Semisynthesis of autophagy protein LC3 conjugates

A Yang, I Hacheney, YW Wu - Bioorganic & medicinal chemistry, 2017 - Elsevier
Autophagy is a conserved catabolic process involved in the elimination of proteins,
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 …

[HTML][HTML] Discovery of E3 ligase ligands for target protein degradation

J Lee, Y Lee, YM Jung, JH Park, HS Yoo, J Park - Molecules, 2022 - mdpi.com
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 …

PROTACting the kinome with covalent warheads

DR Chatterjee, S Kapoor, M Jain, R Das… - Drug Discovery …, 2023 - Elsevier
The dawn of targeted degradation using proteolysis-targeting chimeras (PROTACs) against
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 …

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 …

E3-specific degrader discovery by dynamic tracing of substrate receptor abundance

A Hanzl, E Barone, S Bauer, H Yue… - Journal of the …, 2023 - ACS Publications
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 …

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 …

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 …

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 …