abstract：:Staphylococcal nuclease domain-containing protein 1 (SND1) is a multifunctional oncoprotein overexpressed in breast cancer. Binding of metadherin (MTDH) to SND1 results in the stabilization of SND1 and is important in the initiation and progression of breast cancer. Disruption of such interaction is a potential therap...

journal_title：Molecular cancer therapeutics

authors： Li P,He Y,Chen T,Choy KY,Chow TS,Wong ILK,Yang X,Sun W,Su X,Chan TH,Chow LMC

更新日期：2021-01-01 00:00:00

abstract：:We report the discovery, via a unique high-throughput screening strategy, of a novel bioactive anticancer compound: Thiol Alkylating Compound Inducing Massive Apoptosis (TACIMA)-218. We demonstrate that this molecule engenders apoptotic cell death in genetically diverse murine and human cancer cell lines, irrespective...

journal_title：Molecular cancer therapeutics

authors： Abusarah J,Cui Y,El-Hachem N,El-Kadiry AE,Hammond-Martel I,Wurtele H,Beaudry A,Raynal NJ,Robert F,Pelletier J,Jankovic M,Mercier F,Kamyabiazar S,Annabi B,Rafei M

更新日期：2021-01-01 00:00:00

abstract：:TIGIT is an immune checkpoint inhibitor expressed by effector CD4+ and CD8+ T cells, NK cells, and regulatory T cells (Tregs). Inhibition of TIGIT-ligand binding using antagonistic anti-TIGIT mAbs has shown in vitro potential to restore T-cell function and therapeutic efficacy in murine tumor models when combined with...

journal_title：Molecular cancer therapeutics

authors： Preillon J,Cuende J,Rabolli V,Garnero L,Mercier M,Wald N,Pappalardo A,Denies S,Jamart D,Michaux AC,Pirson R,Pitard V,Bagot M,Prasad S,Houthuys E,Brouwer M,Marillier R,Lambolez F,Marchante JR,Nyawouame F,Carter MJ

更新日期：2021-01-01 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：:Complexities in treating breast cancer with bone metastasis are enhanced by a vicious protumorigenic pathology, involving a shift in skeletal homeostasis toward aggressive osteoclast activity and polarization of immune cells supporting tumor growth and immunosuppression. Recent studies signify the role of receptor act...

journal_title：Molecular cancer therapeutics

authors： Wang H,Ashton R,Hensel JA,Lee JH,Khattar V,Wang Y,Deshane JS,Ponnazhagan S

更新日期：2020-12-01 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：:Enhancer of zester homolog 2 (EZH2), a histone lysine methyltransferase and the catalytic component of polycomb repressive complex 2, has been extensively investigated as a chromatin regulator and a transcriptional suppressor by methylating H3 at lysine 27 (H3K27). EZH2 is upregulated or mutated in most cancers, and i...

journal_title：Molecular cancer therapeutics

authors： Li Q,Liu KY,Liu Q,Wang G,Jiang W,Meng Q,Yi Y,Yang Y,Wang R,Zhu S,Li C,Wu L,Zhao D,Yan L,Zhang L,Kim JS,Zu X,Kozielski AJ,Qian W,Chang JC,Patnaik A,Chen K,Cao Q

更新日期：2020-10-01 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：:Measles viruses (MV) are rapidly inactivated by anti-measles neutralizing antibodies, which has limited their clinical performance as oncolytic agents. Here, by substituting the H and F surface glycoproteins of MV with those from the homologous canine distemper virus (CDV) and engineering the CDV H attachment protein ...

journal_title：Molecular cancer therapeutics

authors： Bah ES,Nace RA,Peng KW,Muñoz-Alía MÁ,Russell SJ

更新日期：2020-10-01 00:00:00

abstract：:Trastuzumab and the related ADC, ado-trastuzumab emtansine (T-DM1), both target HER2-overexpressing cells. Together, these drugs have treatment indications in both early-stage and metastatic settings for HER2+ breast cancer. T-DM1 retains the antibody functionalities of trastuzumab and adds the potency of a cytotoxic ...

journal_title：Molecular cancer therapeutics

authors： Barfield RM,Kim YC,Chuprakov S,Zhang F,Bauzon M,Ogunkoya AO,Yeo D,Hickle C,Pegram MD,Rabuka D,Drake PM

更新日期：2020-09-01 00:00:00

abstract：:To isolate circulating tumor cells (CTC) from women with advanced cervical cancer and estimate the impact of CTCs and treatment on overall survival and progression-free survival (PFS). A total of 7.5 mL of whole blood was drawn pre-cycle 1 and 36 days post-cycle 1 from patients enrolled on Gynecologic Oncology Group 0...

journal_title：Molecular cancer therapeutics

authors： Tewari KS,Sill MW,Monk BJ,Penson RT,Moore DH,Lankes HA,Ramondetta LM,Landrum LM,Randall LM,Oaknin A,Leitao MM,Eisenhauer EL,DiSilvestro P,Van Le L,Pearl ML,Burke JJ,Salani R,Richardson DL,Michael HE,Kindelberger DW

更新日期：2020-08-26 00:00:00

abstract：:The camptothecin derivatives topoisomerase I (TOP1) inhibitors, irinotecan and topotecan, are FDA approved for the treatment of colorectal, ovarian, lung and breast cancers. Because of the chemical instability of camptothecins, short plasma half-life, drug efflux by the multidrug-resistance ABC transporters, and the s...

journal_title：Molecular cancer therapeutics

authors： Marzi L,Sun Y,Huang SN,James A,Difilippantonio S,Pommier Y

更新日期：2020-08-01 00:00:00

abstract：:The PI3K pathway is considered a master regulator for cancer due to its frequent activation, making it an attractive target for pharmacologic intervention. While substantial efforts have been made to develop drugs targeting PI3K signaling, few drugs have been able to achieve the inhibition necessary for effective tumo...

journal_title：Molecular cancer therapeutics

authors： Perino S,Moreau B,Freda J,Cirello A,White BH,Quinn JM,Kriksciukaite K,Someshwar A,Romagnoli J,Robinson M,Movassaghian S,Cipriani T,Wooster R,Bilodeau MT,Whalen KA

更新日期：2020-08-01 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：: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：: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：:Tumor-associated M2-macrophages are one of the most abundant immunosuppressive cell types in the pancreatic ductal adenocarcinoma (PDAC) tumor microenvironment (TME). However, the molecular mechanisms responsible for the generation of M2-macrophages are unclear. Here, we demonstrated that overexpression of DCLK1-isofo...

journal_title：Molecular cancer therapeutics

authors： Chandrakesan P,Panneerselvam J,May R,Weygant N,Qu D,Berry WR,Pitts K,Stanger BZ,Rao CV,Bronze MS,Houchen CW

更新日期：2020-07-01 00:00:00

abstract：:The PI3K-AKT pathway has pleiotropic effects and its inhibition has long been of interest in the management of prostate cancer, where a compensatory increase in PI3K signaling has been reported following androgen receptor (AR) blockade. Prostate cancer cells can also bypass AR blockade through induction of other hormo...

journal_title：Molecular cancer therapeutics

authors： Adelaiye-Ogala R,Gryder BE,Nguyen YTM,Alilin AN,Grayson AR,Bajwa W,Jansson KH,Beshiri ML,Agarwal S,Rodriguez-Nieves JA,Capaldo B,Kelly K,VanderWeele DJ

更新日期：2020-07-01 00:00:00

abstract：:Long noncoding RNAs (lncRNA) have been found to play critical roles in tumorigenesis and the development of various cancers, including hepatocellular carcinoma (HCC). Metastasis associated with lung adenocarcinoma transcript-1 (MALAT1) has been identified as an oncogene and prognostic biomarker in HCC. Here, we demons...

journal_title：Molecular cancer therapeutics

authors： Fan L,Huang X,Chen J,Zhang K,Gu YH,Sun J,Cui SY

更新日期：2020-05-01 00:00:00

abstract：:Androgen deprivation therapy and second-generation androgen receptor signaling inhibitors such as enzalutamide are standard treatments for advanced/metastatic prostate cancer. Unfortunately, most men develop resistance and relapse; signaling via insulin-like growth factor (IGF) has been implicated in castration-resist...

journal_title：Molecular cancer therapeutics

authors： Weyer-Czernilofsky U,Hofmann MH,Friedbichler K,Baumgartinger R,Adam PJ,Solca F,Kraut N,Nguyen HM,Corey E,Liu G,Sprenger CC,Plymate SR,Bogenrieder T

更新日期：2020-04-01 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：:The application of cancer gene therapy has heretofore been restricted to local, or locoregional, neoplastic disease contexts. This is owing to the lack of gene transfer vectors, which embody the requisite target cell selectivity in vivo required for metastatic disease applications. To this end, we have explored novel ...

journal_title：Molecular cancer therapeutics

authors： Lee M,Lu ZH,Li J,Kashentseva EA,Dmitriev IP,Mendonca SA,Curiel DT

更新日期：2020-03-01 00:00:00

abstract：:With the increase of treatment course, resistance to EGFR blockade is inevitable in patients with metastatic colorectal cancer (mCRC). KRAS mutations have been considered to be primary drivers of this resistance; however, the potential function of other genes has not been extensively investigated. This study collected...

journal_title：Molecular cancer therapeutics

authors： Ye S,Hu X,Ni C,Jin W,Xu Y,Chang L,Zhou H,Jiang J,Yang L

更新日期：2020-03-01 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：:This study aims to explore whether E545K, the most common hotspot mutation of PIK3CA in cervical cancer, confers radioresistance to cervical cancer cells, to demonstrate the underling mechanism, and to develop the effective targets. SiHa and MS751 cells with PIK3CA-WT and PIK3CA-E545K were established by lentiviral tr...

journal_title：Molecular cancer therapeutics

authors： Jiang W,Wu Y,He T,Zhu H,Ke G,Xiang L,Yang H

更新日期：2020-02-01 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：:In recent years, HER3 has increasingly been implicated in the progression of a variety of tumor types and in acquired resistance to EGFR and HER2 therapies. Whereas EGFR and HER2 primarily signal through the MAPK pathway, HER3, as a heterodimer with EGFR or HER2, potently activates the PI3K pathway. Despite its critic...

journal_title：Molecular cancer therapeutics

authors： Thakkar D,Sancenon V,Taguiam MM,Guan S,Wu Z,Ng E,Paszkiewicz KH,Ingram PJ,Boyd-Kirkup JD

更新日期：2020-02-01 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：:Viral-based chimeric antigen receptor-engineered T (CAR T)-cell manufacturing has potential safety risks and relatively high costs. The nonviral minicircle DNA (mcDNA) is safer for patients, cheaper to produce, and may be a more suitable technique to generate CAR T cells. In this study, we produced mcDNA-based CAR T c...

journal_title：Molecular cancer therapeutics

authors： Han J,Gao F,Geng S,Ye X,Wang T,Du P,Cai Z,Fu Z,Zhao Z,Shi L,Li Q,Cai J

更新日期：2020-01-01 00:00:00

abstract：:DNA repair mechanisms are crucial for cell survival. It increases the cancer cell's ability to resist DNA damage. FEN1 is involved in DNA replication and repair, specifically long-patch base excision repair. Although the gene function and post-translational modification of FEN1 are well studied, the regulatory mechani...

journal_title：Molecular cancer therapeutics

authors： Zhu H,Wu C,Wu T,Xia W,Ci S,He W,Zhang Y,Li L,Zhou S,Zhang J,Edick AM,Zhang A,Pan FY,Hu Z,He L,Guo Z

更新日期：2019-12-01 00:00:00

abstract：:Accumulated evidence indicates that CCAT1 functions as an oncogene in the progression of a variety of tumors. However, little is known as to how CCAT1 impacts tumorigenesis in human prostate cancer. In this study, we found from The Cancer Genome Atlas and Memorial Sloan Kettering Cancer Center database that CCAT1 is h...

journal_title：Molecular cancer therapeutics

authors： You Z,Liu C,Wang C,Ling Z,Wang Y,Wang Y,Zhang M,Chen S,Xu B,Guan H,Chen M

更新日期：2019-12-01 00:00:00

abstract：:HER3 is overexpressed in several cancers, including colorectal cancer. Although therapies with anti-HER3 antibodies have been investigated, significant clinical benefits have not been reported. U3-1402 is a novel HER3-antibody-drug conjugate (ADC) composed of the HER3 antibody patritumab and a novel topoisomerase I in...

journal_title：Molecular cancer therapeutics

authors： Koganemaru S,Kuboki Y,Koga Y,Kojima T,Yamauchi M,Maeda N,Kagari T,Hirotani K,Yasunaga M,Matsumura Y,Doi T

更新日期：2019-11-01 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：:Metastasis is the primary determinant of death in patients with diverse solid tumors and MDA-9/Syntenin (SDCBP), a pro-metastatic and pro-angiogenic gene, contributes to this process. Recently, we documented that by physically interacting with IGF-1R, MDA-9/Syntenin activates STAT3 and regulates prostate cancer pathog...

journal_title：Molecular cancer therapeutics

authors： Das SK,Kegelman TP,Pradhan AK,Shen XN,Bhoopathi P,Talukdar S,Maji S,Sarkar D,Emdad L,Fisher PB

更新日期：2019-11-01 00:00:00

abstract：:Despite frequent overexpression of numerous growth factor receptors by pancreatic ductal adenocarcinomas (PDAC), such as EGFR, therapeutic antibodies have not proven effective. Desmoplasia, hypovascularity, and hypoperfusion create a functional drug delivery barrier that contributes to treatment resistance. Drug combi...

journal_title：Molecular cancer therapeutics

authors： Wang J,Chan DKW,Sen A,Ma WW,Straubinger RM

更新日期：2019-11-01 00:00:00

abstract：:RX-5902 is a first-in-class anticancer agent targeting phosphorylated-p68 and attenuating nuclear shuttling of β-catenin. The purpose of this study was to evaluate the efficacy of RX-5902 in preclinical models of triple-negative breast cancer (TNBC) and to explore effects on β-catenin expression. A panel of 18 TNBC ce...

journal_title：Molecular cancer therapeutics

authors： Capasso A,Bagby SM,Dailey KL,Currimjee N,Yacob BW,Ionkina A,Frank JG,Kim DJ,George C,Lee YB,Benaim E,Gittleman B,Hartman SJ,Tan AC,Kim J,Pitts TM,Eckhardt SG,Tentler JJ,Diamond JR

更新日期：2019-11-01 00:00:00

abstract：:Repurposing cationic amphiphilic drugs (CAD) for cancer treatment is emerging as an attractive means to enhance the efficacy of chemotherapy. Many commonly used CADs, including several cation amphiphilic antihistamines and antidepressants, induce cancer-specific, lysosome-dependent cell death and sensitize cancer cell...

journal_title：Molecular cancer therapeutics

authors： Anand A,Liu B,Dicroce Giacobini J,Maeda K,Rohde M,Jäättelä M

更新日期：2019-09-01 00:00:00

abstract：:Alpha-emitters can be pharmacologically delivered for irradiation of single cancer cells, but cellular lethality could be further enhanced by targeting alpha-emitters directly to the nucleus. PARP-1 is a druggable protein in the nucleus that is overexpressed in neuroblastoma compared with normal tissues and is associa...

journal_title：Molecular cancer therapeutics

authors： Makvandi M,Lee H,Puentes LN,Reilly SW,Rathi KS,Weng CC,Chan HS,Hou C,Raman P,Martinez D,Xu K,Carlin SD,Greenberg RA,Pawel BR,Mach RH,Maris JM,Pryma DA

更新日期：2019-07-01 00:00:00

abstract：:Human antigen R (HuR) is an RNA-binding protein that posttranscriptionally regulates many cancer-trait genes. CDC6, a central regulator of DNA replication, is regulated by HuR. In this study, we investigated the role of HuR in colorectal cancer tumorigenesis and oxaliplatin (L-OHP) resistance, as well as the underlyin...

journal_title：Molecular cancer therapeutics

authors： Cai J,Wang H,Jiao X,Huang R,Qin Q,Zhang J,Chen H,Feng D,Tian X,Wang H

更新日期：2019-07-01 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