Human leukocyte and porcine pancreatic elastase: x-ray crystal structures, mechanism, substrate specificity, and mechanism-based inhibitors

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

1967 • 5,150 citations

Protein Inhibitors of Proteinases

1980 • 2,220 citations

HUMAN PLASMA PROTEINASE INHIBITORS

1983 • 2,129 citations

Serine Proteases: Structure and Mechanism of Catalysis

1977 • 1,238 citations

Structure of crystalline α-chymotrypsin

1972 • 675 citations

Structural basis of the activation and action of trypsin

1978 • 669 citations

Mapping the extended substrate binding site of cathepsin G and human leukocyte elastase. Studies with peptide substrates related to the alpha 1-protease inhibitor reactive site.

1979 • 602 citations

The geometry of the reactive site and of the peptide groups in trypsin, trypsinogen and its complexes with inhibitors

1983 • 580 citations

Human leukocyte granule elastase: rapid isolation and characterization

1976 • 550 citations

Isolation, properties, and complete amino acid sequence of human secretory leukocyte protease inhibitor, a potent inhibitor of leukocyte elastase.

1986 • 477 citations

The refined crystal structure of bovine β-trypsin at 1·8 Å resolution

1975 • 462 citations

Amino-Acid Sequence of Bovine Chymotrypsinogen-A

1964 • 373 citations

Three-dimensional Structure of Tosyl-elastase

1970 • 299 citations

Structure of α-chymotrypsin refined at 1.68 Å resolution

1985 • 285 citations

Replacement therapy of alpha 1-antitrypsin deficiency. Reversal of protease-antiprotease imbalance within the alveolar structures of PiZ subjects.

1981 • 275 citations

X-ray crystal structure of the complex of human leukocyte elastase (PMN elastase) and the third domain of the turkey ovomucoid inhibitor.

1986 • 272 citations

Inhibition of serine proteases by peptidyl fluoromethyl ketones

1986 • 242 citations

Structure of human neutrophil elastase in complex with a peptide chloromethyl ketone inhibitor at 1.84-A resolution.

1989 • 231 citations

Reaction of serine proteases with substituted isocoumarins: discovery of 3,4-dichloroisocoumarin, a new general mechanism based serine protease inhibitor

1985 • 231 citations

Primary structure of human neutrophil elastase.

1987 • 227 citations

Specificity of porcine pancreatic elastase, human leukocyte elastase and cathepsin G Inhibition with peptide chloromethyl ketones

1977 • 224 citations

Refined 2 Å X-ray crystal structure of porcine pancreatic kallikrein A, a specific trypsin-like serine proteinase

1983 • 224 citations

Amino-acid Sequence of Porcine Pancreatic Elastase and its Homologies with other Serine Proteinases

1970 • 219 citations

Synthesis in yeast of a functional oxidation-resistant mutant of human α1-antitrypsin

1984 • 209 citations

The acid‐stable proteinase inhibitor of human mucous secretions (HUSI‐I, antileukoprotease)

1986 • 178 citations

The atomic structure of crystalline porcine pancreatic elastase at 2.5 Å resolution: Comparisons with the structure of α-chymotrypsin

1978 • 165 citations

Cephalosporin antibiotics can be modified to inhibit human leukocyte elastase

1986 • 165 citations

Structure of native porcine pancreatic elastase at 1.65 Å resolution

1988 • 155 citations

Refined 1.2 A crystal structure of the complex formed between subtilisin Carlsberg and the inhibitor eglin c. Molecular structure of eglin and its detailed interaction with subtilisin.

1986 • 147 citations

Covalent structure of a group-specific protease from rat small intestine. Appendix: Crystallographic data for a group specific protease from rat intestine

1978 • 144 citations

Three-dimensional Fourier Synthesis of Tosyl-elastase at 3.5 Å Resolution

1970 • 144 citations

Refined crystal structure of γ-chymotrypsin at 1.9 Å resolution

1981 • 143 citations

Crystallographic refinement of Japanese quail ovomucoid, a Kazal-type inhibitor, and model building studies of complexes with serine proteases

1982 • 142 citations

The versatility of proteolytic enzymes

1986 • 136 citations

Levels of Elastase Activity in Bronchoalveolar Lavage Fluids of Healthy Smokers and Nonsmokers^1–3

1983 • 131 citations

Rat submaxillary gland serine protease, tonin

1987 • 125 citations

Primary structure of two distinct rat pancreatic preproelastases determined by sequence analysis of the complete cloned mRNA sequences

1982 • 120 citations

Myelomonocytic cell lineage expression of the neutrophil elastase gene.

1988 • 119 citations

The structure of rat mast cell protease II at 1.9-angstrom resolution

1988 • 112 citations

Crystallographie study of a β-lactam inhibitor complex with elastase at 1.84 Å resolution

1987 • 103 citations

Mechanism of slow-binding inhibition of human leukocyte elastase by trifluoromethyl ketones

1987 • 101 citations

Substrate specificity of the elastase and the chymotrypsin-like enzyme of the human granulocyte

1977 • 99 citations

Studies on reactivity of human leukocyte elastase, cathepsin G, and porcine pancreatic elastase toward peptides including sequences related to the reactive site of .alpha.1-protease inhibitor (.alpha.1-antitrypsin)

1980 • 97 citations

Active site mapping of the serine proteases human leukocyte elastase, cathepsin G, porcine pancreatic elastase, rat mast cell proteases I and II, bovine chymotrypsin A.alpha., and Staphylococcus aureus protease V-8 using tripeptide thiobenzyl ester substrates

1984 • 91 citations

A new class of heterocyclic serine protease inhibitors. Inhibition of human leukocyte elastase, porcine pancreatic elastase, cathepsin G, and bovine chymotrypsin A alpha with substituted benzoxazinones, quinazolines, and anthranilates.

1982 • 87 citations

Inhibition of human elastase from polymorphonuclear leucocytes by a glycosaminoglycan polysulfate (Arteparon®)

1980 • 87 citations

Stereochemistry of binding of the tetrapeptide acetyl-Pro-Ala-Pro-Tyr-NH2 to porcine pancreatic elastase

1986 • 85 citations

Reaction of serine proteases with substituted 3-alkoxy-4-chloroisocoumarins and 3-alkoxy-7-amino-4-chloroisocoumarins: new reactive mechanism-based inhibitors

1985 • 80 citations

The refined 2.3 Å crystal structure of human leukocyte elastase in a complex with a valine chloromethyl ketone inhibitor

1988 • 77 citations

Mechanism-based isocoumarin inhibitors for trypsin and blood coagulation serine proteases: new anticoagulants

1988 • 73 citations

Crystallization and characterization of a new protease in mitochondria of bone marrow cells.

1978 • 71 citations

Synthetic inhibitors of human neutrophil elastase

1987 • 69 citations

X-ray diffraction analysis of the inhibition of porcine pancreatic elastase by a peptidyl trifluoromethylketone

1988 • 64 citations

Catalysis by human leukocyte elastase: mechanistic insights into specificity requirements

1987 • 64 citations

Activation of human leukocyte elastase activity by excess substrate, hydrophobic solvents, and ionic strength.

1980 • 62 citations

Reactivity of human leukocyte elastase and porcine pancreatic elastase toward peptide-4-nitroanilides containing model desmosine residues. Evidence that human leukocyte elastase is selective for crosslinked regions of elastin

1981 • 62 citations

Mechanism for slow-binding inhibition of human leukocyte elastase by valine-derived benzoxazinones

1987 • 60 citations

Crystallographic study of the binding of a trifluoroacetyl dipeptide anilide inhibitor with elastase

1982 • 59 citations

Stereochemical aspects of peptide hydrolysis catalyzed by serine proteases of the chymotrypsin type

1981 • 55 citations

Identification of a novel class of elastase isozyme, human pancreatic elastase III, by cDNA and genomic gene cloning.

1988 • 54 citations

Kinetic Studies on the Interaction of Eglincwith Human Leukocyte Elastase and Cathepsin G

1987 • 50 citations

Primary structure of human pancreatic protease E determined by sequence analysis of the cloned mRNA

1987 • 48 citations

The importance of the conformation of the tetrahedral intermediate for the α‐chymotrypsin‐catalyzed hydrolysis of peptide substrates

1975 • 47 citations

Structure of the product complex of acetyl-Ala-Pro-Ala with porcine pancreatic elastase at 1.65 Å resolution

1986 • 47 citations

Elastase Inhibitors for Treatment of Emphysema

1986 • 44 citations

Kinetics of the inhibition of human leucocyte elastase by eglin from the leech Hirudo medicinalis

1984 • 41 citations

Stereospecific reaction of 3-methoxy-4-chloro-7-aminoisocoumarin with crystalline porcine pancreatic elastase

1985 • 39 citations

Lymphocyte granule-mediated cytolysis requires serine protease activity

1987 • 39 citations

Catalysis by human leukocyte elastase: the proton inventory as a mechanistic probe

1987 • 38 citations

A new class of inhibitors of human leucocyte elastase

1985 • 37 citations

Analysis of an enzyme-substrate complex by x-ray crystallography and transferred nuclear overhauser enhancement measurements: porcine pancreatic elastase and a hexapeptide

1988 • 35 citations

Semisynthetic engineering of proteinase inhibitor homologues

1987 • 32 citations

Crystal structures of the complex of porcine pancreatic elastase with two valine-derived benzoxazinone inhibitors

1987 • 32 citations

Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation

1987 • 30 citations

Inhibition of serine proteases by benzoxazinones: effects of electron withdrawal and 5-substitution

1986 • 27 citations

Enzymatic oxidation of alpha- 1-proteinase inhibitor in abnormal tissue turnover

1982 • 23 citations

Some novel inhibitors of porcine pancreatic elastase

1979 • 23 citations

Molecular Cloning of Complementary DNA for Human Medullasin: An Inflammatory Serine Protease in Bone Marrow Cells

1987 • 22 citations

Catalysis by human leukocyte elastase: III. Steady-state kinetics for the hydrolysis of p-nitrophenyl esters

1985 • 22 citations

Crystallization of human neutrophil elastase.

1987 • 15 citations

Synthetic Inhibitors of Human Leukocyte Elastase, Part 3. Peptides with Alkyl groups at the N- or C-Terminus. Non-Toxic Competitive Inhibitors of Human Leukocyte Elastase

1987 • 6 citations