The apoptotic effect of HA14-1, a Bcl-2-interacting small molecular compound, requires Bax translocation and is enhanced by PK11195.

abstract：:Disruption of Cyclin-Dependent Kinase 12 (CDK12) is known to lead to defects in DNA repair and sensitivity to platinum salts and PARP1/2 inhibitors. However, CDK12 has also been proposed as an oncogene in breast cancer. We therefore aimed to assess the frequency and distribution of CDK12 protein expression by IHC in i...

journal_title：Molecular cancer therapeutics

authors： Naidoo K,Wai PT,Maguire SL,Daley F,Haider S,Kriplani D,Campbell J,Mirza H,Grigoriadis A,Tutt A,Moseley PM,Abdel-Fatah TMA,Chan SYT,Madhusudan S,Rhaka EA,Ellis IO,Lord CJ,Yuan Y,Green AR,Natrajan R

更新日期：2018-01-01 00:00:00

abstract：:Genital human papillomavirus (HPV) infection is the primary cause of cervical cancer in women. Although the HPV recombinant L1 protein was recently licensed as an available vaccine, it has numerous shortcomings. New vaccination strategies should be considered. To enable the design of a prophylactic and therapeutic low...

journal_title：Molecular cancer therapeutics

authors： Bian T,Wang Y,Lu Z,Ye Z,Zhao L,Ren J,Zhang H,Ruan L,Tian H

更新日期：2008-05-01 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：:Vascular endothelial growth factor (VEGF)-induced endothelial cell migration is an important component of tumor angiogenesis. Rho and Rho-associated kinase (ROCK) are key regulators of focal adhesion, stress fiber formation, and thus cell motility. Inhibitors of this pathway have been shown to inhibit endothelial cell...

journal_title：Molecular cancer therapeutics

authors： Yin L,Morishige K,Takahashi T,Hashimoto K,Ogata S,Tsutsumi S,Takata K,Ohta T,Kawagoe J,Takahashi K,Kurachi H

更新日期：2007-05-01 00:00:00

abstract：:Insulin-like growth factor-I receptor (IGF-IR) is an important mediator of tumor cell survival and shows prognostic significance in sarcoma. To explore potential therapeutic strategies for interrupting signaling through this pathway, we assessed the ability of cyclolignan picropodophyllin (PPP), a member of the cyclol...

journal_title：Molecular cancer therapeutics

authors： Duan Z,Choy E,Harmon D,Yang C,Ryu K,Schwab J,Mankin H,Hornicek FJ

更新日期：2009-08-01 00:00:00

abstract：:Soft-tissue sarcomas (STS) represent a heterogeneous group of rare, malignant tumors of mesenchymal origin. Reliable in vivo sarcoma research models are scarce. We aimed to establish and characterize histologically and molecularly stable patient-derived xenograft (PDX) models from a broad variety of STS subtypes. A to...

journal_title：Molecular cancer therapeutics

authors： Cornillie J,Wozniak A,Li H,Wang Y,Boeckx B,Gebreyohannes YK,Wellens J,Vanleeuw U,Hompes D,Stas M,Sinnaeve F,Wafa H,Lambrechts D,Debiec-Rychter M,Sciot R,Schöffski P

更新日期：2019-06-01 00:00:00

abstract：:Tumors can exploit the indoleamine 2,3-dioxygenase 1 (IDO1) pathway to create an immunosuppressive microenvironment. Activated IDO1 metabolizes tryptophan into immunosuppressive kynurenine, leading to suppressed effector T-cell (Teff) proliferation, allowing for tumor escape from host immune surveillance. IDO1 inhibit...

journal_title：Molecular cancer therapeutics

authors： Balog A,Lin TA,Maley D,Gullo-Brown J,Kandoussi EH,Zeng J,Hunt JT

更新日期：2020-12-09 00:00:00

abstract：:Uveal melanoma is a rare and aggressive cancer that originates in the eye. Currently, there are no approved targeted therapies and very few effective treatments for this cancer. Although activating mutations in the G protein alpha subunits, GNAQ and GNA11, are key genetic drivers of the disease, few additional drug ta...

journal_title：Molecular cancer therapeutics

authors： Rago F,Elliott G,Li A,Sprouffske K,Kerr G,Desplat A,Abramowski D,Chen JT,Farsidjani A,Xiang KX,Bushold G,Feng Y,Shirley MD,Bric A,Vattay A,Möbitz H,Nakajima K,Adair CD,Mathieu S,Ntaganda R,Smith T,Papillon JPN,

更新日期：2020-10-01 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：:Despite significant advances in combinations of radiotherapy and chemotherapy, altered fractionation schedules and image-guided radiotherapy, many cancer patients fail to benefit from radiation. A prevailing hypothesis is that targeting repair of DNA double strand breaks (DSB) can enhance radiation effects in the tumo...

journal_title：Molecular cancer therapeutics

authors： Efimova EV,Ricco N,Labay E,Mauceri HJ,Flor AC,Ramamurthy A,Sutton HG,Weichselbaum RR,Kron SJ

更新日期：2018-02-01 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：:Epithelial ovarian cancer is characterized by a low recovery rate because the disease is typically diagnosed at an advanced stage, by which time most patients (80%) already exhibit disseminated neoplasia. The cytokine receptor CXCR4 has been implicated in the development of metastasis in various tumor types. Using a p...

journal_title：Molecular cancer therapeutics

authors： Figueras A,Alsina-Sanchís E,Lahiguera Á,Abreu M,Muinelo-Romay L,Moreno-Bueno G,Casanovas O,Graupera M,Matias-Guiu X,Vidal A,Villanueva A,Viñals F

更新日期：2018-02-01 00:00:00

abstract：:Spongistatin 1, a marine experimental substance with chemotherapeutic potential, induces apoptosis and inhibits clonogenic survival of MCF-7 cells. Regarding the apoptotic signaling pathways of spongistatin 1, we present two major facts. Firstly, spongistatin 1-induced cell death, mainly caspase-independent, involves ...

journal_title：Molecular cancer therapeutics

authors： Schneiders UM,Schyschka L,Rudy A,Vollmar AM

更新日期：2009-10-01 00:00:00

abstract：:Breast cancer is a major public health problem all over the world, and the current treatment strategies are not potent enough for some patients, especially those with triple-negative breast cancer (TNBC). Recent studies have demonstrated that microRNAs (miRNA) play vital roles in the development of TNBC. In this study...

journal_title：Molecular cancer therapeutics

authors： Tang H,Liu P,Yang L,Xie X,Ye F,Wu M,Liu X,Chen B,Zhang L,Xie X

更新日期：2014-12-01 00:00:00

abstract：:The expression of cyclooxygenase (COX)-2 is increased in human cancers including cholangiocarcinoma. This study was designed to evaluate the effect and mechanisms of the selective COX-2 inhibitor celecoxib in the growth control of human cholangiocarcinoma cells. Immunohistochemical analysis using human cholangiocarcin...

journal_title：Molecular cancer therapeutics

authors： Wu T,Leng J,Han C,Demetris AJ

更新日期：2004-03-01 00:00:00

abstract：:Hsp90 is widely overexpressed in cancer cells and believed to be essential for the maintenance of malignant phenotypes. Targeting Hsp90 by small molecules has shown promise in solid and hematologic malignancies, which likely involves degradation of client oncoproteins in a cell-type-specific manner. In this study, we ...

journal_title：Molecular cancer therapeutics

authors： He K,Zheng X,Zhang L,Yu J

更新日期：2013-11-01 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：: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：: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：:RAD51 is a key protein in the homologous recombination (HR) pathway of DNA double-strand break repair, and HR represents a novel target for cancer therapy. Because imatinib (Gleevec) has been reported to reduce RAD51 protein levels, we tested the clonogenic survival for RT112, H1299, PANC1, and PC3 tumor cell lines of...

journal_title：Molecular cancer therapeutics

authors： Choudhury A,Zhao H,Jalali F,Al Rashid S,Ran J,Supiot S,Kiltie AE,Bristow RG

更新日期：2009-01-01 00:00:00

abstract：:Recently, pancreatic ductal adenocarcinoma (PDAC) has emerged as one of the most aggressive malignant tumors with the worst prognosis. Previous studies have demonstrated that long noncoding RNA metastasis-associated lung adenocarcinoma transcript 1 (MALAT1) is increased in pancreatic cancer and is identified as a diag...

journal_title：Molecular cancer therapeutics

authors： Li L,Chen H,Gao Y,Wang YW,Zhang GQ,Pan SH,Ji L,Kong R,Wang G,Jia YH,Bai XW,Sun B

更新日期：2016-09-01 00:00:00

abstract：:The effect of vascular endothelial growth factor (VEGF) ligands and cediranib on tumor cell proliferation, migration, and invasion was determined. It has recently been suggested that autocrine signaling through the VEGF receptor (VEGFR) pathway may play a role in tumor cell survival, invasion, and migration. The purpo...

journal_title：Molecular cancer therapeutics

authors： Morelli MP,Brown AM,Pitts TM,Tentler JJ,Ciardiello F,Ryan A,Jürgensmeier JM,Eckhardt SG

更新日期：2009-09-01 00:00:00

abstract：:Plasminogen activator inhibitor-1 (PAI-1) is an important endogenous inhibitor of urokinase-type plasminogen activator. Its action in tumor angiogenesis is complicated, varying with experimental setting and its cellular origin. To further understand the mechanism of the effect of PAI-1 on tumor angiogenesis, especiall...

journal_title：Molecular cancer therapeutics

authors： Chen SC,Henry DO,Reczek PR,Wong MK

更新日期：2008-05-01 00:00:00

abstract：:The secondary T790M mutation in epidermal growth factor receptor (EGFR) is the major mechanism of acquired resistance to EGFR tyrosine kinase inhibitors (TKI) in non-small cell lung cancer (NSCLC). Although irreversible EGFR TKIs, such as afatinib or dacomitinib, have been introduced to overcome the acquired resistanc...

journal_title：Molecular cancer therapeutics

authors： Kim SM,Kwon OJ,Hong YK,Kim JH,Solca F,Ha SJ,Soo RA,Christensen JG,Lee JH,Cho BC

更新日期：2012-10-01 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 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：:Activation of the epidermal growth factor receptor (EGFR) has been observed in many malignant tumors and its constitutive signal transduction facilitates the proliferation of tumors. EGFR-tyrosine kinase inhibitors, such as gefitinib, are widely used as a molecular-targeting agent for the inactivation of EGFR signalin...

journal_title：Molecular cancer therapeutics

authors： Saito K,Takigawa N,Ohtani N,Iioka H,Tomita Y,Ueda R,Fukuoka J,Kuwahara K,Ichihara E,Kiura K,Kondo E

更新日期：2013-08-01 00:00:00

abstract：:TAS-121 is a novel orally active selective covalent inhibitor of the mutant EGFR. We performed preclinical characterization of TAS-121 and compared its efficacy and selectivity for common EGFR mutations (Ex19del and L858R), first- and second- generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) resistance mutation (T7...

journal_title：Molecular cancer therapeutics

authors： Ito K,Nishio M,Kato M,Murakami H,Aoyagi Y,Ohe Y,Okayama T,Hashimoto A,Ohsawa H,Tanaka G,Nonoshita K,Ito S,Matsuo K,Miyadera K

更新日期：2019-05-01 00:00:00

abstract：:Mutations in ERK signaling drive a significant percentage of malignancies. LY3009120, a pan-RAF and dimer inhibitor, has preclinical activity in RAS- and BRAF-mutated cell lines including BRAF-mutant melanoma resistant to BRAF inhibitors. This multicenter, open-label, phase I clinical trial (NCT02014116) consisted of ...

journal_title：Molecular cancer therapeutics

authors： Sullivan RJ,Hollebecque A,Flaherty KT,Shapiro GI,Rodon Ahnert J,Millward MJ,Zhang W,Gao L,Sykes A,Willard MD,Yu D,Schade AE,Crowe K,Flynn DL,Kaufman MD,Henry JR,Peng SB,Benhadji KA,Conti I,Gordon MS,Tiu RV,Hong

更新日期：2020-02-01 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