Cysteinyl Proteinases and Their Selective Inactivation

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

1967 • 5,150 citations

Esters of Methanesulfonic Acid as Irreversible Inhibitors of Acetylcholinesterase

1962 • 1,510 citations

Proteases and biological control

1976 • 1,380 citations

Serine Proteases: Structure and Mechanism of Catalysis

1977 • 1,238 citations

L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L

1982 • 1,024 citations

Isolation of the putative structural gene for the lysine-arginine-cleaving endopeptidase required for processing of yeast prepro-α-factor

1984 • 698 citations

[17] The kinetics of reversible tight-binding inhibition

1979 • 679 citations

Direct Evidence for the Presence of Histidine in the Active Center of Chymotrypsin^*

1963 • 649 citations

The 2.0 A X-ray crystal structure of chicken egg white cystatin and its possible mode of interaction with cysteine proteinases.

1988 • 584 citations

Purification of two high molecular weight proteases from rabbit reticulocyte lysate.

1987 • 542 citations

Evidence for an Active-Center Histidine in Trypsin through Use of a Specific Reagent, 1-Chloro-3-tosylamido-7-amino-2-heptanone, the Chloromethyl Ketone Derived from N^α-Tosyl-L-lysine^*

1965 • 521 citations

Limited Proteolysis of Protein Kinase C Subspecies by Calcium-dependent Neutral Protease (Calpain)

1989 • 470 citations

VIRAL PROTEINASES

1988 • 448 citations

Cysteine proteases of positive strand RNA viruses and chymotrypsin‐like serine proteases

1989 • 446 citations

Viral cysteine proteases are homologous to the trypsin-like family of serine proteases: structural and functional implications.

1988 • 428 citations

TRANSITION STATE ANALOG INHIBITORS AND ENZYME CATALYSIS

1976 • 415 citations

Intraorganellar calcium and pH control proinsulin cleavage in the pancreatic β cell via two distinct site-specific endopeptidases

1988 • 403 citations

On the active site of proteases. III. Mapping the active site of papain; specific peptide inhibitors of papain

1968 • 400 citations

Intracellular Ca2+-dependent protease (CALPAIN) and its high-molecular-weight endogenous inhibitor (CALPASTATIN)

1981 • 374 citations

How Do Enzymes Work?

1988 • 359 citations

Evidence that Pituitary Cation‐Sensitive Neutral Endopeptidase Is a Multicatalytic Protease Complex

1983 • 356 citations

Binding of chloromethyl ketone substrate analogs to crystalline papain

1976 • 352 citations

Cathepsin L

1977 • 341 citations

Determination of the rate constant of enzyme modification by measuring the substrate reaction in the presence of the modifier

1982 • 341 citations

Evolutionary origin of a calcium-dependent protease by fusion of genes for a thiol protease and a calcium-binding protein?

1984 • 337 citations

A malarial cysteine proteinase is necessary for hemoglobin degradation by Plasmodium falciparum.

1988 • 330 citations

Human cathepsin B1. Purification and some properties of the enzyme

1973 • 322 citations

Isolation and characterization of E-64, a new thiol protease inhibitor.

1978 • 319 citations

Calcium‐dependent proteases: an enzyme system active at cellular membranes?

1987 • 308 citations

The cystatins: a new class of peptidase inhibitors

1987 • 293 citations

Comparative specificity and kinetic studies on porcine calpain I and calpain II with naturally occurring peptides and synthetic fluorogenic substrates.

1984 • 291 citations

Structure of actinidin, after refinement at 1.7 Å resolution

1980 • 287 citations

EXTRALYSOSOMAL PROTEIN DEGRADATION

1986 • 279 citations

Thiol proteases

1985 • 274 citations

Ca2+-dependent protease in human platelets. Specific cleavage of platelet polypeptides in the presence of added Ca2+.

1977 • 274 citations

Proteolysis in Neuropeptide Processing and Other Neural Functions

1984 • 264 citations

LEUPEPTINS, NEW PROTEASE INHIBITORS FROM ACTINOMYCETES

1969 • 259 citations

Demonstration of two distinct high molecular weight proteases in rabbit reticulocytes, one of which degrades ubiquitin conjugates.

1987 • 255 citations

Synthesis of a new cell penetrating calpain inhibitor (calpeptin)

1988 • 254 citations

The processing of peptide precursors

1986 • 249 citations

Nucleotide and predicted amino acid sequences of cloned human and mouse preprocathepsin B cDNAs.

1986 • 245 citations

Purification of a liver alkaline protease which degrades oxidatively modified glutamine synthetase. Characterization as a high molecular weight cysteine proteinase.

1985 • 244 citations

Inhibition of serine proteases by peptidyl fluoromethyl ketones

1986 • 242 citations

Yeast KEX2 gene encodes an endopeptidase homologous to subtilisin-like serine proteases

1988 • 236 citations

Homology of amino acid sequences of rat liver cathepsins B and H with that of papain.

1983 • 231 citations

In vivo and in vitro evidence for the involvement of cysteine proteinases in bone resorption

1984 • 229 citations

Proteasomes (multi-protease complexes) as 20 S ring-shaped particles in a variety of eukaryotic cells.

1988 • 225 citations

New Observations on the Substrate Specificity of Cathepsin C (Dipeptidyl Aminopeptidase I)

1969 • 225 citations

BIOLOGICAL ACTIVITIES OF LEUPEPTINS

1969 • 222 citations

Cathepsin B: association with plasma membrane in metastatic tumors.

1986 • 222 citations

Bacterial growth blocked by a synthetic peptide based on the structure of a human proteinase inhibitor

1989 • 222 citations

A factor X-activating cysteine protease from malignant tissue.

1981 • 221 citations

Isolation and characterization of cancer procoagulant: a cysteine proteinase from malignant tissue

1985 • 213 citations

Identification of the probable inhibitory reactive sites of the cysteine proteinase inhibitors human cystatin C and chicken cystatin.

1987 • 212 citations

Peptidyl diazomethyl ketones are specific inactivators of thiol proteinases.

1981 • 208 citations

Purification and characterization of a multicatalytic high-molecular-mass proteinase from rat skeletal muscle

1985 • 208 citations

Leucylglycinamide Released from Oxytocin by Human Uterine Enzyme

1971 • 208 citations

The Chemical Modification of Proteins

1961 • 203 citations

Post-proline cleaving enzyme. Purification of this endopeptidase by affinity chromatography.

1976 • 202 citations

Proline residues in the maturation and degradation of peptide hormones and neuropeptides

1988 • 201 citations

Cathepsin B activity in B16 melanoma cells: a possible marker for metastatic potential.

1982 • 200 citations

Insulin Metabolism and Degradation*

1981 • 197 citations

Human cathepsin H

1980 • 193 citations

Human liver cathepsin L

1985 • 191 citations

Chemical modification of papain

1968 • 189 citations

Selective chemical modification of proteins.

1970 • 187 citations

Post-proline cleaving enzyme

1979 • 182 citations

Use of peptide aldehydes to generate transition-state analogs of elastase

1973 • 181 citations

Poliovirus Protein 3CD Is the Active Protease for Processing of the Precursor Protein P1 in vitro

1988 • 181 citations

Mammalian chymotrypsin-like enzymes. Comparative reactivities of rat mast cell proteases, human and dog skin chymases, and human cathepsin G with peptide 4-nitroanilide substrates and with peptide chloromethyl ketone and sulfonyl fluoride inhibitors

1985 • 180 citations

Purification and characterization of a paired basic residue-specific pro-opiomelanocortin converting enzyme from bovine pituitary intermediate lobe secretory vesicles.

1985 • 179 citations

PURIFICATION AND PROPERTIES OF A PROLYL ENDOPEPTIDASE FROM RABBIT BRAIN

1979 • 179 citations

The effects of inhibitors of cysteine-proteinases and collagenase on the resorptive activity of isolated osteoclasts☆

1987 • 176 citations

In vitro and in vivo inhibition of cysteine proteinases by EST, a new analog of E-64.

1986 • 175 citations

Yeast KEX2 Endopeptidase Correctly Cleaves a Neuroendocrine Prohormone in Mammalian Cells

1988 • 173 citations

The identification of the major excreted protein (MEP) from a transformed mouse fibroblast cell line as a catalytically active precursor form of cathepsin L

1987 • 172 citations

Aldehydes as Inhibitors of Papain

1972 • 169 citations

A GENERAL REACTION OF AMINO ACIDS. II

1928 • 168 citations

Calcium activated neutral protease: domain structure and activity regulation

1987 • 168 citations

Current problems in mechanistic studies of serine and cysteine proteinases

1982 • 165 citations

The specificity of cathepsin B. Hydrolysis of glucagon at the C-terminus by a peptidyldipeptidase mechanism

1978 • 159 citations

A comparison of four cathepsins (B, L, N and S) with collagenolytic activity from rabbit spleen

1988 • 158 citations

Thiol Addition to the Carbonyl Group. Equilibria and Kinetics¹

1966 • 157 citations

Secretion of proteinases from malignant and nonmalignant human breast tissue.

1980 • 156 citations

Induction of the proteolytic activity of a membrane protein in Plasmodium falciparum by phosphatidyl inositol-specific phospholipase C

1988 • 154 citations

Inhibition of Rabbit Brain Prolyl Endopeptidase by N‐Benzyloxycarbonyl‐Prolyl‐Prolinal, a Transition State Aldehyde Inhibitor

1983 • 151 citations

Recording spectrophotometric method for determination of dissociation and phosphorylation constants for the inhibition of acetylcholinesterase by organophosphates in the presence of substrate

1973 • 150 citations

Crystal structure of a papain-E-64 complex

1989 • 150 citations

The major excreted protein of transformed fibroblasts is an activable acid-protease.

1986 • 147 citations

ANTIPAIN, A NEW PROTEASE INHIBITOR ISOLATED FROM AGTINOMYCETES

1972 • 144 citations

Cysteine Proteinases and their Inhibitors

1986 • 142 citations

Human Insulin-Degrading Enzyme Shares Structural and Functional Homologies with E. coli Protease III

1988 • 141 citations

INHIBITION OF THROMBIN AND TRYPSIN BY TRIPEPTIDE ALDEHYDES

1978 • 140 citations

The design of peptidyldiazomethane inhibitors to distinguish between the cysteine proteinases calpain II, cathepsin L and cathepsin B

1988 • 139 citations

GHYMOSTATIN, A NEW GHYMOTRYPSIN INHIBITOR PRODUCED BY ACTINOMYGETES

1970 • 139 citations

Affinity purification and biochemical characterization of histolysin, the major cysteine proteinase of Entamoeba histolytica

1988 • 134 citations

Inhibition of proteolytic activity of calcium activated neutral protease by leupeptin and antipain

1978 • 130 citations

A new procoagulant in acute leukemia

1988 • 128 citations

A GENERAL REACTION OF AMINO ACIDS

1928 • 125 citations

Synthesis of peptide fluoromethyl ketones and the inhibition of human cathepsin B

1985 • 125 citations

Spectrin is associated with membrane-bound actin filaments in platelets and is hydrolyzed by the Ca2+-dependent protease during platelet activation

1987 • 123 citations

Purification and Properties of a New Cathepsin from Rat Liver1

1978 • 122 citations

Biosyntheses and processing of lysosomal cysteine proteinases in rat macrophages

1988 • 121 citations

Inhibition of bone resorption in culture by inhibitors of thiol proteinases

1980 • 120 citations

Preparation, assay, and partial characterization of a neutral endopeptidase from rabbit brain

1973 • 119 citations

Inhibition of insulin degradation by hepatoma cells after microinjection of monoclonal antibodies to a specific cytosolic protease.

1986 • 118 citations

Isolation of brain endopeptidases: influence of size and sequence of substrates structurally related to bradykinin

1976 • 118 citations

Regulation of activity of calcium activated neutral protease

1988 • 116 citations

Degradation of elastin by a cysteine proteinase from Staphylococcus aureus.

1988 • 116 citations

The Structure of Bovine Proinsulin

1971 • 115 citations

Polypeptide halomethyl ketones bind to serine proteases as analogs of the tetrahedral intermediate. X-ray crystallographic comparison of lysine- and phenylalanine-polypeptide chloromethyl ketone-inhibited subtilisin.

1976 • 115 citations

The Cysteine proteinases

1976 • 115 citations

Characterization of KEX2-encoded endopeptidase from yeast Saccharomyces, cerevisiae

1989 • 114 citations

Hormone processing and membrane-bound proteinases in yeast.

1985 • 114 citations

Amino acid sequence of proteinase K from the mold Tritirachium album Limber

1986 • 114 citations

Cancer procoagulant in human tumor cells: evidence from melanoma patients.

1986 • 113 citations

SECRETION OF ACID HYDROLASES AND ITS INTRACELLULAR SOURCE IN TETRAHYMENA PYRIFORMIS

1972 • 109 citations

A new method to synthesize .ALPHA.-aminoaldehydes.

1975 • 108 citations

DIRECT EVIDENCE FOR AN ACYLATED THIOL AS AN INTERMEDIATE IN PAPAIN- AND FICIN-CATALYSED HYDROLYSES

1965 • 106 citations

Calpain inhibition by peptide epoxides

1985 • 106 citations

ELASTATINAL, A NEW ELASTASE INHIBITOR PRODUCED BY ACTINOMYCETES

1973 • 105 citations

Leishmania mexicana: Amastigote hydrolases in unusual lysosomes

1986 • 105 citations

CRYSTALLINE PAPAIN: NUMBER AND REACTIVITY OF THIOL GROUPS; CHROMATOGRAPHIC BEHAVIOR

1958 • 105 citations

Inhibition of calpain in intact platelets by the thiol protease inhibitor E-64d

1989 • 105 citations

Kinetic specificity in papain-catalysed hydrolyses

1971 • 103 citations

Postproline cleaving enzyme: identification as serine protease using active site specific inhibitors

1977 • 103 citations

Characterization of “thyroliberin-deamidating enzyme” as a post-proline-cleaving enzyme. Partial purification and enzyme-chemical analysis of the enzyme from anterior pituitary tissue.

1979 • 102 citations

Human kidney cathepsins B and L. Characterization and potential role in degradation of glomerular basement membrane

1988 • 102 citations

The Identification of the Histidine Residue at the Active Center of Chymotrypsin

1965 • 102 citations

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

1987 • 101 citations

Inhibitions by E-64 Derivatives of Rat Liver Cathepsin B and Cathepsin L In Vitro and In Vivo 1

1980 • 99 citations

Effects of the proteinase inhibitors leupeptin and E-64 on osteoclastic bone resorption

1988 • 97 citations

CURRENT STATUS OF THE STRUCTURE OF PAPAIN: THE LINEAR SEQUENCE, ACTIVE SULFHYDRYL GROUP, AND THE DISULFIDE BRIDGES

1964 • 96 citations

Papain Inhibitions by Optically Active E-64 Analogs

1981 • 96 citations

Rapid inactivation of cathepsin L by Z-Phe-PheCHN2 and Z-Phe-AlaCHN2

1981 • 95 citations

Degradation products of insulin generated by hepatocytes and by insulin protease.

1988 • 95 citations

Degradation of fructose-1,6-bisphosphate aldolase by cathepsin B

1980 • 95 citations

Plasmodium falciparum: Protease inhibitors and inhibition of erythrocyte invasion

1986 • 95 citations

Effect of proteinase inhibitors on intracellular processing of cathepsin B, H and L in rat macrophages

1988 • 94 citations

The Slow, Tight‐Binding Inhibition of Cathepsin B by Leupeptin

1982 • 93 citations

The Kinetics and Mechanism of Papain-Catalyzed Hydrolyses¹

1966 • 92 citations

Carboxyl-modified amino acids and peptides as protease inhibitors

1986 • 91 citations

Human cathepsin B. Application of the substrate N-benzyloxycarbonyl-<scp>l</scp>-arginyl-<scp>l</scp>-arginine 2-naphthylamide to a study of the inhibition by leupeptin

1980 • 91 citations

Plasminogen activator of islets of Langerhans: modulation by glucose and correlation with insulin production.

1980 • 90 citations

Cathepsin B-related proteases in the insulin secretory granule.

1984 • 89 citations

Amino acid sequences of the human kidney cathepsins H and L

1988 • 87 citations

The identification of active forms of cysteine proteinases in Kirsten-virus-transformed mouse fibroblasts by use of a specific radiolabelled inhibitor

1989 • 86 citations

Structure and synthesis of E-64, a new thiol protease inhibitor.

1978 • 86 citations

Porcine Muscle Prolyl Endopeptidase and Its Endogenous Substrates

1988 • 85 citations

Yeast KEX2 Protease Has the Properties of a Human Proalbumin Converting Enzyme

1987 • 85 citations

Transition-state stabilization at the oxyanion binding sites of serine and thiol proteinases: hydrolyses of thiono and oxygen esters

1983 • 85 citations

Isolation of two forms of the high‐molecular‐mass serine protease, ingensin, from porcine skeletal muscle

1985 • 84 citations

Enzymes that process somatostatin precursors. A novel endoprotease that cleaves before the arginine-lysine doublet is involved in somatostatin-28 convertase activity of rat brain cortex.

1987 • 84 citations

Purification of cathepsin B by a new form of affinity chromatography

1986 • 83 citations

Juvenile and adult metachromatic leukodystrophy: partial restoration of arylsulfatase A (cerebroside sulfatase) activity by inhibitors of thiol proteinases.

1983 • 83 citations

Isolation and Characterization of Leupeptins produced by Actinomycetes

1969 • 83 citations

Thiohemiacetal formation by inhibitory aldehydes at the active site of papain

1977 • 83 citations

Interrelationship of active and latent secreted human cathepsin B precursors

1986 • 82 citations

The synthesis of peptidylfluoromethanes and their properties as inhibitors of serine proteinases and cysteine proteinases

1986 • 80 citations

Identification of three stage-specific proteinases of Plasmodium falciparum.

1987 • 79 citations

Polypeptide 2A of human rhinovirus type 2: Identification as a protease and characterization by mutational analysis

1989 • 78 citations

The inhibition of macrophage protein turnover by a selective inhibitor of thiol proteinases

1980 • 75 citations

A group-specific inhibitor of lysosomal cysteine proteinases selectively inhibits both proteolytic degradation and presentation of the antigen dinitrophenyl-poly-L-lysine by guinea pig accessory cells to T cells.

1986 • 74 citations

Lysosomal and non‐lysosomal peptidyl hydrolases of the bloodstream forms of Trypanosoma brucei brucei

1987 • 74 citations

Transport systems for amphipathic compounds in normal and neoplastic hepatocytes

1988 • 74 citations

Characterization of a thiol proteinase secreted by malignant human breast tumours

1980 • 72 citations

Cathepsin S The cysteine proteinase from bovine lymphoid tissue is distinct from cathepsin L (EC 3.4.22.15)

1986 • 72 citations

Dissociation of ionizing groups in the binding cleft inversely controls the endo- and exopeptidase activities of cathepsin B.

1987 • 72 citations

Purification of rabbit brain endooligopeptidases and preparation of antienzyme antibodies

1981 • 70 citations

Cloning and gene expression of Schistosoma mansoni protease.

1987 • 70 citations

Destruction of Leishmania mexicana amazonensis amastigotes within macrophages by lysosomotropic amino acid esters.

1986 • 70 citations

Species variants of cathepsin L and their immunological identification

1986 • 69 citations

Proteolytic conversion of proinsulin into insulin. Identification of a Ca2+-dependent acidic endopeptidase in isolated insulin-secretory granules

1987 • 69 citations

Post-Proline Cleaving Enzyme from Lamb Brain1

1981 • 69 citations

Antiproteolytic aldehydes and ketones: substituent and secondary deuterium isotope effects on equilibrium addition of water and other nucleophiles

1977 • 68 citations

STRUCTURE OF ANTIPAIN, A NEW SAKAGUGHI-POSITIVE PRODUCT OF STREPTOMYCES

1972 • 67 citations

Brain Endo‐Oligopeptidase A, a Putative Enkephalin Converting Enzyme

1987 • 67 citations

Reversible covalent inhibition of papain by a peptide nitrile. Carbon-13 NMR evidence for a thioimidate ester adduct

1986 • 67 citations

Studies on the Active Site of Clostripain

1971 • 66 citations

A versatile synthesis of peptidyl fluoromethyl ketones

1986 • 66 citations

Proteinase yscE of yeast shows homology with the 20 S cylinder particles of Xenopus laevis

1988 • 66 citations

Active center differences between cathepsins L and B: The S₁ binding region

1988 • 66 citations

Thiazolidine Derivatives as Potent Inhibitors Specific for Pro1yl Endopeptidase1

1988 • 65 citations

Inhibition of Epoxide Derivatives on Chicken Calcium-Activated Neutral Protease (CANP) In Vitro and In Vivo1

1980 • 64 citations

Inhibition of Macromolecular Synthesis in Escherichia coli by Protease Inhibitors

1974 • 64 citations

Cloning and expression of the gene for the major excreted protein of transformed mouse fibroblasts. A secreted lysosomal protease regulated by transformation.

1988 • 64 citations

Collagenase expression and endogenous activation in rabbit synovial fibroblasts stimulated by the calcium ionophore A23187.

1988 • 63 citations

New inhibitors of cysteine proteinases. Peptidyl acyloxymethyl ketones and the quiescent nucleofuge strategy

1988 • 63 citations

Sequential cleavage of proinsulin by human pancreatic kallikrein and a human pancreatic kininase

1979 • 62 citations

Efficient synthetic method for ethyl (+)-(2S,3S)-3-((S)-3-methyl-1-(3-methylbutylcarbamoyl)butylcarbamoyl)-2-oxiranecarboxylate (EST), a new inhibitor of cysteine proteinases.

1987 • 62 citations

Characterization of proline endopeptidase from rat brain

1980 • 61 citations

Structures and Syntheses of Leupeptins Pr-LL and Ac-LL

1969 • 61 citations

Degradation of neurotensin by rabbit brain endo-oligopeptidase A and endo-oligopeptidase B (proline-endopeptidase)

1983 • 61 citations

Thiol protease-specific inhibitor E-64 arrests human epidermoid carcinoma A431 cells at mitotic metaphase.

1988 • 60 citations

Action of cathepsin L on the oxidized B‐chain of bovine insulin

1980 • 60 citations

Active‐site geometry of proteinase K

1986 • 60 citations

Mechanism of inactivation of human leukocyte elastase by a chloromethyl ketone: kinetic and solvent isotope effect studies

1986 • 59 citations

Acid sulphydryl protease from calf lymph nodes

1975 • 59 citations

A cysteine proteinase secreted from human breast tumours is immunologically related to cathepsin B

1982 • 58 citations

Stereospecific Alkylation with Asymmetric Reagents

1968 • 58 citations

Primary structure of streptococcal proteinase. III. Isolation of cyanogen bromide peptides: complete covalent structure of the polypeptide chain.

1976 • 57 citations

Identification of three high molecular mass cysteine proteinases from rat skeletal muscle

1983 • 57 citations

Diazomethyl ketone substrate derivatives as active-site-directed inhibitors of thiol proteases. Papain

1977 • 56 citations

A comparison of the behavior of chymotrypsin and cathepsin B towards peptidyl diazomethyl ketones

1979 • 56 citations

Active and Inactive Forms of the Transition-state Analog Protease Inhibitor Leupeptin: Explanation of the Observed Slow Binding of Leupeptin to Cathepsin B and Papain

1989 • 56 citations

Purification and partial characterization of poliovirus protease 2A by means of a functional assay

1988 • 55 citations

pH dependencies of individual rate constants in papain-catalyzed reactions

1969 • 55 citations

A membrane-bound, calcium-dependent protease in yeast α-cell cleaving on the carboxyl side of paired basic residues

1987 • 55 citations

Inhibitory activities of E-64 derivatives on papain.

1978 • 54 citations

Structure and stereochemistry of tetrahedral inhibitor complexes of papain by direct NMR observation

1983 • 53 citations

Prolyl Endopeptidase: Inhibition In Vivo by N‐Benzyloxycarbonyl‐Prolyl‐Prolinal

1984 • 53 citations

Dynorphin converting enzyme with unusual specificity from rat brain.

1984 • 53 citations

Properties of the single sulfhydryl group of carboxypeptidase Y. Effects of alkyl and aromatic mercurials on activities toward various synthetic substrates.

1979 • 52 citations

Identification of a 31,500 molecular weight islet cell protease as cathepsin B.

1983 • 52 citations

An exploration of the primary specificity site of cathepsin B

1983 • 51 citations

Covalent linkage of 125I-insulin to a cytosolic insulin-degrading enzyme.

1985 • 50 citations

Procalpain is activated on the plasma membrane and the calpain acts on the membrane

1987 • 49 citations

Inhibition of Papain by N‐Acyl‐aminoacetaldehydes and N‐Acyl‐aminopropanones

1977 • 49 citations

Dipeptidylpeptidase Iv - Inactivation with N-Peptidyl-O-Aroyl Hydroxylamines

1988 • 49 citations

Preferential action of rat brain cathepsin B as a peptidyl dipeptidase converting pro-opioid oligopeptides

1986 • 48 citations

Effect of Ca²⁺ on the inhibition of calcium‐activated neutral protease by leupeptin, antipain and epoxysuccinate derivatives

1981 • 47 citations

Mechanism of action of cysteine proteinases: oxyanion binding site is not essential in the hydrolysis of specific substrates

1985 • 47 citations

Evidence for conformational restrictions within the active site of acyl papains which influence the rates of hydrolysis

1970 • 47 citations

The synthesis of lysylfluoromethanes and their properties as inhibitors of trypsin, plasmin and cathepsin B

1987 • 46 citations

Chapter 2 Cysteine proteinases

1987 • 46 citations

Precursors to regulatory peptides: their proteolytic processing

1987 • 46 citations

Inhibition of cathepsin B by peptidyl aldehydes and ketones: slow-binding behavior of a trifluoromethyl ketone

1988 • 45 citations

Effects of chymostatin and other proteinase inhibitors on protein breakdown and proteolytic activities in muscle

1980 • 45 citations

Mode of binding of E‐64‐c, a potent thiol protease inhibitor, to papain as determined by X‐ray crystal analysis of the complex

1989 • 45 citations

Reaction of Ficin with Diisopropylphosphorofluoridate. Evidence for a Contaminating Inhibitor^*

1965 • 44 citations

Purification and characterization of a low molecular weight thiol proteinase from the flagellate protozoon Tritrichomonas foetus.

1979 • 44 citations

Inhibition of papain by nitriles: Mechanistic studies using NMR and kinetic measurements

1987 • 44 citations

Irreversible inhibition of papain by epoxysuccinyl peptides. Carbon-13 NMR characterization of the site of alkylation

1988 • 44 citations

Purification of cysteine proteinases from adult Schistosoma mansoni

1987 • 43 citations

The Amidotransferases

1973 • 43 citations

Action of human liver cathepsin B on the oxidized insulin B chain

1983 • 43 citations

Atrioactivase, a specific peptidase in bovine atria for the processing of pro-atrial natriuretic factor. Purification and characterization.

1988 • 42 citations

Purification and Characterization of Cathepsin B from Monkey Skeletal Muscle1

1984 • 42 citations

Isolation and characterization of an insulin-degrading enzyme from Drosophila melanogaster

1988 • 42 citations

Crystalline Papain

1937 • 41 citations

Inactivation of Calpain I and Calpain II by Specificity-Oriented Tripeptidyl Chloromethyl Ketones1

1986 • 41 citations

Mechanism of the reaction of papain with substrate-derived diazomethyl ketones. Implications for the difference in site specificity of halomethyl ketones for serine proteinases and cysteine proteinases and for stereoelectronic requirements in the papain catalytic mechanism

1978 • 41 citations

Human rhinovirus 3C protease: cloning and expression of an active form in Escherichia coli

1988 • 41 citations

Porcine spleen cathepsin H hydrolyzes oligopeptides solely by aminopeptidase activity.

1988 • 40 citations

Inhibitions of degradation of rat liver aldolase and lactic dehydrogenase by N-[N-(L-3-trans-carboxyoxirane-2-carbonyl)-L-leucyl]agmatine or leupeptin in vivo

1980 • 40 citations

Differences in the chemical and catalytic characteristics of two crystallographically ‘identical’ enzyme catalytic sites. Characterization of actinidin and papain by a combination of pH-dependent substrate catalysis kinetics and reactivity probe studies targeted on the catalytic-site thiol group and its immediate microenvironment

1987 • 40 citations

Carbon-13 NMR study of the ionizations within a trypsin-chloromethyl ketone inhibitor complex

1985 • 39 citations

Reaction of Calcium-Activated Neutral Protease (CANP) with an Epoxysuccinyl Derivative (E64c) and Iodoacetic Acid1

1983 • 39 citations

Chromophoric and fluorophoric peptide substrates cleaved through the dipeptidyl carboxypeptidase activity of cathepsin B

1987 • 38 citations

[62] Inactivation of thiol proteases with peptidyl diazomethyl ketones

1981 • 38 citations

Carbon-13 NMR study of the stereospecificity of the thiohemiacetals formed on inhibition of papain by specific enantiomeric aldehydes

1986 • 38 citations

N‐tosyl‐L‐phenylalanylchloromethane reacts with cysteine 81 in the molecule of elongation factor Tu from Escherichia coli

1982 • 38 citations

Supracrystallographic resolution of interactions contributing to enzyme catalysis by use of natural structural variants and reactivity-probe kinetics

1988 • 38 citations

Reaction of a Specific Tyrosine Residue of Papain with Diisopropylfluorophosphate

1969 • 38 citations

Pyroglutamyl diazomethyl ketone: Potent inhibitor of mammalian pyroglutamyl peptide hydrolase

1985 • 38 citations

Consequences of molecular recognition in the S1-S2 intersubsite region of papain for catalytic-site chemistry. Change in pH-dependence characteristics and generation of an inverse solvent kinetic isotope effect by introduction of a P1-P2 amide bond into a two-protonic-state reactivity probe

1988 • 37 citations

CRYSTALLINE PAPAIN

1937 • 37 citations

Peptidyl O-acyl hydroxamates: Potent new inactivators of cathepsin B

1988 • 36 citations

Selective inhibition of lysosomal protein degradation by the thiol proteinase inhibitors e-64, ep-459 and ep-475 in isolated rat hepatocytes

1982 • 35 citations

The Acyl-enzyme Intermediate, trans-Cinnamoylpapain

1964 • 35 citations

Proteinase inhibitors as antileishmanial agents

1982 • 35 citations

Peptidyl sulfonium salts. A new class of protease inhibitors.

1988 • 35 citations

Substrate-derived two-protonic-state electrophiles as sensitive kinetic specificity probes for cysteine proteinases. Activation of 2-pyridyl disulphides by hydrogen-bonding

1987 • 35 citations

A new subfamily of microbial serine proteinases? Structural similarities of Bacillus thuringiensis and Thermoactinomyces vulgaris extracellular serine proteinases

1981 • 35 citations

Benzoylamidoacetonitrile as an inhibitor of papain

1973 • 35 citations

Benzoylamidoacetonitrile is bound as a thioimidate in the active site of papain.

1986 • 34 citations

Kinin and angiotensin metabolism by purified renal post-proline cleaving enzyme

1987 • 34 citations

Peptide aldehydes inhibiting chymotrypsin

1972 • 34 citations

Inactivation of cathepsin B1 by diazomethyl ketones

1977 • 34 citations

Synthesis of fluorinated α-amino ketones part I: α-benzamidoalkyl mono- di- and trifluoromethyl ketones

1986 • 33 citations

Detection of a tetrahedral adduct in a trypsin-chloromethyl ketone specific inhibitor complex by carbon-13 NMR

1983 • 33 citations

The inhibition of proinsulin-processing endopeptidase activities by active-site-directed peptides

1989 • 33 citations

Mechanism of association of N-acetyl-L-phenylalanylglycinal to papain

1981 • 33 citations

The cysteine proteinase inhibitor, E-64, reduces proteinuria in an experimental model of glomerulonephritis

1988 • 32 citations

Cathepsins J and K: High molecular weight cysteine proteinases from human tissues

1984 • 31 citations

Drosophila insulin degrading enzyme and rat skeletal muscle insulin protease cleave insulin at similar sites

1989 • 31 citations

Synthesis and properties of peptidyl derivatives of arginylfluoromethanes

1988 • 31 citations

Paradoxical effect of leupeptin in vivo on Cathepsin B activity

1983 • 31 citations

Cryoenzymology of proteases: NMR detection of a productive thioacyl derivative of papain at subzero temperatures

1982 • 30 citations

Inhibition of tyrosine protein kinases by halomethyl ketones

1982 • 30 citations

Synthesis and properties of Cbz-Phe-Arg-CHN2 (benzyloxycarbonylphenylalanylarginyldiazomethane) as a proteinase inhibitor

1988 • 30 citations

Insulin proteinase liberates from glucagon a fragment known to have enhanced activity against Ca2+ + Mg2+-dependent ATPase

1988 • 30 citations

Reversible, slow, tight-binding inhibition of human Leukocyte elastase

1987 • 29 citations

Prolongation of life span of dystrophic hamster by cysteine proteinase inhibitor, loxistatin (EST).

1987 • 29 citations

Inhibition of ficin by the chloromethyl ketone derivatives of N-tosyl-L-lysine and N-tosyl-L-phenylalanine

1967 • 28 citations

Inactivation of cathepsin B by active site-directed disulfide exchange. Application in covalent affinity chromatography.

1983 • 27 citations

Ficin- and papain-catalyzed reactions. Changes in reactivity of the essential sulfhydryl group in the presence of substrates and competitive inhibitors

1969 • 27 citations

5-Oxoprolinal: transition-state aldehyde inhibitor of pyroglutamyl-peptide hydrolase

1985 • 26 citations

Cysteine proteases: The S₂P₂ hydrogen bond is more important for catalysis than is the analogous S₁P₁ bond

1988 • 25 citations

Evidence for hemiketals as intermediates in the inactivation of serine proteinases with halomethyl ketones

1986 • 25 citations

Identification of cell surface cathepsin B-like activity on murine melanomas and fibrosarcomas: modulation by butanol extraction.

1988 • 24 citations

SYNTHETIC STUDIES ON LEUPEPTINS AND THEIR ANALOGS

1972 • 24 citations

Synthesis of a tripeptide with a C‐terminal nitrile moiety and the inhibition of proteinases

1988 • 23 citations

Conversion and inactivation of opioid peptides by rabbit brain endo-oligopeptidase a

1985 • 22 citations

Neuropeptide processing by single-step cleavage: Conversion of leumorphin (dynorphin B-29) to dynorphin B

1985 • 22 citations

[64] Affinity methods using argininal derivatives

1981 • 22 citations

Interaction of clostripain with natural trypsin inhibitors and its affinity labeling by N^α‐p‐nitrobenzyloxycarbonyl arginine chlormethyl ketone

1976 • 22 citations

Detection and characterization of a selective endopeptidase from Plasmodium berghei by using fluorogenic peptidyl substrates

1984 • 22 citations

Purification and characterization of hemoglobin-hydrolyzing acidic thiol protease induced by leupeptin in rat liver.

1984 • 21 citations

Some characteristics of hormone (pheromone) processing enzymes in yeast

1987 • 21 citations

Purification and characterization of a rat liver cytosol neutral thiol peptidase that degrades glucagon, insulin, and isolated insulin A and B chains

1985 • 21 citations

Specific inhibition of post proline cleaving enzyme by benzyloxycarbonyl-gly-pro-diazomethyl ketone

1986 • 21 citations

Cancer cells and parasites: two of a kind

1986 • 20 citations

Protease-inhibitory activities of leupeptin analogues.

1988 • 20 citations

Synthetic analogues of the proteinase inhibitor: chymostatin

1984 • 20 citations

Several murine metastasizing tumors possess a cysteine proteinase with cancer procoagulant characteristics

1987 • 19 citations

Heterogeneity in late-onset metachromatic leukodystrophy. Effect of inhibitors of cysteine proteinases.

1986 • 19 citations

Stereochemistry of Substrate Binding and Hydrolysis in the Trypsin Family of Enzymes

1974 • 19 citations

Evidence for an active‐center cysteine in the SH‐proteinase α‐clostripain through use of N‐tosyl‐L‐lysine chloromethyl ketone

1984 • 18 citations

Primary structure of alpha-clostripain light chain

1984 • 18 citations

The thiol proteinase inhibitors, Z-Phe-PheCHN2 and Z-Phe-AlaCHN2, inhibit lysosomal protein degradation in isolated rat hepatocytes

1983 • 18 citations

Specificity of a cysteine proteinase of Entamoeba histolytica towards the α1-CB2 peptide of bovine collagen type I

1987 • 17 citations

Synthesis of Leupeptins and Inhibition of Proteinases. I. Inhibition of Acrosin and Trypsin

1981 • 17 citations

Thionesters as a probe for electrophilic catalysis in the serine protease mechanism.

1983 • 17 citations

Inhibition with NCO-700, a protease inhibitor, of degradation of cardiac myofibrillar proteins during ischemia in dogs

1985 • 17 citations

A prolyl endopeptidase from murine macrophages, its assay and specific inactivation

1983 • 17 citations

Stereospecific synthesis of α-aminoacyl aldehydes and their interaction with α-chymotrypsin

1979 • 17 citations

Transition-state affinity chromatography of trypsin-like proteinases with dipeptidyl argininal ligands

1983 • 17 citations

An insulin epidermal growth factor-binding protein from Drosophila has insulin-degrading activity.

1989 • 17 citations

Inhibition of hepatic protein degradation by synthetic analogues of chymostatin.

1983 • 16 citations

Synthesis of fluorescent peptidyl thioneamides and the assay of papain in the presence of trypsin

1987 • 16 citations

The properties of peptidyl diazoethanes and chloroethanes as protease inactivators

1989 • 16 citations

Iodination of peptidyl chloromethyl ketones for protease affinity labels

1988 • 16 citations

N-α-carbobenzoxy pyroglutamyl diazomethyl ketone as active-site-directed inhibitor for pyroglutamyl peptidase

1982 • 15 citations

Induction of hemoglobin-hydrolase activity by the thiol-protease inhibitors leupeptin and antipain in adult rat liver cells in primary culture

1979 • 15 citations

Characterization of Cysteine Proteases Functioning in Degradation of Dynorphin in Neuroblastoma Cells: Evidence for the Presence of a Novel Enzyme with Strict Specificity Toward Paired Basic Residues

1989 • 14 citations

Synthesis of lysine-containing sulphonium salts and their properties as proteinase inhibitors

1988 • 14 citations

Study on thiol protease inhibitors. Part IV. Relationship between structure and papain inhibitory activity of epoxysuccinyl amino acid derivatives.

1981 • 14 citations

Influence of a calcium dependent protease inhibitor on platelet activation and secretion

1987 • 14 citations

Inactivation of Pyroglutamyl Aminopeptidase by Na-Carbobenzoxy-L-Pyroglutamyl Chloromethyl Ketone

1981 • 13 citations

Plasmodium berghei and Plasmodium chabaudi: A neutral endopeptidase in parasite extracts and plasma of infected animals

1987 • 13 citations

An Alternate Synthesis of Leupeptins and Their Analogs

1973 • 12 citations

Binding of monoclonal antibody to cathepsin M located on the external surface of rabbit lysosomes

1984 • 12 citations

Conformation of ethyl (+)-(2S,3S)-3-{1-[N-(3-methylbutyl)amino]leucylcarbonyl}oxi-rane-2-carboxylate (loxistatin), a cysteine protease inhibitor: X-ray crystallographic and 1H nuclear magnetic resonance studies

1988 • 12 citations

Detection of enzyme-bound intermediates by cross-saturation in nuclear magnetic resonance spectroscopy; an investigation of the papain–N-benzoylaminoacetaldehyde complex

1977 • 11 citations

A Proton‐Magnetic‐Resonance Study of N‐Trifluoroacetyl‐<scp>l</scp>‐alanyl‐<scp>l</scp>‐phenylalaninal Binding to α‐Chymotrypsin

1980 • 11 citations

Procoagulant activity of mouse and human cultured cells following various types of transformation

1985 • 10 citations

The synthesis and properties of peptidylmethylsulphonium salts with two cationic residues as potential inhibitors of prohormone processing

1988 • 8 citations

Comparison of the substrate conformations in the active sites of papain, chymopapain, ficin and bromelain by resonance Raman spectroscopy

1983 • 8 citations

Conformational variability in an enzyme's active site: resonance Raman evidence for different acyl group conformations in N-acylglycine and N-acylalanine dithioacyl papains

1988 • 8 citations

Degradation of dynorphin-(1–13) and dynorphin-(1–17) by the neuroblastoma cell membrane. Evidence for the involvement of a cysteine protease

1986 • 7 citations

The effect of L‐1‐tosylamido‐2‐phenylethyl chloromethyl ketone on the activity of procaryote and eucaryote tRNA binding factors

1974 • 7 citations

Relation between in vivo effects and in vitro effects of serine and thiol proteinase inhibitors.

1983 • 7 citations

The effect of pepstatin A, an inhibitor of the pro‐opiomelanocortin (POMC)‐converting enzyme, on POMC processing in mouse intermediate pituitary

1988 • 6 citations

Mechanism of action of papain: aryldehydroalanines as spectroscopic probes of acyl enzyme formation

1978 • 6 citations

Purification and properties of rabbit liver cathepsin M and cathepsin B

1985 • 5 citations

Post-proline endopeptidase, further characterization of the enzyme from pig kidneys

1984 • 4 citations