Abcam MMP14 Inhibitor Screening Assay Kit (Fluorometric) (ab139455) is a complete assay system designed to screen MMP14 inhibitors using a quenched fluorogenic peptide: MMP Fluorogenic Substrate Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 [Mca=(7-methoxycoumarin-4-yl)-acetyl; Dpa=N-3-(2,4-dinitrophenyl)-L-α-β-diaminopropionyl].
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Key facts
- Detection method
- Fluorescent
- Sample types
- Inhibitor compounds
- Assay type
- Enzyme activity
Target data
Function
Endopeptidase that degrades various components of the extracellular matrix such as collagen (PubMed:8015608). Essential for pericellular collagenolysis and modeling of skeletal and extraskeletal connective tissues during development (By similarity). Activates progelatinase A/MMP2, thereby acting as a positive regulator of cell growth and migration (PubMed:22065321, PubMed:8015608). Involved in the formation of the fibrovascular tissues in association with pro-MMP2 (PubMed:12714657, PubMed:22065321). May be involved in actin cytoskeleton reorganization by cleaving PTK7 (PubMed:20837484). Acts as a regulator of Notch signaling by mediating cleavage and inhibition of DLL1 (PubMed:21572390). Cleaves ADGRB1 to release vasculostatin-40 which inhibits angiogenesis (PubMed:22330140). Acts as a negative regulator of the GDF15-GFRAL aversive response by mediating cleavage and inactivation of GFRAL (PubMed:35177851).
Alternative names
Matrix metalloproteinase-14, MMP-14, MMP-X1, Membrane-type matrix metalloproteinase 1, Membrane-type-1 matrix metalloproteinase, MT-MMP 1, MTMMP1, MT1-MMP, MT1MMP, MMP14
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Abcam MMP14 Inhibitor Screening Assay Kit (Fluorometric) (ab139455) is a complete assay system designed to screen MMP14 inhibitors using a quenched fluorogenic peptide: MMP Fluorogenic Substrate Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 [Mca=(7-methoxycoumarin-4-yl)-acetyl; Dpa=N-3-(2,4-dinitrophenyl)-L-α-β-diaminopropionyl].
Key facts
- Detection method
- Fluorescent
- Sample types
- Inhibitor compounds
- Assay type
- Enzyme activity
- Assay Platform
- Microplate reader
Storage
- Shipped at conditions
- Dry Ice
- Appropriate short-term storage conditions
- -80°C
- Appropriate long-term storage conditions
- Multi
- Storage information
- Please refer to protocols
Notes
Abcam MMP14 Inhibitor Screening Assay Kit (Fluorometric) (ab139455) is a complete assay system designed to screen MMP14 inhibitors using a quenched fluorogenic peptide: MMP Fluorogenic Substrate Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 [Mca=(7-methoxycoumarin-4-yl)-acetyl; Dpa=N-3-(2,4-dinitrophenyl)-L-α-β-diaminopropionyl]. Mca fluorescence is quenched by the Dpa group until cleavage by MMPs at the Gly-Leu bond separates the two moieties. The assays are performed in a convenient 96-well microplate format.
This kit is useful to screen inhibitors of MMP14, a potential therapeutic target. The MMP inhibitor NNGH is also included as a prototypic control inhibitor.
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Matrix metalloproteinase 14 (MMP14) also known as MT1-MMP is a membrane-bound enzyme involved in the breakdown of the extracellular matrix. This protease has a molecular weight of approximately 66 kDa and consists of various structural domains including a catalytic domain and a hinge region. MMP14 is expressed in many tissues including the stromal and cancer cells where it facilitates cell migration and tissue remodeling.
- Biological function summary
MMP14 influences extracellular matrix degradation enabling cellular invasion and migration. It exists as a part of macromolecular complexes at the cell surface interacting with other metalloproteinases. This interaction assists in the activation of other MMPs such as pro-MMP2 which further amplify matrix remodeling activities. The hinge region of MMP14 lends flexibility allowing it to effectively engage with substrate proteins.
- Pathways
MMP14 significantly affects cell signaling and tissue remodeling pathways. One critical pathway involves the activation of pro-MMP2 which is dependent on MMP14's proteolytic activity. MMP14 also plays a role in the regulation of cell proliferation and apoptosis through its interaction with proteins such as TIMP-2. This relationship between MMP14 and other regulatory proteins emphasizes its functional integration within major biological networks.
- Associated diseases and disorders
High MMP14 levels correlate strongly with cancer progression especially in cancers such as breast cancer and melanoma. The ability of MMP14 to degrade the extracellular matrix facilitates tumor invasion and metastasis. Through its regulatory activities MMP14 connects with other proteins like VEGF influencing angiogenesis within tumor microenvironments. Additionally MMP14 involvement in arthritic conditions highlights its role in joint degradation processes worsening the disease through augmented cartilage breakdown.
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Functional Studies - MMP14 Inhibitor Screening Assay Kit (Fluorometric) (ab139455)
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