Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide α', β'-epoxyketones

Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules

1994 • 2,480 citations

Solid phase peptide synthesis utilizing 9‐fluorenylmethoxycarbonyl amino acids

1990 • 2,426 citations

Structure of 20S proteasome from yeast at 2.4Å resolution

1997 • 2,211 citations

The ubiquitinproteasome pathway is required for processing the NF-κB1 precursor protein and the activation of NF-κB

1994 • 2,124 citations

Inhibition of Proteasome Activities and Subunit-Specific Amino-Terminal Threonine Modification by Lactacystin

1995 • 1,601 citations

Crystal Structure of the 20 S Proteasome from the Archaeon T. acidophilum at 3.4 Å Resolution

1995 • 1,513 citations

Proteasome inhibitors: valuable new tools for cell biologists

1998 • 1,453 citations

1-Hydroxy-7-azabenzotriazole. An efficient peptide coupling additive

1993 • 1,416 citations

How Proteolysis Drives the Cell Cycle

1996 • 1,277 citations

Epoxomicin, a potent and selective proteasome inhibitor, exhibitsin vivoantiinflammatory activity

1999 • 914 citations

The Behavior and Significance of Slow‐Binding Enzyme Inhibitors

1988 • 828 citations

Potent and selective inhibitors of the proteasome: Dipeptidyl boronic acids

1998 • 674 citations

Vinyl Sulfones as Mechanism-Based Cysteine Protease Inhibitors

1995 • 496 citations

Covalent modification of the active site threonine of proteasomal β subunits and theEscherichia colihomolog HslV by a new class of inhibitors

1997 • 441 citations

Lactacystin and clasto-Lactacystin β-Lactone Modify Multiple Proteasome β-Subunits and Inhibit Intracellular Protein Degradation and Major Histocompatibility Complex Class I Antigen Presentation

1997 • 388 citations

A Giant Protease with Potential to Substitute for Some Functions of the Proteasome

1999 • 377 citations

Evidence for the presence of five distinct proteolytic components in the pituitary multicatalytic proteinase complex. Properties of two components cleaving bonds on the carboxyl side of branched chain and small neutral amino acids

1993 • 323 citations

The MHC class I ligand‐generating system: roles of immunoproteasomes and the interferon‐4gMY‐inducible proteasome activator PA28

1998 • 288 citations

Cytotoxicity Is Mandatory for CD8+ T Cell–mediated Contact Hypersensitivity

1999 • 258 citations

Structural Features of the 26 S Proteasome Complex

1993 • 255 citations

The ubiquitin-proteasome pathway in cancer

1998 • 223 citations

Racemization studies during solid-phase peptide synthesis using azabenzotriazole-based coupling reagents

1994 • 204 citations

Epoxomicin, a new antitumor agent of microbial origin.

1992 • 202 citations

Total synthesis of the-potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology

1999 • 200 citations

A New Inhibitor of the Chymotrypsin‐Like Activity of the Multicatalytic Proteinase Complex (20S Proteasome) Induces Accumulation of Ubiquitin‐Protein Conjugates in a Neuronal Cell

1994 • 183 citations

Substrate binding and sequence preference of the proteasome revealed by active-site-directed affinity probes

1998 • 179 citations

PA28 Activator Protein Forms Regulatory Caps on Proteasome Stacked Rings

1994 • 167 citations

Proteasomes: Structure and Biology

1998 • 158 citations

Eponemycin exerts its antitumor effect through the inhibition of proteasome function.

1999 • 158 citations

Dissection of antigenic and irritative effects of epicutaneously applied haptens in mice. Evidence that not the antigenic component but nonspecific proinflammatory effects of haptens determine the concentration-dependent elicitation of allergic contact dermatitis.

1996 • 155 citations

New insights into the mechanisms and importance of the proteasome in intracellular protein degradation.

1997 • 140 citations

Chemical genetics: exploring and controlling cellular processes with chemical probes

1999 • 118 citations

Lactacystin, a Specific Inhibitor of the Proteasome, Inhibits Human Platelet Lysosomal Cathepsin A-like Enzyme

1997 • 116 citations

The high molecular weight multicatalytic proteinase, macropain, exists in a latent form in human erythrocytes

1989 • 115 citations

The ubiquitin-mediated proteolytic pathway as a therapeutic area

1997 • 113 citations

Purification and characterization of a high molecular weight proteinase (macropain) from human erythrocytes

1986 • 107 citations

Bivalency as a principle for proteasome inhibition

1999 • 102 citations

Eponemycin, a new antibiotic active against B16 melanoma. I. Production, isolation, structure and biological activity.

1990 • 98 citations

Bifunctional inhibitors of the trypsin-like activity of eukaryotic proteasomes

1999 • 69 citations

Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl α-keto aldehydes (glyoxals)

1998 • 66 citations

Eponemycin analogues: syntheses and use as probes of angiogenesis

1998 • 63 citations

Active Site-directed Inhibitors of Rhodococcus 20 S Proteasome

1997 • 61 citations

Design and synthesis of novel protease inhibitors. Tripeptide α′,β′-epoxyketones as nanomolar inactivators of the proteasome

1996 • 50 citations

Design and synthesis of dipeptidyl α′,β′-epoxy ketones, potent irreversible inhibitors of the cysteine protease cruzain

1998 • 36 citations

ChemInform Abstract: Design and Synthesis of Novel Protease Inhibitors. Tripeptide α′, β′‐Epoxyketones as Nanomolar Inactivators of the Proteasome.

1996 • 13 citations