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8-Fluorotryptanthrin, an immunomodulatory IDO-1 inhibitor enhances the efficacy of artemether-lumefantrine in the treatment of malaria
Malaria is a lethal disease caused by Plasmodium parasites, transmitted through the bites of infected Anopheles mosquitoes...
3H-pyrazolo[4,3-f]quinoline hinge binder, a tunable scaffold for development of novel kinase inhibitors against FLT3-driven leukemia
The 3H-pyrazolo[4,3-f]quinoline moiety, synthesized via a Doebner or Povarov multi-component reaction, has been described ...
Radiosynthesis and PET evaluation of [18F]Fuzuloparib as a PARP-targeted imaging agent in breast cancer
The global burden of breast cancer has risen markedly in recent years. In 2020, breast cancer surpassed lung cancer to bec...
Coixol derivatives induce DNA damage by targeting PARP1
Poly(ADP-ribose)polymerases (PARPs) family consists of 18 members that play pivotal roles in many cellular processes, incl...
Pyrrolopyrimidines: A promising scaffold for the development of novel cathepsin K inhibitors
Osteoporosis is a prevalent condition characterized by a reduction in bone mass and a high risk of fracture, particularly ...
Discovery of highly selective and potent HPK1 inhibitors for cancer immunotherapy
Hematopoietic progenitor kinase 1 (HPK1, also known as MAP4K1), a member of the Ste20-related serine/threonine kinase fami...
An adamantylureido-benzylamide aniline as FLAP/sEH dual inhibitor: Rational design, in vitro and in vivo lipidomic profiling
Inflammation is a host response to various noxious stimuli, including thermal, mechanical, chemical injuries, as well as p...
Structural insights into frog skin-derived cyclic peptides as selective matriptase inhibitors
Matriptase and TMPRSS6 (also known as matriptase 2) are type II transmembrane serine proteases (TTSPs) that share signific...
Advancing the antituberculosis activity of nitropicolinic acids and amides
WHOWorld Health OrganisationDprE1decaprenylphosphoryl-β-d-ribose 2′-oxidaseDprE2decaprenylphosphoryl-2-keto-β-d-erythropen...
Functionalized nitrogen- and chalcogen-containing heterocyclic compounds as aromatase inhibitors: Design, synthesis and biological evaluation
Aromatase inhibition remains a key therapeutic strategy for hormone-dependent breast cancer (HDBC). Among non-steroidal ar...
Design, synthesis and structural development of nonsecosteroidal VDR ligands based on the C,C′-diphenyl-m-carborane scaffold
Vitamin D receptor (VDR) is a nuclear receptor that acts as a ligand-dependent transcription factor in response to 1α,25-d...
FXR-targeted drug discovery: Recent advances and therapeutic perspectives
Farnesoid X receptor (FXR), a core member of the nuclear receptor (NR) superfamily, is a bile acid-activated nuclear trans...
Discovery of XRF-1021, a 2,4-disubstituted-5-fluoropyrimidine derivative as a homeodomain-interacting protein kinase 2 inhibitor for the treatment of chronic kidney disease
Chronic kidney disease (CKD) affects 10–13 % of the global population and is characterized by persistent inflammation and ...
Design, synthesis and preliminary biological evaluation of novel carbamoyl pyridone derivatives as potent inhibitors of Crimean-Congo hemorrhagic fever virus
Crimean-Congo hemorrhagic fever virus (CCHFV) is an enveloped negative-sense RNA virus that belongs to the order Hareavira...
Fabrication and analysis of polydatin-loaded gelatin-coated Polycaprolactone nanoparticles for targeting radioresistant lung cancer cells
Advancements in phytochemistry have led to the development of phytochemicals as promising agents for cancer treatment and ...
Novel imidazo[1,2-a]pyridine-based tubulin polymerization inhibitors: Structure-activity relationships and anti-tumor immune potentiation
Microtubules composed of α-tubulin and β-tubulin heterodimers are an organelle widely present in cells, with multiple biol...
From tetrazole to isoquinolinone: Structure-based optimization and late-stage diversification of AR-C118925-derived P2Y2 receptor antagonists
The P2Y2 receptor is a G protein-coupled receptor activated by extracellular nucleotides, is implicated in various patholo...
Discovery of a novel napabucasin derivative B16 as a potent STAT3 inhibitor for the treatment of triple-negative breast cancer
Breast cancers are malignant tumors that originate from the excessive proliferation of breast epithelial cells. Among them...
Exploring the influence of the glycone space on the therapeutic potential of sp2-iminoglycolipids
Extensive structure-activity relationship studies performed on sp2-iminoglycolipids revealed the fundamental role played b...
Synthesis of β-boswellic acid-amino acid conjugates for targeting KRASG13D mutant colon cancer
Boswellic acids, a class of pentacyclic triterpenes derived from the resin of Boswellia species, have garnered considerabl...
Exploring social determinants of disability among older filipinos: insights from a polysocial score approach
Exploring social determinants of disability among older filipinos: insights from a polysocial score approach
The rapid aging in the Philippines presents significant challenges, including high rates of activities of daily living (AD...
The outbreak, response, and reflections on the chikungunya fever epidemic in Foshan City, China
The outbreak, response, and reflections on the chikungunya fever epidemic in Foshan City, China
Driven by climate change, viral evolution, intensified human mobility, and increasing population susceptibility, mosquito-...
Understanding the Molecular Toxicity of Metal-Based Nanoparticles Through Nanotoxicomics
Understanding the Molecular Toxicity of Metal-Based Nanoparticles Through Nanotoxicomics
Understanding the Molecular Toxicity of Metal-Based Nanoparticles Through Nanotoxicomics
Self-Assembled Safflower Polysaccharide Nanoparticles as a Targeted Drug Delivery System for Enhanced Therapy of Hepatocellular Carcinoma
Self-Assembled Safflower Polysaccharide Nanoparticles as a Targeted Drug Delivery System for Enhanced Therapy of Hepatocellular Carcinoma
This study highlights the potential of cationic SPS as a drug delivery material
A pH/H2O2 Dual-Responsive Cobalt–Manganese-Based Nano-Delivery System for Chemo/Chemodynamic Therapy in Triple-Negative Breast Cancer
A pH/H2O2 Dual-Responsive Cobalt–Manganese-Based Nano-Delivery System for Chemo/Chemodynamic Therapy in Triple-Negative Breast Cancer
In this study we innovatively developed a TME-responsive nano-delivery system named ZIF-67/MnO2/DOX/BSA/SDS for TNBC chemo...
Fabrication and Characterization of Electrospun Sr/Zn-Doped Nano-Hydroxyapatite-Collagen-PLGA Nanofibrous Scaffolds for Bone Tissue Engineering
Fabrication and Characterization of Electrospun Sr/Zn-Doped Nano-Hydroxyapatite-Collagen-PLGA Nanofibrous Scaffolds for Bone Tissue Engineering
This study aims to develop and evaluate biomimetic composite scaffolds consisting of Sr/Zn-doped nHAp, collagen, and PLGA,...
Ginger-Derived Exosome-Like Nanoparticles: The Effect of Extraction Methods on Metabolites and in vitro Anti-Lung Cancer Activity
Ginger-Derived Exosome-Like Nanoparticles: The Effect of Extraction Methods on Metabolites and in vitro Anti-Lung Cancer Activity
The differences among ginger-derived exosome-like nanoparticles extracted by various methods & their anti-lung cancer ...
Strike Mitochondria By Enzyme-Instructed Self-Assembled Peptides for Effective Immunogenic Anti-Tumor Therapy
Strike Mitochondria By Enzyme-Instructed Self-Assembled Peptides for Effective Immunogenic Anti-Tumor Therapy
To investigate the lack of precise and efficient ICD induction at the tumor site and poor synergy with other therapeutic m...
Innovative Applications of Nucleic Acid Aptamers in Colorectal Cancer Diagnosis and Therapy: From Selection Optimization to Clinical Translation
Innovative Applications of Nucleic Acid Aptamers in Colorectal Cancer Diagnosis and Therapy: From Selection Optimization to Clinical Translation
Reviews immunotherapeutic regimens that employ PD-1/PD-L1 blocking aptamers alone or in combination with immunomodulatory ...
Strategies for Pancreatic Cancer-Responsive Nanodrug Platforms Targeting Tumor Hypoxic Environments
Strategies for Pancreatic Cancer-Responsive Nanodrug Platforms Targeting Tumor Hypoxic Environments
Exploring strategies for a promising route toward more effective, selective, and personalized nanomedicines for pancreatic...
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