Proteasome Inhibitors: Recent Progress and Future Directions

[1]  D. Filippov,et al.  Acetylene functionalized BODIPY dyes and their application in the synthesis of activity based proteasome probes. , 2007, Bioorganic & medicinal chemistry letters.

[2]  H. Ovaa,et al.  Profiling proteasome activity in tissue with fluorescent probes. , 2007, Molecular pharmaceutics.

[3]  S. Demo,et al.  Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. , 2007, Cancer research.

[4]  H. Overkleeft,et al.  A cell-permeable inhibitor and activity-based probe for the caspase-like activity of the proteasome. , 2007, Bioorganic & medicinal chemistry letters.

[5]  K. Kim,et al.  LMP2-specific inhibitors: chemical genetic tools for proteasome biology. , 2007, Chemistry & biology.

[6]  W. Koltun,et al.  Enhanced Intestinal Expression of the Proteasome Subunit Low Molecular Mass Polypeptide 2 in Patients with Inflammatory Bowel Disease , 2007, Diseases of the colon and rectum.

[7]  M. Groll,et al.  20S proteasome and its inhibitors: crystallographic knowledge for drug development. , 2007, Chemical reviews.

[8]  M. Bogyo,et al.  Tagging and detection strategies for activity-based proteomics. , 2007, Current opinion in chemical biology.

[9]  Guoqing Shi,et al.  The Tumor Proteasome Is a Primary Target for the Natural Anticancer Compound Withaferin A Isolated from “Indian Winter Cherry” , 2007, Molecular Pharmacology.

[10]  D. Filippov,et al.  A fluorescent broad-spectrum proteasome inhibitor for labeling proteasomes in vitro and in vivo. , 2006, Chemistry & biology.

[11]  T. Hunter,et al.  Proteasome inhibitor drugs on the rise. , 2006, Cancer research.

[12]  W. Koltun,et al.  Dextran Sulfate Sodium-Induced Colitis Is Associated with Enhanced Low Molecular Mass Polypeptide 2 (LMP2) Expression and Is Attenuated in LMP2 Knockout Mice , 2006, Digestive Diseases and Sciences.

[13]  D. McConkey,et al.  The proteasome inhibitor NPI-0052 is a more effective inducer of apoptosis than bortezomib in lymphocytes from patients with chronic lymphocytic leukemia , 2006, Molecular Cancer Therapeutics.

[14]  Di Chen,et al.  Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. , 2006, Cancer research.

[15]  R. Huber,et al.  Crystal structures of Salinosporamide A (NPI-0052) and B (NPI-0047) in complex with the 20S proteasome reveal important consequences of beta-lactone ring opening and a mechanism for irreversible binding. , 2006, Journal of the American Chemical Society.

[16]  C. Xia,et al.  INVESTIGATION OF DRUG-DRUG INTERACTION POTENTIAL OF BORTEZOMIB IN VIVO IN FEMALE SPRAGUE-DAWLEY RATS AND IN VITRO IN HUMAN LIVER MICROSOMES , 2006, Drug Metabolism and Disposition.

[17]  A. Goldberg,et al.  Importance of the Different Proteolytic Sites of the Proteasome and the Efficacy of Inhibitors Varies with the Protein Substrate* , 2006, Journal of Biological Chemistry.

[18]  D. Soejarto,et al.  Biodiversity as a source of anticancer drugs. , 2006, Current drug targets.

[19]  Kinneret Keren,et al.  Dynamic imaging of protease activity with fluorescently quenched activity-based probes , 2005, Nature chemical biology.

[20]  J. Yewdell,et al.  Immunoproteasomes: regulating the regulator. , 2005, Proceedings of the National Academy of Sciences of the United States of America.

[21]  Di Chen,et al.  Dietary flavonoids as proteasome inhibitors and apoptosis inducers in human leukemia cells. , 2005, Biochemical pharmacology.

[22]  K. Anderson,et al.  Activity probe for in vivo profiling of the specificity of proteasome inhibitor bortezomib , 2005, Nature Methods.

[23]  N. Munshi,et al.  Targeting mitochondria to overcome conventional and bortezomib/proteasome inhibitor PS-341 resistance in multiple myeloma (MM) cells. , 2004, Blood.

[24]  Di Chen,et al.  Green tea and tea polyphenols in cancer prevention. , 2004, Frontiers in bioscience : a journal and virtual library.

[25]  K. Daniel,et al.  Inhibition of the proteasome activity, a novel mechanism associated with the tumor cell apoptosis-inducing ability of genistein. , 2003, Biochemical pharmacology.

[26]  T. Mincer,et al.  Salinosporamide A: a highly cytotoxic proteasome inhibitor from a novel microbial source, a marine bacterium of the new genus salinospora. , 2003, Angewandte Chemie.

[27]  J. Adams.  Development of the proteasome inhibitor PS-341. , 2002, The oncologist.

[28]  H. Naganawa,et al.  Isolation and structural determination of phepropeptins A, B, C, and D, new proteasome inhibitors, produced by Streptomyces sp. , 2001, The Journal of antibiotics.

[29]  H. Ploegh,et al.  Extended peptide-based inhibitors efficiently target the proteasome and reveal overlapping specificities of the catalytic beta-subunits. , 2001, Chemistry and Biology.

[30]  R. Huber,et al.  Crystal structure of the 20 S proteasome:TMC-95A complex: a non-covalent proteasome inhibitor. , 2001, Journal of molecular biology.

[31]  C. Crews,et al.  The ubiquitin‐proteasome pathway and proteasome inhibitors , 2001, Medicinal research reviews.

[32]  David M. Smith,et al.  Ester Bond-containing Tea Polyphenols Potently Inhibit Proteasome Activity in Vitro and in Vivo * , 2001, The Journal of Biological Chemistry.

[33]  M. Bogyo,et al.  Global analysis of proteasomal substrate specificity using positional-scanning libraries of covalent inhibitors , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[34]  P. Kloetzel,et al.  Ubiquitin and proteasomes: Antigen processing by the proteasome , 2001, Nature Reviews Molecular Cell Biology.

[35]  K. Lindsten,et al.  Lack of proteasome active site allostery as revealed by subunit-specific inhibitors. , 2001, Molecular cell.

[36]  A. Ciechanover,et al.  The ubiquitin system , 2000, Nature Medicine.

[37]  S. Ōmura,et al.  Separation of cathepsin A-like enzyme and the proteasome: evidence that lactacystin/beta-lactone is not a specific inhibitor of the proteasome. , 2000, The international journal of biochemistry & cell biology.

[38]  R. Deshaies,et al.  A Proteasome Howdunit The Case of the Missing Signal , 2000, Cell.

[39]  A. Ciechanover,et al.  Ubiquitin‐mediated proteolysis: biological regulation via destruction , 2000, BioEssays : news and reviews in molecular, cellular and developmental biology.

[40]  Kohei Takahashi,et al.  TMC-95A, B, C, and D, novel proteasome inhibitors produced by Apiospora montagnei Sacc. TC 1093. Taxonomy, production, isolation, and biological activities. , 2000, The Journal of antibiotics.

[41]  M. Kuroda,et al.  Structures of TMC-95A-D: novel proteasome inhibitors from Apiospora montagnei sacc. TC 1093. , 2000, The Journal of organic chemistry.

[42]  R. Huber,et al.  Crystal Structure of Epoxomicin:20S Proteasome reveals a molecular basis for selectivity of alpha,beta-Epoxyketone Proteasome Inhibitors , 2000 .

[43]  M. Groll,et al.  Synthesis of bivalent inhibitors of eucaryotic proteasomes , 2000, Journal of peptide science : an official publication of the European Peptide Society.

[44]  K. Takahashi,et al.  TMC-86A, B and TMC-96, new proteasome inhibitors from Streptomyces sp. TC 1084 and Saccharothrix sp. TC 1094. II. Physico-chemical properties and structure determination. , 1999, The Journal of antibiotics.

[45]  C. Crews,et al.  Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide α', β'-epoxyketones , 1999 .

[46]  C. Crews,et al.  Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity. , 1999, Proceedings of the National Academy of Sciences of the United States of America.

[47]  C. Crews,et al.  Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology. , 1999, Bioorganic & medicinal chemistry letters.

[48]  C. Crews,et al.  Eponemycin exerts its antitumor effect through the inhibition of proteasome function. , 1999, Cancer research.

[49]  R. Huber,et al.  Bivalency as a principle for proteasome inhibition. , 1999, Proceedings of the National Academy of Sciences of the United States of America.

[50]  A. Harvey,et al.  Medicines from nature: are natural products still relevant to drug discovery? , 1999, Trends in pharmacological sciences.

[51]  R. Huber,et al.  Bifunctional inhibitors of the trypsin-like activity of eukaryotic proteasomes. , 1999, Chemistry & biology.

[52]  C. Crews,et al.  Eponemycin analogues: syntheses and use as probes of angiogenesis. , 1998, Bioorganic & medicinal chemistry.

[53]  Sunny Shin,et al.  Substrate binding and sequence preference of the proteasome revealed by active-site-directed affinity probes. , 1998, Chemistry & biology.

[54]  L. Dick,et al.  Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids. , 1998, Bioorganic & medicinal chemistry letters.

[55]  P. Weber,et al.  Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile. , 1998, Bioorganic & medicinal chemistry letters.

[56]  A. Goldberg,et al.  Covalent modification of the active site threonine of proteasomal beta subunits and the Escherichia coli homolog HslV by a new class of inhibitors. , 1997, Proceedings of the National Academy of Sciences of the United States of America.

[57]  S. Ōmura,et al.  Lactacystin, a specific inhibitor of the proteasome, inhibits human platelet lysosomal cathepsin A-like enzyme. , 1997, Biochemical and biophysical research communications.

[58]  R. Huber,et al.  Structure of 20S proteasome from yeast at 2.4Å resolution , 1997, Nature.

[59]  L. Dick,et al.  Mechanistic Studies on the Inactivation of the Proteasome by Lactacystin in Cultured Cells* , 1997, The Journal of Biological Chemistry.

[60]  Marc W. Kirschner,et al.  How Proteolysis Drives the Cell Cycle , 1996, Science.

[61]  Wei Chen,et al.  The Antitumor Drug Aclacinomycin A, Which Inhibits the Degradation of Ubiquitinated Proteins, Shows Selectivity for the Chymotrypsin-like Activity of the Bovine Pituitary 20 S Proteasome* , 1996, The Journal of Biological Chemistry.

[62]  J. Leban,et al.  Design and Synthesis of Novel Protease Inhibitors. Tripeptide α′, β′-Epoxyketones as Nanomolar Inactivators of the Proteasome. , 1996 .

[63]  J. Palmer,et al.  Peptidyl vinyl sulphones: a new class of potent and selective cysteine protease inhibitors: S2P2 specificity of human cathepsin O2 in comparison with cathepsins S and L. , 1996, The Biochemical journal.

[64]  L. Dick,et al.  Mechanistic Studies on the Inactivation of the Proteasome by Lactacystin , 1996, The Journal of Biological Chemistry.

[65]  A. Murzin,et al.  A protein catalytic framework with an N-terminal nucleophile is capable of self-activation , 1995, Nature.

[66]  J. Palmer,et al.  Vinyl sulfones as mechanism-based cysteine protease inhibitors. , 1995, Journal of medicinal chemistry.

[67]  R F Standaert,et al.  Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin , 1995, Science.

[68]  R. Huber,et al.  Crystal structure of the 20S proteasome from the archaeon T. acidophilum at 3.4 A resolution. , 1995, Science.

[69]  M. Figueiredo-Pereira,et al.  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, Journal of neurochemistry.

[70]  A. Goldberg,et al.  Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules , 1994, Cell.

[71]  M. Orlowski.  The multicatalytic proteinase complex (proteasome) and intracellular protein degradation: diverse functions of an intracellular particle. , 1993, The Journal of laboratory and clinical medicine.

[72]  T. Oki,et al.  Epoxomicin, a new antitumor agent of microbial origin. , 1992, The Journal of antibiotics.

[73]  S. Ōmura,et al.  Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells. , 1991, The Journal of antibiotics.

[74]  T. Oki,et al.  Eponemycin, a new antibiotic active against B16 melanoma. I. Production, isolation, structure and biological activity. , 1990, The Journal of antibiotics.

[75]  M. Orłowski,et al.  Evidence that Pituitary Cation‐Sensitive Neutral Endopeptidase Is a Multicatalytic Protease Complex , 1983, Journal of neurochemistry.

[76]  M. Orłowski,et al.  Inhibition of Rabbit Brain Prolyl Endopeptidase by N‐Benzyloxycarbonyl‐Prolyl‐Prolinal, a Transition State Aldehyde Inhibitor , 1983, Journal of neurochemistry.

[77]  D. Chauhan,et al.  A novel proteasome inhibitor NPI-0052 as an anticancer therapy , 2006, British Journal of Cancer.

[78]  H. Overkleeft,et al.  Chemical proteomics profiling of proteasome activity. , 2006, Methods in molecular biology.

[79]  R. Orlowski.  The ubiquitin proteasome pathway from bench to bedside. , 2005, Hematology. American Society of Hematology. Education Program.

[80]  C. Crews,et al.  Natural Product and Synthetic Proteasome Inhibitors , 2004 .

[81]  A. Goldberg,et al.  Proteasome inhibitors: from research tools to drug candidates. , 2001, Chemistry & biology.

[82]  M. Karin,et al.  Phosphorylation meets ubiquitination: the control of NF-[kappa]B activity. , 2000, Annual review of immunology.

[83]  J. Rouvinen,et al.  Structural comparison of Ntn‐hydrolases , 2000, Protein science : a publication of the Protein Society.

[84]  M. Figueiredo-Pereira,et al.  Synthetic inhibitors of the multicatalytic proteinase complex (proteasome). , 1993, Enzyme & protein.

[85]  C. Cardozo,et al.  Catalytic components of the bovine pituitary multicatalytic proteinase complex (proteasome). , 1993, Enzyme & protein.