Harnessing Proteasome Dynamics and Allostery in Drug Design

Allostery in Disease and in Drug Discovery

(2013) Ruth Nussinov et al.   CELL

Proteasome Regulation by ADP-Ribosylation

(2013) Park F. Cho-Park et al.   CELL

The Proteasome in Health and Disease

(2013) Elzbieta Jankowska et al.   CURRENT PHARMACEUTICAL DESIGN

Conformational switching of the 26S proteasome enables substrate degradation

(2013) Mary E Matyskiela et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Oral biodrug delivery using cell-penetrating peptide

(2012) El-Sayed Khafagy et al.   ADVANCED DRUG DELIVERY REVIEWS

Differential roles of proteasome and immunoproteasome regulators Pa28αβ, Pa28γ and Pa200 in the degradation of oxidized proteins

(2012) Andrew M. Pickering et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

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

(2012) Eva M. Huber et al.   CELL

β5t-containing thymoproteasome: specific expression in thymic cortical epithelial cells and role in positive selection of CD8+ T cells

(2012) Yousuke Takahama et al.   CURRENT OPINION IN IMMUNOLOGY

Structure and Allostery of the Chaperonin GroEL

(2012) Helen R. Saibil et al.   JOURNAL OF MOLECULAR BIOLOGY

Molecular Model of the Human 26S Proteasome

(2012) Paula C.A. da Fonseca et al.   MOLECULAR CELL

Complete subunit architecture of the proteasome regulatory particle

(2012) Gabriel C. Lander et al.   NATURE

Proteasome allostery as a population shift between interchanging conformers

(2012) A. M. Ruschak et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Molecular architecture of the 26S proteasome holocomplex determined by an integrative approach

(2012) K. Lasker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Proteasome-based mechanisms of intrinsic and acquired bortezomib resistance in non-small cell lung cancer

(2011) Leonie H.A.M. de Wilt et al.   BIOCHEMICAL PHARMACOLOGY

Proteasomal AAA-ATPases: Structure and function

(2011) Shoshana Bar-Nun et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Intracellular protein degradation: From a vague idea thru the lysosome and the ubiquitin–proteasome system and onto human diseases and drug targeting

(2011) Aaron Ciechanover   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

A Conserved F Box Regulatory Complex Controls Proteasome Activity in Drosophila

(2011) Maya Bader et al.   CELL

Nonproteasomal Targets of the Proteasome Inhibitors Bortezomib and Carfilzomib: a Link to Clinical Adverse Events

(2011) S. Arastu-Kapur et al.   CLINICAL CANCER RESEARCH

Second Generation Proteasome Inhibitors: Carfilzomib and Immunoproteasome-Specific Inhibitors (IPSIs)

(2011) D. J. Kuhn et al.   CURRENT CANCER DRUG TARGETS

Impaired bortezomib binding to mutant β5 subunit of the proteasome is the underlying basis for bortezomib resistance in leukemia cells

(2011) N E Franke et al.   LEUKEMIA

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

(2011) Daniel Krahn et al.   NATURAL PRODUCT REPORTS

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

Molecular Mechanisms of Bortezomib Resistant Adenocarcinoma Cells

(2011) Erika Suzuki et al.   PLoS One

Potential allosteric modulators of the proteasome activity

(2010) E. Jankowska et al.   BIOPOLYMERS

The C Terminus of Rpt3, an ATPase Subunit of PA700 (19 S) Regulatory Complex, Is Essential for 26 S Proteasome Assembly but Not for Activation

(2010) Brajesh Kumar et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Effect of Noncompetitive Proteasome Inhibition on Bortezomib Resistance

(2010) Xiaoming Li et al.   JNCI-Journal of the National Cancer Institute

Structure of a Blm10 Complex Reveals Common Mechanisms for Proteasome Binding and Gate Opening

(2010) Kianoush Sadre-Bazzaz et al.   MOLECULAR CELL

Dynamic Regulation of Archaeal Proteasome Gate Opening As Studied by TROSY NMR

(2010) T. L. Religa et al.   SCIENCE

Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome

(2009) F. Parlati et al.   BLOOD

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

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

Architecture and Molecular Mechanism of PAN, the Archaeal Proteasome Regulatory ATPase

(2009) Noa Medalia et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Rapamycin fed late in life extends lifespan in genetically heterogeneous mice

(2009) David E. Harrison et al.   NATURE

A Tetrahedral Transition State at the Active Sites of the 20S Proteasome Is Coupled to Opening of the α-Ring Channel

(2009) Pawel A. Osmulski et al.   STRUCTURE

The Origin of Allosteric Functional Modulation: Multiple Pre-existing Pathways

(2009) Antonio del Sol et al.   STRUCTURE

TROSY-Based NMR Evidence for a Novel Class of 20S Proteasome Inhibitors†

(2008) Remco Sprangers et al.   BIOCHEMISTRY

Mammalian 26S Proteasomes Remain Intact during Protein Degradation

(2008) Franziska Kriegenburg et al.   CELL

AFM of biological complexes: What can we learn?

(2008) Maria Gaczynska et al.   CURRENT OPINION IN COLLOID & INTERFACE SCIENCE

Structure of the Human 26S Proteasome

(2008) Paula C. A. da Fonseca et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Differential Roles of the COOH Termini of AAA Subunits of PA700 (19 S Regulator) in Asymmetric Assembly and Activation of the 26 S Proteasome

(2008) Thomas G. Gillette et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure of a Conserved Dimerization Domain within the F-box Protein Fbxo7 and the PI31 Proteasome Inhibitor

(2008) Rebecca Kirk et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2008) Michael Groll et al.   NATURE

Allosteric regulation and catalysis emerge via a common route

(2008) Nina M Goodey et al.   Nature Chemical Biology

Light-activated DNA binding in a designed allosteric protein

(2008) D. Strickland et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA