Novel Miniaturized Drug Conjugate Leverages HSP90-driven Tumor Accumulation to Overcome PI3K Inhibitor Delivery Challenges to Solid Tumors.

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：:Cyclin-dependent kinases 4 and 6 (CDK4/6) have emerged as important therapeutic targets. Pharmacologic inhibitors of these kinases function to inhibit cell-cycle progression and exert other important effects on the tumor and host environment. Because of their impact on the cell cycle, CDK4/6 inhibitors (CDK4/6i) have ...

journal_title：Molecular cancer therapeutics

authors： Roberts PJ,Kumarasamy V,Witkiewicz AK,Knudsen ES

更新日期：2020-08-01 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：: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：:Upregulation of HER2 is a hallmark of 20% to 30% of invasive breast cancers, rendering this receptor an attractive target for cancer therapy. Although HER2-targeting agents have provided substantial clinical benefit as cancer therapeutics, there is a need for the development of new agents aiming at circumventing anti-...

journal_title：Molecular cancer therapeutics

authors： Brack S,Attinger-Toller I,Schade B,Mourlane F,Klupsch K,Woods R,Hachemi H,von der Bey U,Koenig-Friedrich S,Bertschinger J,Grabulovski D

更新日期：2014-08-01 00:00:00

abstract：:17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) converts estrone (E1) into estradiol (E2) and is expressed in many steroidogenic tissues and breast cancer cell lines. Because the potent estrogen E2 stimulates the growth and development of hormone-dependent diseases, inhibition of the final step of E2 synthesis is c...

journal_title：Molecular cancer therapeutics

authors： Ayan D,Maltais R,Roy J,Poirier D

更新日期：2012-10-01 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：: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：:Inhibition of both the de novo (DNP) and salvage (NSP) pathways of nucleoside synthesis has been demonstrated to impair leukemia cells. We endeavored to determine whether this approach would be efficacious in glioblastoma. To diminish nucleoside biosynthesis, we utilized compound DI-39, which selectively targets NSP, ...

journal_title：Molecular cancer therapeutics

authors： Laks DR,Ta L,Crisman TJ,Gao F,Coppola G,Radu CG,Nathanson DA,Kornblum HI

更新日期：2016-06-01 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

abstract：:The epithelial-mesenchymal transition (EMT) is an important mechanism of resistance to angiogenesis inhibition. The ability of EMT pathway genetic variants to predict the efficacy of antiangiogenic therapy is unknown. We analyzed associations between functional SNPs in EMT-related genes and outcomes in metastatic colo...

journal_title：Molecular cancer therapeutics

authors： Matsusaka S,Zhang W,Cao S,Hanna DL,Sunakawa Y,Sebio A,Ueno M,Yang D,Ning Y,Parekh A,Okazaki S,Berger MD,Ichikawa W,Mizunuma N,Lenz HJ

更新日期：2016-06-01 00:00:00

abstract：:The NF-κB transcription factor functions as a crucial regulator of cell survival and chemoresistance in pancreatic cancer. Recent studies suggest that tocotrienols, which are the unsaturated forms of vitamin E, are a promising class of anticancer compounds that inhibit the growth and survival of many cancer cells, inc...

journal_title：Molecular cancer therapeutics

authors： Husain K,Francois RA,Yamauchi T,Perez M,Sebti SM,Malafa MP

更新日期：2011-12-01 00:00:00

abstract：:During camptothecin- and etoposide (VP-16)-induced apoptosis in HL-60 cells, the expression level of cell death receptor-3 (DR3), cell death receptor-4 (DR4), and FAS remained mostly unchanged, whereas the expression of silencers of death domain (SODD) and FLICE inhibitory proteins, inhibitors of the cell death recept...

journal_title：Molecular cancer therapeutics

authors： Bergeron S,Beauchemin M,Bertrand R

更新日期：2004-12-01 00:00:00

abstract：:The cytosine analogue decitabine alters hematopoietic differentiation. For example, decitabine treatment increases self-renewal of normal hematopoietic stem cells. The mechanisms underlying decitabine-induced shifts in differentiation are poorly understood, but likely relate to the ability of decitabine to deplete the...

journal_title：Molecular cancer therapeutics

authors： Hu Z,Negrotto S,Gu X,Mahfouz R,Ng KP,Ebrahem Q,Copelan E,Singh H,Maciejewski JP,Saunthararajah Y

更新日期：2010-06-01 00:00:00

abstract：:Multiple myeloma is a slowly proliferating B-cell malignancy that accumulates apoptosis-resistant and replication-quiescent cell populations, posing a challenge for current chemotherapeutics that target rapidly replicating cells. Multiple myeloma remains an incurable disease in need of new therapeutic approaches. The ...

journal_title：Molecular cancer therapeutics

authors： Ghias K,Ma C,Gandhi V,Platanias LC,Krett NL,Rosen ST

更新日期：2005-04-01 00:00:00

abstract：:Small cell lung cancer (SCLC) easily acquires multidrug resistance after successful initial therapy. Overexpression of ATP-binding cassette (ABC) transporters is important for the multidrug resistance. Among them, ABCB1 and ABCG2 are known to be upregulated in chemoresistant SCLC cells. We found that human epidermal g...

journal_title：Molecular cancer therapeutics

authors： Minami T,Kijima T,Otani Y,Kohmo S,Takahashi R,Nagatomo I,Hirata H,Suzuki M,Inoue K,Takeda Y,Kida H,Tachibana I,Kumanogoh A

更新日期：2012-04-01 00:00:00

abstract：:Localized activation of the prodrug ifosfamide in or close to tumors by implanting encapsulated ifosfamide-activating cells is an efficacious strategy for tumor therapy. The aim of this study was to evaluate the feasibility of subsieve-size agarose capsules for enclosing the cells in this application. Compared with ma...

journal_title：Molecular cancer therapeutics

authors： Sakai S,Kawabata K,Tanaka S,Harimoto N,Hashimoto I,Mu C,Salmons B,Ijima H,Kawakami K

更新日期：2005-11-01 00:00:00

abstract：:The spindle assembly checkpoint kinase TTK (Mps1) is a key regulator of chromosome segregation and is the subject of novel targeted therapy approaches by small-molecule inhibitors. Although the first TTK inhibitors have entered phase I dose escalating studies in combination with taxane chemotherapy, a patient stratifi...

journal_title：Molecular cancer therapeutics

authors： Zaman GJR,de Roos JADM,Libouban MAA,Prinsen MBW,de Man J,Buijsman RC,Uitdehaag JCM

更新日期：2017-11-01 00:00:00

abstract：:The MET receptor tyrosine kinase, the receptor for hepatocyte growth factor (HGF), has been implicated in cancer growth, invasion, migration, angiogenesis, and metastasis in a broad variety of human cancers, including human hepatocellular carcinoma (HCC). Recently, MET was suggested to be a potential target for the pe...

journal_title：Molecular cancer therapeutics

authors： Jo JC,Choi EK,Shin JS,Moon JH,Hong SW,Lee HR,Kim SM,Jung SA,Lee DH,Jung SH,Lee SH,Kim JE,Kim KP,Hong YS,Suh YA,Jang SJ,Choi EK,Lee JS,Jin DH,Kim TW

更新日期：2015-11-01 00:00:00

abstract：:Aberrant overexpression of antiapoptotic members of the Bcl-2 protein family, including Bcl-2 and Bcl-X(L), contributes to malignant transformation and subsequent resistance to traditional chemotherapeutics. Thus, these proteins represent attractive targets for novel anticancer agents. The small molecule, gossypol, wa...

journal_title：Molecular cancer therapeutics

authors： Oliver CL,Miranda MB,Shangary S,Land S,Wang S,Johnson DE

更新日期：2005-01-01 00:00:00

abstract：:Using the "one-bead one-peptide" combinatorial technology, a library of random cyclic octapeptides and nonapeptides, consisting of natural and unnatural amino acids, was synthesized on polystyrene beads. This library was used to screen for peptides that promoted attachment and proliferation of bronchioloalveolar carci...

journal_title：Molecular cancer therapeutics

authors： Mikawa M,Wang H,Guo L,Liu R,Marik J,Takada Y,Lam K,Lau D

更新日期：2004-10-01 00:00:00

abstract：:DNA cytosine methylation plays a considerable role in normal development, gene regulation, and carcinogenesis. Hypermethylation of the promoters of some tumor suppressor genes and the associated silencing of these genes often occur in certain cancer types. The reversal of this process by DNA methylation inhibitors is ...

journal_title：Molecular cancer therapeutics

authors： Chuang JC,Yoo CB,Kwan JM,Li TW,Liang G,Yang AS,Jones PA

更新日期：2005-10-01 00:00:00

abstract：:The treatment of breast cancer cells obtained by blocking the aberrant activation of the proliferation signaling pathways PI3K/Akt/mTOR and MEK/ERK has received considerable attention in recent years. Previous studies showed that Taiwanin A inhibited the proliferation of several types of cancer cells. In this study, w...

journal_title：Molecular cancer therapeutics

authors： Kuo YH,Chiang EI,Chao CY,Rodriguez RL,Chou PY,Tsai SY,Pai MH,Tang FY

更新日期：2017-03-01 00:00:00

abstract：:Marine invertebrates, algae, and microorganisms are prolific producers of novel secondary metabolites. Some of these secondary metabolites have the potential to be developed as chemotherapeutic agents for the treatment of a wide variety of diseases, including cancer. We describe here the mechanism leading to apoptosis...

journal_title：Molecular cancer therapeutics

authors： Whibley CE,McPhail KL,Keyzers RA,Maritz MF,Leaner VD,Birrer MJ,Davies-Coleman MT,Hendricks DT

更新日期：2007-09-01 00:00:00

abstract：:Our previous studies and those of others have indicated that X-linked inhibitor of apoptosis protein (XIAP) holds promise as a target gene in colon cancer gene therapy. In this study, we constructed an adenoviral vector to deliver small hairpin RNA (shRNA) against XIAP (XIAP-shRNA) into colon cancer cells and tested i...

journal_title：Molecular cancer therapeutics

authors： Dai Y,Qiao L,Chan KW,Yang M,Ye J,Zhang R,Ma J,Zou B,Lam CS,Wang J,Pang R,Tan VP,Lan HY,Wong BC

更新日期：2009-09-01 00:00:00

abstract：:The mammalian target of rapamycin (mTOR) is a serine/threonine protein kinase that exists in two complexes (mTORC1 and mTORC2) and integrates extracellular and intracellular signals to act as a master regulator of cell growth, survival, and metabolism. The PI3K/AKT/mTOR prosurvival pathway is often dysregulated in mul...

journal_title：Molecular cancer therapeutics

authors： Slotkin EK,Patwardhan PP,Vasudeva SD,de Stanchina E,Tap WD,Schwartz GK

更新日期：2015-02-01 00:00:00

abstract：:While epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors improve the prognosis of patients with EGFR mutant lung cancer, the prognosis of patients with nonmutant EGFR lung cancer, especially those with metastases, is still extremely poor. We have assessed the therapeutic efficacy of E7080, an orally av...

journal_title：Molecular cancer therapeutics

authors： Ogino H,Hanibuchi M,Kakiuchi S,Trung VT,Goto H,Ikuta K,Yamada T,Uehara H,Tsuruoka A,Uenaka T,Wang W,Li Q,Takeuchi S,Yano S,Nishioka Y,Sone S

更新日期：2011-07-01 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：: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：:Antiangiogenic therapies targeting VEGFA have been commonly used in clinics to treat cancers over the past decade. However, their clinical efficacy has been limited, with drawbacks including acquisition of resistance and activation of compensatory pathways resulting from elevated circulating VEGFB and placental growth...

journal_title：Molecular cancer therapeutics

authors： Lee JE,Kim C,Yang H,Park I,Oh N,Hua S,Jeong H,An HJ,Kim SC,Lee GM,Koh GY,Kim HM

更新日期：2015-02-01 00:00:00