Page last updated: 2024-08-07 15:36:02
Interstitial collagenase
An interstitial collagenase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P03956]
Synonyms
EC 3.4.24.7;
Fibroblast collagenase;
Matrix metalloproteinase-1;
MMP-1
Research
Bioassay Publications (90)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 14 (15.56) | 18.2507 |
| 2000's | 51 (56.67) | 29.6817 |
| 2010's | 19 (21.11) | 24.3611 |
| 2020's | 6 (6.67) | 2.80 |
Compounds (60)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| N-[4-(4-morpholinyl)butyl]-2-benzofurancarboxamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| doxazosin | Homo sapiens (human) | IC50 | 5.7490 | 1 | 0 |
| way 151693 | Homo sapiens (human) | IC50 | 0.2153 | 4 | 6 |
| nafamostat | Homo sapiens (human) | IC50 | 420.0000 | 1 | 1 |
| nimesulide | Homo sapiens (human) | IC50 | 23.3450 | 1 | 0 |
| prazosin | Homo sapiens (human) | IC50 | 4.0360 | 1 | 0 |
| sulfasalazine | Homo sapiens (human) | IC50 | 23.5490 | 1 | 0 |
| irinotecan | Homo sapiens (human) | IC50 | 6.0600 | 1 | 0 |
| secoisolariciresinol | Homo sapiens (human) | IC50 | 50.1200 | 1 | 1 |
| piloty's acid | Homo sapiens (human) | Ki | 56.4100 | 3 | 10 |
| aminoquinuride | Homo sapiens (human) | IC50 | 31.0000 | 1 | 1 |
| marimastat | Homo sapiens (human) | IC50 | 0.8358 | 12 | 12 |
| marimastat | Homo sapiens (human) | Ki | 0.0010 | 4 | 4 |
| n-(2-isobutyl-3-(n'-hydroxycarbonylamido)propanoyl)-o-methyltyrosinemethylamide | Homo sapiens (human) | IC50 | 0.0115 | 2 | 1 |
| n-(2-isobutyl-3-(n'-hydroxycarbonylamido)propanoyl)-o-methyltyrosinemethylamide | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| ilomastat | Homo sapiens (human) | IC50 | 0.0025 | 11 | 11 |
| ilomastat | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| bb3497 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| 3-((benzyl)(methylaminocarbonyl)methylaminocarbonyl)n-hydroxy-5-methylhexanamide | Homo sapiens (human) | IC50 | 0.0293 | 3 | 3 |
| 3-((benzyl)(methylaminocarbonyl)methylaminocarbonyl)n-hydroxy-5-methylhexanamide | Homo sapiens (human) | Ki | 0.0070 | 1 | 1 |
| actinonin | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| cgs 27023a | Homo sapiens (human) | IC50 | 0.0310 | 2 | 4 |
| cgs 27023a | Homo sapiens (human) | Ki | 0.0211 | 2 | 5 |
| prinomastat | Homo sapiens (human) | IC50 | 0.0209 | 7 | 7 |
| prinomastat | Homo sapiens (human) | Ki | 0.0082 | 3 | 3 |
| isoliquiritigenin | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
| caffeic acid | Homo sapiens (human) | IC50 | 0.2389 | 1 | 1 |
| rs-130830 | Homo sapiens (human) | IC50 | 0.2062 | 7 | 9 |
| rs-130830 | Homo sapiens (human) | Ki | 0.2224 | 4 | 9 |
| pnu 142372 | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| pnu 107859 | Homo sapiens (human) | Ki | 31.0000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 1.4900 | 1 | 1 |
| luteolin | Homo sapiens (human) | IC50 | 3.0300 | 1 | 1 |
| kaempferol | Homo sapiens (human) | IC50 | 2.6350 | 1 | 2 |
| norathyriol | Homo sapiens (human) | IC50 | 11.3600 | 1 | 1 |
| morin | Homo sapiens (human) | IC50 | 4.8500 | 1 | 1 |
| myricetin | Homo sapiens (human) | IC50 | 2.9200 | 1 | 1 |
| rosmarinic acid | Homo sapiens (human) | IC50 | 5.6000 | 1 | 1 |
| tmi-1 | Homo sapiens (human) | IC50 | 0.0115 | 3 | 8 |
| benzyloxycarbonyl-phe-ala-fluormethylketone | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| batimastat | Homo sapiens (human) | IC50 | 0.3158 | 7 | 7 |
| gi 129471 | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
| Methyl rosmarinate | Homo sapiens (human) | IC50 | 14.7200 | 2 | 2 |
| ik 682 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| ik 682 | Homo sapiens (human) | Ki | 30.0000 | 2 | 2 |
| bay 12-9566 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| bay 12-9566 | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| (11c)cgs 25966 | Homo sapiens (human) | IC50 | 0.0330 | 1 | 1 |
| (11c)cgs 25966 | Homo sapiens (human) | Ki | 0.0335 | 2 | 2 |
| ro 32-3555 | Homo sapiens (human) | IC50 | 0.0235 | 2 | 4 |
| ro 32-3555 | Homo sapiens (human) | Ki | 1.7510 | 4 | 4 |
| abt-770 | Homo sapiens (human) | IC50 | 4.6000 | 3 | 3 |
| sb 3ct compound | Homo sapiens (human) | Ki | 172.7500 | 4 | 4 |
| pd 166793 | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| sc 78080 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sc 78080 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| ro 31-9790 | Homo sapiens (human) | IC50 | 0.0058 | 4 | 4 |
| ro 31-9790 | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| n-((2s)-2-mercapto-1-oxo-4-(3,4,4- trimethyl-2,5-dioxo-1-imidazolidinyl)butyl)-l-leucyl-n,3- dimethyl-l-valinamide | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| arp-100 | Homo sapiens (human) | IC50 | 29.4833 | 6 | 6 |
| kb r8301 | Homo sapiens (human) | IC50 | 0.0003 | 1 | 1 |
| s 3304 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| N(2)-([biphenyl]-4-ylsulfonyl)-N-hydroxy-N(2)-isopropoxy-D-valinamide | Homo sapiens (human) | IC50 | 0.3185 | 2 | 2 |
| bms-566394 | Homo sapiens (human) | Ki | 7.4740 | 2 | 2 |
| ks370g | Homo sapiens (human) | IC50 | 3.3013 | 1 | 1 |
| apratastat | Homo sapiens (human) | IC50 | 0.0330 | 1 | 1 |
| incb3619 | Homo sapiens (human) | IC50 | 5.0000 | 2 | 2 |
| alendronate sodium | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| grassystatin a | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| (4-(n-hydroxyamino)-2r-isobutyl-3s-methylsuccinyl)-l-phenylglycine-n-methylamide | Homo sapiens (human) | IC50 | 0.0013 | 1 | 1 |
| 2-[(4-chlorophenyl)methylthio]-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-4-one | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 4-[[(4-oxo-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)thio]methyl]benzoic acid methyl ester | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| marimastat | Homo sapiens (human) | Activity | 0.0029 | 1 | 1 |
| prinomastat | Homo sapiens (human) | Activity | 0.0235 | 1 | 1 |
| rs-130830 | Homo sapiens (human) | Activity | 0.8000 | 1 | 1 |
The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups.Bioorganic & medicinal chemistry letters, , Aug-20, Volume: 11, Issue:16, 2001
Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.Bioorganic & medicinal chemistry letters, , Nov-19, Volume: 11, Issue:22, 2001
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential TreatJournal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 13, Issue:16, 2003
Structure--activity relationships of azasugar-based MMP/ADAM inhibitors.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 13, Issue:16, 2003
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
alpha-Alkyl-alpha-amino-beta-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1.Bioorganic & medicinal chemistry letters, , Oct-22, Volume: 11, Issue:20, 2001
Selective, orally active MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Sep-17, Volume: 11, Issue:18, 2001
Synthesis and activity of selective MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 9, Issue:12, 1999
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 9, Issue:19, 1999
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 8, Issue:22, 1998
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers.Journal of medicinal chemistry, , Jul-31, Volume: 46, Issue:16, 2003
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.Journal of medicinal chemistry, , Oct-11, Volume: 44, Issue:21, 2001
[no title available],
Discovery of Aryloxyphenyl-Heptapeptide Hybrids as Potent and Selective Matrix Metalloproteinase-2 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.European journal of medicinal chemistry, , Volume: 62, 2013
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Simultaneous presence of unsaturation and long alkyl chain at P'1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 15, Issue:14, 2007
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.The Journal of biological chemistry, , Sep-21, Volume: 282, Issue:38, 2007
Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives.Bioorganic & medicinal chemistry letters, , May-19, Volume: 13, Issue:10, 2003
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Peptidyl 3-substituted 1-hydroxyureas as isosteric analogues of succinylhydroxamate MMP inhibitors.European journal of medicinal chemistry, , Volume: 43, Issue:5, 2008
Design and synthesis of dual inhibitors for matrix metalloproteinase and cathepsin.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
Selective inhibition of low affinity IgE receptor (CD23) processing.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 8, Issue:1, 1998
Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group.Journal of medicinal chemistry, , Jul-07, Volume: 38, Issue:14, 1995
Design, synthesis and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP).Bioorganic & medicinal chemistry, , 01-01, Volume: 27, Issue:1, 2019
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Receptor flexibility in the in silico screening of reagents in the S1' pocket of human collagenase.Journal of medicinal chemistry, , May-20, Volume: 47, Issue:11, 2004
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Selective, orally active MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Sep-17, Volume: 11, Issue:18, 2001
Synthesis and activity of selective MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Nov-04, Volume: 42, Issue:22, 1999
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.Journal of medicinal chemistry, , 01-26, Volume: 60, Issue:2, 2017
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
Selective, orally active MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Sep-17, Volume: 11, Issue:18, 2001
Synthesis and activity of selective MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Current perspective of TACE inhibitors: a review.Bioorganic & medicinal chemistry, , Jan-15, Volume: 17, Issue:2, 2009
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheuThe Journal of pharmacology and experimental therapeutics, , Volume: 309, Issue:1, 2004
[no title available]RSC medicinal chemistry, , Oct-20, Volume: 12, Issue:10, 2021
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers.Journal of medicinal chemistry, , Jul-31, Volume: 46, Issue:16, 2003
Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality.Bioorganic & medicinal chemistry letters, , Feb-26, Volume: 11, Issue:4, 2001
Hydroxamate-based inhibitors of low affinity IgE receptor (CD23) processing.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 8, Issue:1, 1998
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Selective inhibition of low affinity IgE receptor (CD23) processing.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 8, Issue:1, 1998
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 8, Issue:22, 1998
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Identification of potent and selective TACE inhibitors via the S1 pocket.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 17, Issue:1, 2007
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 16, Issue:10, 2006
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Structure-Activity Relationship for Thiirane-Based Gelatinase Inhibitors.ACS medicinal chemistry letters, , Jun-14, Volume: 3, Issue:6, 2012
Sulfonate-containing thiiranes as selective gelatinase inhibitors.ACS medicinal chemistry letters, , Feb-10, Volume: 2, Issue:2, 2011
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs.Bioorganic & medicinal chemistry, , Mar-15, Volume: 15, Issue:6, 2007
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.Bioorganic & medicinal chemistry letters, , Aug-20, Volume: 11, Issue:16, 2001
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases.Bioorganic & medicinal chemistry letters, , May-19, Volume: 8, Issue:10, 1998
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.Journal of medicinal chemistry, , Mar-25, Volume: 53, Issue:6, 2010
N-O-isopropyl sulfonamido-based hydroxamates: design, synthesis and biological evaluation of selective matrix metalloproteinase-13 inhibitors as potential therapeutic agents for osteoarthritis.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain. [http://merops.sanger.ac.uk/about/glossary.htm#ENDOPEPTIDASE] |
| metalloendopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a mechanism in which water acts as a nucleophile, one or two metal ions hold the water molecule in place, and charged amino acid side chains are ligands for the metal ions. [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE, https://www.ebi.ac.uk/merops/about/glossary.shtml#ENDOPEPTIDASE] |
| serine-type endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] |
| peptidase activity | molecular function | Catalysis of the hydrolysis of a peptide bond. A peptide bond is a covalent bond formed when the carbon atom from the carboxyl group of one amino acid shares electrons with the nitrogen atom from the amino group of a second amino acid. [GOC:jl, ISBN:0815332181] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| extracellular matrix | cellular component | A structure lying external to one or more cells, which provides structural support, biochemical or biomechanical cues for cells or tissues. [GOC:BHF, GOC:mah, GOC:rph, NIF_Subcellular:nlx_subcell_20090513, PMID:21123617, PMID:28089324] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
| protein metabolic process | biological process | The chemical reactions and pathways involving a protein. Includes protein modification. [GOC:ma] |
| extracellular matrix disassembly | biological process | A process that results in the breakdown of the extracellular matrix. [GOC:jid] |
| collagen catabolic process | biological process | The proteolytic chemical reactions and pathways resulting in the breakdown of collagen in the extracellular matrix, usually carried out by proteases secreted by nearby cells. [GOC:mah, ISBN:0815316194] |
| positive regulation of protein-containing complex assembly | biological process | Any process that activates or increases the frequency, rate or extent of protein complex assembly. [GOC:mah] |
| cellular response to UV-A | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a UV-A radiation stimulus. UV-A radiation (UV-A light) spans the wavelengths 315 to 400 nm. [GOC:mah] |
| extracellular matrix organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of an extracellular matrix. [GOC:mah] |