Structural diversity of ubiquitin E3 ligase
S Toma-Fukai, T Shimizu - Molecules, 2021 - mdpi.com
The post-translational modification of proteins regulates many biological processes. Their
dysfunction relates to diseases. Ubiquitination is one of the post-translational modifications …
dysfunction relates to diseases. Ubiquitination is one of the post-translational modifications …
E1 enzymes as therapeutic targets in cancer
SH Barghout, AD Schimmer - Pharmacological reviews, 2021 - ASPET
Post-translational modifications of cellular substrates with ubiquitin and ubiquitin-like
proteins (UBLs), including ubiquitin, SUMOs, and neural precursor cell–expressed …
proteins (UBLs), including ubiquitin, SUMOs, and neural precursor cell–expressed …
A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment
ML Hyer, MA Milhollen, J Ciavarri, P Fleming… - Nature medicine, 2018 - nature.com
The ubiquitin–proteasome system (UPS) comprises a network of enzymes that is
responsible for maintaining cellular protein homeostasis. The therapeutic potential of this …
responsible for maintaining cellular protein homeostasis. The therapeutic potential of this …
Discovery of TAK-981, a first-in-class inhibitor of SUMO-activating enzyme for the treatment of cancer
SP Langston, S Grossman, D England… - Journal of medicinal …, 2021 - ACS Publications
SUMOylation is a reversible post-translational modification that regulates protein function
through covalent attachment of small ubiquitin-like modifier (SUMO) proteins. The process of …
through covalent attachment of small ubiquitin-like modifier (SUMO) proteins. The process of …
Efficiency of the four proteasome subtypes to degrade ubiquitinated or oxidized proteins
J Abi Habib, E De Plaen, V Stroobant, D Zivkovic… - Scientific reports, 2020 - nature.com
The proteasome is responsible for selective degradation of proteins. It exists in mammalian
cells under four main subtypes, which differ by the combination of their catalytic subunits: the …
cells under four main subtypes, which differ by the combination of their catalytic subunits: the …
Preclinical evaluation of the selective small-molecule UBA1 inhibitor, TAK-243, in acute myeloid leukemia
SH Barghout, PS Patel, X Wang, GW Xu, S Kavanagh… - Leukemia, 2019 - nature.com
Acute myeloid leukemia (AML) is an aggressive hematologic malignancy for which new
therapeutic approaches are required. One such potential therapeutic strategy is to target the …
therapeutic approaches are required. One such potential therapeutic strategy is to target the …
Molecular mechanism of a covalent allosteric inhibitor of SUMO E1 activating enzyme
Z Lv, L Yuan, JH Atkison, KM Williams, R Vega… - Nature …, 2018 - nature.com
E1 enzymes activate ubiquitin (Ub) and ubiquitin-like modifiers (Ubls) in the first step of
Ub/Ubl conjugation cascades and represent potential targets for therapeutic intervention in …
Ub/Ubl conjugation cascades and represent potential targets for therapeutic intervention in …
Structural basis for adenylation and thioester bond formation in the ubiquitin E1
ZS Hann, C Ji, SK Olsen, X Lu… - Proceedings of the …, 2019 - National Acad Sciences
The ubiquitin (Ub) and Ub-like (Ubl) protein-conjugation cascade is initiated by E1 enzymes
that catalyze Ub/Ubl activation through C-terminal adenylation, thioester bond formation with …
that catalyze Ub/Ubl activation through C-terminal adenylation, thioester bond formation with …
Crystal structure of a human ubiquitin E1–ubiquitin complex reveals conserved functional elements essential for activity
Z Lv, KM Williams, L Yuan, JH Atkison… - Journal of Biological …, 2018 - ASBMB
Ubiquitin (Ub) signaling plays a key regulatory role in nearly every aspect of eukaryotic
biology and is initiated by E1 enzymes that activate and transfer Ub to E2 Ub-conjugating …
biology and is initiated by E1 enzymes that activate and transfer Ub to E2 Ub-conjugating …
Differential oligomerization of the deubiquitinases USP25 and USP28 regulates their activities
Deubiquitinases have emerged as promising drug targets for cancer therapy. The two DUBs
USP25 and USP28 share high similarity but vary in their cellular functions. USP28 is known …
USP25 and USP28 share high similarity but vary in their cellular functions. USP28 is known …