8 Synthetic Inhibitors of Bacterial and Mammalian Interstitial Collagenases

On the size of the active site in proteases. I. Papain

1967 • 5,150 citations

Matrix metalloproteinases and their inhibitors in connective tissue remodeling

1991 • 3,309 citations

Design of Specific Inhibitors of Angiotensin-Converting Enzyme: New Class of Orally Active Antihypertensive Agents

1977 • 1,851 citations

Metastatic potential correlates with enzymatic degradation of basement membrane collagen

1980 • 1,778 citations

The cysteine switch: a principle of regulation of metalloproteinase activity with potential applicability to the entire matrix metalloproteinase gene family.

1990 • 1,423 citations

COLLAGENOLYTIC ACTIVITY IN AMPHIBIAN TISSUES: A TISSUE CULTURE ASSAY

1962 • 1,275 citations

A novel metalloproteinase gene specifically expressed in stromal cells of breast carcinomas

1990 • 1,140 citations

SV40-transformed Human Lung Fibroblasts Secrete a 92-kDa Type IV Collagenase Which Is Identical to That Secreted by Normal Human Macrophages

1989 • 1,122 citations

H-ras oncogene-transformed human bronchial epithelial cells (TBE-1) secrete a single metalloprotease capable of degrading basement membrane collagen.

1988 • 1,050 citations

Extracellular matrix biochemistry

1984 • 1,038 citations

Proteinases in mammalian cells and tissues

1978 • 981 citations

Tumor invasion and the extracellular matrix.

1983 • 960 citations

Multiple modes of activation of latent human fibroblast collagenase: evidence for the role of a Cys73 active-site zinc complex in latency and a "cysteine switch" mechanism for activation.

1990 • 699 citations

Structural basis of the action of thermolysin and related zinc peptidases

1988 • 675 citations

Structure and Function of Collagen Types

1987 • 653 citations

Human fibroblast collagenase. Complete primary structure and homology to an oncogene transformation-induced rat protein.

1986 • 645 citations

Biochemical and immunological characterization of the secreted forms of human neutrophil gelatinase.

1985 • 625 citations

Tumor interactions with the vasculature: angiogenesis and tumor metastasis

1990 • 598 citations

Angiotensin-converting enzyme inhibitors from the venom of Bothrops jararaca. Isolation, elucidation of structure, and synthesis

1971 • 516 citations

A metalloproteinase from human rheumatoid synovial fibroblasts that digests connective tissue matrix components. Purification and characterization.

1986 • 515 citations

Stromelysin, a connective tissue-degrading metalloendopeptidase secreted by stimulated rabbit synovial fibroblasts in parallel with collagenase. Biosynthesis, isolation, characterization, and substrates.

1985 • 506 citations

Stromelysin is an activator of procollagenase. A study with natural and recombinant enzymes

1987 • 474 citations

Oxidative Autoactivation of Latent Collagenase by Human Neutrophils

1985 • 466 citations

Enzymes of the Renin-Angiotensin System and their Inhibitors

1982 • 465 citations

Antisense RNA-Induced Reduction in Murine TIMP Levels Confers Oncogenicity on Swiss 3T3 Cells

1989 • 459 citations

Comparison of human stromelysin and collagenase by cloning and sequence analysis

1986 • 443 citations

Matrix metalloproteinase 2 from human rheumatoid synovial fibroblasts

1990 • 428 citations

Cell Biology of Extracellular Matrix

1983 • 414 citations

Human neutrophil collagenase. A distinct gene product with homology to other matrix metalloproteinases.

1990 • 406 citations

Human skin collagenase: isolation of precursor and active forms from both fibroblast and organ cultures

1977 • 387 citations

The collagen substrate specificity of human skin fibroblast collagenase.

1981 • 371 citations

The collagenase gene family in humans consists of at least four members

1988 • 364 citations

Epidermal growth factor and oncogenes induce transcription of the same cellular mRNA in rat fibroblasts.

1985 • 344 citations

Specific degradation of the collagen molecule by tadpole collagenolytic enzyme.

1965 • 339 citations

Isolation of the oncogene and epidermal growth factor-induced transin gene: complex control in rat fibroblasts.

1986 • 339 citations

Human skin fibroblast stromelysin: structure, glycosylation, substrate specificity, and differential expression in normal and tumorigenic cells.

1987 • 323 citations

Tetracyclines inhibit tissue collagenase activity

1984 • 318 citations

Inhibition by human recombinant tissue inhibitor of metalloproteinases of human amnion invasion and lung colonization by murine B16-F10 melanoma cells.

1988 • 312 citations

A Non-antibacterial Chemically-modified Tetracycline Inhibits Mammalian Collagenase Activity

1987 • 307 citations

The collagen substrate specificity of human neutrophil collagenase.

1987 • 285 citations

Heparin Osteoporosis

1965 • 276 citations

Collagenolytic activity during mammalian wound repair

1967 • 261 citations

Rat collagenase. Cloning, amino acid sequence comparison, and parathyroid hormone regulation in osteoblastic cells.

1990 • 249 citations

Purification and characterization of a murine basement membrane collagen-degrading enzyme secreted by metastatic tumor cells.

1983 • 245 citations

[1] The collagens: An overview and update

1987 • 244 citations

[1] Collagen: An overview

1982 • 241 citations

Low‐dose doxycycline therapy: Effect on gingival and crevicular fluid collagenase activity in humans

1990 • 228 citations

The complete primary structure of human matrix metalloproteinase-3. Identity with stromelysin.

1988 • 227 citations

Collagenase at Sites of Cartilage Erosion in the Rheumatoid Joint

1977 • 218 citations

Further evidence that tetracyclines inhibit collagenase activity in human crevicular fluid and from other mammalian sources

1985 • 215 citations

Characterization of the individual collagenases from Clostridium histolyticum

1984 • 215 citations

Human skin fibroblast procollagenase: mechanisms of activation by organomercurials and trypsin

1983 • 208 citations

Shark Cartilage Contains Inhibitors of Tumor Angiogenesis

1983 • 204 citations

Granulocyte collagenase: selective digestion of type I relative to type III collagen.

1977 • 201 citations

Human alveolar macrophages produce a fibroblast-like collagenase and collagenase inhibitor.

1985 • 199 citations

Mouse osteoblasts synthesize collagenase in response to bone resorbing agents

1984 • 192 citations

Pathobiology of the Endothelial Cell

1982 • 190 citations

Matrix metalloproteinases. A review.

1990 • 187 citations

Cleavage of type II and III collagens with mammalian collagenase: site of cleavage and primary structure at the amino-terminal portion of the smaller fragment released from both collagens

1976 • 171 citations

Proteinases and tumor invasion

1980 • 170 citations

Structure-function relationships in the collagenase family member transin.

1988 • 169 citations

Human Fibroblast Collagenase-α-Macroglobulin Interactions

1989 • 164 citations

Inhibition of purified collagenase from alkali-burned rabbit corneas.

1989 • 160 citations

Purification and separation of individual collagenases of Clostridium histolyticum using red dye ligand chromatography

1984 • 157 citations

Comparison of vertebrate collagenase and gelatinase using a new fluorogenic substrate peptide

1989 • 154 citations

Control of tumor growth in animals by infusion of an angiogenesis inhibitor.

1980 • 154 citations

[8] Catabolism and turnover of collagens: Collagenases

1987 • 151 citations

Cleavage of type VII collagen by interstitial collagenase and type IV collagenase (gelatinase) derived from human skin

1989 • 151 citations

Human Skin Collagenase: Relationship to the Pathogenesis of Epidermolysis Bullosa Dystrophica*

1969 • 148 citations

Sequence specificities of human fibroblast and neutrophil collagenases.

1991 • 146 citations

Animal collagenases: Specificity of action, and structures of the substrate cleavage site

1974 • 144 citations

Effect of Natural Protease Inhibitors and a Chemoattractant on Tumor Cell Invasion In Vitro

1982 • 141 citations

Characterization of collagenolytic activity from strains of Bacteroides gingivalis

1988 • 132 citations

Sequences coding for part of oncogene-induced transin are highly conserved in a related rat gene

1987 • 127 citations

Human fibroblast collagenase: glycosylation and tissue-specific levels of enzyme synthesis.

1986 • 125 citations

Synthesis of collagenase and collagenase inhibitors by osteoblast-like cells in culture

1984 • 125 citations

Collagenase from rat uterus. Isolation and partial characterization

1970 • 123 citations

Collagenase Inhibitors: Their Design and Potential Therapeutic Use

1987 • 121 citations

Differential susceptibility of type X collagen to cleavage by two mammalian interstitial collagenases and 72-kDa type IV collagenase.

1990 • 121 citations

Sequence specificity of human skin fibroblast collagenase. Evidence for the role of collagen structure in determining the collagenase cleavage site.

1987 • 120 citations

Evidence that human rheumatoid synovial matrix metalloproteinase 3 is an endogenous activator of procollagenase

1988 • 120 citations

Systemic Tetracycline Treatment of Alkali-Induced Corneal Ulceration in Rabbits

1987 • 120 citations

Myelomonocytic cell lineage expression of the neutrophil elastase gene.

1988 • 119 citations

Mammalian collagenase: Direct demonstration in homogenates of involuting rat uterus

1971 • 118 citations

Tetradecanoyl phorbol acetate stimulates latent collagenase production by cultured human endothelial cells

1980 • 117 citations

A gene for rabbit synovial cell collagenase: member of a family of metalloproteinases that degrades the connective tissue matrix

1987 • 115 citations

Bone-Resorbing Agents Affect the Production and Distribution of Procollagenase as well as the Activity of Collagenase in Bone Tissue*

1988 • 114 citations

Inhibitors of Mammalian Tissue Collagenase and Metalloproteinases Suppress Ovulation in the Perfused Rat Ovary*

1988 • 113 citations

Continuously recording fluorescent assays optimized for five human matrix metalloproteinases

1991 • 111 citations

Type X collagen contains two cleavage sites for a vertebrate collagenase.

1986 • 106 citations

The gelatinolytic activity of human skin fibroblast collagenase.

1982 • 105 citations

Cleavage and inactivation of alpha 1-antitrypsin by metalloproteinases released from neutrophils.

1988 • 104 citations

Limited proteolysis of type I collagen at hyperreactive sites by class I and II Clostridium histolyticum collagenases: complementary digestion patterns

1987 • 102 citations

Characterization and activation of procollagenase from human polymorphonuclear leucocytes

1990 • 101 citations

Proteolytic inactivation of alpha-1-proteinase inhibitor by a neutrophil metalloproteinase.

1988 • 99 citations

A new synthetic inhibitor of mammalian tissue collagenase inhibits bone resorption in culture

1985 • 98 citations

Degradation of type IX collagen by matrix metalloproteinase 3 (stromelysin) from human rheumatoid synovial cells

1989 • 98 citations

Tetracyclines inhibit parathyroid hormone-induced bone resorption in organ culture

1984 • 95 citations

Randomized controlled trial of doxycycline in prevention of recurrent periodontitis in high-risk patients: antimicrobial activity and collagenase inhibition.

1990 • 94 citations

Characterization of 58-kilodalton human neutrophil collagenase: comparison with human fibroblast collagenase

1990 • 93 citations

Spectrophotometric assay for vertebrate collagenase

1985 • 91 citations

Monoclonal antibodies to human fibroblast procollagenase. Inhibition of enzymatic activity, affinity purification of the enzyme, and evidence for clustering of epitopes in the amino-terminal end of the activated enzyme

1988 • 91 citations

Collagenase and rheumatoid arthritis

1970 • 89 citations

Interaction of Human Rheumatoid Synovial Collagenase (Matrix Metalloproteinase 1) and Stromelysin (Matrix Metalloproteinase 3) with Human α2-Macroglobulin and Chicken Ovostatin

1989 • 87 citations

Cloning of a complementary dna for rabbit proactivator. a metalloproteinase that activates synovial cell collagenase, shares homology with stromelysin and transin, and is coordinately regulated with collagenase

1987 • 86 citations

Production of procollagenase by cultured human keratinocytes.

1987 • 86 citations

Synthetic substrates of vertebrate collagenase

1985 • 84 citations

Synovial collagenase: Its presence in culture from joint disease of diverse etiology

1969 • 83 citations

Randomized controlled trial of doxycycline in prevention of recurrent periodontitis in high‐risk patients: antimicrobial activity and collagenase inhibition

1990 • 82 citations

Multiplicity of Clostridium histolyticum Collagenases^*

1964 • 82 citations

Collagenolytic Activity of Alkali-Burned Corneas

1969 • 81 citations

Monocyte procollagenase and tissue inhibitor of metalloproteinases. Identification, characterization, and regulation of secretion.

1987 • 79 citations

X Collagenolytic Activity in Middle Ear Cholesteatoma

1969 • 78 citations

Minocycline treatment for rheumatoid arthritis: an open dose finding study.

1990 • 75 citations

Complementary substrate specificities of class I and class II collagenases from Clostridium histolyticum

1985 • 75 citations

12-o-Tetradecanoyl-phorbol-13-acetate-differentiated U937 cells express a macrophage-like profile of neutral proteinases. High levels of secreted collagenase and collagenase inhibitor accompany low levels of intracellular elastase and cathepsin G.

1986 • 74 citations

Susceptibility of cartilage collagens type II, IX, X, and XI to human synovial collagenase and neutrophil elastase

1988 • 73 citations

Direct extraction and assay of bone tissue collagenase and its relation to parathyroid-hormone-induced bone resorption

1986 • 71 citations

Inactivation of human plasma α₁‐proteinase inhibitor by human PMN leucocyte collagenase

1990 • 65 citations

Repair and Regeneration: The Scientific Basis for Surgical Practice

1969 • 64 citations

Relationship between the individual collagenases of Clostridium histolyticum: evidence for evolution by gene duplication

1984 • 63 citations

Heberden Oration 1980: aspects of the cell biology of the rheumatoid synovial lesion.

1981 • 58 citations

Structure and expression of the cDNA encoding human neutrophil collagenase

1991 • 57 citations

Inhibition of alkali-induced corneal ulceration and perforation by a thiol peptide.

1990 • 56 citations

Collagenase and bone resorption: Isolation of collagenase from culture medium containing serum after stimulation of bone resorption by addition of parathyroid hormone extract

1975 • 55 citations

Degradation of type I collagen by rat mucosal keratinocytes. Evidence for secretion of a specific epithelial collagenase.

1987 • 53 citations

Molecular cloning of human synovial cell collagenase and selection of a single gene from genomic DNA.

1987 • 51 citations

18 The Collagenases

1971 • 50 citations

Tetracycline in the treatment of rheumatoid arthritis. A double blind controlled study

1971 • 49 citations

Phosphonamidate inhibitors of human neutrophil collagenase

1987 • 47 citations

Cleavage of bovine skin type III collagen by proteolytic enzymes. Relative resistance of the fibrillar form.

1985 • 47 citations

Transforming growth factor-β suppresses the invasiveness of human fibrosarcoma cells in vitro by increasing expression of tissue inhibitor of metalloprotease

1991 • 44 citations

Proteolytic activities of human fibroblast collagenase: hydrolysis of a broad range of substrates at a single active site

1990 • 44 citations

Purification to homogeneity of latent and active 58-kilodalton forms of human neutrophil collagenase

1990 • 43 citations

Systemic administration of TIMP in the treatment of collagen-induced arthritis in mice

1989 • 42 citations

Phosphoramidate peptide inhibitors of human skin fibroblast collagenase

1990 • 40 citations

Collagenase production by Achromobacter iophagus

1975 • 40 citations

Systemic Tetracycline Hydrochloride as Adjunctive Therapy in the Treatment of Persistent Epithelial Defects

1986 • 39 citations

Thiol-based inhibitors of mammalian collagenase. Substituted amide and peptide derivatives of the leucine analogue, 2-[(R,S)-mercaptomethyl]-4-methylpentanoic acid.

1990 • 39 citations

Clostridium histolyticum collagenase: development of new thio ester, fluorogenic, and depsipeptide substrates and new inhibitors

1985 • 36 citations

<b>ISOLATION AND CHARACTERIZATION OF COLLAGENASE SYNTHESIZED BY MOUSE BONE CELLS IN </b><b>CULTURE </b>

1984 • 35 citations

Collagenase: Current Concepts and Relevance to Periodontal Disease

1976 • 35 citations

Substrate specificity of beta-collagenase from Clostridium histolyticum.

1985 • 35 citations

Accurate, quantitative assays for the hydrolysis of soluble type I, II, and III 3H-acetylated collagens by bacterial and tissue collagenases

1986 • 34 citations

Properties of radiolabeled type I, II, and III collagens related to their use as substrates in collagenase assays

1986 • 34 citations

Metal binding peptide inhibitors of vertebrate collagenase

1981 • 31 citations

Covalent structure of collagen

1989 • 30 citations

Cleavage of Collagen Type X by Human Synovial Collagenase and Neutrophil Elastase

1989 • 29 citations

Inhibition of Clostridium histolyticum collagenases by phosphonamide peptide inhibitors

1990 • 29 citations

Low Molecular Weight, Sequence Based, Collagenase Inhibitors Selectively Block the Interaction Between Collagenase and TIMP (Tissue Inhibitor of Metalloproteinases)

1990 • 27 citations

Mode of hydrolysis of collagen-like peptides by class I and class II Clostridium histolyticum collagenases: evidence for both endopeptidase and tripeptidylcarboxypeptidase activities

1985 • 27 citations

Preparation and reconstitution with divalent metal ions of class I and class II Clostridium histolyticum apocollagenases

1988 • 25 citations

Inhibition of the collagenase from Clostridium histolyticum by phosphoric and phosphonic amides

1983 • 25 citations

Peptide hydroxamic acids inhibit skin collagenase

1986 • 25 citations

Inhibition of mammalian collagenases by thiol‐containing peptides

1986 • 23 citations

Collagen breakdown in relation to tooth eruption and resorption in the dog

1974 • 22 citations

Preparation by direct metal exchange and kinetic study of active site metal substituted class I and class II Clostridium histolyticum collagenases

1988 • 21 citations

Inhibition of human collagenases by sulfur-based substrate analogs

1991 • 21 citations

Purification and characterization of two high-molecular-mass forms of Achromobacter collagenase

1986 • 20 citations

New thiol inhibitor of Achromobacter iophagus collagenase. Specificity of the enzyme's S3' subsite

1986 • 16 citations

Aldehyde and ketone substrate analogs inhibit the collagenase of Clostridium histolyticum

1985 • 16 citations

Effect of systemic tetracycline on progression of Pseudomonas aeruginosa keratitis in the rabbit.

1990 • 16 citations

An inhibitor of mammalian collagenase active at micromolar concentrations from an Actinomycete culture broth.

1987 • 15 citations

Nucleotide sequence of a cDNA for porcine type I collagenase, obtained by PCR

1990 • 15 citations

Vertebrate collagenase inhibitor. I. Tripeptidyl hydroxamic acids.

1990 • 15 citations

Crystallization and preliminary X-ray analysis of porcine synovial collagenase

1989 • 13 citations

Pharmacological studies on 6-amidino-2-naphthyl(4-(4,5-dihydro-1H-imidazol-2-yl)amino) benzoate dimethane sulfonate (FUT-187). I: Inhibitory activities on various kinds of enzymes in vitro and anticomplement activity in vivo.

1990 • 13 citations

New thiol inhibitors of Clostridium histolyticum collagenase

1988 • 12 citations

[Inhibition of synovial collagenase by actinonin. Study of structure/activity relationship].

1989 • 12 citations

Vertebrate collagenase inhibitor. I. Tripeptidyl hydroxamic acids.

1990 • 11 citations

Ketone-substrate analogues of Clostridium histolyticum collagenases: tight-binding transition-state analogue inhibitors

1988 • 11 citations

Functional constituents of the active site of human neutrophil collagenase

1986 • 10 citations

Competitive inhibition of human skin collagenase by N-benzyloxycarbonyl-<scp>l</scp>-prolyl-<scp>l</scp>-alanyl-3-amino-2-oxopropyl-<scp>l</scp>-leucyl-<scp>l</scp>- alanylglycine ethyl ester

1986 • 8 citations

Phthaloyl-Glycyl^P-Isoleucyl-Tryptophan Benzylamide is a Potent Inhibitor of Human Skin Fibroblast Collagenase with AK_iof 25nM

1989 • 7 citations

A novel inhibitor of mammalian collagenase

1985 • 5 citations

Synthesis of peptidic inhibitors of the collagenase from Achromobacter iophagus.

1977 • 2 citations

The ketone cinnamoyl-(1-13C-Phe)-CGly-Pro-Pro is a tetrahedral transition state analog inhibitor of C. histolyticum collagenase

1989 • 1 citations