Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i)

M3258 Is a Selective Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) Delivering Efficacy in Multiple Myeloma Models

(2021) Michael P. Sanderson et al.   MOLECULAR CANCER THERAPEUTICS

Recent insights how combined inhibition of immuno/proteasome subunits enables therapeutic efficacy

(2020) Michael Basler et al.   GENES AND IMMUNITY

Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability

(2019) Ena Ladi et al.   JOURNAL OF MEDICINAL CHEMISTRY

A dual inhibitor of the proteasome catalytic subunits LMP2 and Y attenuates disease progression in mouse models of Alzheimer’s disease

(2019) In Jun Yeo et al.   Scientific Reports

Discovery of a Novel Small-Molecule Modulator of C–X–C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis

(2018) Elnaz Menhaji-Klotz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Immunoproteasome-selective and non-selective inhibitors: A promising approach for the treatment of multiple myeloma

(2018) Roberta Ettari et al.   PHARMACOLOGY & THERAPEUTICS

The safety of bortezomib for the treatment of multiple myeloma

(2018) Guldane Cengiz Seval et al.   Expert Opinion On Drug Safety

Co‐inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity

(2018) Michael Basler et al.   EMBO REPORTS

Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)-N-((S)-3-(Cyclopent-1-en-1-yl)-1-((R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propenamide)

(2018) Henry W. B. Johnson et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Inhibition and deficiency of the immunoproteasome subunit LMP7 suppress the development and progression of colorectal carcinoma in mice

(2017) Julia Koerner et al.   Oncotarget

Immunoproteasome β5i-Selective Dipeptidomimetic Inhibitors

(2016) Pradeep K. Singh et al.   ChemMedChem

A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit β5i

(2016) Eva M Huber et al.   EMBO JOURNAL

Safety of proteasome inhibitors for treatment of multiple myeloma

(2016) Danielle Schlafer et al.   Expert Opinion On Drug Safety

Brief treatment with a highly selective immunoproteasome inhibitor promotes long-term cardiac allograft acceptance in mice

(2016) Esilida Sula Karreci et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective Inhibition of the Immunoproteasome by Structure-Based Targeting of a Non-catalytic Cysteine

(2015) Christian Dubiella et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Benzofuran analogues of amphetamine and methamphetamine: studies on the metabolism and toxicological analysis of 5-APB and 5-MAPB in urine and plasma using GC-MS and LC-(HR)-MSn techniques

(2014) Jessica Welter et al.   ANALYTICAL AND BIOANALYTICAL CHEMISTRY

The Immunoproteasome as a Therapeutic Target for Hematological Malignancies

(2014) Zachary Miller et al.   CURRENT CANCER DRUG TARGETS

Proteasome inhibitors - molecular basis and current perspectives in multiple myeloma

(2014) Lenka Kubiczkova et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Interferon-γ-induced upregulation of immunoproteasome subunit assembly overcomes bortezomib resistance in human hematological cell lines

(2014) Denise Niewerth et al.   Journal of Hematology & Oncology

Peptide-Based Proteasome Inhibitors in Anticancer Drug Design

(2014) Nicola Micale et al.   MEDICINAL RESEARCH REVIEWS

Higher ratio immune versus constitutive proteasome level as novel indicator of sensitivity of pediatric acute leukemia cells to proteasome inhibitors

(2013) D. Niewerth et al.   HAEMATOLOGICA

Proteasome Inhibitors: An Expanding Army Attacking a Unique Target

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

Purification and separation of the 20S immunoproteasome from the constitutive proteasome and identification of the subunits by LC–MS

(2012) Vincent Dechavanne et al.   PROTEIN EXPRESSION AND PURIFICATION

The Immunoproteasome as a Target in Hematologic Malignancies

(2012) Deborah J. Kuhn et al.   SEMINARS IN HEMATOLOGY

Immune and non-immune functions of the immunoproteasome

(2011) Arkhjamil Angeles   Frontiers in Bioscience-Landmark

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

PR-924, a selective inhibitor of the immunoproteasome subunit LMP-7, blocks multiple myeloma cell growth both in vitro and in vivo

(2010) Ajita V. Singh et al.   BRITISH JOURNAL OF HAEMATOLOGY

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

(2009) F. Parlati et al.   BLOOD

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

Novel Prodrugs of Tegafur that Display Improved Anticancer Activity and Antiangiogenic Properties

(2007) Dikla Engel et al.   JOURNAL OF MEDICINAL CHEMISTRY