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SPR is a fast and straightforward method to estimate the binding constants of cyclic dinucleotides to their binding partners, such as STING or poxin.
Biophys Chem
January 2025
Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic. Electronic address:
The development of small molecule drugs that target protein binders is the central goal in medicinal chemistry. During the lead compound development process, hundreds or even thousands of compounds are synthesized, with the primary focus on their binding affinity to protein targets. Typically, IC or EC values are used to rank these compounds.
View Article and Find Full Text PDFSurface receptor-targeted Protein-based nanocarriers for drug delivery: Advances in cancer therapy.
Nanotechnology
January 2025
Department of Biotechnology, Kalasalingam Academy of Research and Education (Deemed to be University), Anand Nagar, School of Bio, Chemical & Process Enginneering, Krishnankoil, Krishnan Kovil, Tamil Nadu, 626126, INDIA.
Significant progress has been made in cancer therapy with protein-based nanocarriers targeted directly to surface receptors for drug delivery. The nanocarriers are a potentially effective solution for the potential drawbacks of traditional chemotherapy, such as lack of specificity, side effects, and development resistance. Peptides as nanocarriers have been designed based on their biocompatible, biodegradable, and versatile functions to deliver therapeutic agents into cancer cells, reduce systemic toxicity, and maximize therapy efficacy through utilizing targeted ligands such as antibodies, amino acids, vitamins, and other small molecules onto protein-based nanocarriers and thus ensuring that drugs selectively accumulate in the cancer cells instead of healthy organs/drug release at a target site without effects on normal cells, which inherently caused less systemic toxicity/off-target effect.
View Article and Find Full Text PDFThe interaction between antithrombin and endothelial heparan sulfate mitigates pulmonary thromboinflammation after trauma and hemorrhagic shock.
Shock
January 2025
The University of Alabama, Birmingham, Department of Surgery and Center for Injury Science, Division of Trauma and Acute Care Surgery, Birmingham, AL.
Introduction: Trauma and hemorrhagic shock (T/HS) are associated with multiple organ injury. Antithrombin (AT) has anti-inflammatory and organ protective activity through its interaction with endothelial heparan sulfate containing a 3-O-sulfate modification. Our objective was to examine the effects of T/HS on 3-O-sulfated (3-OS) heparan sulfate expression and determine whether AT-heparan sulfate interactions are necessary for its anti-inflammatory properties.
View Article and Find Full Text PDFDesign of ()-3-(5-Thienyl)carboxamido-2-aminopropanoic Acid Derivatives as Novel NMDA Receptor Glycine Site Agonists: Variation in Molecular Geometry to Improve Potency and Augment GluN2 Subunit-Specific Activity.
J Med Chem
January 2025
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, DK-2100, Denmark.
NMDA receptor ligands have therapeutic potential in neurological and psychiatric disorders. We designed ()-3-(5-thienyl)carboxamido-2-aminopropanoic acid derivatives with nanomolar agonist potencies at NMDA receptor subtypes (GluN12/A-D). These compounds are superagonists at GluN1/2C compared to glycine and partial to full agonists at GluN1/2A and GluN1/2D but display functional antagonism at GluN1/2B due to low agonist efficacy.
View Article and Find Full Text PDFPeripheral Evolution of Tanshinone IIA and Cryptotanshinone for Discovery of a Potent and Specific NLRP3 Inflammasome Inhibitor.
J Med Chem
January 2025
College of Pharmaceutical Sciences, State Key Laboratory of Advanced Drug Delivery and Release Systems, Zhejiang University, Hangzhou 310058, China.
Natural products (NPs) continue to serve as an invaluable source in drug discovery, and peripheral evolution of NPs is a highly efficient evolution strategy. Herein, we describe a unified "methyl to amide" peripheral evolution of Tanshinone IIA and Cryptotanshinone for discovery of NLRP3 inflammasome inhibitors. There were 54 compounds designed and prepared, while the chemoinformatic analysis revealed that these evolved NP analogues occupy a unique chemical space.
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