3.4.24.80: membrane-type matrix metalloproteinase-1

This is an abbreviated version!
For detailed information about membrane-type matrix metalloproteinase-1, go to the full flat file.

Reaction

endopeptidase activity. Activates progelatinase A by cleavage of the propeptide at Asn37-/-Leu. Other bonds hydrolysed include Gly35-/-Ile in the propeptide of collagenase 3, and Asn341-/-Phe, Asp441-/-Leu and Gln354-/-Thr in the aggrecan interglobular domain =

Synonyms

ectMMP-14, gelatinase A, interstitial MT1-MMP, matrix metalloprotease 14, matrix metalloproteinase 14, matrix metalloproteinase MT 1, matrix metalloproteinase MT-MMP-1, matrix metalloproteinase MT1-MMP, matrix metalloproteinase-14, membrane type 1 matrix, membrane type 1 matrix metalloproteinase, membrane type 1 MMP, membrane type 1-matrix metalloproteinase, membrane type 1-MMP, membrane type I MMP, membrane type matrix metalloproteinase, membrane type MMP-1, membrane type MT1-MMP, membrane type-1 matrix metalloprotease, membrane type-1 matrix metalloprotease 1, membrane type-1 matrix metalloproteinase, membrane type-1 MMP, membrane type-I matrix metalloproteinase, membrane type-I MMP, membrane-anchored matrix metalloproteinase 14, membrane-type 1 matrix metalloproteinase, membrane-type 1 matrix metalloproteinase 1, membrane-type 1 MMP, membrane-type 1-matrix metalloproteinase, membrane-type I matrix metalloproteinase, membrane-type matrix metalloproteinase MT1-MMP, membrane-type matrix metalloproteinase-1, membrane-type metalloproteinase MT1-MMP, membrane-type MMP, metalloproteinase, MMP-14, MMP-2, MMP-8, MMP14, mmp14a, mmp14b, More, MT-MMP-1, MT-MMP1, MT1-MMP, MT1-MMP/MMP-14, MT1-MPP, MTI-MMP, pericellular collagenase, proteinase, matrix metallo-, sMT1-MMP

ECTree

     3 Hydrolases

         3.4 Acting on peptide bonds (peptidases)

             3.4.24 Metalloendopeptidases

                3.4.24.80 membrane-type matrix metalloproteinase-1

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Results	in table
35	Activating Compound
325	AA Sequence
23	Application
1	CAS Registry Number
52	Cloned(Commentary)
3	Crystallization (Commentary)
3431	Disease/ Diagnostics
10	Expression
63	General Information
1	General Stability
20	IC50 Value
172	Inhibitors
24	kcat/KM [mM/s]
24	Ki Value [mM]
32	KM Value [mM]
87	Localization
24	Metals/Ions
54	Molecular Weight [Da]
81	Natural Substrates/ Products (Substrates)
136	Organism
12	PDB ID
5	pH Optimum
1	pH Range
21	Posttranslational Modification
63	Protein Variants
15	Purification (Commentary)
1	Reaction
2	Reaction Type
134	Reference
4	Renatured (Commentary)
207	Source Tissue
3	Specific Activity [micromol/min/mg]
299	Substrates and Products (Substrate)
24	Subunits
249	Synonyms
16	Temperature Optimum [°C]
1	Temperature Range [°C]
29	Turnover Number [1/s]

KI Value

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KI Value on EC 3.4.24.80 - membrane-type matrix metalloproteinase-1

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Ki VALUE [mM]

INHIBITOR

ORGANISM

UNIPROT

COMMENTARY

LITERATURE

IMAGE

0.0000002 - 0.000004

DX-2400

4 entries

-

0.001 - 0.1

GM6001

2 entries

0.000199

TIMP-1(M66A)

Homo sapiens

-

27°C

656167

-

0.000254

TIMP-1(M66G)

Homo sapiens

-

27°C

656167

-

0.000146

TIMP-1(M66I)

Homo sapiens

-

27°C

656167

-

0.000462

TIMP-1(M66K)

Homo sapiens

-

27°C

656167

-

0.000237

TIMP-1(M66L)

Homo sapiens

-

27°C

656167

-

0.000183

TIMP-1(M66V)

Homo sapiens

-

27°C

656167

-

0.000165

TIMP-1(P6A)

Homo sapiens

-

27°C

656167

-

0.000095

TIMP-1(P6S)

Homo sapiens

-

27°C

656167

-

0.000078

TIMP-1(P6V)

Homo sapiens

-

27°C

656167

-

0.00022

TIMP-1(T2S)

Homo sapiens

-

27°C

656167

-

0.0000111

TIMP-1(T98L)

Homo sapiens

-

27°C

656167

-

0.000066

TIMP-1(V4A)

Homo sapiens

-

27°C

656167

-

0.000081

TIMP-1(V4S)

Homo sapiens

-

27°C

656167

-

0.000259

TIMP-1(V69L)

Homo sapiens

-

27°C

656167

-

0.00000005 - 0.00000006

TIMP-2

2 entries

-

additional information

additional information

2 entries

-

0.0000002

DX-2400

Rattus norvegicus

-

-

697105

-

0.0000003

DX-2400

Mus musculus

-

-

697105

-

0.0000008

DX-2400

Homo sapiens

-

-

697105

-

0.000004

DX-2400

Macaca fascicularis

-

-

697105

-

0.001 - 0.01

GM6001

Homo sapiens

P50281

partial blockade of autolysis of both wild type and CHO-4 mutant MT1-MMP

669303

0.1

GM6001

Homo sapiens

P50281

complete blockade of autolysis of both wild type and CHO-4 mutant MT1-MMP

669303

0.00000005

TIMP-2

Homo sapiens

P50281

Tyr112-Gly288 fragment

638812

-

0.00000006

TIMP-2

Homo sapiens

P50281

Tyr112-Gly288 fragment

638812

-

additional information

additional information

Homo sapiens

-

between 0.000049 mM and 0.012 mM, significant decrease in inhibition potency with a homophenylalanine side chain compared with leucine, P1' substituent is interacting at the S1' pocket

667519

-

additional information

additional information

Homo sapiens

-

values generally lower for cdMT1-MMP when compared with those for deltaTM-MT1-MMP

667467

-