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Safety and efficacy of multi-target TKI combined with nivolumab in check-point inhibitor-refractory patients with advanced NSCLC: a prospective, single-arm, two-stage study
BackgroundResistance to immune checkpoint inhibitors (ICIs) represents a major unmet medical need in non-small cell lung cancer (NSCLC) patients....
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CTLA-4 Inhibitors for the Treatment of Lung Cancer
One of the most prevalent malignancies and the main reason for cancer-related deaths globally is lung cancer. The majority of these non-small-cell...
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Computational Modeling of DYRK1A Inhibitors as Potential Anti-Alzheimer Agents
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a promising target for the treatment of different neurodegenerative...
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The gut microbiome, immune check point inhibition and immune-related adverse events in non-small cell lung cancer
Systemic treatment options for patients with lung cancer have expanded in recent years, with a number of immunotherapeutic strategies now in our...
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Ecarin-Based Methods for Measuring Thrombin Inhibitors
Ecarin is a venom from the saw-scaled viper, Echis carinatus, which catalyzes prothrombin into meizothrombin. This venom is used in several...
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Exploring isoindolin-1-ones as potential CDK7 inhibitors using cheminformatic tools
In women who die from cancer, breast cancer is the most common cause of death. The development of small molecular scaffolds as specific...
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Tumor immune checkpoints and their associated inhibitors
Immunological evasion is one of the defining characteristics of cancers, as the immune modification of an immune checkpoint (IC) confers immune...
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In-silico identification of small molecule benzofuran-1,2,3-triazole hybrids as potential inhibitors targeting EGFR in lung cancer via ligand-based pharmacophore modeling and molecular docking studies
Lung cancer is one of the most common and deadly types of cancer worldwide, and the epidermal growth factor receptor (EGFR) has emerged as a...
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Computational Modeling of Kinase Inhibitors as Anti-Alzheimer Agents
Alzheimer’s disease (AD) is a progressive neurodegenerative disease distinguished by memory loss, cognitive dysfunction, impaired functional...
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Quantitative evaluation of the efficacy and safety profiles of two types of targeted inhibitors combined with endocrine therapy in ER+/HER2− metastatic breast cancer
PurposeThe aim of this study was to quantitatively compare the efficacy and safety of CDK4/6 inhibitors and PI3K/AKT/mTOR inhibitors for...
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High-Throughput Cell-Based Screening of Small Molecule KRAS Signaling Inhibitors Using a Homogeneous Time-Resolved Fluorescence (HTRF) Assay
With recent advances proving that effective inhibition of KRAS is possible, there have been significant efforts made to develop inhibitors of...
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Immunotherapy in triple negative breast cancer: beyond checkpoint inhibitors
The development of immunotherapy agents has revolutionized the field of oncology. The only FDA-approved immunotherapeutic approach in breast cancer...
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A high-throughput screening campaign against PFKFB3 identified potential inhibitors with novel scaffolds
The growth of solid tumors depends on tumor vascularization and the endothelial cells (ECs) that line the lumen of blood vessels. ECs generate a...
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Update on histone deacetylase inhibitors in peripheral T-cell lymphoma (PTCL)
Peripheral T-cell lymphomas (PTCLs) are a group of highly aggressive malignancies with generally poor prognoses, and the first-line chemotherapy of...
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Computer-Assisted Drug Design: A Toolbox for Novel Tau Kinase Inhibitors and Its Implications in Alzheimer’s Disease
Kinases/phosphatases are a novel class of enzymes that maintains the equilibrium of the amino acids’ optimum phosphorylation/dephosphorylation...
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Expression of PD1 and PDL1 as immune-checkpoint inhibitors in mantle cell lymphoma
BackgroundMantle cell lymphoma (MCL) has remained incurable in most patients. The expression of PD-L1 as a prognostic and predictive marker has not...
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In vitro evaluation of the reductive carbonyl idarubicin metabolism to evaluate inhibitors of the formation of cardiotoxic idarubicinol via carbonyl and aldo–keto reductases
The most important dose-limiting factor of the anthracycline idarubicin is the high risk of cardiotoxicity, in which the secondary alcohol metabolite...
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Inhibitors against New Delhi metallo-betalactamase-1 (NDM-1) and its variants endemic in Indian settings along with the laboratory functional gain mutant of NDM-1
PurposeThe emergence of NDM-1 producing bacteria has become common in both hospital and community settings, but no inhibitor has yet been available...
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Hansch-Type QSAR Models for the Rational Design of MAO Inhibitors: Basic Principles and Methodology
Hansch-type regression analysis enables the derivation of quantitative structure-activity relationship (QSAR) equations correlating bioactivity data...