Aurora kinase inhibitors--rising stars in cancer therapeutics?

abstract：:As the population ages, more elderly patients require radiotherapy-based treatment for their pelvic malignancies, including muscle-invasive bladder cancer, as they are unfit for major surgery. Therefore, there is an urgent need to find radiosensitizing agents minimally toxic to normal tissues, including bowel and blad...

journal_title：Molecular cancer therapeutics

authors： Groselj B,Ruan JL,Scott H,Gorrill J,Nicholson J,Kelly J,Anbalagan S,Thompson J,Stratford MRL,Jevons SJ,Hammond EM,Scudamore CL,Kerr M,Kiltie AE

更新日期：2018-02-01 00:00:00

abstract：:Pulmonary metastasis is the most significant prognostic determinant for osteosarcoma, but methods for its prediction and treatment have not been established. Using oligonucleotide microarrays, we compared the global gene expression of biopsy samples between seven osteosarcoma patients who developed pulmonary metastasi...

journal_title：Molecular cancer therapeutics

authors： Kobayashi E,Masuda M,Nakayama R,Ichikawa H,Satow R,Shitashige M,Honda K,Yamaguchi U,Shoji A,Tochigi N,Morioka H,Toyama Y,Hirohashi S,Kawai A,Yamada T

更新日期：2010-03-01 00:00:00

abstract：:Survivin, an inhibitor of apoptosis protein, is highly expressed in most cancers and associated with chemotherapy resistance, increased tumor recurrence, and shorter patient survival, making antisurvivin therapy an attractive cancer treatment strategy. However, growing evidence indicates that survivin is expressed in ...

journal_title：Molecular cancer therapeutics

authors： Fukuda S,Pelus LM

更新日期：2006-05-01 00:00:00

abstract：:Camptothecin and Adriamycin are clinically important inhibitors for topoisomerase (Topo) I and Topo II, respectively. The ataxia-telangiectasia mutated (ATM) product is essential for ionizing radiation-induced DNA damage responses, but the role of ATM in Topo poisons-induced checkpoints remains unresolved. We found th...

journal_title：Molecular cancer therapeutics

authors： Siu WY,Lau A,Arooz T,Chow JP,Ho HT,Poon RY

更新日期：2004-05-01 00:00:00

abstract：:Antibody-drug conjugates (ADC) represent a promising therapeutic modality for the clinical management of cancer. We sought to develop a novel ADC that targets 5T4, an oncofetal antigen expressed on tumor-initiating cells (TIC), which comprise the most aggressive cell population in the tumor. We optimized an anti-5T4 A...

journal_title：Molecular cancer therapeutics

authors： Sapra P,Damelin M,Dijoseph J,Marquette K,Geles KG,Golas J,Dougher M,Narayanan B,Giannakou A,Khandke K,Dushin R,Ernstoff E,Lucas J,Leal M,Hu G,O'Donnell CJ,Tchistiakova L,Abraham RT,Gerber HP

更新日期：2013-01-01 00:00:00

abstract：:Soluble copolymers of camptothecin (CPT), based on poly[N-(2-hydroxypropyl) methacrylamide] (pHPMA), were obtained by conjugation through the degradable spacers -Gly-Phe-Leu-Gly- or -Gly-6-aminohexanoyl-Gly-. We investigated to what extent passive accumulation and retention of hydroxypropyl methacrylamide copolymer of...

journal_title：Molecular cancer therapeutics

authors： Zamai M,VandeVen M,Farao M,Gratton E,Ghiglieri A,Castelli MG,Fontana E,D'Argy R,Fiorino A,Pesenti E,Suarato A,Caiolfa VR

更新日期：2003-01-01 00:00:00

abstract：:Clinical decision making for human papillomavirus (HPV)-negative head and neck squamous cell carcinoma (HNSCC) is predominantly guided by disease stage and anatomic location, with few validated biomarkers. The epidermal growth factor receptor (EGFR) is an important therapeutic target, but its value in guiding therapeu...

journal_title：Molecular cancer therapeutics

authors： Beck TN,Georgopoulos R,Shagisultanova EI,Sarcu D,Handorf EA,Dubyk C,Lango MN,Ridge JA,Astsaturov I,Serebriiskii IG,Burtness BA,Mehra R,Golemis EA

更新日期：2016-10-01 00:00:00

abstract：:The majority of patients with HER2-overexpressing metastatic breast cancer who initially respond to the HER2-targeted antibody trastuzumab show disease progression within 1 year. The identification of novel agents that effectively inhibit survival of cancer cells that have progressed on trastuzumab is critical for imp...

journal_title：Molecular cancer therapeutics

authors： Rowe DL,Ozbay T,Bender LM,Nahta R

更新日期：2008-07-01 00:00:00

abstract：:Tumor glycans constitute attractive targets for therapeutic antibodies. The sialylated glycocalyx plays a prominent role in cancer progression and immune evasion. Here, we describe the characterization of the mAb, FG129, which targets tumor-associated sialylated glycan, and demonstrate its potential for multimodal can...

journal_title：Molecular cancer therapeutics

authors： Tivadar ST,McIntosh RS,Chua JX,Moss R,Parsons T,Zaitoun AM,Madhusudan S,Durrant LG,Vankemmelbeke M

更新日期：2020-03-01 00:00:00

abstract：:Acquired resistance to cancer drugs is common, also for modern targeted drugs like the Bruton tyrosine kinase (BTK) inhibitor ibrutinib, a new drug approved for the treatment of the highly aggressive and relapsing mantle cell lymphoma (MCL). The tumor microenvironment often impacts negatively on drug response. Here, w...

journal_title：Molecular cancer therapeutics

authors： Guan J,Huang D,Yakimchuk K,Okret S

更新日期：2018-05-01 00:00:00

abstract：:There is a growing recognition that current preclinical models do not reflect the tumor microenvironment in cellular, biological, and biophysical content and this may have a profound effect on drug efficacy testing, especially in the era of molecular-targeted agents. Here, we describe a method to directly embed low-pa...

journal_title：Molecular cancer therapeutics

authors： Onion D,Argent RH,Reece-Smith AM,Craze ML,Pineda RG,Clarke PA,Ratan HL,Parsons SL,Lobo DN,Duffy JP,Atherton JC,McKenzie AJ,Kumari R,King P,Hall BM,Grabowska AM

更新日期：2016-04-01 00:00:00

abstract：:Constitutively activated STAT3 and STAT5 are expressed in a wide variety of human malignancies including solid and hematopoietic cancers and often correlate with a poor prognosis and resistance to multiple therapies. Given the well established role of STAT3 in tumorigenesis, inhibition of Janus-activated kinase 2 (JAK...

journal_title：Molecular cancer therapeutics

authors： Seavey MM,Lu LD,Stump KL,Wallace NH,Hockeimer W,O'Kane TM,Ruggeri BA,Dobrzanski P

更新日期：2012-04-01 00:00:00

abstract：:The cytotoxicity of 5-aza-2'-deoxycytidine (DAC) has been linked to demethylation of the INK4a/ARF tumor suppressor gene locus in various cell systems, but the causality of this association remains unproven. To test this assumption, we have examined the effects of DAC in two human cancer cell lines of differing INK4a/...

journal_title：Molecular cancer therapeutics

authors： Xiong J,Epstein RJ

更新日期：2009-04-01 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：:Small cell lung cancer (SCLC) has a poor prognosis. Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase regulating cell proliferation, survival, migration, and invasion, which is overexpressed and/or activated in several cancers, including SCLC. We wanted to determine whether FAK contributes to SCLC aggressi...

journal_title：Molecular cancer therapeutics

authors： Aboubakar Nana F,Lecocq M,Ladjemi MZ,Detry B,Dupasquier S,Feron O,Massion PP,Sibille Y,Pilette C,Ocak S

更新日期：2019-01-01 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：:Imatinib mesylate is a potent, molecularly targeted therapy against the oncogenic tyrosine kinase BCR-ABL. Although imatinib mesylate has considerable efficacy against chronic myeloid leukemia (CML), advanced-stage CML patients frequently become refractory to this agent. The bone marrow is the predominant microenviron...

journal_title：Molecular cancer therapeutics

authors： Bewry NN,Nair RR,Emmons MF,Boulware D,Pinilla-Ibarz J,Hazlehurst LA

更新日期：2008-10-01 00:00:00

abstract：:Floxuridine is a clinically proven anticancer agent in the treatment of metastatic colon carcinomas and hepatic metastases. However, prodrug strategies may be necessary to improve its physiochemical properties and selectivity and to reduce undesirable toxicity effects. Previous studies with amino acid ester prodrugs o...

journal_title：Molecular cancer therapeutics

authors： Landowski CP,Vig BS,Song X,Amidon GL

更新日期：2005-04-01 00:00:00

abstract：:Clinical circumvention of multidrug resistance (MDR) is a Sisyphian task faced in the treatment of many cancers. Identification of several mechanisms of acquired MDR has led to the development of chemosensitizing agents that counter specific mechanisms of MDR. Initial successes in therapy using "chemosensitizers" ofte...

journal_title：Molecular cancer therapeutics

authors： Shain KH,Dalton WS

更新日期：2001-11-01 00:00:00

abstract：:IPI-504 is a novel, highly soluble small-molecule inhibitor of heat shock protein 90 (Hsp90), a protein chaperone essential for regulating homeostasis of oncoproteins and cell signaling proteins. Human epidermal growth factor receptor 2 (HER2; ErbB2) oncoprotein, expressed in a subset of metastatic breast cancers, is ...

journal_title：Molecular cancer therapeutics

authors： Leow CC,Chesebrough J,Coffman KT,Fazenbaker CA,Gooya J,Weng D,Coats S,Jackson D,Jallal B,Chang Y

更新日期：2009-08-01 00:00:00

abstract：:Deregulation of the cell cycle has long been recognized as an essential driver of tumorigenesis, and agents that selectively target key cell cycle components continue to hold promise as potential therapeutics. We have developed AZD5438, a 4-(1-isopropyl-2-methylimidazol-5-yl)-2-(4-methylsulphonylanilino) pyrimidine, a...

journal_title：Molecular cancer therapeutics

authors： Byth KF,Thomas A,Hughes G,Forder C,McGregor A,Geh C,Oakes S,Green C,Walker M,Newcombe N,Green S,Growcott J,Barker A,Wilkinson RW

更新日期：2009-07-01 00:00:00

abstract：:Nucleoside phosphonates are widely used therapeutic agents with a broad spectrum of antiviral activity. However, only a few of them are reported to have antitumor activity. In this study, we show that a tetrahydrofuran phosphonate analogue of guanosine, (-)-2-R-dihydroxyphosphinoyl-5-(S)-(guanin-9'-ylmethyl) tetrahydr...

journal_title：Molecular cancer therapeutics

authors： Leblond L,Attardo G,Hamelin B,Bouffard DY,Nguyen-Ba N,Gourdeau H

更新日期：2002-07-01 00:00:00

abstract：:p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is...

journal_title：Molecular cancer therapeutics

authors： Canon J,Osgood T,Olson SH,Saiki AY,Robertson R,Yu D,Eksterowicz J,Ye Q,Jin L,Chen A,Zhou J,Cordover D,Kaufman S,Kendall R,Oliner JD,Coxon A,Radinsky R

更新日期：2015-03-01 00:00:00

abstract：:The KiSS-1 gene has been reported to be a metastasis suppressor gene in human melanoma. The gene product was isolated from human placenta as the ligand of GPR54, a G protein-coupled receptor, and the C-terminally amidated peptide of 54 amino acids is called metastin. The binding of metastin to GPR54 has been shown to ...

journal_title：Molecular cancer therapeutics

authors： Takeda T,Kikuchi E,Mikami S,Suzuki E,Matsumoto K,Miyajima A,Okada Y,Oya M

更新日期：2012-04-01 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：:Sulfonylurea receptor 1 (SUR1) is the regulatory subunit of ATP-sensitive potassium channels (KATP channels) and the receptor of antidiabetic drugs, such as glibenclamide, which induce insulin secretion in pancreatic β cells. However, the expression and role of SUR1 in cancer are unknown. In this study, we found that ...

journal_title：Molecular cancer therapeutics

authors： Xu K,Sun G,Li M,Chen H,Zhang Z,Qian X,Li P,Xu L,Huang W,Wang X

更新日期：2019-11-01 00:00:00

abstract：:We previously showed that in innately resistant tumors, silencing of the estrogen receptor (ER) could be reversed by treatment with a histone deacetylase (HDAC) inhibitor, entinostat. Tumors were then responsive to aromatase inhibitor (AI) letrozole. Here, we investigated whether ER in the acquired letrozole-resistant...

journal_title：Molecular cancer therapeutics

authors： Sabnis GJ,Goloubeva OG,Kazi AA,Shah P,Brodie AH

更新日期：2013-12-01 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：:HER2-positive breast cancer is currently managed with chemotherapy in combination with specific anti-HER2 therapies, including trastuzumab. However, a high percentage of patients with HER2-positive tumors do not respond to trastuzumab (primary resistance) or either recur (acquired resistance), mostly due to molecular ...

journal_title：Molecular cancer therapeutics

authors： Zazo S,González-Alonso P,Martín-Aparicio E,Chamizo C,Luque M,Sanz-Álvarez M,Mínguez P,Gómez-López G,Cristóbal I,Caramés C,García-Foncillas J,Eroles P,Lluch A,Arpí O,Rovira A,Albanell J,Madoz-Gúrpide J,Rojo F

更新日期：2020-08-01 00:00:00

abstract：:GA101 is a novel glycoengineered Type II CD20 monoclonal antibody. When compared with rituximab, it mediates less complement-dependent cytotoxicity (CDC). As expected for a Type II antibody, GA101 appears not to act through CDC and is more potent than the Type I antibody rituximab in inducing cell death via nonclassic...

journal_title：Molecular cancer therapeutics

authors： Dalle S,Reslan L,Besseyre de Horts T,Herveau S,Herting F,Plesa A,Friess T,Umana P,Klein C,Dumontet C

更新日期：2011-01-01 00:00:00