Microbial proteasomes as drug targets

Development of a highly selective Plasmodium falciparum proteasome inhibitor with anti‐malaria activity in humanized mice

(2021) Gang Lin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis

(2021) Michael Thomas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Macrocyclic Peptides that Selectively Inhibit the Mycobacterium tuberculosis Proteasome

(2021) Hao Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evidence of Artemisinin-Resistant Malaria in Africa

(2021) Betty Balikagala et al.   NEW ENGLAND JOURNAL OF MEDICINE

Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases

(2020) Advait Nagle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

(2019) Susan Wyllie et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Improvement of Asparagine Ethylenediamines as Anti-malarial Plasmodium-Selective Proteasome Inhibitors

(2019) Wenhu Zhan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Phenylimidazole-based Inhibitors of the Mycobacterium tuberculosis Proteasome

(2019) Wenhu Zhan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a 4-fluorobenzyl l -valinate amide benzoxaborole ( AN11736 ) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT)

(2018) Tsutomu Akama et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A meta-analysis of the prevalence of African animal trypanosomiasis in Nigeria from 1960 to 2017

(2018) Paul Olalekan Odeniran et al.   Parasites & Vectors

Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance

(2018) Laura A. Kirkman et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The immunoproteasome and thymoproteasome: functions, evolution and human disease

(2018) Shigeo Murata et al.   NATURE IMMUNOLOGY

Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome

(2018) Stanley C. Xie et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug Discovery for Kinetoplastid Diseases: Future Directions

(2018) Srinivasa P. S. Rao et al.   ACS Infectious Diseases

Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity

(2017) Gregory M. LaMonte et al.   JOURNAL OF MEDICINAL CHEMISTRY

New developments in anti-malarial target candidate and product profiles

(2017) Jeremy N. Burrows et al.   MALARIA JOURNAL

Mycobacterium tuberculosis proteasomal ATPase Mpa has a β-grasp domain that hinders docking with the proteasome core protease

(2017) Yujie Wu et al.   MOLECULAR MICROBIOLOGY

Mycobacterium tuberculosis Proteasome Accessory Factor A (PafA) Can Transfer Prokaryotic Ubiquitin-Like Protein (Pup) between Substrates

(2017) Susan Zhang et al.   mBio

Structure of human immunoproteasome with a reversible and noncompetitive inhibitor that selectively inhibits activated lymphocytes

(2017) Ruda de Luna Almeida Santos et al.   Nature Communications

Malaria

(2017) Margaret A. Phillips et al.   Nature Reviews Disease Primers

Structure- and function-based design of Plasmodium-selective proteasome inhibitors

(2016) Hao Li et al.   NATURE

Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness

(2016) Shilpi Khare et al.   NATURE

Specialized proteasome subunits have an essential role in the thymic selection of CD8+ T cells

(2016) Eleanor Z Kincaid et al.   NATURE IMMUNOLOGY

Structural analysis of the dodecameric proteasome activator PafE inMycobacterium tuberculosis

(2016) Lin Bai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Animal African Trypanosomiasis: Time to Increase Focus on Clinically Relevant Parasite and Host Species

(2016) Liam J. Morrison et al.   TRENDS IN PARASITOLOGY

Past and Ongoing Tsetse and Animal Trypanosomiasis Control Operations in Five African Countries: A Systematic Review

(2016) Anne Meyer et al.   PLoS Neglected Tropical Diseases

Rational Design of Selective and Bioactive Inhibitors of the Mycobacterium tuberculosis Proteasome

(2016) Kyle A. Totaro et al.   ACS Infectious Diseases

Bacterial Proteasomes

(2015) Jordan B. Jastrab et al.   Annual Review of Microbiology

Inhibition and deficiency of the immunoproteasome subunit LMP7 attenuates LCMV-induced meningitis

(2015) Sarah Mundt et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Assessing Subunit Dependency of the Plasmodium Proteasome Using Small Molecule Inhibitors and Active Site Probes

(2014) Hao Li et al.   ACS Chemical Biology

Time to contain artemisinin resistance

(2014) The Lancet   LANCET

A draft map of the human proteome

(2014) Min-Sik Kim et al.   NATURE

Mass-spectrometry-based draft of the human proteome

(2014) Mathias Wilhelm et al.   NATURE

Toxoplasma gondii infection of activated J774-A1 macrophages causes inducible nitric oxide synthase degradation by the proteasome pathway

(2014) Juliana da Cruz Padrão et al.   PARASITOLOGY INTERNATIONAL

Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome

(2014) Hao Fan et al.   ACS Medicinal Chemistry Letters

Profound Activity of the Anti-cancer Drug Bortezomib against Echinococcus multilocularis Metacestodes Identifies the Proteasome as a Novel Drug Target for Cestodes

(2014) Britta Stadelmann et al.   PLoS Neglected Tropical Diseases

Broad-Spectrum Antimalarial Activity of Peptido Sulfonyl Fluorides, a New Class of Proteasome Inhibitors

(2013) Serena Tschan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

N,C-Capped Dipeptides with Selectivity for Mycobacterial Proteasome over Human Proteasomes: Role of S3 and S1 Binding Pockets

(2013) Gang Lin et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Blocking Plasmodium falciparum Development via Dual Inhibition of Hemoglobin Degradation and the Ubiquitin Proteasome System by MG132

(2013) Rajesh Prasad et al.   PLoS One

Proteasome inhibitors in multiple myeloma: 10 years later

(2012) P. Moreau et al.   BLOOD

Transcriptome analysis reveals unique metabolic features in the Cryptosporidium parvum Oocysts associated with environmental survival and stresses

(2012) Haili Zhang et al.   BMC GENOMICS

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

(2012) Alban R. Pereira et al.   CHEMBIOCHEM

Validation of the Proteasome as a Therapeutic Target in Plasmodium Using an Epoxyketone Inhibitor with Parasite-Specific Toxicity

(2012) Hao Li et al.   CHEMISTRY & BIOLOGY

Emergence of artemisinin-resistant malaria on the western border of Thailand: a longitudinal study

(2012) Aung Pyae Phyo et al.   LANCET

Loss of malarial susceptibility to artemisinin in Thailand

(2012) Anne-Catrin Uhlemann et al.   LANCET

Artemisinin-resistant malaria in the Asia-Pacific region

(2012) Jim Tulloch et al.   LANCET

Resistance to artemisinin-based combination therapy

(2012) Joel G Breman   LANCET INFECTIOUS DISEASES

The Cryptosporidium Parvum Transcriptome during In Vitro Development

(2012) Mary J. Mauzy et al.   PLoS One

The socioeconomic burden of parasitic zoonoses: Global trends

(2011) Paul R. Torgerson et al.   VETERINARY PARASITOLOGY

Impairment of Immunoproteasome Function by β5i/LMP7 Subunit Deficiency Results in Severe Enterovirus Myocarditis

(2011) Elisa Opitz et al.   PLoS Pathogens

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

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

Artemisinin resistance—the clock is ticking

(2010) Nicholas J White   LANCET

“Depupylation” of Prokaryotic Ubiquitin-like Protein from Mycobacterial Proteasome Substrates

(2010) Kristin E. Burns et al.   MOLECULAR CELL

Molecular analysis of the prokaryotic ubiquitin-like protein (Pup) conjugation pathway in Mycobacterium tuberculosis

(2010) Francisca A. Cerda-Maira et al.   MOLECULAR MICROBIOLOGY

Ubiquitin-like protein conjugation and the ubiquitin–proteasome system as drug targets

(2010) Lynn Bedford et al.   NATURE REVIEWS DRUG DISCOVERY

The Mycobacterium tuberculosis Proteasome Active Site Threonine Is Essential for Persistence Yet Dispensable for Replication and Resistance to Nitric Oxide

(2010) Sheetal Gandotra et al.   PLoS Pathogens

Critical role for the immunoproteasome subunit LMP7 in the resistance of mice toToxoplasma gondiiinfection

(2009) Liping Tu et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Artemisinin resistance on the Thai–Cambodian border

(2009) Olaf Müller et al.   LANCET

Inhibitors selective for mycobacterial versus human proteasomes

(2009) Gang Lin et al.   NATURE

Bacterial ubiquitin-like modifier Pup is deamidated and conjugated to substrates by distinct but homologous enzymes

(2009) Frank Striebel et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structural Insights on the Mycobacterium tuberculosis Proteasomal ATPase Mpa

(2009) Tao Wang et al.   STRUCTURE

Thymoproteasome: probable role in generating positively selecting peptides

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

Distinct Specificities ofMycobacterium tuberculosisand Mammalian Proteasomes forN-Acetyl Tripeptide Substrates

(2008) Gang Lin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Kinetoplastids: related protozoan pathogens, different diseases

(2008) Ken Stuart et al.   JOURNAL OF CLINICAL INVESTIGATION

Ubiquitin-Like Protein Involved in the Proteasome Pathway of Mycobacterium tuberculosis

(2008) M. J. Pearce et al.   SCIENCE