Development of Novel Quaternary Ammonium Linkers for Antibody-Drug Conjugates.

abstract：:Nasopharyngeal carcinoma (NPC) is relatively rare in Western countries but is a common cancer in southern Asia. Many differentially expressed genes have been linked to NPC; however, how to prioritize therapeutic targets and potential drugs from unsorted gene lists remains largely unknown. We first collected 558 upregu...

journal_title：Molecular cancer therapeutics

authors： Lan MY,Chen CL,Lin KT,Lee SA,Yang WL,Hsu CN,Wu JC,Ho CY,Lin JC,Huang CY

更新日期：2010-09-01 00:00:00

abstract：:We previously reported that a pan-PAD inhibitor, YW3-56, activates p53 target genes to inhibit cancer growth. However, the p53-independent anticancer activity and molecular mechanisms of YW3-56 remain largely elusive. Here, gene expression analyses found that ATF4 target genes involved in endoplasmic reticulum (ER) st...

journal_title：Molecular cancer therapeutics

authors： Wang S,Chen XA,Hu J,Jiang JK,Li Y,Chan-Salis KY,Gu Y,Chen G,Thomas C,Pugh BF,Wang Y

更新日期：2015-04-01 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：:The tyrosine kinase receptor c-Met and its ligand hepatocyte growth factor (HGF) are frequently overexpressed and the tumor suppressor PTEN is often mutated in glioblastoma. Because PTEN can interact with c-Met-dependent signaling, we studied the effects of PTEN on c-Met-induced malignancy and associated molecular eve...

journal_title：Molecular cancer therapeutics

authors： Li Y,Guessous F,DiPierro C,Zhang Y,Mudrick T,Fuller L,Johnson E,Marcinkiewicz L,Engelhardt M,Kefas B,Schiff D,Kim J,Abounader R

更新日期：2009-02-01 00:00:00

abstract：:Raf inhibitors are under clinical investigation, specifically in patients with tumor types harboring frequent activating mutations in B-Raf. Here, we show that cell lines and tumors harboring mutant B-Raf were sensitive to a novel series of Raf inhibitors (e.g., (V600E)B-Raf A375, IC(50) on cells = 2 nmol/L; ED(50) on...

journal_title：Molecular cancer therapeutics

authors： Carnahan J,Beltran PJ,Babij C,Le Q,Rose MJ,Vonderfecht S,Kim JL,Smith AL,Nagapudi K,Broome MA,Fernando M,Kha H,Belmontes B,Radinsky R,Kendall R,Burgess TL

更新日期：2010-08-01 00:00:00

abstract：:Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and for maintaining the spindle assembly checkpoint until all chromosomes are properly attached. Mps1 is expressed at high levels during mitosis and is abundantly expressed in cancer cells. Disr...

journal_title：Molecular cancer therapeutics

authors： Tardif KD,Rogers A,Cassiano J,Roth BL,Cimbora DM,McKinnon R,Peterson A,Douce TB,Robinson R,Dorweiler I,Davis T,Hess MA,Ostanin K,Papac DI,Baichwal V,McAlexander I,Willardsen JA,Saunders M,Christophe H,Kumar DV,Wet

更新日期：2011-12-01 00:00:00

abstract：:Phosphatidylinositol 3-kinase/phosphatidylinositide-dependent protein kinase 1 (PDPK1)/Akt signaling plays a critical role in activating proliferation and survival pathways within cancer cells. We report the molecular pharmacology and antitumor activity of PHT-427, a compound designed to bind to the pleckstrin homolog...

journal_title：Molecular cancer therapeutics

authors： Meuillet EJ,Zuohe S,Lemos R,Ihle N,Kingston J,Watkins R,Moses SA,Zhang S,Du-Cuny L,Herbst R,Jacoby JJ,Zhou LL,Ahad AM,Mash EA,Kirkpatrick DL,Powis G

更新日期：2010-03-01 00:00:00

abstract：:Acquired resistance severely hinders the application of small-molecule inhibitors. Our understanding of acquired resistance related to FGFRs is limited. Here, to explore the underlying mechanism of acquired resistance in FGFR-aberrant cancer cells, we generated cells resistant to multiple FGFR inhibitors (FGFRi) and i...

journal_title：Molecular cancer therapeutics

authors： Wang X,Ai J,Liu H,Peng X,Chen H,Chen Y,Su Y,Shen A,Huang X,Ding J,Geng M

更新日期：2019-03-01 00:00:00

abstract：:STAT3 has been recognized for its key role in the progression of cancer, where it is frequently upregulated or constitutively hyperactivated, contributing to tumor cell proliferation, survival, and migration, as well as angiogenesis and suppression of antitumor immunity. Given the ubiquity of dysregulated STAT3 activi...

journal_title：Molecular cancer therapeutics

authors： Shiah JV,Grandis JR,Johnson DE

更新日期：2020-11-17 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：:The serine/threonine kinase AKT/PKB plays a critical role in cancer and represents a rational target for therapy. Although efforts in targeting AKT pathway have accelerated in recent years, relatively few small molecule inhibitors of AKT have been reported. The development of selective AKT inhibitors is further challe...

journal_title：Molecular cancer therapeutics

authors： Toral-Barza L,Zhang WG,Huang X,McDonald LA,Salaski EJ,Barbieri LR,Ding WD,Krishnamurthy G,Hu YB,Lucas J,Bernan VS,Cai P,Levin JI,Mansour TS,Gibbons JJ,Abraham RT,Yu K

更新日期：2007-11-01 00:00:00

abstract：:Recent studies have shown that up to 90% of viral vectors could disseminate to normal organs following intratumoral infusion. The amount of dissemination might be dependent on the infusion conditions. Therefore, we investigated the effects of infusion rate, volume, and dose on transgene expression in liver and tumor t...

journal_title：Molecular cancer therapeutics

authors： Wang Y,Wang H,Li CY,Yuan F

更新日期：2006-02-01 00:00:00

abstract：:Previously, we constructed a recombinant Bifidobacterium longum displaying a partial mouse Wilms' tumor 1 (WT1) protein (B. longum 420) as an oral cancer vaccine using a bacterial vector and demonstrated that oral administration of B. longum 420 significantly inhibited tumor growth compared with the Db126 WT1 peptide ...

journal_title：Molecular cancer therapeutics

authors： Kitagawa K,Gonoi R,Tatsumi M,Kadowaki M,Katayama T,Hashii Y,Fujisawa M,Shirakawa T

更新日期：2019-05-01 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：:Multiple myeloma remains incurable and the majority of patients die within 5 years of diagnosis. Reolysin, the infusible form of human reovirus (RV), is a novel viral oncolytic therapy associated with antitumor activity likely resulting from direct oncolysis and a virus-mediated antitumor immune response. Results from...

journal_title：Molecular cancer therapeutics

authors： Stiff A,Caserta E,Sborov DW,Nuovo GJ,Mo X,Schlotter SY,Canella A,Smith E,Badway J,Old M,Jaime-Ramirez AC,Yan P,Benson DM,Byrd JC,Baiocchi R,Kaur B,Hofmeister CC,Pichiorri F

更新日期：2016-05-01 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：:For a subpopulation of acute myeloid leukemia (AML) patients, the constitutively activated tyrosine kinase, mutant FLT3, has emerged as a promising target for therapy. The development of drug resistance, however, is a growing concern for mutant FLT3 inhibitors, such as PKC412. Potential therapeutic benefit can arise f...

journal_title：Molecular cancer therapeutics

authors： Weisberg E,Choi HG,Barrett R,Zhou W,Zhang J,Ray A,Nelson EA,Jiang J,Moreno D,Stone R,Galinsky I,Fox E,Adamia S,Kung AL,Gray NS,Griffin JD

更新日期：2010-09-01 00:00:00

abstract：:NB1011, a phosphoramidate derivative of (E)-5-(2-bromovinyl)-2'-deoxyuridine, is a novel small molecule anticancer agent. NB1011 is selectively active against tumor cells expressing high levels of thymidylate synthase (TS), a critical enzyme in DNA biosynthesis. NB1011 is different from the current TS-targeted drugs, ...

journal_title：Molecular cancer therapeutics

authors： Neuteboom ST,Karjian PL,Boyer CR,Beryt M,Pegram M,Wahl GM,Shepard HM

更新日期：2002-04-01 00:00:00

abstract：:Tumor cells are efficiently killed after incubation with alpha-emitter immunoconjugates targeting tumor-specific antigens. Therefore, application of alpha-emitter immunoconjugates is a promising therapeutic option for treatment of carcinomas that are characterized by dissemination of single tumor cells in the peritone...

journal_title：Molecular cancer therapeutics

authors： Seidl C,Port M,Gilbertz KP,Morgenstern A,Bruchertseifer F,Schwaiger M,Röper B,Senekowitsch-Schmidtke R,Abend M

更新日期：2007-08-01 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：:Nanotechnology has enabled significant advances in the areas of cancer diagnosis and therapy. The field of drug delivery is a sterling example, with nanoparticles being increasingly used for generating therapeutic formulations of poorly water-soluble, yet potent anticancer drugs. Whereas a number of nanoparticle-drug ...

journal_title：Molecular cancer therapeutics

authors： Bisht S,Feldmann G,Koorstra JB,Mullendore M,Alvarez H,Karikari C,Rudek MA,Lee CK,Maitra A,Maitra A

更新日期：2008-12-01 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 cancer is the fifth leading cause of cancer death in North America. Gemcitabine improves the quality of life of patients but fails to significantly reduce mortality. Our laboratory has demonstrated previously that the phosphatidylinositol 3'-kinase inhibitor wortmannin promotes gemcitabine antitumor activit...

journal_title：Molecular cancer therapeutics

authors： Ng SS,Tsao MS,Nicklee T,Hedley DW

更新日期：2002-08-01 00:00:00

abstract：:In 2017, an estimated 17,000 individuals were diagnosed with esophageal adenocarcinoma (EAC), and less than 20% will survive 5 years. Positron emission tomography avidity is indicative of high glucose utilization and is nearly universal in EAC. TXNIP blocks glucose uptake and exhibits proapoptotic functions. Higher ex...

journal_title：Molecular cancer therapeutics

authors： Feingold PL,Surman DR,Brown K,Xu Y,McDuffie LA,Shukla V,Reardon ES,Crooks DR,Trepel JB,Lee S,Lee MJ,Gao S,Xi S,McLoughlin KC,Diggs LP,Beer DG,Nancarrow DJ,Neckers LM,Davis JL,Hoang CD,Hernandez JM,Schrump DS,R

更新日期：2018-09-01 00:00:00

abstract：:Molecular characterization of radical prostatectomy specimens after systemic therapy may identify a gene expression profile for resistance to therapy. This study assessed tumor cells from patients with prostate cancer participating in a phase II neoadjuvant docetaxel and androgen deprivation trial to identify mediator...

journal_title：Molecular cancer therapeutics

authors： Marín-Aguilera M,Codony-Servat J,Reig Ò,Lozano JJ,Fernández PL,Pereira MV,Jiménez N,Donovan M,Puig P,Mengual L,Bermudo R,Font A,Gallardo E,Ribal MJ,Alcaraz A,Gascón P,Mellado B

更新日期：2014-05-01 00:00:00

abstract：:The tumor-associated Tn antigen has been investigated extensively as a biomarker and therapeutic target. Cancer vaccines containing the Tn antigen as a single tumor antigen or as a component of a polyvalent vaccine have progressed into phase I and II clinical trials. One major focus of Tn-based vaccines is the treatme...

journal_title：Molecular cancer therapeutics

authors： Li Q,Anver MR,Butcher DO,Gildersleeve JC

更新日期：2009-04-01 00:00:00

abstract：:Resistance to antiandrogen drugs, like MDV3100, occurs in patients with castration-resistant prostate cancer (CRPC). Thus, preventing or treating antiandrogen resistance is a major clinical challenge. We identified a novel antiandrogen, Compound 30, and compared its efficacy with MDV3100. We found that Compound 30 inh...

journal_title：Molecular cancer therapeutics

authors： Kuruma H,Matsumoto H,Shiota M,Bishop J,Lamoureux F,Thomas C,Briere D,Los G,Gleave M,Fanjul A,Zoubeidi A

更新日期：2013-05-01 00:00:00

abstract：:EP-100 is a synthetic lytic peptide that specifically targets the gonadotropin-releasing hormone receptor on cancer cells. To extend the utility of EP-100, we aimed to identify effective combination therapies with EP-100 for ovarian cancer and explore potential mechanisms of this combination. A series of in vitro (MTT...

journal_title：Molecular cancer therapeutics

authors： Ma S,Pradeep S,Villar-Prados A,Wen Y,Bayraktar E,Mangala LS,Kim MS,Wu SY,Hu W,Rodriguez-Aguayo C,Leuschner C,Liang X,Ram PT,Schlacher K,Coleman RL,Sood AK

更新日期：2019-05-01 00:00:00

abstract：:One hallmark of cancer cells is their adaptation to rely upon an altered metabolic scheme that includes changes in the glycolytic pathway, known as the Warburg effect, and elevated glutamine metabolism. Glutaminase, a mitochondrial enzyme, plays a key role in the metabolism of glutamine in cancer cells, and its inhibi...

journal_title：Molecular cancer therapeutics

authors： Katt WP,Ramachandran S,Erickson JW,Cerione RA

更新日期：2012-06-01 00:00:00

abstract：:We reported previously that 5-fluorouracil (FUra) efficacy could be enhanced by increasing tumoral thymidine phosphorylase (TP) activity. Potentiated TP yield was achieved by either transfecting cells with human TP gene (A. Evrard et al., Br. J. Cancer, 80: 1726-1733, 1999) or associating FUra with 2'-deoxyinosine (d-...

journal_title：Molecular cancer therapeutics

authors： Ciccolini J,Cuq P,Evrard A,Giacometti S,Pelegrin A,Aubert C,Cano JP,Iliadis A

更新日期：2001-12-01 00:00:00