ArticleCancer research2012
Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth.
Article in Cancer research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 73 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
73 citing papers in PubMed, 135 citations in OpenAlex.
- Article
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- Matrix Metalloproteinase 14 in Corneal Neovascularization.International journal of molecular sciences · 2026Review
- Targeting matrix metalloproteinase-14 disrupts DNA repair and reduces viability in adrenocortical carcinoma.bioRxiv : the preprint server for biology · 2026Article
- Matrix Metalloproteinase Inhibition in Melanoma.Experimental dermatology · 2026Review
- Using High-Throughput Screening to Identify Crosslinking Peptides That Control Cell-Mediated Matrix Degradation.Advanced healthcare materials · 2025Article
- Matrix Metalloproteinases in Inflammatory Dermatoses.International journal of molecular sciences · 2025Review
- Inhibition of Metalloproteinases-2, -9, and -14 Suppresses Papillary Thyroid Carcinoma Cell Migration and Invasion.International journal of molecular sciences · 2025Article
- Matrix Metalloproteinases and Their Inhibitors in the Pathogenesis of Epithelial Differentiation, Vascular Disease, Endometriosis, and Ocular Fibrotic Pterygium.International journal of molecular sciences · 2025Review
- LRP1 regulates asthmatic airway smooth muscle proliferation through FGF2/ERK signaling.JCI insight · 2025Article
- Targeting Matrix Metalloproteinases and Their Inhibitors in Melanoma.International journal of molecular sciences · 2024Review
- Dura immunity configures leptomeningeal metastasis immunosuppression for cerebrospinal fluid barrier invasion.Nature cancer · 2024Article
- An injury-responsiveScience advances · 2023Article
- Matrix Metalloproteinases Inhibitors in Cancer Treatment: An Updated Review (2013-2023).Molecules (Basel, Switzerland) · 2023Review
- The regenerative response of cardiac interstitial cells.Journal of molecular cell biology · 2023Article
- Article
- Influenza virus decreases albumin uptake and megalin expression in alveolar epithelial cells.Frontiers in immunology · 2023Article
- Immunomodulatory roles of metalloproteinases in rheumatoid arthritis.Frontiers in pharmacology · 2023Review
- Detecting the PEX Like Domain of Matrix Metalloproteinase-14 (MMP-14) with Therapeutic Conjugated CNTs.Biosensors · 2022Article
13 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
Membrane type-1 matrix metalloproteinase (MT1-MMP) is a promising drug target in malignancy. The structure of MT1-MMP includes the hemopexin domain (PEX) that is distinct from and additional to the catalytic domain. Current MMP inhibitors target the conserved active site in the catalytic domain and, as a result, repress the proteolytic activity of multiple MMPs instead of MT1-MMP alone. In our search for noncatalytic inhibitors of MT1-MMP, we compared the protumorigenic activity of wild-type MT1-MMP with an MT1-MMP mutant lacking PEX (ΔPEX). In contrast to MT1-MMP, ΔPEX did not support tumor growth in vivo, and its expression resulted in small fibrotic tumors that contained increased levels of collagen. Because these findings suggested an important role for PEX in tumor growth, we carried out an inhibitor screen to identify small molecules targeting the PEX domain of MT1-MMP. Using the Developmental Therapeutics Program (National Cancer Institute/NIH), virtual ligand screening compound library as a source and the X-ray crystal structure of PEX as a target, we identified and validated a novel PEX inhibitor. Low dosage, intratumoral injections of PEX inhibitor repressed tumor growth and caused a fibrotic, ΔPEX-like tumor phenotype in vivo. Together, our findings provide a preclinical proof of principle rationale for the development of novel and selective MT1-MMP inhibitors that specifically target the PEX domain.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.