Semisynthesis of autophagy protein LC3 conjugates
Autophagy is a conserved catabolic process involved in the elimination of proteins,
organelles and pathogens. Autophagosome formation is the key process in autophagy …
organelles and pathogens. Autophagosome formation is the key process in autophagy …
[PDF][PDF] Identification and selectivity profiling of small-molecule degraders via multi-omics approaches
NS Scholes, C Mayor-Ruiz, GE Winter - Cell Chemical Biology, 2021 - cell.com
The therapeutic modality of targeted protein degradation promises to overcome limitations of
traditional pharmacology. Small-molecule degraders recruit disease-causing proteins to E3 …
traditional pharmacology. Small-molecule degraders recruit disease-causing proteins to E3 …
[HTML][HTML] Discovery of E3 ligase ligands for target protein degradation
Target protein degradation has emerged as a promising strategy for the discovery of novel
therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a …
therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a …
PROTACting the kinome with covalent warheads
The dawn of targeted degradation using proteolysis-targeting chimeras (PROTACs) against
recalcitrant proteins has prompted numerous efforts to develop complementary drugs …
recalcitrant proteins has prompted numerous efforts to develop complementary drugs …
Connecting the dots: combined control of endocytic recycling and degradation
E MacDonald, B Savage, T Zech - Biochemical Society …, 2020 - portlandpress.com
Endocytosis is an essential process where proteins and lipids are internalised from the
plasma membrane in membrane-bound carriers, such as clathrin-coated vesicles. Once …
plasma membrane in membrane-bound carriers, such as clathrin-coated vesicles. Once …
Targeted protein knockdown using small molecule degraders
K Raina, CM Crews - Current opinion in chemical biology, 2017 - Elsevier
Highlights•Small molecule protein degraders (PROTACs) can target the 'undruggable'
proteome.•Ligands that bind the target anywhere on its surface can be used to make …
proteome.•Ligands that bind the target anywhere on its surface can be used to make …
E3-specific degrader discovery by dynamic tracing of substrate receptor abundance
Targeted protein degradation (TPD) is a new pharmacology based on small-molecule
degraders that induce proximity between a protein of interest (POI) and an E3 ubiquitin …
degraders that induce proximity between a protein of interest (POI) and an E3 ubiquitin …
High-throughput quantitative assay technologies for accelerating the discovery and optimization of targeted protein degradation therapeutics
JR Simard, L Lee, E Vieux, R Improgo… - … the Science of Drug …, 2021 - journals.sagepub.com
The aberrant regulation of protein expression and function can drastically alter cellular
physiology and lead to numerous pathophysiological conditions such as cancer …
physiology and lead to numerous pathophysiological conditions such as cancer …
Aptamer‐LYTACs for targeted degradation of extracellular and membrane proteins
Y Wu, B Lin, Y Lu, L Li, K Deng, S Zhang… - Angewandte Chemie …, 2023 - Wiley Online Library
Recently, lysosome targeting chimeras (LYTACs) have emerged as a promising technology
that expands the scope of targeted protein degradation to extracellular targets. However, the …
that expands the scope of targeted protein degradation to extracellular targets. However, the …
Assessing different E3 ligases for small molecule induced protein ubiquitination and degradation
P Ottis, M Toure, PM Cromm, E Ko… - ACS chemical …, 2017 - ACS Publications
Proteolysis targeting chimera (PROTAC) technology, the recruitment of E3 ubiquitin ligases
to induce the degradation of a protein target, is rapidly impacting chemical biology, as well …
to induce the degradation of a protein target, is rapidly impacting chemical biology, as well …