Active-Site Targeting Paramagnetic Probe for Matrix Metalloproteinases.

Chempluschem

Department of Chemistry "Ugo Schiff", University of Florence, Via della Lastruccia 3-13, 50019, Sesto Fiorentino, Italy.

Published: December 2016

AI Article Synopsis

  • The study focuses on creating and analyzing Ln complexes with a DOTA-based inhibitor designed to target matrix metalloproteinases.
  • The presence of the Ln-DOTA component does not interfere with the inhibitor's strong binding to the enzyme's catalytic domain.
  • The magnetic properties of the Ln complex are utilized to understand ligand-protein interactions and assess how variations in the linker length affect paramagnetic restraints.

Article Abstract

The design and synthesis of the Ln complexes of a DOTA-containing (DOTA=1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) inhibitor of matrix metalloproteinases are reported. The tight binding of the sulfonamide scaffold to the catalytic domain of the investigated matrix metalloproteinase is not impaired by the presence of the Ln -DOTA moiety. The paramagnetic properties of the Ln complex are exploited to obtain insights into the structural features of the ligand-protein interactions and to evaluate the influence of the linker length on the quality of the paramagnetic restraints.

Download full-text PDF

Source
http://dx.doi.org/10.1002/cplu.201600375DOI Listing

Publication Analysis

Top Keywords

matrix metalloproteinases
8
active-site targeting
4
targeting paramagnetic
4
paramagnetic probe
4
probe matrix
4
metalloproteinases design
4
design synthesis
4
synthesis complexes
4
complexes dota-containing
4
dota-containing dota=14710-tetraazacyclododecane-14710-tetraacetic
4

Similar Publications

Background: Exosomes are small extracellular vesicles (30-150 nm in size) that play a critical role in cellular communication, transporting proteins, lipids, and nucleic acids between cells. This literature review focuses on evaluating the potential benefits and limitations of exosomes in enhancing skin health and aesthetics through indications such as skin rejuvenation, hair restoration, and pigmentation disorders.

Methods: A thorough literature search was conducted on PubMed using specific MeSH, including "exosomes," "aesthetics," "cosmetic dermatology," "skin rejuvenation," "hair growth," and "wrinkle reduction.

View Article and Find Full Text PDF

Glioblastoma presents a significant treatment challenge due to the blood-brain barrier (BBB) hindering drug delivery, and the overexpression of matrix metalloproteinases (MMPs), which promotes tumor invasiveness. This study introduces a novel nanostructured lipid carrier (NLC) system designed for the delivery of batimastat, an MMP inhibitor, across the BBB and into the glioblastoma microenvironment. The NLCs were functionalized with epidermal growth factor (EGF) and a transferrin receptor-targeting construct to enhance BBB penetration and entrapment within the tumor microenvironment.

View Article and Find Full Text PDF

Rheumatoid arthritis (RA), a condition characterized by joint deterioration through the action of matrix metalloproteinases (MMPs), is prevalent worldwide. Bee venom (BV) has traditionally been used in Chinese medicine for pain, arthritis, rheumatism, skin diseases, etc. BV is enriched with active substances, notably melittin and phospholipase A2 (PLA2), offering significant therapeutic potential.

View Article and Find Full Text PDF

Purpose: Studying the effect of interleukin-17 (IL-17) on the mechanism of CD4+ T-cell immune regulation and the Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway may offer new ideas and methods for the therapy of dilated cardiomyopathy.

Methods: Naive CD4+ T cells were isolated from mice using a magnetic bead sorting reagent and manipulated by overexpression or knockdown of IL-17. Protein levels of Janus kinase 2 (JAK2), phosphorylated JAK2 (p-JAK2), signal transducer and activator of transcription 3 (STAT3), phosphorylated STAT3 (p-STAT3), matrix metalloproteinase-2 (MMP-2), and matrix metalloproteinase-9 (MMP-9) were determined by Western blotting.

View Article and Find Full Text PDF

A Slimming/Excavating Strategy for Enhanced Intratumoral Penetration of Acid-Disassemblable NO-Releasing Nanomedicines.

Adv Healthc Mater

January 2025

Shanghai Key Laboratory of Hydrogen Science & Center of Hydrogen Science, School of Materials Science and Engineering, Shanghai Jiao Tong University, Shanghai, 200240, China.

Poor tumor penetration is the major predicament of nanomedicines that limits their anticancer efficacy. The dense extracellular matrix (ECM) in the tumor is one of the major barriers against the deep penetration of nanomedicines. In this work, a slimming/excavating strategy is proposed for enhanced intratumoral penetration based on an acid-disassemblable nanomicelles-assembled nanomedicine and the NO-mediated degradation of ECM.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!