Extended peptide-based inhibitors efficiently target the proteasome and reveal overlapping specificities of the catalytic beta-subunits.

PubWeight™: 1.52‹?› | Rank: Top 4%

🔗 View Article (PMID 11564559)

Published in Chem Biol on September 01, 2001

Authors

B M Kessler1, D Tortorella, M Altun, A F Kisselev, E Fiebiger, B G Hekking, H L Ploegh, H S Overkleeft

Author Affiliations

1: Department of Pathology, Harvard Medical School, Boston, MA 02115, USA.

Articles citing this

Proteasome inhibitors disrupt the unfolded protein response in myeloma cells. Proc Natl Acad Sci U S A (2003) 4.47

A photoreactive small-molecule probe for 2-oxoglutarate oxygenases. Chem Biol (2011) 1.58

Dissection of the dislocation pathway for type I membrane proteins with a new small molecule inhibitor, eeyarestatin. Mol Biol Cell (2004) 1.44

The 26S proteasome complex: an attractive target for cancer therapy. Biochim Biophys Acta (2011) 1.36

Muscle wasting in aged, sarcopenic rats is associated with enhanced activity of the ubiquitin proteasome pathway. J Biol Chem (2010) 1.28

Comprehensive study of proteasome inhibitors against Plasmodium falciparum laboratory strains and field isolates from Gabon. Malar J (2008) 1.27

Activity-based probes as a tool for functional proteomic analysis of proteases. Expert Rev Proteomics (2008) 1.26

A novel proteasome inhibitor NPI-0052 as an anticancer therapy. Br J Cancer (2006) 1.25

Antigen processing by nardilysin and thimet oligopeptidase generates cytotoxic T cell epitopes. Nat Immunol (2010) 1.24

Proteasome inhibition decreases cardiac remodeling after initiation of pressure overload. Am J Physiol Heart Circ Physiol (2008) 1.23

Proteasome inhibition suppresses essential immune functions of human CD4+ T cells. Immunology (2008) 1.14

Specific cell-permeable inhibitor of proteasome trypsin-like sites selectively sensitizes myeloma cells to bortezomib and carfilzomib. Chem Biol (2011) 1.13

Activity-based profiling reveals reactivity of the murine thymoproteasome-specific subunit beta5t. Chem Biol (2010) 1.01

Relative quantification of proteasome activity by activity-based protein profiling and LC-MS/MS. Nat Protoc (2013) 0.96

Effects of proteasome inhibitors MG132, ZL3VS and AdaAhx3L3VS on protein metabolism in septic rats. Int J Exp Pathol (2004) 0.95

Simultaneous fluorescent monitoring of proteasomal subunit catalysis. J Am Chem Soc (2010) 0.92

Tumors acquire inhibitor of apoptosis protein (IAP)-mediated apoptosis resistance through altered specificity of cytosolic proteolysis. J Exp Med (2003) 0.91

α,β-Unsaturated carbonyl system of chalcone-based derivatives is responsible for broad inhibition of proteasomal activity and preferential killing of human papilloma virus (HPV) positive cervical cancer cells. J Med Chem (2010) 0.88

The ubiquitin-proteasome system as a drug target in cerebrovascular disease: therapeutic potential of proteasome inhibitors. Curr Opin Investig Drugs (2005) 0.86

Management of post-chemotherapy extra-retroperitoneal residual masses. World J Urol (2009) 0.86

Cryo-EM reveals the conformation of a substrate analogue in the human 20S proteasome core. Nat Commun (2015) 0.86

Bortezomib Amplifies Effect on Intracellular Proteasomes by Changing Proteasome Structure. EBioMedicine (2015) 0.85

PI 3 kinase related kinases-independent proteolysis of BRCA1 regulates Rad51 recruitment during genotoxic stress in human cells. PLoS One (2010) 0.84

A cytosolic protein factor from the naked mole-rat activates proteasomes of other species and protects these from inhibition. Biochim Biophys Acta (2014) 0.84

Trypanocidal activities of trileucine methyl vinyl sulfone proteasome inhibitors. Parasitol Res (2004) 0.83

The African swine fever virus nonstructural protein pB602L is required for formation of the icosahedral capsid of the virus particle. J Virol (2006) 0.82

Ca2+ homeostasis regulates Xenopus oocyte maturation. Biol Reprod (2007) 0.81

Proteasome dysfunction induces muscle growth defects and protein aggregation. J Cell Sci (2014) 0.79

Activity-based imaging probes of the proteasome. Cell Biochem Biophys (2013) 0.79

Broad-spectrum antimalarial activity of peptido sulfonyl fluorides, a new class of proteasome inhibitors. Antimicrob Agents Chemother (2013) 0.78

Live-cell imaging of ubiquitin-proteasome system function. Methods Mol Biol (2012) 0.78

Mining the Active Proteome of Arabidopsis thaliana. Front Plant Sci (2011) 0.77

Synthesis of Lithocholic Acid Derivatives as Proteasome Regulators. ACS Med Chem Lett (2012) 0.77

Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells. Int J Pept Res Ther (2006) 0.77

Harnessing proteasome dynamics and allostery in drug design. Antioxid Redox Signal (2014) 0.75

High-resolution cryo-EM proteasome structures in drug development. Acta Crystallogr D Struct Biol (2017) 0.75

Articles by these authors

The human cytomegalovirus US11 gene product dislocates MHC class I heavy chains from the endoplasmic reticulum to the cytosol. Cell (1996) 8.25

Sec61-mediated transfer of a membrane protein from the endoplasmic reticulum to the proteasome for destruction. Nature (1996) 7.90

Segregation of MHC class II molecules from MHC class I molecules in the Golgi complex for transport to lysosomal compartments. Nature (1991) 5.90

Major histocompatibility antigens: the human (HLA-A, -B, -C) and murine (H-2K, H-2D) class I molecules. Cell (1981) 5.81

Viral subversion of the immune system. Annu Rev Immunol (2000) 5.76

TAP1 mutant mice are deficient in antigen presentation, surface class I molecules, and CD4-8+ T cells. Cell (1992) 4.76

Monoclonal antibodies raised against denatured HLA-B locus heavy chains permit biochemical characterization of certain HLA-C locus products. J Immunol (1986) 4.30

The biosynthetic pathway of MHC class II but not class I molecules intersects the endocytic route. Cell (1990) 4.18

Isolation and characterization of the intracellular MHC class II compartment. Nature (1994) 3.50

Direct binding of peptide to empty MHC class I molecules on intact cells and in vitro. Cell (1990) 3.44

A novel active site-directed probe specific for deubiquitylating enzymes reveals proteasome association of USP14. EMBO J (2001) 3.42

Uvomorulin: a nonintegral membrane protein of early mouse embryo. Proc Natl Acad Sci U S A (1983) 3.42

Cell-free translation of the mRNAs for the heavy and light chains of HLA-A and HLA-B antigens. Proc Natl Acad Sci U S A (1979) 3.29

Human cytomegalovirus US3 impairs transport and maturation of major histocompatibility complex class I heavy chains. Proc Natl Acad Sci U S A (1996) 3.17

The human beta 2-microglobulin gene. Primary structure and definition of the transcriptional unit. J Immunol (1987) 3.09

Cathepsin S required for normal MHC class II peptide loading and germinal center development. Immunity (1999) 3.01

Molecular cloning of a human histocompatibility antigen cDNA fragment. Proc Natl Acad Sci U S A (1980) 2.99

Essential role for cathepsin S in MHC class II-associated invariant chain processing and peptide loading. Immunity (1996) 2.93

The ER-luminal domain of the HCMV glycoprotein US6 inhibits peptide translocation by TAP. Immunity (1997) 2.93

Covalent modification of the active site threonine of proteasomal beta subunits and the Escherichia coli homolog HslV by a new class of inhibitors. Proc Natl Acad Sci U S A (1997) 2.81

Cathepsins B and D are dispensable for major histocompatibility complex class II-mediated antigen presentation. Proc Natl Acad Sci U S A (1998) 2.75

Interference with HIV-induced syncytium formation and viral infectivity by inhibitors of trimming glucosidase. Nature (1987) 2.72

TAP1-dependent peptide translocation in vitro is ATP dependent and peptide selective. Cell (1993) 2.43

Human cytomegalovirus down-regulates HLA class I expression by reducing the stability of class I H chains. J Immunol (1993) 2.40

The WD-40 repeat. FEBS Lett (1992) 2.37

Stable binding of the herpes simplex virus ICP47 protein to the peptide binding site of TAP. EMBO J (1996) 2.26

Secreted cathepsin L generates endostatin from collagen XVIII. EMBO J (2000) 2.24

How MHC class II molecules acquire peptide cargo: biosynthesis and trafficking through the endocytic pathway. Annu Rev Cell Dev Biol (1995) 2.24

The alpha chain of the T cell antigen receptor is degraded in the cytosol. Immunity (1997) 2.20

Dislocation of type I membrane proteins from the ER to the cytosol is sensitive to changes in redox potential. J Cell Biol (1998) 2.16

HLA-A- and HLA-B-specific monoclonal antibodies reactive with free heavy chains in western blots, in formalin-fixed, paraffin-embedded tissue sections and in cryo-immuno-electron microscopy. Int Immunol (1990) 2.12

26S proteasomes and immunoproteasomes produce mainly N-extended versions of an antigenic peptide. EMBO J (2001) 2.09

Allele and locus-specific differences in cell surface expression and the association of HLA class I heavy chain with beta 2-microglobulin: differential effects of inhibition of glycosylation on class I subunit association. Eur J Immunol (1988) 2.03

Peptide selection by MHC class I molecules. Nature (1991) 2.01

A mouse cytomegalovirus glycoprotein, gp34, forms a complex with folded class I MHC molecules in the ER which is not retained but is transported to the cell surface. EMBO J (1997) 1.98

Peptide contributes to the specificity of positive selection of CD8+ T cells in the thymus. Cell (1993) 1.96

Comparison of amino acid sequences of two human histocompatibility antigens, HLA-A2 and HLA-B7: location of putative alloantigenic sites. Proc Natl Acad Sci U S A (1979) 1.94

Biosynthesis and cell surface localization of nonglycosylated human histocompatibility antigens. J Immunol (1981) 1.91

Expression of functional high affinity immunoglobulin E receptors (Fc epsilon RI) on monocytes of atopic individuals. J Exp Med (1994) 1.85

How MHC class II molecules reach the endocytic pathway. EMBO J (1995) 1.80

Major histocompatibility class I presentation of soluble antigen facilitated by Mycobacterium tuberculosis infection. Proc Natl Acad Sci U S A (1996) 1.76

Cathepsin S activity regulates antigen presentation and immunity. J Clin Invest (1998) 1.76

A proteolytic system that compensates for loss of proteasome function. Nature (1998) 1.76

The pathway of US11-dependent degradation of MHC class I heavy chains involves a ubiquitin-conjugated intermediate. J Cell Biol (1999) 1.74

Peptide length and sequence specificity of the mouse TAP1/TAP2 translocator. J Exp Med (1994) 1.73

Inhibition of endosomal proteolytic activity by leupeptin blocks surface expression of MHC class II molecules and their conversion to SDS resistance alpha beta heterodimers in endosomes. EMBO J (1992) 1.72

Peptide translocation by variants of the transporter associated with antigen processing. Science (1993) 1.71

Polyubiquitination is required for US11-dependent movement of MHC class I heavy chain from endoplasmic reticulum into cytosol. Mol Biol Cell (2001) 1.69

Loss of transporter protein, encoded by the TAP-1 gene, is highly correlated with loss of HLA expression in cervical carcinomas. J Exp Med (1994) 1.69

An improved biochemical method for the analysis of HLA-class I antigens. Definition of new HLA-class I subtypes. Hum Immunol (1986) 1.67

First evidence of a possible association between gastric acid suppression during pregnancy and childhood asthma: a population-based register study. Clin Exp Allergy (2008) 1.66

Antigen presentation subverted: Structure of the human cytomegalovirus protein US2 bound to the class I molecule HLA-A2. Proc Natl Acad Sci U S A (2001) 1.60

Human leukocyte activation antigen M6, a member of the Ig superfamily, is the species homologue of rat OX-47, mouse basigin, and chicken HT7 molecule. J Immunol (1992) 1.59

The high affinity IgE receptor (Fc epsilon RI) mediates IgE-dependent allergen presentation. J Immunol (1995) 1.59

A myristoylated pseudosubstrate peptide, a novel protein kinase C inhibitor. J Biol Chem (1993) 1.58

Cathepsin S controls the trafficking and maturation of MHC class II molecules in dendritic cells. J Cell Biol (1999) 1.58

Major histocompatibility complex class II compartments in human B lymphoblastoid cells are distinct from early endosomes. J Exp Med (1995) 1.57

Use of HLA loss mutants to analyse the structure of the human major histocompatibility complex. Nature (1982) 1.56

Proteases involved in MHC class II antigen presentation. Immunol Rev (1999) 1.54

Processive degradation of proteins and other catalytic properties of the proteasome from Thermoplasma acidophilum. J Biol Chem (1997) 1.52

The HCMV gene products US11 and US2 differ in their ability to attack allelic forms of murine major histocompatibility complex (MHC) class I heavy chains. J Exp Med (1997) 1.51

Substrate binding and sequence preference of the proteasome revealed by active-site-directed affinity probes. Chem Biol (1998) 1.51

Peptide loading of empty major histocompatibility complex molecules on RMA-S cells allows the induction of primary cytotoxic T lymphocyte responses. Eur J Immunol (1991) 1.51

Role for cathepsin F in invariant chain processing and major histocompatibility complex class II peptide loading by macrophages. J Exp Med (2000) 1.49

Peptide antagonism and T cell receptor interactions with peptide-MHC complexes. Immunity (1998) 1.46

Purification, cDNA-cloning and expression of human diacylglycerol kinase. FEBS Lett (1990) 1.45

In vitro translation and assembly of a complete T cell receptor-CD3 complex. J Exp Med (1997) 1.45

Isolation, expression, and the primary structure of HLA-Cw1 and HLA-Cw2 genes: evolutionary aspects. Immunogenetics (1987) 1.41

Characterization of the ubiquitin-proteasome system in bortezomib-adapted cells. Leukemia (2009) 1.40

Cell-free synthesis and processing of the heavy and light chains of HLA-DR antigens. J Exp Med (1980) 1.39

Release of signal peptide fragments into the cytosol requires cleavage in the transmembrane region by a protease activity that is specifically blocked by a novel cysteine protease inhibitor. J Biol Chem (2000) 1.38

Peptide influences the folding and intracellular transport of free major histocompatibility complex class I heavy chains. J Exp Med (1995) 1.38

The active site of ICP47, a herpes simplex virus-encoded inhibitor of the major histocompatibility complex (MHC)-encoded peptide transporter associated with antigen processing (TAP), maps to the NH2-terminal 35 residues. J Exp Med (1997) 1.37

Assembly of HLA DR1 molecules translated in vitro: binding of peptide in the endoplasmic reticulum precludes association with invariant chain. EMBO J (1994) 1.37

The cytosolic tail of class I MHC heavy chain is required for its dislocation by the human cytomegalovirus US2 and US11 gene products. Proc Natl Acad Sci U S A (1999) 1.35

N-linked glycan modification on antigen-presenting cells restores an allospecific cytotoxic T cell response. J Exp Med (1990) 1.34

Mapping functional regions in the lumenal domain of the class II-associated invariant chain. J Exp Med (1994) 1.32

Proteolysis in MHC class II antigen presentation: who's in charge? Immunity (2000) 1.32

Nasopharyngeal cancer: epidemiology, staging, and treatment. Semin Oncol (1994) 1.31

Mechanisms of induction of primary virus-specific cytotoxic T lymphocyte responses. Eur J Immunol (1992) 1.30

Why certain antibodies cross-react with HLA-A and HLA-G: epitope mapping of two common MHC class I reagents. Mol Immunol (1998) 1.29

Altered natural killer cell repertoire in Tap-1 mutant mice. Proc Natl Acad Sci U S A (1994) 1.28

Cytomegaloviruses use multiple mechanisms to elude the host immune response. Immunol Lett (1997) 1.28

Degradation of mouse invariant chain: roles of cathepsins S and D and the influence of major histocompatibility complex polymorphism. J Exp Med (1997) 1.25

Involvement of the vacuolar H(+)-ATPases in the secretory pathway of HepG2 cells. J Biol Chem (1993) 1.25

Intracellular transport of MHC class II molecules. Immunol Today (1992) 1.24

Trophoblast class I major histocompatibility complex (MHC) products are resistant to rapid degradation imposed by the human cytomegalovirus (HCMV) gene products US2 and US11. J Exp Med (1998) 1.24

Intracellular targeting of the proteasome. Trends Cell Biol (2000) 1.24

Signal peptide cleavage of a type I membrane protein, HCMV US11, is dependent on its membrane anchor. EMBO J (2001) 1.24

Misfolded major histocompatibility complex class I molecules accumulate in an expanded ER-Golgi intermediate compartment. J Cell Biol (1995) 1.24

Differential effects of Usp14 and Uch-L1 on the ubiquitin proteasome system and synaptic activity. Mol Cell Neurosci (2008) 1.22

The eS-Sence of -SH in the ER. Cell (1998) 1.22

Peptide-induced stabilization and intracellular localization of empty HLA class I complexes. J Exp Med (1992) 1.22

Human cytomegalovirus US2 endoplasmic reticulum-lumenal domain dictates association with major histocompatibility complex class I in a locus-specific manner. J Virol (2001) 1.21