A practical review of proteasome pharmacology
TA Thibaudeau, DM Smith - Pharmacological reviews, 2019 - ASPET
The ubiquitin proteasome system (UPS) degrades individual proteins in a highly regulated
fashion and is responsible for the degradation of misfolded, damaged, or unneeded cellular …
fashion and is responsible for the degradation of misfolded, damaged, or unneeded cellular …
Targeting the ubiquitin-proteasome pathway to overcome anti-cancer drug resistance
Drug resistance is a major obstacle in the field of pre-clinical and clinical therapeutics. The
development of novel technologies and targeted therapies have yielded new modalities to …
development of novel technologies and targeted therapies have yielded new modalities to …
[HTML][HTML] Site-specific proteasome inhibitors
AF Kisselev - Biomolecules, 2021 - mdpi.com
Proteasome is a multi-subunit protein degradation machine, which plays a key role in the
maintenance of protein homeostasis and, through degradation of regulatory proteins, in the …
maintenance of protein homeostasis and, through degradation of regulatory proteins, in the …
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 …
HWB Johnson, E Lowe, JL Anderl, A Fan… - Journal of medicinal …, 2018 - ACS Publications
Selective immunoproteasome inhibition is a promising approach for treating autoimmune
disorders, but optimal proteolytic active site subunit inhibition profiles remain unknown. We …
disorders, but optimal proteolytic active site subunit inhibition profiles remain unknown. We …
Immunoproteasome functions explained by divergence in cleavage specificity and regulation
The immunoproteasome (iP) has been proposed to perform specialized roles in MHC class I
antigen presentation, cytokine modulation, and T cell differentiation and has emerged as a …
antigen presentation, cytokine modulation, and T cell differentiation and has emerged as a …
[HTML][HTML] Emerging new approaches in desensitization: targeted therapies for HLA sensitization
There is an urgent need for therapeutic interventions for desensitization and antibody-
mediated rejection (AMR) in sensitized patients with preformed or de novo donor-specific …
mediated rejection (AMR) in sensitized patients with preformed or de novo donor-specific …
Binding of the microbial cyclic tetrapeptide trapoxin A to the class I histone deacetylase HDAC8
NJ Porter, DW Christianson - ACS chemical biology, 2017 - ACS Publications
Trapoxin A is a microbial cyclic tetrapeptide that is an essentially irreversible inhibitor of
class I histone deacetylases (HDACs). The inhibitory warhead is the α, β-epoxyketone side …
class I histone deacetylases (HDACs). The inhibitory warhead is the α, β-epoxyketone side …
Recent insights how combined inhibition of immuno/proteasome subunits enables therapeutic efficacy
M Basler, M Groettrup - Genes & Immunity, 2020 - nature.com
The proteasome is a multicatalytic protease in the cytosol and nucleus of all eukaryotic cells
that controls numerous cellular processes through regulated protein degradation …
that controls numerous cellular processes through regulated protein degradation …
The immunoproteasome: an emerging target in cancer and autoimmune and neurological disorders
The immunoproteasome (iCP) is an isoform of the 20S proteasome that is expressed when
cells are stressed or receive an inflammatory signal. The primary role of the iCP is to …
cells are stressed or receive an inflammatory signal. The primary role of the iCP is to …
[HTML][HTML] Immunoproteasome function in normal and malignant hematopoiesis
The ubiquitin–proteasome system (UPS) is a central part of protein homeostasis, degrading
not only misfolded or oxidized proteins but also proteins with essential functions. The fact …
not only misfolded or oxidized proteins but also proteins with essential functions. The fact …