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Heteronemin suppresses EGF‑induced proliferation through the PI3K/PD‑L1 signaling pathways in cholangiocarcinoma.
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Graduate Institute of Nanomedicine and Medical Engineering, College of Medical Engineering, Taipei Medical University, Taipei 11031, Taiwan, R.O.C.
Epidermal growth factor (EGF) binds with its surface receptor to stimulate gene expression and cancer cell proliferation. EGF stimulates cancer cell growth via phosphoinositide 3‑kinase (PI3K) and programmed cell death ligand 1 (PD‑L1) pathways. As an integrin αvβ3 antagonist, heteronemin exhibits potent cytotoxic effects against cancer cells.
View Article and Find Full Text PDFA Review on Branched-Chain Amino Acid Aminotransferase (BCAT) Inhibitors: Current Status, Challenges and Perspectives.
Curr Med Chem
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School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.
Branched-chain amino acids (BCAAs) are essential amino acids for humans and play an indispensable role in many physiological and pathological processes. Branched-chain amino acid aminotransferase (BCAT) is a key enzyme that catalyzes the metabolism of BCAAs. BCAT is upregulated in many cancers and implicated in the development and progress of some other diseases, such as metabolic and neurological diseases; and therefore, targeting BCAT might be a potential therapeutic approach for these diseases.
View Article and Find Full Text PDFMicrowave-synthesized NiZrO@GNP and NiZrO3@MWCNT nanocomposites: enhanced antimicrobial efficacy against biofilms and .
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Catalysis and Nanomaterials Research Laboratory, Department of Chemistry, Loyola College, Chennai, Tamil Nadu 600034 India.
Unlabelled: The persistent challenge posed by antibiotic-resistant bacteria and tuberculosis necessitates innovative approaches to antimicrobial treatment. This study explores the synthesis and characterization of NiZrO₃ nanoparticles integrated with graphene nanoplatelets (GNP) and multi-walled carbon nanotubes (MWCNT), using a microwave-assisted green synthesis route, employing fenugreek () seed extract as a gelling agent. The synthesised nanocomposites were systematically analyzed using XRD, FT-IR, Raman spectroscopy, HR-SEM and HR TEM analysis to assess structural, optical, and morphological properties.
View Article and Find Full Text PDFBreaking the energy chain: importance of ATP synthase in and its potential as a drug target.
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Infectious Diseases Division, CSIR - Indian Institute of Integrative Medicine Jammu-180001 India
Unveiling novel pathways for drug discovery forms the foundation of a new era in the combat against tuberculosis. The discovery of a novel drug, bedaquiline, targeting mycobacterial ATP synthase highlighted the targetability of the energy metabolism pathway. The significant potency of bedaquiline against heterogeneous population of marks ATP synthase as an important complex of the electron transport chain.
View Article and Find Full Text PDFAdvances in cryo-electron microscopy (cryoEM) for structure-based drug discovery.
Expert Opin Drug Discov
January 2025
Department of Molecular Physiology and Biological Physics, University of Virginia, Charlottesville, VA, USA.
Introduction: Macromolecular X-ray crystallography (XRC), nuclear magnetic resonance (NMR), and cryo-electron microscopy (cryoEM) are the primary techniques for determining atomic-level, three-dimensional structures of macromolecules essential for drug discovery. With advancements in artificial intelligence (AI) and cryoEM, the Protein Data Bank (PDB) is solidifying its role as a key resource for 3D macromolecular structures. These developments underscore the growing need for enhanced quality metrics and robust validation standards for experimental structures.
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