Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …
proteasome system that recruits substrates such as the hypoxia inducible factor for …
Targeted protein degradation: expanding the toolbox
M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
The molecular details of cytokine signaling via the JAK/STAT pathway
More than 50 cytokines signal via the JAK/STAT pathway to orchestrate hematopoiesis,
induce inflammation and control the immune response. Cytokines are secreted …
induce inflammation and control the immune response. Cytokines are secreted …
The ZSWIM8 ubiquitin ligase mediates target-directed microRNA degradation
INTRODUCTION MicroRNAs (miRNAs) are short RNAs that direct widespread gene
repression in the cells of humans and other animals. Each miRNA associates with an …
repression in the cells of humans and other animals. Each miRNA associates with an …
Post-translational control of beige fat biogenesis by PRDM16 stabilization
Q Wang, H Li, K Tajima, ARP Verkerke, ZH Taxin… - Nature, 2022 - nature.com
Compelling evidence shows that brown and beige adipose tissue are protective against
metabolic diseases,. PR domain-containing 16 (PRDM16) is a dominant activator of the …
metabolic diseases,. PR domain-containing 16 (PRDM16) is a dominant activator of the …
[PDF][PDF] A cellular mechanism to detect and alleviate reductive stress
AG Manford, F Rodríguez-Pérez, KY Shih, Z Shi… - Cell, 2020 - cell.com
Metazoan organisms rely on conserved stress response pathways to alleviate adverse
conditions and preserve cellular integrity. Stress responses are particularly important in stem …
conditions and preserve cellular integrity. Stress responses are particularly important in stem …
[HTML][HTML] Structural insights into NEDD8 activation of cullin-RING ligases: conformational control of conjugation
DM Duda, LA Borg, DC Scott, HW Hunt, M Hammel… - Cell, 2008 - cell.com
Cullin-RING ligases (CRLs) comprise the largest ubiquitin E3 subclass, in which a central
cullin subunit links a substrate-binding adaptor with an E2-binding RING. Covalent …
cullin subunit links a substrate-binding adaptor with an E2-binding RING. Covalent …
[PDF][PDF] Structures of SPOP-substrate complexes: insights into molecular architectures of BTB-Cul3 ubiquitin ligases
In the largest E3 ligase subfamily, Cul3 binds a BTB domain, and an associated protein-
interaction domain such as MATH recruits substrates for ubiquitination. Here, we present …
interaction domain such as MATH recruits substrates for ubiquitination. Here, we present …
Targeting Cullin–RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation
In the last decade, the ubiquitin–proteasome system has emerged as a valid target for the
development of novel therapeutics. E3 ubiquitin ligases are particularly attractive targets …
development of novel therapeutics. E3 ubiquitin ligases are particularly attractive targets …