Details of the Target

General Information of Target

Target ID LDTP04352
Target Name Matrix metalloproteinase-14 (MMP14)
Gene Name MMP14
Gene ID 4323
Synonyms
Matrix metalloproteinase-14; MMP-14; EC 3.4.24.80; MMP-X1; Membrane-type matrix metalloproteinase 1; MT-MMP 1; MTMMP1; Membrane-type-1 matrix metalloproteinase; MT1-MMP; MT1MMP
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSPAPRPPRCLLLPLLTLGTALASLGSAQSSSFSPEAWLQQYGYLPPGDLRTHTQRSPQS
LSAAIAAMQKFYGLQVTGKADADTMKAMRRPRCGVPDKFGAEIKANVRRKRYAIQGLKWQ
HNEITFCIQNYTPKVGEYATYEAIRKAFRVWESATPLRFREVPYAYIREGHEKQADIMIF
FAEGFHGDSTPFDGEGGFLAHAYFPGPNIGGDTHFDSAEPWTVRNEDLNGNDIFLVAVHE
LGHALGLEHSSDPSAIMAPFYQWMDTENFVLPDDDRRGIQQLYGGESGFPTKMPPQPRTT
SRPSVPDKPKNPTYGPNICDGNFDTVAMLRGEMFVFKERWFWRVRNNQVMDGYPMPIGQF
WRGLPASINTAYERKDGKFVFFKGDKHWVFDEASLEPGYPKHIKELGRGLPTDKIDAALF
WMPNGKTYFFRGNKYYRFNEELRAVDSEYPKNIKVWEGIPESPRGSFMGSDEVFTYFYKG
NKYWKFNNQKLKVEPGYPKSALRDWMGCPSGGRPDEGTEEETEVIIIEVDEEGGGAVSAA
AVVLPVLLLLLVLAVGLAVFFFRRHGTPRRLLYCQRSLLDKV
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Peptidase M10A family
Subcellular location
Membrane
Function
Endopeptidase that degrades various components of the extracellular matrix such as collagen. Activates progelatinase A. Essential for pericellular collagenolysis and modeling of skeletal and extraskeletal connective tissues during development. May be involved in actin cytoskeleton reorganization by cleaving PTK7. Acts as a positive regulator of cell growth and migration via activation of MMP15. Involved in the formation of the fibrovascular tissues in association with pro-MMP2. Cleaves ADGRB1 to release vasculostatin-40 which inhibits angiogenesis.
TTD ID
T65019
Uniprot ID
P50281
DrugMap ID
TTJ4QE7
Ensemble ID
ENST00000311852.11
HGNC ID
HGNC:7160
ChEMBL ID
CHEMBL3869

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		8.32  LDD0402  [1]
Alkylaryl probe 2
 Probe Info  		10.00  LDD0391  [2]
STPyne
 Probe Info  		K383(7.26); K386(6.46); K404(6.71); K434(5.55)  LDD0277  [3]
OPA-S-S-alkyne
 Probe Info  		K337(1.70)  LDD3494  [4]
Alkylaryl probe 1
 Probe Info  		13.00  LDD0388  [2]
DBIA
 Probe Info  		C574(5.17)  LDD3310  [5]
JZ128-DTB
 Probe Info  		N.A.  LDD0462  [6]
BTD
 Probe Info  		C574(1.47)  LDD1700  [7]
AHL-Pu-1
 Probe Info  		C574(2.71)  LDD0171  [8]
IPM
 Probe Info  		C574(49.39)  LDD1701  [7]
NAIA_4
 Probe Info  		N.A.  LDD2226  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C574(0.97)  LDD2112  [7]
 LDCM0026  4SU-RNA+native RNA DM93 C574(2.71)  LDD0171  [8]
 LDCM0156  Aniline NCI-H1299 7.12  LDD0403  [1]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C574(50.23)  LDD1702  [7]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [6]
 LDCM0022  KB02 42-MG-BA C127(1.90)  LDD2244  [5]
 LDCM0023  KB03 MDA-MB-231 C574(49.39)  LDD1701  [7]
 LDCM0024  KB05 COLO792 C574(5.17)  LDD3310  [5]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C574(1.49)  LDD2092  [7]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C574(1.02)  LDD2093  [7]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C574(2.21)  LDD2094  [7]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C574(1.00)  LDD2097  [7]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C574(1.04)  LDD2098  [7]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C574(1.92); C93(0.77)  LDD2100  [7]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C574(1.53); C93(1.71)  LDD2104  [7]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C574(0.73)  LDD2108  [7]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C574(0.79)  LDD2109  [7]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C574(1.11)  LDD2111  [7]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C574(2.17)  LDD2119  [7]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C574(0.92)  LDD2120  [7]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C574(1.09)  LDD2127  [7]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C574(1.00)  LDD2128  [7]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C574(0.87)  LDD2129  [7]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C574(0.67)  LDD2133  [7]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C574(0.48)  LDD2134  [7]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C574(0.89)  LDD2135  [7]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C574(1.85)  LDD2136  [7]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C574(1.47)  LDD1700  [7]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C574(0.63)  LDD2140  [7]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C574(0.93)  LDD2143  [7]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C574(0.99)  LDD2146  [7]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C574(1.96)  LDD2147  [7]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C574(0.59)  LDD2148  [7]
 LDCM0099  Phenelzine MDA-MB-231 13.00  LDD0388  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Acireductone dioxygenase (ADI1) Acireductone dioxygenase (ARD) family Q9BV57
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (EBP) EBP family Q15125
Very long chain fatty acid elongase 4 (ELOVL4) ELO family Q9GZR5
Zinc finger-containing ubiquitin peptidase 1 (ZUP1) Peptidase C78 family Q96AP4
Furin (FURIN) Peptidase S8 family P09958
LIM domain kinase 1 (LIMK1) TKL Ser/Thr protein kinase family P53667
Fibroblast growth factor receptor 4 (FGFR4) Tyr protein kinase family P22455
17-beta-hydroxysteroid dehydrogenase 13 (HSD17B13) Short-chain dehydrogenases/reductases (SDR) family Q7Z5P4
Methylsterol monooxygenase 1 (MSMO1) Sterol desaturase family Q15800
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Stomatin (STOM) Band 7/mec-2 family P27105
Aquaporin-6 (AQP6) MIP/aquaporin (TC 1.A.8) family Q13520
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Junctional adhesion molecule A (F11R) Immunoglobulin superfamily Q9Y624
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Breast cancer anti-estrogen resistance protein 1 (BCAR1) CAS family P56945
Metalloproteinase inhibitor 2 (TIMP2) Protease inhibitor I35 (TIMP) family P16035
Lumican (LUM) Small leucine-rich proteoglycan (SLRP) family P51884
Four and a half LIM domains protein 3 (FHL3) . Q13643
Protein KASH5 (KASH5) . Q8N6L0

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Epigallocatechin Gallate Small molecular drug D0U2BH
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bt1718 Bicycle toxin conjugate DE2Z7V
Investigative
Click To Hide/Show 13 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2-(4-bromophenylsulfonamido)-n-hydroxyacetamide Small molecular drug D0NV9C
2-(Biphenyl-4-ylsulfonamido)-n-hydroxyacetamide Small molecular drug D09ZOA
2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Small molecular drug D05THD
Ik-862 Small molecular drug D0W2UK
Marimastat Small molecular drug DB00786
Mmi270 Small molecular drug D0A4TC
N-hydroxy-2-(4-methoxyphenylsulfonamido)Acetamide Small molecular drug D0XK7G
N-hydroxy-2-(4-phenoxy-benzenesulfonyl)Benzamide Small molecular drug D0S9OL
Pmid23631440c29e Small molecular drug D07DRT
Sr-973 Small molecular drug D03AMR
Uk-356618 Small molecular drug D0NP8A
[2-(Biphenyl-4-sulfonyl)Phenyl]Acetic Acid Small molecular drug D07MJD
Dx-2400 . D03XBB
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gm6001 Small molecular drug D0T9HG

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Hydrazines as versatile chemical biology probes and drug-discovery tools for cofactor-dependent enzymes. bioRxiv, 2020-06.
3 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
4 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
5 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
6 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
7 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
8 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
9 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264