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High-affinity peptide against MT1-MMP for in vivo tumor imaging
Lei Zhu1, Huiling Wang, Lin Wang
1Key Laboratory of Molecular Enzymology and Enzyme Engineering of the Ministry of Education, Jilin University, Changchun 130023, PR China.
Abstract:
Membrane type-1 matrix metalloproteinase (MT1-MMP) is a key member of the matrix metalloproteinase (MMP) family. It participates in pericellular proteolysis of extracellular matrix (ECM) macromolecules and is essential for many biological and pathological processes, such as tumor development, angiogenesis and metastasis. A ligand that specifically binds to MT1-MMP may facilitate the labeling of this molecule, allow imaging at the cellular and organism levels, and provide a means for targeted drug delivery specific to MT1-MMP. A non-substrate MT1-MMP binding peptide was identified by screening a Ph.D.-12™ phage display peptide library and conjugated with near-infrared fluorescent (NIRF) dye Cy5.5 for tumor imaging. Peptide HWKHLHNTKTFL (denoted as MT1-AF7p) showed high MT1-MMP binding affinity. Computer modeling verified that MT1-AF7p binds to the MT-loop region of MT1-MMP and interacts with MT1-MMP through hydrogen bonding and hydrophobic interactions. MDA-MB-435 xenografts with high MT1-MMP expression had significantly higher tumor accumulation and better tumor contrast than the low MT1-MMP expressing A549 xenografts after intravenous injection of Cy5.5-MT1-AF7p. Using NIRF imaging, we have demonstrated specific targeting of MT1-AF7p to MT1-MMP-expressing tumors. Thus, MT1-AF7p is an important tool for noninvasive monitoring of MT1-MMP expression in tumors, and it shows great potential as an imaging agent for MT1-MMP-positive tumors.
Insights
A novel peptide, MT1-AF7p, specifically binds to membrane type-1 matrix metalloproteinase (MT1-MMP). This peptide, when conjugated with a fluorescent dye, enables noninvasive imaging and monitoring of MT1-MMP expression in tumors.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Membrane type-1 matrix metalloproteinase (MT1-MMP) is crucial for extracellular matrix remodeling and implicated in tumor progression.
- Targeting MT1-MMP is vital for cancer diagnostics and therapeutics.
- Developing specific ligands for MT1-MMP facilitates molecular imaging and drug delivery.
Purpose of the Study:
- To identify and characterize a novel peptide ligand that specifically binds to MT1-MMP.
- To evaluate the potential of this peptide as an imaging agent for MT1-MMP-expressing tumors.
Main Methods:
- Screening a phage display peptide library to identify MT1-MMP binding peptides.
- Conjugating the identified peptide (MT1-AF7p) with a near-infrared fluorescent (NIRF) dye (Cy5.5).
- Evaluating peptide binding affinity and tumor targeting in xenograft models using NIRF imaging.
Main Results:
- The peptide MT1-AF7p demonstrated high binding affinity to MT1-MMP.
- Computer modeling indicated specific binding to the MT-loop region of MT1-MMP.
- Cy5.5-MT1-AF7p showed significant tumor accumulation and contrast in MT1-MMP-expressing xenografts compared to low-expression tumors.
Conclusions:
- MT1-AF7p specifically targets MT1-MMP-expressing tumors.
- This peptide serves as a valuable tool for noninvasive monitoring of MT1-MMP expression.
- MT1-AF7p holds potential as an imaging agent for MT1-MMP-positive tumors.
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