC,Tagliaferri P,Tassone P

更新日期：2016-06-01 00:00:00

abstract：:Transforming growth factor-beta (TGF-beta) is a multifunctional cytokine that promotes malignant glioma invasion, angiogenesis, and immunosuppression. Antisense oligonucleotide suppression of TGF-beta(2) ligand expression has shown promise in preclinical and clinical studies but at least two ligands mediate the effect...

journal_title：Molecular cancer therapeutics

authors： Hjelmeland MD,Hjelmeland AB,Sathornsumetee S,Reese ED,Herbstreith MH,Laping NJ,Friedman HS,Bigner DD,Wang XF,Rich JN

更新日期：2004-06-01 00:00:00

abstract：:Signaling from the human hematopoietic stem cell (HSC) niche formed by osteoblastic cells regulates hematopoiesis. We previously found that retinoic acid receptor alpha (RARα), a transcription factor activated by retinoic acid (RA), mediates both granulocytic and osteoblastic differentiation. This effect depends on de...

journal_title：Molecular cancer therapeutics

authors： Chaudhry P,Yang X,Wagner M,Jong A,Wu L

更新日期：2012-02-01 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：:We previously reported that angiotensin II type 1 receptor (AT1R) antagonists enhanced the cytotoxity of cis-dichlorodiammineplatinum (CDDP) in a bladder cancer xenograft model. To elucidate the synergistic mechanism, we investigated whether reactive oxygen species (ROS) generation induced by CDDP may affect the regul...

journal_title：Molecular cancer therapeutics

authors： Tanaka N,Miyajima A,Kosaka T,Shirotake S,Hasegawa M,Kikuchi E,Oya M

更新日期：2010-11-01 00:00:00

abstract：:Neuroblastoma is the most common extracranial solid tumor of childhood. The activity of J1 (l-melphalanyl-p-l-fluorophenylalanine ethyl ester), an enzymatically activated melphalan prodrug, was evaluated in neuroblastoma models in vitro and in vivo. Seven neuroblastoma cell lines with various levels of drug resistance...

journal_title：Molecular cancer therapeutics

authors： Wickström M,Johnsen JI,Ponthan F,Segerström L,Sveinbjörnsson B,Lindskog M,Lövborg H,Viktorsson K,Lewensohn R,Kogner P,Larsson R,Gullbo J

更新日期：2007-09-01 00:00:00

abstract：:TNF-like weak inducer of apoptosis (TWEAK) and fibroblast growth factor (FGF)-inducible 14 (Fn14) are a TNF superfamily ligand-receptor pair involved in many cellular processes including proliferation, migration, differentiation, inflammation, and angiogenesis. The Fn14 receptor is expressed at relatively low levels i...

journal_title：Molecular cancer therapeutics

authors： Zhou H,Marks JW,Hittelman WN,Yagita H,Cheung LH,Rosenblum MG,Winkles JA

更新日期：2011-07-01 00:00:00

abstract：:STAT3 is an important transcriptional factor for cell growth, differentiation, and apoptosis. Although evidence suggests a positive role for STAT3 in cancer, the inhibitory effects of tumor STAT3 on natural killer (NK) cell functions in human hepatocellular carcinoma are unclear. In this study, we found that blocking ...

journal_title：Molecular cancer therapeutics

authors： Sun X,Sui Q,Zhang C,Tian Z,Zhang J

更新日期：2013-12-01 00:00:00