Synthesis and Pharmacology of Proteasome Inhibitors

Celastrol potentiates striatal dopamine metabolism and increases cell death under conditions of proteasome inhibition: in vivo and in vitro studies

(2014) Tomasz Lenda et al.   Pharmacological Reports

Inhibitors for the Immuno- and Constitutive Proteasome: Current and Future Trends in Drug Development

(2012) Eva Maria Huber et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A new series of N5 derivatives of the 1,1,5-trimethyl furo[3,4-c]pyridine-3,4-dione (cerpegin) selectively inhibits the post-acid activity of mammalian 20S proteasomes

(2012) The Hien Pham et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Serendipity in discovery of proteasome inhibitors

(2012) Derek Dunn et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Immuno- and Constitutive Proteasome Crystal Structures Reveal Differences in Substrate and Inhibitor Specificity

(2012) Eva M. Huber et al.   CELL

The Carmaphycins: New Proteasome Inhibitors Exhibiting an α,β-Epoxyketone Warhead from a Marine Cyanobacterium

(2012) Alban R. Pereira et al.   CHEMBIOCHEM

Proteasome Inhibitors: An Expanding Army Attacking a Unique Target

(2012) Alexei F. Kisselev et al.   CHEMISTRY & BIOLOGY

Immunoproteasomes at the interface of innate and adaptive immune responses: two faces of one enzyme

(2012) Elke Krüger et al.   CURRENT OPINION IN IMMUNOLOGY

Paraptosis accompanied by autophagy and apoptosis was induced by celastrol, a natural compound with influence on proteasome, ER stress and Hsp90

(2012) Wen-Bo Wang et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Proteomic Profiling of Germ Cell Cancer Cells Treated with Aaptamine, a Marine Alkaloid with Antiproliferative Activity

(2012) Sergey A. Dyshlovoy et al.   JOURNAL OF PROTEOME RESEARCH

Cationic Porphyrins Are Reversible Proteasome Inhibitors

(2012) Anna Maria Santoro et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Fundamental Reaction Pathway and Free Energy Profile for Inhibition of Proteasome by Epoxomicin

(2012) Donghui Wei et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects

(2012) M A Hurchla et al.   LEUKEMIA

Synthesis and biological activity of simplified belactosin C analogues

(2012) Armin de Meijere et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Stereoselective Synthesis of Deuterium-Labeled (2S)-Cyclohexenyl Alanines, Biosynthetic Intermediates of Cinnabaramide

(2012) Philipp Barbie et al.   ORGANIC LETTERS

Suberitine A–D, Four New Cytotoxic Dimeric Aaptamine Alkaloids from the Marine Sponge Aaptos suberitoides

(2012) Caixia Liu et al.   ORGANIC LETTERS

Stereoselective functionalization of pyrrolidinone moiety towards the synthesis of salinosporamide A

(2012) Julien Barbion et al.   TETRAHEDRON

Hydroxyureas as Noncovalent Proteasome Inhibitors

(2011) Nerea Gallastegui et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A meta-analysis on alcohol drinking and gastric cancer risk

(2011) I. Tramacere et al.   ANNALS OF ONCOLOGY

Thiostrepton and Derivatives Exhibit Antimalarial and Gametocytocidal Activity by Dually Targeting Parasite Proteasome and Apicoplast

(2011) Makoah N. Aminake et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Preclinical evaluation of the antitumor activity of bortezomib in combination with vitamin C or with epigallocatechin gallate, a component of green tea

(2011) Bret Bannerman et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

(-)-Epigallocatechin-3-gallate and DZNep reduce polycomb protein level via a proteasome-dependent mechanism in skin cancer cells

(2011) S. R. Choudhury et al.   CARCINOGENESIS

The role of the proteasome in the generation of MHC class I ligands and immune responses

(2011) E. J. A. M. Sijts et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Exploiting nature's rich source of proteasome inhibitors as starting points in drug development

(2011) Melissa Ann Gräwert et al.   CHEMICAL COMMUNICATIONS

Specific Cell-Permeable Inhibitor of Proteasome Trypsin-like Sites Selectively Sensitizes Myeloma Cells to Bortezomib and Carfilzomib

(2011) Anne C. Mirabella et al.   CHEMISTRY & BIOLOGY

Natural Product Inhibitors of the Ubiquitin-Proteasome Pathway

(2011) John S. Schneekloth et al.   CURRENT DRUG TARGETS

Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE

(2011) Matthew M. Seavey et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

The chemistry and biology of syringolins, glidobactins and cepafungins (syrbactins)

(2011) Daniel Krahn et al.   NATURAL PRODUCT REPORTS

Synthesis and biological activity of optimized belactosin C congeners

(2011) Vadim S. Korotkov et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Discovery of a potent and highly β1 specific proteasome inhibitor from a focused library of urea-containing peptide vinyl sulfones and peptide epoxyketones

(2011) Wouter A. van der Linden et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Total Synthesis of (−)-Salinosporamide A

(2011) Nobuhiro Satoh et al.   ORGANIC LETTERS

Stereoselective Synthesis of Deuterated β-Cyclohexenylserine, a Biosynthetic Intermediate of the Salinosporamides§

(2011) Jan Deska et al.   ORGANIC LETTERS

Syringolin B-inspired proteasome inhibitor analogue TIR-203 exhibits enhanced biological activity in multiple myeloma and neuroblastoma

(2011) John Opoku-Ansah et al.   PHARMACEUTICAL BIOLOGY

Syntheses and cytotoxicity of syringolin B-based proteasome inhibitors

(2011) Tannya R. Ibarra-Rivera et al.   TETRAHEDRON

Elucidation of the α-Keto-Aldehyde Binding Mechanism: A Lead Structure Motif for Proteasome Inhibition

(2010) Melissa Ann Gräwert et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Chemical Proteomics Discloses Petrosapongiolide M, an Antiinflammatory Marine Sesterterpene, as a Proteasome Inhibitor

(2010) Luigi Margarucci et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Elucidation of the Structure and Intermolecular Interactions of a Reversible Cyclic-Peptide Inhibitor of the Proteasome by NMR Spectroscopy and Molecular Modeling

(2010) Benjamin Stauch et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Antiplasmodial Thiostrepton Derivatives: Proteasome Inhibitors with a Dual Mode of Action

(2010) Sebastian Schoof et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fellutamide B is a potent inhibitor of the Mycobacterium tuberculosis proteasome

(2010) Gang Lin et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Aaptamine, an alkaloid from the sponge Aaptos suberitoides, functions as a proteasome inhibitor

(2010) Sachiko Tsukamoto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma

(2010) D. Chauhan et al.   BLOOD

Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer

(2010) E. Kupperman et al.   CANCER RESEARCH

Immunoproteasomes Preserve Protein Homeostasis upon Interferon-Induced Oxidative Stress

(2010) Ulrike Seifert et al.   CELL

The natural product hybrid of Syringolin A and Glidobactin A synergizes proteasome inhibition potency with subsite selectivity

(2010) Jérôme Clerc et al.   CHEMICAL COMMUNICATIONS

Activity-Based Profiling Reveals Reactivity of the Murine Thymoproteasome-Specific Subunit β5t

(2010) Bogdan I. Florea et al.   CHEMISTRY & BIOLOGY

Total Synthesis of (−)-Salinosporamide A

(2010) Yuji Kaiya et al.   Chemistry-An Asian Journal

Synthesis and Biological Characterization of Argyrin F

(2010) Leila Bülow et al.   ChemMedChem

Celastrol can inhibit proteasome activity and upregulate the expression of heat shock protein genes, hsp30 and hsp70, in Xenopus laevis A6 cells

(2010) Shantel E. Walcott et al.   COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY A-MOLECULAR & INTEGRATIVE PHYSIOLOGY

Proteasome Inhibitors: Recent Advances and New Perspectives In Medicinal Chemistry

(2010) E. Genin et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Convergent Synthesis and Biological Evaluation of Syringolin A and Derivatives as Eukaryotic 20S Proteasome Inhibitors

(2010) Jérôme Clerc et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

An Enantio- and Diastereocontrolled Synthesis of (–)-Salinosporamide A

(2010) Yoshiharu Iwabuchi et al.   HETEROCYCLES

Mode of Action of Epoxyphomalins A and B and Characterization of Related Metabolites from the Marine-Derived FungusParaconiothyriumsp.

(2010) Ietidal E. Mohamed et al.   JOURNAL OF NATURAL PRODUCTS

Concise Formal Synthesis of (−)-Salinosporamide A (Marizomib) Using a Regio- and Stereoselective Epoxidation and Reductive Oxirane Ring-Opening Strategy

(2010) Taotao Ling et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthetic studies of salinosporamide A through the intramolecular hydroamidation of alkynes

(2010) Haruhi Kamisaki et al.   JOURNAL OF ORGANOMETALLIC CHEMISTRY

Formal Synthesis of Belactosin A and Hormaomycin via a Diastereoselective Intramolecular Cyclopropanation of an α-Nitro Diazoester

(2010) Sébastien F. Vanier et al.   ORGANIC LETTERS

Total Synthesis of Syringolin A and B

(2010) Michael C. Pirrung et al.   ORGANIC LETTERS

Total Synthesis of Syringolin A

(2010) Chunhui Dai et al.   ORGANIC LETTERS

Natural Proteasome Inhibitor Celastrol Suppresses Androgen-Independent Prostate Cancer Progression by Modulating Apoptotic Proteins and NF-kappaB

(2010) Yao Dai et al.   PLoS One

Thiopeptide Antibiotic Biosynthesis

(2009) Hans-Dieter Arndt et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Recognition and Processing of Ubiquitin-Protein Conjugates by the Proteasome

(2009) Daniel Finley   Annual Review of Biochemistry

Green tea polyphenols block the anticancer effects of bortezomib and other boronic acid-based proteasome inhibitors

(2009) E. B. Golden et al.   BLOOD

The peptide-semicarbazone S-2209, a representative of a new class of proteasome inhibitors, induces apoptosis and cell growth arrest in multiple myeloma cells

(2009) Philipp Baumann et al.   BRITISH JOURNAL OF HAEMATOLOGY

The proteasome inhibitor CEP-18770 enhances the anti-myeloma activity of bortezomib and melphalan

(2009) Eric Sanchez et al.   BRITISH JOURNAL OF HAEMATOLOGY

Selective Inhibitor of Proteasome's Caspase-like Sites Sensitizes Cells to Specific Inhibition of Chymotrypsin-like Sites

(2009) Matthew Britton et al.   CHEMISTRY & BIOLOGY

Proteasome Inhibitors in Cancer Therapy

(2009) Ugo Testa   CURRENT DRUG TARGETS

Targeting the proteasome pathway

(2009) Sachiko Tsukamoto et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Enantioselective Synthesis and Proteasome Inhibition of A-Ring Analogs of (-)-Epigallocatechin Gallate (EGCG), the Active Ingredient of Green Tea Extract

(2009) Tak Hang Chan et al.   HETEROCYCLES

The 26 S Proteasome: From Basic Mechanisms to Drug Targeting

(2009) Ami Navon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Spirodiepoxides: Synthesis of Epoxomicinoids

(2009) Yue Zhang et al.   JOURNAL OF ORGANIC CHEMISTRY

A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis

(2009) Tony Muchamuel et al.   NATURE MEDICINE

Increased proteasome subunit protein expression and proteasome activity in colon cancer relate to an enhanced activation of nuclear factor E2-related factor 2 (Nrf2)

(2009) A Arlt et al.   ONCOGENE

Three-dimensional structure-activity relationship study of belactosin A and its stereo- and regioisomers: development of potent proteasome inhibitors by a stereochemical diversity-oriented strategy

(2009) Keisuke Yoshida et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Apigenin, Chrysin, and Luteolin Selectively Inhibit Chymotrypsin-Like and Trypsin-Like Proteasome Catalytic Activities in Tumor Cells

(2009) Yi-Xin Wu et al.   PLANTA MEDICA

Synthetic and structural studies on syringolin A and B reveal critical determinants of selectivity and potency of proteasome inhibition

(2009) J. Clerc et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Formal synthesis of salinosporamide A via NHC-catalyzed intramolecular lactonization

(2009) Justin R. Struble et al.   TETRAHEDRON

Entry to Heterocycles Based on Indium-Catalyzed Conia-Ene Reactions: Asymmetric Synthesis of (−)-Salinosporamide A

(2008) Keisuske Takahashi et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Mutasynthesis of Fluorosalinosporamide, a Potent and Reversible Inhibitor of the Proteasome

(2008) Alessandra S. Eustáquio et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Inhibition of proteasome activity by anthocyanins and anthocyanidins

(2008) Andrea Dreiseitel et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Physalin B, a novel inhibitor of the ubiquitin-proteasome pathway, triggers NOXA-associated apoptosis

(2008) Isabelle Vandenberghe et al.   BIOCHEMICAL PHARMACOLOGY

Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives

(2008) Li Huang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Affinity labeling of the proteasome by a belactosin A derived inhibitor

(2008) Makoto Hasegawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Argyrin A Reveals a Critical Role for the Tumor Suppressor Protein p27kip1 in Mediating Antitumor Activities in Response to Proteasome Inhibition

(2008) Irina Nickeleit et al.   CANCER CELL

Proteasome Inhibition by Fellutamide B Induces Nerve Growth Factor Synthesis

(2008) John Hines et al.   CHEMISTRY & BIOLOGY

Proteasome Inhibitors in Cancer Therapy: Lessons from the First Decade

(2008) R. Z. Orlowski et al.   CLINICAL CANCER RESEARCH

The potential of proteasome inhibitors in cancer therapy

(2008) Jan Sterz et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Bortezomib in the front-line treatment of multiple myeloma

(2008) Paul G Richardson et al.   Expert Review of Anticancer Therapy

Leaving Groups Prolong the Duration of 20S Proteasome Inhibition and Enhance the Potency of Salinosporamides

(2008) Rama Rao Manam et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemical Genetics: Exploring the Role of the Proteasome in Cell Biology Using Natural Products and Other Small Molecule Proteasome Inhibitors

(2008) Kyung Bo Kim et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Potent, Selective, and Orally Active Proteasome Inhibitor for the Treatment of Cancer

(2008) Bruce D. Dorsey et al.   JOURNAL OF MEDICINAL CHEMISTRY

The persisting challenge of selective and specific proteasome inhibition

(2008) Michael Groll et al.   JOURNAL OF PEPTIDE SCIENCE

Structural Analysis of Spiro β-Lactone Proteasome Inhibitors

(2008) Michael Groll et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Asymmetric Copper-Catalyzed Synthesis of α-Amino Boronate Esters fromN-tert-Butanesulfinyl Aldimines

(2008) Melissa A. Beenen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A plant pathogen virulence factor inhibits the eukaryotic proteasome by a novel mechanism

(2008) Michael Groll et al.   NATURE

Total Synthesis of Salinosporamide A

(2008) Takeo Fukuda et al.   ORGANIC LETTERS

Formal synthesis of salinosporamide A using a nickel-catalyzed reductive aldol cyclization–lactonization as a key step

(2008) Isabel Villanueva Margalef et al.   TETRAHEDRON

New synthetic route to access (±) salinosporamide A via an oxazolone-mediated ene-type reaction

(2008) Robert A. Mosey et al.   TETRAHEDRON LETTERS