Matrix metalloproteinase-8 (MMP-8), a type II collagenase, is a key enzyme in the degradation of collagens and is implicated in various pathological processes, making it a promising target for drug discovery. Despite advancements in the development of MMP-8 inhibitors, concerns over potential adverse effects persist. This study aims to address these concerns by focusing on the development of novel compounds with improved safety profiles while maintaining efficacy. In this study, we employed a computational approach to screen potent and safe inhibitors of MMP-8 from the Natural Product Activity and Species Source Database (NPASS). Initially, we constructed a pharmacophore model based on the crystal structure of the MMP-8-FIN complex (PDB ID: 4EY6) utilizing the Pharmit tool. This model then guided the selection of 44 promising molecules from NPASS, setting the stage for further analysis and evaluation. We comprehensively evaluated their drug-likeness and toxicity profiles. Molecules 21, 4, and 44 were identified as potentially effective MMP-8 inhibitors through a robust pipeline that included ADMET profiling, molecular docking, and molecular dynamics simulations. Notably, molecule 21 stood out for its low toxicity, high binding stability, and favorable ADMET profile, while molecule 44 demonstrated excellent affinity. These compounds offer structural novelty compared to known MMP-8 inhibitors. These computational results can be combined with in vitro experiments in the future to validate their activity and safety. These findings provide an important reference for drug design of MMP-8 inhibitors.
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http://dx.doi.org/10.1007/s40203-024-00299-w | DOI Listing |
In Silico Pharmacol
January 2025
College of Chemistry and Chemical Engineering, China University of Petroleum, Qingdao, 266580 China.
Matrix metalloproteinase-8 (MMP-8), a type II collagenase, is a key enzyme in the degradation of collagens and is implicated in various pathological processes, making it a promising target for drug discovery. Despite advancements in the development of MMP-8 inhibitors, concerns over potential adverse effects persist. This study aims to address these concerns by focusing on the development of novel compounds with improved safety profiles while maintaining efficacy.
View Article and Find Full Text PDFLyme disease, caused by , is the most common tick-borne infection in the United States. Arthritis is a major clinical manifestation of infection, and synovial tissue damage has been attributed to the excessive pro-inflammatory responses. The secretory leukocyte protease inhibitor (SLPI) promotes tissue repair and exerts anti-inflammatory effects.
View Article and Find Full Text PDFFolia Neuropathol
November 2024
Department of Neurosurgery, Prof. Dr. Cemil Taşçıoğlu City Hospital, İstanbul, Turkey.
Introduction: Vasospasm has been reported as the most important cause of mortality and morbidity in patients with subarachnoid haemorrhage (SAH) who can reach the hospital. Matrix metalloproteinases (MMPs) are a gene family, which are called neutral proteases in the central nervous system (CNS). In this experimental study we studied the upregulation of MMPs (MMP-8, MMP-9, and MMP-13) gene expression and the inhibitor effects of doxycycline after experimental SAH model in rats.
View Article and Find Full Text PDFInt J Mol Sci
August 2024
Oral Health Sciences Centre, Post Graduate Institute of Medical Education & Research, Chandigarh 160012, India.
This study aimed to compare several potential mouthrinse biomarkers for periodontitis including active matrix-metalloproteinase-8 (aMMP-8), total MMP-8, and other inflammatory biomarkers in diagnosing and monitoring the effects of nonsurgical periodontal therapy. Thirteen patients with stage III/IV periodontitis were recruited, along with thirteen periodontally and systemically healthy controls. These 13 patients were representative of the number of outpatients visiting any dentist in a single day.
View Article and Find Full Text PDFJ Clin Periodontol
October 2024
Oral Sciences Research Group, Special Needs Unit, Department of Surgery and Medical-Surgical Specialties, School of Medicine and Dentistry, Universidade de Santiago de Compostela, Health Research Institute of Santiago (IDIS), Santiago de Compostela, Spain.
Aim: To identify new biomarkers to detect untreated and treated periodontitis in gingival crevicular fluid (GCF) using sequential window acquisition of all theoretical mass spectra (SWATH-MS).
Materials And Methods: GCF samples were collected from 44 periodontally healthy subjects and 40 with periodontitis (Stages III-IV). In the latter, 25 improved clinically 2 months after treatment.
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