Novel semisynthetic analogues of betulinic acid with diverse cytoprotective, antiproliferative, and proapoptotic activities.

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：:Aptamers, also termed as decoys or "chemical antibodies," represent an emerging class of therapeutics. They are short DNA or RNA oligonucleotides or peptides that assume a specific and stable three-dimensional shape in vivo, thereby providing specific tight binding to protein targets. In some cases and as opposed to a...

journal_title：Molecular cancer therapeutics

authors： Ireson CR,Kelland LR

更新日期：2006-12-01 00:00:00

abstract：:The humanized anti-HER2 monoclonal antibody (mAb) trastuzumab (Herceptin; Genentech) effectively inhibits human epidermal growth factor receptor 2 (HER2)-positive breast tumors. However, many patients responding to treatment often develop resistance. Cross-talk between type I insulin-like growth factor receptor (IGF-I...

journal_title：Molecular cancer therapeutics

authors： Chen C,Zhang Y,Zhang Y,Li J,Tsao SW,Zhang MY

更新日期：2014-01-01 00:00:00

abstract：:The PI3K-AKT pathway has pleiotropic effects and its inhibition has long been of interest in the management of prostate cancer, where a compensatory increase in PI3K signaling has been reported following androgen receptor (AR) blockade. Prostate cancer cells can also bypass AR blockade through induction of other hormo...

journal_title：Molecular cancer therapeutics

authors： Adelaiye-Ogala R,Gryder BE,Nguyen YTM,Alilin AN,Grayson AR,Bajwa W,Jansson KH,Beshiri ML,Agarwal S,Rodriguez-Nieves JA,Capaldo B,Kelly K,VanderWeele DJ

更新日期：2020-07-01 00:00:00

abstract：:Nasopharyngeal carcinoma (NPC) is a common cancer in Southern China and EBV is the most important pathogenesis. In this study, we explore the potential that a recombinant adeno-associated virus (rAAV) carrying a fusing gene containing heat shock protein as an adjuvant, EBV latent membrane proteins (LMP1 and LMP2) CTL ...

journal_title：Molecular cancer therapeutics

authors： Pan J,Zhang Q,Zhou J,Ma D,Xiao X,Wang DW

更新日期：2009-09-01 00:00:00

abstract：:Ras signaling can be modulated by the scaffolding activity of kinase suppressor of Ras-1 (KSR-1) and by the hKSR-2 protein, resulting in diverse phenotypic outcomes. The mitogen-activated protein kinase cascade downstream from Ras and KSRs includes Raf-1 and extracellular signal-regulated kinase 1/2 kinases, known to ...

journal_title：Molecular cancer therapeutics

authors： Wang X,Patel R,Studzinski GP

更新日期：2008-09-01 00:00:00

abstract：:The PI3K/AKT/mTOR pathway is frequently activated in head and neck squamous cell carcinoma (HNSCC), but pathway inhibition has variable efficacy. Identification of predictive biomarkers and mechanisms of resistance would allow selection of patients most likely to respond and novel therapeutic combinations. The purpose...

journal_title：Molecular cancer therapeutics

authors： Mazumdar T,Byers LA,Ng PK,Mills GB,Peng S,Diao L,Fan YH,Stemke-Hale K,Heymach JV,Myers JN,Glisson BS,Johnson FM

更新日期：2014-11-01 00:00:00

abstract：:Radiosensitization caused by the poly(ADP-ribose) polymerase (PARP) inhibitor 4-amino-1,8-naphthalimide (ANI) was investigated in 10 asynchronously growing rodent (V79, CHO-Xrs6, CHO-K1, PARP-1+/+ 3T3, and PARP-1-/- 3T3) or human (HeLa, MRC5VI, IMR90, M059J, and M059K) cell lines, either repair proficient or defective...

journal_title：Molecular cancer therapeutics

authors： Noël G,Godon C,Fernet M,Giocanti N,Mégnin-Chanet F,Favaudon V

更新日期：2006-03-01 00:00:00

abstract：:Several caged Garcinia xanthone natural products have potent bioactivity and a documented value in traditional Eastern medicine. Previous synthesis and structure activity relationship studies of these natural products resulted in the identification of the pharmacophore represented by the structure of cluvenone. In the...

journal_title：Molecular cancer therapeutics

authors： Batova A,Altomare D,Chantarasriwong O,Ohlsen KL,Creek KE,Lin YC,Messersmith A,Yu AL,Yu J,Theodorakis EA

更新日期：2010-11-01 00:00:00

abstract：:In recent years, HER3 has increasingly been implicated in the progression of a variety of tumor types and in acquired resistance to EGFR and HER2 therapies. Whereas EGFR and HER2 primarily signal through the MAPK pathway, HER3, as a heterodimer with EGFR or HER2, potently activates the PI3K pathway. Despite its critic...

journal_title：Molecular cancer therapeutics

authors： Thakkar D,Sancenon V,Taguiam MM,Guan S,Wu Z,Ng E,Paszkiewicz KH,Ingram PJ,Boyd-Kirkup JD

更新日期：2020-02-01 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is a deadly malignancy that frequently metastasizes and that overexpresses transforming growth factor-beta s (TGF-beta s). To determine whether TGF-beta s can act to enhance the metastatic potential of PDAC, PANC-1 human pancreatic cancer cells were transfected with an expressio...

journal_title：Molecular cancer therapeutics

authors： Rowland-Goldsmith MA,Maruyama H,Matsuda K,Idezawa T,Ralli M,Ralli S,Korc M

更新日期：2002-01-01 00:00:00

abstract：:Checkpoint kinase 1 (ChK1) is a serine/threonine kinase that functions as a central mediator of the intra-S and G2-M cell-cycle checkpoints. Following DNA damage or replication stress, ChK1-mediated phosphorylation of downstream effectors delays cell-cycle progression so that the damaged genome can be repaired. As a t...

journal_title：Molecular cancer therapeutics

authors： Blackwood E,Epler J,Yen I,Flagella M,O'Brien T,Evangelista M,Schmidt S,Xiao Y,Choi J,Kowanetz K,Ramiscal J,Wong K,Jakubiak D,Yee S,Cain G,Gazzard L,Williams K,Halladay J,Jackson PK,Malek S

更新日期：2013-10-01 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：:The protein kinase family represents an enormous opportunity for drug development. However, the current limitation in structural diversity of kinase inhibitors has complicated efforts to identify effective treatments of diseases that involve protein kinase signaling pathways. We have identified a new structural class ...

journal_title：Molecular cancer therapeutics

authors： Hamdouchi C,Keyser H,Collins E,Jaramillo C,De Diego JE,Spencer CD,Dempsey JA,Anderson BD,Leggett T,Stamm NB,Schultz RM,Watkins SA,Cocke K,Lemke S,Burke TF,Beckmann RP,Dixon JT,Gurganus TM,Rankl NB,Houck KA,Zhang F

更新日期：2004-01-01 00:00:00

abstract：:Imatinib mesylate has shown remarkable efficacy in the treatment of patients in the chronic phase of chronic myeloid leukemia. However, despite an overall significant hematological and cytogenetic response, imatinib therapy may favor the emergence of drug-resistant clones, ultimately leading to relapse. Some imatinib ...

journal_title：Molecular cancer therapeutics

authors： Deville L,Hillion J,Pendino F,Samy M,Nguyen E,Ségal-Bendirdjian E

更新日期：2011-05-01 00:00:00

abstract：:Invasion into deep myometrium and/or lymphovascular space is a well-known risk factor for endometrial cancer metastasis, resulting in poor prognosis. It is therefore clinically important to identify novel molecules that suppress tumor invasion. Reduced expression of the metastasis suppressor, kisspeptin (KISS1), and i...

journal_title：Molecular cancer therapeutics

authors： Kang HS,Baba T,Mandai M,Matsumura N,Hamanishi J,Kharma B,Kondoh E,Yoshioka Y,Oishi S,Fujii N,Murphy SK,Konishi I

更新日期：2011-04-01 00:00:00

abstract：:Head and neck squamous cell carcinoma (HNSCC) is characterized by epidermal growth factor receptor (EGFR) overexpression, where EGFR levels correlate with survival. To date, EGFR targeting has shown limited antitumor effects in head and neck cancer when administrated as monotherapy. We previously identified a gastrin-...

journal_title：Molecular cancer therapeutics

authors： Zhang Q,Bhola NE,Lui VW,Siwak DR,Thomas SM,Gubish CT,Siegfried JM,Mills GB,Shin D,Grandis JR

更新日期：2007-04-01 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：:Bortezomib is highly effective in the treatment of multiple myeloma; however, emergent drug resistance is common. Consequently, we employed CRISPR targeting 19,052 human genes to identify unbiased targets that contribute to bortezomib resistance. Specifically, we engineered an RPMI8226 multiple myeloma cell line to ex...

journal_title：Molecular cancer therapeutics

authors： Shi CX,Kortüm KM,Zhu YX,Bruins LA,Jedlowski P,Votruba PG,Luo M,Stewart RA,Ahmann J,Braggio E,Stewart AK

更新日期：2017-12-01 00:00:00

abstract：:In bone metastatic lesions, osteoclasts play a key role in the development of osteolysis. Previous studies have shown that macrophage colony-stimulating factor (M-CSF) is important for the differentiation of osteoclasts. In this study, we investigated whether an inhibitor of M-CSF receptor (c-Fms) suppresses osteoclas...

journal_title：Molecular cancer therapeutics

authors： Ohno H,Kubo K,Murooka H,Kobayashi Y,Nishitoba T,Shibuya M,Yoneda T,Isoe T

更新日期：2006-11-01 00:00:00

abstract：:Although proteasome inhibitors such as bortezomib had significant therapeutic effects in multiple myeloma and mantel cell lymphoma, they exhibited minimal clinical activity as a monotherapy for solid tumors, including colorectal cancer. We found in this study that proteasome inhibition induced a remarkable nuclear exp...

journal_title：Molecular cancer therapeutics

authors： Wu T,Chen W,Zhong Y,Hou X,Fang S,Liu CY,Wang G,Yu T,Huang YY,Ouyang X,Li HQ,Cui L,Yang Y

更新日期：2017-04-01 00:00:00

abstract：:Wee1 is a critical component of the G(2)-M cell-cycle checkpoint control and mediates cell-cycle arrest by regulating the phosphorylation of CDC2. Inhibition of Wee1 by a selective small molecule inhibitor MK1775 can abrogate G(2)-M checkpoint, resulting in premature mitotic entry and cell death. MK1775 has recently b...

journal_title：Molecular cancer therapeutics

authors： Kreahling JM,Gemmer JY,Reed D,Letson D,Bui M,Altiok S

更新日期：2012-01-01 00:00:00

abstract：:The oncogenic beta-catenin/T-cell factor (TCF) signal is a common trigger inducing expressions of various cancer-related genes and is activated in various types of human malignancy. The aim of this study was to create an effective double-stranded DNA decoy that would interfere with endogenous TCF hyperactivity in tumo...

journal_title：Molecular cancer therapeutics

authors： Seki Y,Yamamoto H,Ngan CY,Yasui M,Tomita N,Kitani K,Takemasa I,Ikeda M,Sekimoto M,Matsuura N,Albanese C,Kaneda Y,Pestell RG,Monden M

更新日期：2006-04-01 00:00:00

abstract：:Members of the signal transducer and activator of transcription (STAT) family of transcription factors are potential targets for the treatment and prevention of cancers including non-small-cell lung cancer. STAT proteins can be phosphorylated and activated by diverse upstream kinases including cytokine receptors and t...

journal_title：Molecular cancer therapeutics

authors： Song L,Rawal B,Nemeth JA,Haura EB

更新日期：2011-03-01 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：:B-Raf is an important mediator of cell proliferation and survival signals transduced via the Ras-Raf-MEK-ERK cascade. BRAF mutations have been detected in several tumors, including papillary thyroid carcinoma, but the precise role of B-Raf as a therapeutic target for thyroid carcinoma is still under investigation. We ...

journal_title：Molecular cancer therapeutics

authors： Mitsiades CS,Negri J,McMullan C,McMillin DW,Sozopoulos E,Fanourakis G,Voutsinas G,Tseleni-Balafouta S,Poulaki V,Batt D,Mitsiades N

更新日期：2007-03-01 00:00:00

abstract：:Targeted thrombotic eradication of solid tumors is a novel therapeutic strategy. The feasibility, efficacy, selectivity, and safety are dependent on multiple variables of protein design, molecular assembly, vascular target, and exclusive restriction of function to the tumor vasculature. To advance this strategy, we de...

journal_title：Molecular cancer therapeutics

authors： Liu C,Dickinson C,Shobe J,Doñate F,Ruf W,Edgington T

更新日期：2004-07-01 00:00:00

abstract：:Bifunctional antibody fusion proteins engaging effector T cells for targeted elimination of tumor cells via CD3 binding have shown efficacy in both preclinical and clinical studies. Different from such a polyclonal T-cell recruitment, an alternative concept is to engage only antigen-specific T-cell subsets. Recruitmen...

journal_title：Molecular cancer therapeutics

authors： Schmittnaegel M,Hoffmann E,Imhof-Jung S,Fischer C,Drabner G,Georges G,Klein C,Knoetgen H

更新日期：2016-09-01 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：:Patients with non-small cell lung carcinoma (NSCLC) with activating mutations in epidermal growth factor receptor (EGFR) initially respond well to the EGFR inhibitors erlotinib and gefitinib. However, all patients relapse because of the emergence of drug-resistant mutations, with T790M mutations accounting for approxi...

journal_title：Molecular cancer therapeutics

authors： Tjin Tham Sjin R,Lee K,Walter AO,Dubrovskiy A,Sheets M,Martin TS,Labenski MT,Zhu Z,Tester R,Karp R,Medikonda A,Chaturvedi P,Ren Y,Haringsma H,Etter J,Raponi M,Simmons AD,Harding TC,Niu D,Nacht M,Westlin WF,Pette

更新日期：2014-06-01 00:00:00