Recent advances in proteasome inhibitor discovery

Drug Repurposing: Far Beyond New Targets for Old Drugs

(2012) T. I. Oprea et al.   AAPS Journal

Activity Enhancement of the Synthetic Syrbactin Proteasome Inhibitor Hybrid and Biological Evaluation in Tumor Cells

(2012) Crystal R. Archer et al.   BIOCHEMISTRY

Proteasome inhibitors for cancer therapy

(2012) Mohamed Iqbal et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Serendipity in discovery of proteasome inhibitors

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

Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors

(2012) Kai Xu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Modulation of Proteasome Machinery by Natural and Synthetic Analogues of the Marine Bioactive Compound Petrosaspongiolide M

(2012) Luigi Margarucci et al.   CHEMBIOCHEM

Proteasome Inhibitors: An Expanding Army Attacking a Unique Target

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

Noncovalent inhibition of 20S proteasome by pegylated dimerized inhibitors

(2012) Xavier Maréchal et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Disulfiram, an old drug with new potential therapeutic uses for human hematological malignancies

(2012) Concetta Conticello et al.   INTERNATIONAL JOURNAL OF CANCER

Impairment of the Ubiquitin-Proteasome Pathway by MethylN-(6-Phenylsulfanyl-1H-benzimidazol-2-yl)carbamate Leads to a Potent Cytotoxic Effect in Tumor Cells

(2012) Nilambra Dogra et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cellular and computational studies of proteasome inhibition and apoptosis induction in human cancer cells by amino acid Schiff base–copper complexes

(2012) Jian Zuo et al.   JOURNAL OF INORGANIC BIOCHEMISTRY

Discovery and Synthesis of Hydronaphthoquinones as Novel Proteasome Inhibitors

(2012) Yiyu Ge et al.   JOURNAL OF MEDICINAL CHEMISTRY

Palau’amine and Related Oroidin Alkaloids Dibromophakellin and Dibromophakellstatin Inhibit the Human 20S Proteasome

(2012) Theresa A. Lansdell et al.   JOURNAL OF NATURAL PRODUCTS

Cationic Porphyrins Are Reversible Proteasome Inhibitors

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

Hydroxyureas as Noncovalent Proteasome Inhibitors

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

MG132 treatment attenuates cardiac remodeling and dysfunction following aortic banding in rats via the NF-κB/TGFβ1 pathway

(2011) Yuedong Ma et al.   BIOCHEMICAL PHARMACOLOGY

Identification of an EGCG oxidation derivative with proteasome modulatory activity

(2011) Laura Bonfili et al.   BIOCHIMIE

New betulinic acid derivatives as potent proteasome inhibitors

(2011) Keduo Qian et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and proteasome inhibition of lithocholic acid derivatives

(2011) Zhao Dang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Mining the Cinnabaramide Biosynthetic Pathway to Generate Novel Proteasome Inhibitors

(2011) Shwan Rachid et al.   CHEMBIOCHEM

Development of Novel Peptidomimetics Containing a Vinyl Sulfone Moiety as Proteasome Inhibitors

(2011) Roberta Ettari et al.   ChemMedChem

New aldehyde and vinylsulfone proteasome inhibitors for targeted melanoma therapy

(2011) Magali Vivier et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Proteasome Inhibitors from Neoboutonia melleri

(2011) Christophe Long et al.   JOURNAL OF NATURAL PRODUCTS

Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome

(2011) Yuheng Ma et al.   MOLECULES

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

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

(2010) Luigi Margarucci 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

Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S β5-subunit

(2010) Christopher Blackburn et al.   BIOCHEMICAL JOURNAL

Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors

(2010) Harshani R. Lawrence et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis, and biological evaluation of dibromotyrosine analogues inspired by marine natural products as inhibitors of human prostate cancer proliferation, invasion, and migration

(2010) Asmaa A. Sallam et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure–activity relationship of boronic acid derivatives of tyropeptin: Proteasome inhibitors

(2010) Takumi Watanabe et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2010) Jérôme Clerc et al.   CHEMICAL COMMUNICATIONS

20S Proteasome Inhibition: Designing Noncovalent Linear Peptide Mimics of the Natural Product TMC-95A

(2010) Michael Groll et al.   ChemMedChem

Synthesis and Biological Characterization of Argyrin F

(2010) Leila Bülow et al.   ChemMedChem

Sent to Destroy

(2010) Monte S. Willis et al.   CIRCULATION RESEARCH

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

The ubiquitin–proteasome system and assays to determine responses to inhibitors

(2010) Lyuben Tsvetkov et al.   Expert Opinion on Drug Discovery

Nature of Pharmacophore Influences Active Site Specificity of Proteasome Inhibitors

(2010) Michael Screen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Incorporation of Fluorinated Phenylalanine Generates Highly Specific Inhibitor of Proteasome’s Chymotrypsin-like Sites

(2010) Paul P. Geurink et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, in Vitro and in Vivo Biological Evaluation, Docking Studies, and Structure−Activity Relationship (SAR) Discussion of Dipeptidyl Boronic Acid Proteasome Inhibitors Composed of β-Amino Acids

(2010) Yongqiang Zhu et al.   JOURNAL OF MEDICINAL CHEMISTRY

α,β-UnsaturatedN-Acylpyrrole Peptidyl Derivatives: New Proteasome Inhibitors

(2010) Anna Baldisserotto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, in Vitro and in Vivo Biological Evaluation, and Comprehensive Understanding of Structure−Activity Relationships of Dipeptidyl Boronic Acid Proteasome Inhibitors Constructed from β-Amino Acids

(2010) Yongqiang Zhu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Scytonemides A and B, Cyclic Peptides with 20S Proteasome Inhibitory Activity from the Cultured CyanobacteriumScytonema hofmanii

(2010) Aleksej Krunic et al.   JOURNAL OF NATURAL PRODUCTS

Bioinspired Total Synthesis and Human Proteasome Inhibitory Activity of (−)-Salinosporamide A, (−)-Homosalinosporamide A, and Derivatives Obtained via Organonucleophile Promoted Bis-cyclizations

(2010) Henry Nguyen et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis and proteasome inhibition of N-allyl vinyl ester-based peptides

(2010) Anna Baldisserotto et al.   JOURNAL OF PEPTIDE SCIENCE

Studies on terrein as a new class of proteasome inhibitors

(2010) M. Demasi et al.   JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY

20S proteasome inhibitory activity of flavonoids isolated from Spatholobus suberectus

(2010) Sang Hee Shim   PHYTOTHERAPY RESEARCH

The Role of Proteasome Inhibition With Bortezomib in the Treatment of Antibody-Mediated Rejection After Kidney-Only or Kidney-Combined Organ Transplantation

(2010) Stuart M. Flechner et al.   TRANSPLANTATION

Capillary electrophoresis for screening of 20S proteasome inhibitors

(2009) Wenjing Chen et al.   ANALYTICAL BIOCHEMISTRY

Design, synthesis and biological evaluation of tripeptide boronic acid proteasome inhibitors

(2009) Yongqiang Zhu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Proteasome inhibition in human breast cancer cells with high catechol-O-methyltransferase activity by green tea polyphenol EGCG analogs

(2009) Congde Huo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

New cyclic peptide proteasome inhibitors

(2009) Anna Baldisserotto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis of boronic acid derivatives of tyropeptin: Proteasome inhibitors

(2009) Takumi Watanabe et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors

(2009) Hiroyuki Nakamura et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Proteasome inhibition during myocardial infarction

(2009) X. Yu et al.   CARDIOVASCULAR RESEARCH

The tumor proteasome as a novel target for gold(III) complexes: Implications for breast cancer therapy

(2009) Vesna Milacic et al.   COORDINATION CHEMISTRY REVIEWS

Metals in anticancer therapy: Copper(II) complexes as inhibitors of the 20S proteasome

(2009) Sarmad Sahiel Hindo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Comparative Activities of Nickel(II) and Zinc(II) Complexes of Asymmetric [NN′O] Ligands as 26S Proteasome Inhibitors

(2009) Michael Frezza et al.   INORGANIC CHEMISTRY

Inhibitory Effect of Flavonoids on 26S Proteasome Activity

(2009) Tsui-Ling Chang   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

Pharmacophore Modeling, Docking Studies, and Synthesis of Novel Dipeptide Proteasome Inhibitors Containing Boron Atoms

(2009) Meng Lei et al.   Journal of Chemical Information and Modeling

Design, Synthesis, Biological Evaluation, and Structure−Activity Relationship (SAR) Discussion of Dipeptidyl Boronate Proteasome Inhibitors, Part I: Comprehensive Understanding of the SAR of α-Amino Acid Boronates

(2009) Yongqiang Zhu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of an Orally Bioavailable and Selective Peptide Epoxyketone Proteasome Inhibitor (PR-047)

(2009) Han-Jie Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Organic Proteasome Inhibitors Identified by Virtual and in Vitro Screening

(2009) Nicolas Basse et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Difluoro Knoevenagel Condensates of Curcumin, Their Schiff Bases and Copper Complexes as Proteasome Inhibitors and Apoptosis Inducers in Cancer Cells

(2009) Subhash Padhye et al.   PHARMACEUTICAL RESEARCH

Discovery of Novel Proteasome Inhibitors Using a High-Content Cell-Based Screening System

(2009) Irena Lavelin et al.   PLoS One

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

Dysfunction of the ubiquitin-proteasome system in multiple disease conditions: therapeutic approaches

(2008) Subhankar Paul   BIOESSAYS

Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives

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

Discovery, design, and synthesis of anti-metastatic lead phenylmethylene hydantoins inspired by marine natural products

(2008) Mudit Mudit et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery and development of the anticancer agent salinosporamide A (NPI-0052)

(2008) William Fenical et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel fluorinated pseudopeptides as proteasome inhibitors

(2008) Lucia Formicola 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

Curcumin Inhibits the Proteasome Activity in Human Colon Cancer Cells In vitro and In vivo

(2008) V. Milacic et al.   CANCER RESEARCH

Curcumin: From ancient medicine to current clinical trials

(2008) H. Hatcher et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Thymoproteasome: probable role in generating positively selecting peptides

(2008) Shigeo Murata et al.   CURRENT OPINION IN IMMUNOLOGY

Mechanisms of proteasome inhibitor action and resistance in cancer

(2008) David J. McConkey et al.   DRUG RESISTANCE UPDATES

Natural polyphenols as proteasome modulators and their role as anti-cancer compounds

(2008) Laura Bonfili et al.   FEBS Journal

Ni(II), Cu(II), and Zn(II) Diethyldithiocarbamate Complexes Show Various Activities Against the Proteasome in Breast Cancer Cells

(2008) Boris Cvek 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

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

(2008) Michael Groll et al.   NATURE