[HTML][HTML] Recent advances in PROTACs for drug targeted protein research
Proteolysis-targeting chimera (PROTAC) is a heterobifunctional molecule. Typically,
PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and …
PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and …
Clinical translation of targeted protein degraders
NR Kong, LH Jones - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Targeted protein degradation (TPD) has emerged as a potentially transformational
therapeutic modality with considerable promise. Molecular glue degraders remodel the …
therapeutic modality with considerable promise. Molecular glue degraders remodel the …
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an
approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera …
approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera …
Targeting the epigenome to reinvigorate T cells for cancer immunotherapy
D Xiong, L Zhang, ZJ Sun - Military Medical Research, 2023 - Springer
Cancer immunotherapy using immune-checkpoint inhibitors (ICIs) has revolutionized the
field of cancer treatment; however, ICI efficacy is constrained by progressive dysfunction of …
field of cancer treatment; however, ICI efficacy is constrained by progressive dysfunction of …
Natural product-based proteolysis targeting chimeras (PROTACs)
Covering: upto 2022 Natural products have an embedded recognition of protein surfaces.
They possess this property as they are produced by biosynthetic enzymes and are …
They possess this property as they are produced by biosynthetic enzymes and are …
Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues
S Ramachandran, A Ciulli - Current Opinion in Structural Biology, 2021 - Elsevier
Highlights•E3 ligase machineries confer specificity to protein ubiquitination.•Multi-subunit
assembly and substrate recognition impact E3 ligase activity.•Molecular glues and …
assembly and substrate recognition impact E3 ligase activity.•Molecular glues and …
[HTML][HTML] Expanding the ligand spaces for E3 ligases for the design of protein degraders
Targeted protein degradation (TPD) has recently emerged as an exciting new drug modality.
However, the strategy of developing small molecule-based protein degraders has evolved …
However, the strategy of developing small molecule-based protein degraders has evolved …
Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules that
trigger the poly-ubiquitination of the protein of interest (POI) inducing its degradation via the …
trigger the poly-ubiquitination of the protein of interest (POI) inducing its degradation via the …
[HTML][HTML] Development of PROTACS degrading KRAS and SOS1
G Hamilton, MT Eggerstorfer, S Stickler - Oncology Research, 2024 - ncbi.nlm.nih.gov
The Kirsten rat sarcoma virus—son of sevenless 1 (KRAS-SOS1) axis drives tumor growth
preferentially in pancreatic, colon, and lung cancer. Now, KRAS G12C mutated tumors can …
preferentially in pancreatic, colon, and lung cancer. Now, KRAS G12C mutated tumors can …
Design and pharmaceutical applications of proteolysis-targeting chimeric molecules
Y Liang, KS Nandakumar, K Cheng - Biochemical pharmacology, 2020 - Elsevier
Abstract Proteolysis-targeting chimeras (PROTACs), the hetero-bifunctional compounds
containing a specific ligand to bind the target protein, a suitable linker, and an E3 ubiquitin …
containing a specific ligand to bind the target protein, a suitable linker, and an E3 ubiquitin …