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 …

[HTML][HTML] Applications of protein ubiquitylation and deubiquitylation in drug discovery

Y Chen, H Xue, J Jin - Journal of Biological Chemistry, 2024 - Elsevier
The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …

PROTACs: Novel tools for improving immunotherapy in cancer

S Li, T Chen, J Liu, H Zhang, J Li, Z Wang, G Shang - Cancer Letters, 2023 - Elsevier
Posttranslational modifications (PTMs), such as phosphorylation, methylation, ubiquitination,
and acetylation, are important in governing protein expression levels. Proteolysis targeting …

Recent progress in degradation of membrane proteins by PROTACs and alternative targeted protein degradation techniques

S Chen, J Cui, H Chen, B Yu, S Long - European Journal of Medicinal …, 2023 - Elsevier
Targeted protein degradation (TPD) is one of the key strategies of current targeted cancer
therapy, and it can eliminate some of the root causes of cancer, and effectively avoid drug …

Discovery of NAFLD-improving agents by promoting the degradation of Keap1

M Qi, H Zhong, Z Cheng, S Chen, H Xiao… - Journal of Medicinal …, 2023 - ACS Publications
Activating Nrf2 through inhibiting Keap1 has been proven to alleviate oxidative stress and
related diseases, including nonalcoholic fatty liver disease (NAFLD). Traditional Keap1 …

Discovery of novel flavonoid-based CDK9 degraders for prostate cancer treatment via a PROTAC strategy

T Wu, Z Zhang, G Gong, Z Du, Y Xu, S Yu, F Ma… - European Journal of …, 2023 - Elsevier
CDK9 plays a vital role in regulating RNA transcription and significantly impacts the
expression of short-lived proteins such as Mcl-1 and c-Myc. Thus, targeting CDK9 holds …

Novel approaches to targeted protein degradation technologies in drug discovery

Y Xue, AA Bolinger, J Zhou - Expert opinion on drug discovery, 2023 - Taylor & Francis
Introduction Target protein degradation (TPD) provides a novel therapeutic modality, other
than inhibition, through the direct depletion of target proteins. Two primary human protein …

Age-related bone diseases: Role of inflammaging

J Bi, C Zhang, C Lu, C Mo, J Zeng, M Yao, B Jia… - Journal of …, 2024 - Elsevier
Bone aging is characterized by an imbalance in the physiological and pathological
processes of osteogenesis, osteoclastogenesis, adipogenesis, and chondrogenesis …

Discovery of a drug-like, natural product-inspired Dcaf11 ligand Chemotype

G Xue, J Xie, M Hinterndorfer, M Cigler… - Nature …, 2023 - nature.com
Targeted proteasomal and autophagic protein degradation, often employing bifunctional
modalities, is a new paradigm for modulation of protein function. In an attempt to explore …

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 …