E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …
Targeted protein degradation by electrophilic PROTACs that stereoselectively and site-specifically engage DCAF1
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …
New opportunities for immunomodulation of the tumour microenvironment using chemical tools
JY Su, WH Li, YM Li - Chemical Society Reviews, 2022 - pubs.rsc.org
Immunotherapy is recognised as an attractive method for the treatment of cancer, and
numerous treatment strategies have emerged over recent years. Investigations of the tumour …
numerous treatment strategies have emerged over recent years. Investigations of the tumour …
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 …
Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …
therapeutic resistance, which is partially driven by the undruggable proteome. The …
Mitochondrial protease targeting chimeras for mitochondrial matrix protein degradation
D Wang, W Wang, L Fang, L Qi, Y Zhang… - Journal of the …, 2023 - ACS Publications
Targeted protein degradation (TPD) is an emerging technique for protein regulation.
Currently, all TPD developed in eukaryotic cells relies on either ubiquitin-proteasome or …
Currently, all TPD developed in eukaryotic cells relies on either ubiquitin-proteasome or …
DNA framework-engineered chimeras platform enables selectively targeted protein degradation
L Zhou, B Yu, M Gao, R Chen, Z Li, Y Gu, J Bian… - Nature …, 2023 - nature.com
A challenge in developing proteolysis targeting chimeras (PROTACs) is the establishment of
a universal platform applicable in multiple scenarios for precise degradation of proteins of …
a universal platform applicable in multiple scenarios for precise degradation of proteins of …
[HTML][HTML] Chemical tools targeting readers of lysine methylation
G Ortiz, TG Kutateladze, DG Fujimori - Current opinion in chemical biology, 2023 - Elsevier
Reader domains that recognize methylated lysine and arginine residues on histones play a
role in the recruitment, stabilization, and regulation of chromatin regulatory proteins …
role in the recruitment, stabilization, and regulation of chromatin regulatory proteins …
Covalent immune proximity-induction strategy using SuFEx-engineered bifunctional viral peptides
HM McCann, BPM Lake, KS Hoffman… - ACS Chemical …, 2022 - ACS Publications
Covalent antibody recruiting molecules (cARMs) constitute a proximity-inducing chemical
strategy to modulate the recognition and elimination of cancer cells by the immune system …
strategy to modulate the recognition and elimination of cancer cells by the immune system …