Protein degraders enter the clinic—a new approach to cancer therapy
D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
Small-molecule discovery through DNA-encoded libraries
AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …
discovery platforms that enable access to chemical diversity and can quickly reveal new …
[HTML][HTML] Expanding PROTACtable genome universe of E3 ligases
Proteolysis-targeting chimera (PROTAC) and other targeted protein degradation (TPD)
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …
Rational chemical design of molecular glue degraders
ES Toriki, JW Papatzimas, K Nishikawa… - ACS central …, 2023 - ACS Publications
Targeted protein degradation with molecular glue degraders has arisen as a powerful
therapeutic modality for eliminating classically undruggable disease-causing proteins …
therapeutic modality for eliminating classically undruggable disease-causing proteins …
[HTML][HTML] Chemoproteomics-enabled discovery of a covalent molecular glue degrader targeting NF-κB
EA King, Y Cho, NS Hsu, D Dovala, JM McKenna… - Cell chemical …, 2023 - cell.com
Targeted protein degradation has arisen as a powerful therapeutic modality for degrading
disease targets. While proteolysis-targeting chimera (PROTAC) design is more modular, the …
disease targets. While proteolysis-targeting chimera (PROTAC) design is more modular, the …
Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design
D Mi, Y Li, H Gu, Y Li, Y Chen - European Journal of Medicinal Chemistry, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) as an emerging drug discovery modality has
been extensively concerned in recent years. Over 20 years development, accumulated …
been extensively concerned in recent years. Over 20 years development, accumulated …
Targeted protein degradation through E2 recruitment
N Forte, D Dovala, MJ Hesse, JM McKenna… - ACS chemical …, 2023 - ACS Publications
Targeted protein degradation (TPD) with proteolysis targeting chimeras (PROTACs),
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …
[HTML][HTML] Antiviral PROTACs: Opportunity borne with challenge
J Liang, Y Wu, K Lan, C Dong, S Wu, S Li, HB Zhou - Cell Insight, 2023 - Elsevier
Proteolysis targeting chimera (PROTAC) degradation of pathogenic proteins by hijacking of
the ubiquitin-proteasome-system has become a promising strategy in drug design. The …
the ubiquitin-proteasome-system has become a promising strategy in drug design. The …
[HTML][HTML] Proteomic approaches advancing targeted protein degradation
G Sathe, GP Sapkota - Trends in pharmacological sciences, 2023 - cell.com
Targeted protein degradation (TPD) is an emerging modality for research and therapeutics.
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …