Search Results - "Molecular cancer therapeutics"
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Tumor Mutational Burden as an Independent Predictor of Response to Immunotherapy in Diverse Cancers
Published in Molecular cancer therapeutics (01-11-2017)“…Immunotherapy induces durable responses in a subset of patients with cancer. High tumor mutational burden (TMB) may be a response biomarker for PD-1/PD-L1…”
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Matrix Metalloproteinase Inhibitors in Cancer Therapy: Turning Past Failures Into Future Successes
Published in Molecular cancer therapeutics (01-06-2018)“…The matrix metalloproteinases (MMP) are a family of proteolytic enzymes that degrade multiple components of the extracellular matrix. A large body of…”
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PD-L1 Expression as a Predictive Biomarker in Cancer Immunotherapy
Published in Molecular cancer therapeutics (01-04-2015)“…The resurgence of cancer immunotherapy stems from an improved understanding of the tumor microenvironment. The PD-1/PD-L1 axis is of particular interest, in…”
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Resistance to Systemic Therapies in Clear Cell Renal Cell Carcinoma: Mechanisms and Management Strategies
Published in Molecular cancer therapeutics (01-07-2018)“…Renal cell carcinoma (RCC) is the most common form of kidney cancer. It is categorized into various subtypes, with clear cell RCC (ccRCC) representing about…”
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Datopotamab Deruxtecan, a Novel TROP2-directed Antibody-drug Conjugate, Demonstrates Potent Antitumor Activity by Efficient Drug Delivery to Tumor Cells
Published in Molecular cancer therapeutics (01-12-2021)“…Trophoblast cell surface antigen 2 (TROP2) is highly expressed on various epithelial tumors and correlates with poor prognosis. We developed the novel…”
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Acquired Resistance to BET-PROTACs (Proteolysis-Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 Ligase Complexes
Published in Molecular cancer therapeutics (01-07-2019)“…Proteolysis-targeting chimeras (PROTAC) are bifunctional molecules that hijack endogenous E3 ubiquitin ligases to induce ubiquitination and subsequent…”
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Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2 -deficient Mesothelioma
Published in Molecular cancer therapeutics (01-06-2021)“…Mutations in the neurofibromatosis type 2 ( ) gene that limit or abrogate expression of functional Merlin are common in malignant mesothelioma. Merlin…”
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ATM Mutations in Cancer: Therapeutic Implications
Published in Molecular cancer therapeutics (01-08-2016)“…Activation of checkpoint arrest and homologous DNA repair are necessary for maintenance of genomic integrity during DNA replication. Germ-line mutations of the…”
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Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer
Published in Molecular cancer therapeutics (01-04-2014)“…Glutamine serves as an important source of energy and building blocks for many tumor cells. The first step in glutamine utilization is its conversion to…”
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Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models
Published in Molecular cancer therapeutics (01-04-2020)“…HER2 is a transmembrane tyrosine kinase receptor that mediates cell growth, differentiation, and survival. HER2 is overexpressed in approximately 20% of breast…”
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CSF1/CSF1R Signaling Inhibitor Pexidartinib (PLX3397) Reprograms Tumor-Associated Macrophages and Stimulates T-cell Infiltration in the Sarcoma Microenvironment
Published in Molecular cancer therapeutics (01-08-2021)“…Colony-stimulating factor 1 (CSF1) is a primary regulator of the survival, proliferation, and differentiation of monocyte/macrophage that sustains the…”
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Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor
Published in Molecular cancer therapeutics (01-06-2017)“…Fibroblast growth factor (FGF) signaling plays critical roles in key biological processes ranging from embryogenesis to wound healing and has strong links to…”
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Spectrum and Degree of CDK Drug Interactions Predicts Clinical Performance
Published in Molecular cancer therapeutics (01-10-2016)“…Therapeutically targeting aberrant intracellular kinase signaling is attractive from a biological perspective but drug development is often hindered by…”
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Stereospecific PARP trapping by BMN 673 and comparison with olaparib and rucaparib
Published in Molecular cancer therapeutics (01-02-2014)“…Anti-PARP drugs were initially developed as catalytic inhibitors to block the repair of DNA single-strand breaks. We recently reported that several PARP…”
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Plk1 Inhibitors in Cancer Therapy: From Laboratory to Clinics
Published in Molecular cancer therapeutics (01-07-2016)“…Polo-like kinase 1 (Plk1) overexpression has been shown to occur in a wide range of tumors, prompting research and development of Plk1 inhibitors as a means of…”
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MALAT1 Is Associated with Poor Response to Oxaliplatin-Based Chemotherapy in Colorectal Cancer Patients and Promotes Chemoresistance through EZH2
Published in Molecular cancer therapeutics (01-04-2017)“…A major reason for oxaliplatin chemoresistance in colorectal cancer is the acquisition of epithelial-mesenchymal transition (EMT) in cancer cells. The long…”
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ARX788, a Site-specific Anti-HER2 Antibody–Drug Conjugate, Demonstrates Potent and Selective Activity in HER2-low and T-DM1–resistant Breast and Gastric Cancers
Published in Molecular cancer therapeutics (01-09-2020)“…Abstract First-generation antibody–drug conjugates (ADC) are heterogeneous mixtures that have shown clinical benefit, but generally exhibited safety issues and…”
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The Novel ATR Inhibitor BAY 1895344 Is Efficacious as Monotherapy and Combined with DNA Damage-Inducing or Repair-Compromising Therapies in Preclinical Cancer Models
Published in Molecular cancer therapeutics (01-01-2020)“…The DNA damage response (DDR) secures the integrity of the genome of eukaryotic cells. DDR deficiencies can promote tumorigenesis but concurrently may increase…”
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Characterization of KRAS Mutation Subtypes in Non-small Cell Lung Cancer
Published in Molecular cancer therapeutics (01-12-2021)“…is the most commonly mutated oncogene in NSCLC and development of direct KRAS inhibitors has renewed interest in this molecular variant. Different mutations…”
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FLT3 Inhibitors in Acute Myeloid Leukemia: Current Status and Future Directions
Published in Molecular cancer therapeutics (01-06-2017)“…The receptor tyrosine kinase -like tyrosine kinase 3 (FLT3), involved in regulating survival, proliferation, and differentiation of hematopoietic…”
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