The cellular phenotype of AZ703, a novel selective imidazo[1,2-a]pyridine cyclin-dependent kinase inhibitor.

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：:The serine protease granzyme B (GrB; 25 kDa) is capable of inducing apoptosis through both caspase-dependent and caspase-independent mechanisms. We designed a novel vascular-targeting fusion construct designated as GrB/vascular endothelial growth factor (VEGF)121, which is composed of a non-heparin-binding isoform of ...

journal_title：Molecular cancer therapeutics

authors： Liu Y,Cheung LH,Thorpe P,Rosenblum MG

更新日期：2003-10-01 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：:Metastatic castration-resistant prostate cancer (CRPC) is currently incurable. Cancer growth and progression is intimately affected by its interaction with host microenvironment. Cotargeting of the stroma and prostate cancer is therefore an emerging therapeutic strategy for metastatic CRPC. Cancer-induced osteoclastog...

journal_title：Molecular cancer therapeutics

authors： Hsieh CL,Huang HS,Chen KC,Saka T,Chiang CY,Chung LWK,Sung SY

更新日期：2020-01-01 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：:Ligand activation of peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) and inhibition of cyclooxygenase-2 (COX2) activity by nonsteroidal anti-inflammatory drugs (NSAID) can both attenuate skin tumorigenesis. The present study examined the hypothesis that combining ligand activation of PPARβ/δ with inhibition o...

journal_title：Molecular cancer therapeutics

authors： Zhu B,Bai R,Kennett MJ,Kang BH,Gonzalez FJ,Peters JM

更新日期：2010-12-01 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 both erlotinib and gefitinib target the EGF receptor (EGFR), erlotinib is effective in patients with EGFR wild-type or mutated tumors, whereas gefitinib is only beneficial for patients with activating mutations. To determine whether these differences in clinical outcomes can be attributed to their respective ...

journal_title：Molecular cancer therapeutics

authors： Augustin A,Lamerz J,Meistermann H,Golling S,Scheiblich S,Hermann JC,Duchateau-Nguyen G,Tzouros M,Avila DW,Langen H,Essioux L,Klughammer B

更新日期：2013-04-01 00:00:00

abstract：:In the current study, we examined a panel of serially passaged glioblastoma xenografts, in the context of an intracranial tumor therapy response model, to identify associations between glioblastoma molecular characteristics and tumor sensitivity to the epidermal growth factor receptor (EGFR) kinase inhibitor erlotinib...

journal_title：Molecular cancer therapeutics

authors： Sarkaria JN,Yang L,Grogan PT,Kitange GJ,Carlson BL,Schroeder MA,Galanis E,Giannini C,Wu W,Dinca EB,James CD

更新日期：2007-03-01 00:00:00

abstract：:Zoledronic acid, a third-generation bisphosphonate, has been shown to reduce cell migration, invasion, and metastasis. However, the effects of zoledronic acid on the epithelial-mesenchymal transition (EMT), a cellular process essential to the metastatic cascade, remain unclear. Therefore, the effects of zoledronic aci...

journal_title：Molecular cancer therapeutics

authors： Schech AJ,Kazi AA,Gilani RA,Brodie AH

更新日期：2013-07-01 00:00:00

abstract：:Previous work has shown that cisplatin (CDDP) becomes concentrated in lysosomes, and that acquired resistance to CDDP is associated with abnormalities of protein trafficking and secretion. The lysosomal compartment in CDDP-sensitive 2008 human ovarian carcinoma cells was compared with that in CDDP-resistant 2008/C13*5...

journal_title：Molecular cancer therapeutics

authors： Safaei R,Larson BJ,Cheng TC,Gibson MA,Otani S,Naerdemann W,Howell SB

更新日期：2005-10-01 00:00:00

abstract：:Endocrine therapy is important for management of patients with estrogen receptor (ER)-positive breast cancer; however, positive ER staining does not reliably predict therapy response. We assessed the potential to improve prediction of response to endocrine treatment of a novel test that quantifies functional ER pathwa...

journal_title：Molecular cancer therapeutics

authors： Inda MA,Blok EJ,Kuppen PJK,Charehbili A,den Biezen-Timmermans EC,van Brussel A,Fruytier SE,Meershoek-Klein Kranenbarg E,Kloet S,van der Burg B,Martens JWM,Sims AH,Turnbull AK,Dixon JM,Verhaegh W,Kroep JR,van de Velde CJH

更新日期：2020-02-01 00:00:00

abstract：:Arsenic trioxide (As(2)O(3)) has been used successfully in the treatment of acute promyelocytic leukemia. However, effects of As(2)O(3) in normal peripheral blood T cells have not been studied in detail. The purpose of this study was to investigate whether As(2)O(3) would induce apoptosis in normal T cells and therefo...

journal_title：Molecular cancer therapeutics

authors： Gupta S,Yel L,Kim D,Kim C,Chiplunkar S,Gollapudi S

更新日期：2003-08-01 00:00:00

abstract：:A novel series of 3,5-diaryl-oxadiazoles was identified as apoptosis-inducing agents through our cell and chemical genetics-based screening assay for compounds that induce apoptosis using a chemical genetics approach. Several analogues from this series including MX-74420 and MX-126374 were further characterized. MX-12...

journal_title：Molecular cancer therapeutics

authors： Jessen KA,English NM,Yu Wang J,Maliartchouk S,Archer SP,Qiu L,Brand R,Kuemmerle J,Zhang HZ,Gehlsen K,Drewe J,Tseng B,Cai SX,Kasibhatla S

更新日期：2005-05-01 00:00:00

abstract：:Several antiangiogenic drugs targeting VEGF/VEGF receptor (VEGFR) that were approved by the Food and Drug Administration for many cancer types, including colorectal and lung cancer, can effectively reduce tumor growth. However, targeting the VEGF signaling pathway will probably influence the normal function of endothe...

journal_title：Molecular cancer therapeutics

authors： Chen CT,Yamaguchi H,Lee HJ,Du Y,Lee HH,Xia W,Yu WH,Hsu JL,Yen CJ,Sun HL,Wang Y,Yeh ET,Hortobagyi GN,Hung MC

更新日期：2011-08-01 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：:DNA topoisomerase I (Top1) inhibition by camptothecin derivatives can impair the hypoxia-induced cell transcriptional response. In the present work, we determined molecular aspects of the mechanism of camptothecin's effects on hypoxia-inducible factor-1α (HIF-1α) activity in human cancer cells. In particular, we provi...

journal_title：Molecular cancer therapeutics

authors： Bertozzi D,Marinello J,Manzo SG,Fornari F,Gramantieri L,Capranico G

更新日期：2014-01-01 00:00:00

abstract：:Crizotinib (PF02341066) is a tyrosine kinase inhibitor of anaplastic lymphoma kinase (ALK) that has been shown to selectively inhibit growth of cancer cells that harbor the EML4-ALK fusion found in a subset of patients with non-small cell lung cancer (NSCLC). While in clinical trials, PF02341066 has shown a significan...

journal_title：Molecular cancer therapeutics

authors： Sun Y,Nowak KA,Zaorsky NG,Winchester CL,Dalal K,Giacalone NJ,Liu N,Werner-Wasik M,Wasik MA,Dicker AP,Lu B

更新日期：2013-05-01 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：:Hepatocellular carcinoma is highly chemoresistant, and ATP-binding cassette subfamily G member 2 (ABCG2) is thought to play a critical role in this drug resistance. The present study aims to develop effective therapeutic strategies to decrease ABCG2 expression level and to surmount drug resistance in hepatocellular ca...

journal_title：Molecular cancer therapeutics

authors： Hou H,Sun H,Lu P,Ge C,Zhang L,Li H,Zhao F,Tian H,Zhang L,Chen T,Yao M,Li J

更新日期：2013-12-01 00:00:00

abstract：:Bortezomib combination with gemcitabine/cisplatin in patients with advanced tumors, predominantly non-small cell lung cancer (NSCLC), showed an unexpected transient drop in the deoxycytidine plasma levels, a marker for gemcitabine activity. This study investigates the pharmacokinetic/pharmacodynamic effect of bortezom...

journal_title：Molecular cancer therapeutics

authors： Ceresa C,Giovannetti E,Voortman J,Laan AC,Honeywell R,Giaccone G,Peters GJ

更新日期：2009-05-01 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：:Activation of anaplastic lymphoma receptor tyrosine kinase (ALK) is involved in the pathogenesis of several carcinomas, including non-small cell lung cancer (NSCLC). Echinoderm microtubule-associated protein like 4 (EML4)-ALK, which is derived from the rearrangement of ALK and EML4 genes, has been validated as a thera...

journal_title：Molecular cancer therapeutics

authors： Mori M,Ueno Y,Konagai S,Fushiki H,Shimada I,Kondoh Y,Saito R,Mori K,Shindou N,Soga T,Sakagami H,Furutani T,Doihara H,Kudoh M,Kuromitsu S

更新日期：2014-02-01 00:00:00

abstract：:Prostate-specific membrane antigen (PSMA) is a membrane-bound glutamate carboxypeptidase that is highly expressed in nearly all prostate cancers with the highest expression in metastatic castration-resistant prostate cancer (mCRPC). The prevalence of increased surface expression and constitutive internalization of PSM...

journal_title：Molecular cancer therapeutics

authors： Cho S,Zammarchi F,Williams DG,Havenith CEG,Monks NR,Tyrer P,D'Hooge F,Fleming R,Vashisht K,Dimasi N,Bertelli F,Corbett S,Adams L,Reinert HW,Dissanayake S,Britten CE,King W,Dacosta K,Tammali R,Schifferli K,Strout P

更新日期：2018-10-01 00:00:00

abstract：:Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) selectively kills tumor cells. However, its short half-life, poor delivery, and TRAIL-resistant tumor cells have diminished its clinical efficacy. In this study, we explored whether novel delivery methods will represent new and effective ways to treat gli...

journal_title：Molecular cancer therapeutics

authors： Hingtgen S,Ren X,Terwilliger E,Classon M,Weissleder R,Shah K

更新日期：2008-11-01 00:00:00

abstract：:The present study aimed to investigate the therapeutic efficacy of combining vascular endothelial growth factor (VEGF) receptor blockade using tyrosine kinase inhibitor PTK787 with hypoxia for the treatment of hepatocellular carcinoma (HCC). The in vivo effects of the treatments were determined in a rat orthotopic HCC...

journal_title：Molecular cancer therapeutics

authors： Yang ZF,Poon RT,Liu Y,Lau CK,Ho DW,Tam KH,Lam CT,Fan ST

更新日期：2006-09-01 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：:Conditionally replicating adenoviruses (CRAd) can replicate specifically in cancer cells and lyse them. The CRAds were widely used in the preclinical and clinical studies of cancer therapy. We hypothesize that more precisely regulated replication of CRAds may further improve the vector safety profile and enhance its a...

journal_title：Molecular cancer therapeutics

authors： Wang X,Su C,Cao H,Li K,Chen J,Jiang L,Zhang Q,Wu X,Jia X,Liu Y,Wang W,Liu X,Wu M,Qian Q

更新日期：2008-06-01 00:00:00

abstract：:Why does it seem that, repeatedly, when a new treatment with a striking effect is discovered in the cancer field, it is effective for a very rare cancer type? For example, groundbreaking therapeutic discoveries have been made for extremely uncommon malignancies such as hairy cell leukemia, chronic myelogenous leukemia...

journal_title：Molecular cancer therapeutics

authors： Braiteh F,Kurzrock R

更新日期：2007-04-01 00:00:00

abstract：:Many malignant human tumors, including melanomas, are auxotrophic for arginine due to reduced expression of argininosuccinate synthetase-1 (ASS1), the rate-limiting enzyme for arginine biosynthesis. Pegylated arginine deiminase (ADI-PEG20), which degrades extracellular arginine, resulting in arginine deprivation, has ...

journal_title：Molecular cancer therapeutics

authors： Long Y,Tsai WB,Wangpaichitr M,Tsukamoto T,Savaraj N,Feun LG,Kuo MT

更新日期：2013-11-01 00:00:00