[HTML][HTML] Advancing targeted protein degradation for metabolic diseases therapy

QQ Zhou, HT Xiao, F Yang, YD Wang, P Li… - Pharmacological …, 2023 - Elsevier
The development and application of traditional drugs represented by small molecule
chemical drugs and biological agents, especially inhibitors, have become the mainstream …

The recent advance of Interleukin-1 receptor associated kinase 4 inhibitors for the treatment of inflammation and related diseases

YR Bai, WG Yang, XH Hou, DD Shen, SN Zhang… - European Journal of …, 2023 - Elsevier
The interleukin-1 receptor associated kinase 4 (IRAK-4) is a member of serine-threonine
kinase family, which plays an important role in the regulation of interleukin-1 receptors (IL …

Discovery of BWA-522, a first-in-class and orally bioavailable PROTAC degrader of the androgen receptor targeting N-terminal domain for the treatment of prostate …

B Zhang, C Liu, Z Yang, S Zhang, X Hu… - Journal of medicinal …, 2023 - ACS Publications
We report small molecular PROTAC compounds targeting the androgen receptor N-terminal
domain (AR-NTD), which were obtained by tethering AR-NTD antagonists and different …

Structure-activity relationship study of RSL3-based GPX4 degraders and its potential noncovalent optimization

C Zheng, C Wang, D Sun, H Wang, B Li, G Liu… - European Journal of …, 2023 - Elsevier
Ferroptosis is an iron-dependent, non-apoptotic form of cell death involving in various
disease processes. Mechanistically, glutathione peroxidase 4 (GPX4) which belongs to the …

Targeting epigenetic modifications in Parkinson's disease therapy

D Zhang, J Zhang, Y Wang, G Wang… - Medicinal Research …, 2023 - Wiley Online Library
Parkinson's disease (PD) is a multifactorial disease due to a complex interplay between
genetic and epigenetic factors. Recent efforts shed new light on the epigenetic mechanisms …

Application of novel degraders employing autophagy for expediting medicinal research

X Li, Q Liu, X Xie, C Peng, Q Pang, B Liu… - Journal of Medicinal …, 2023 - ACS Publications
Targeted protein degradation (TPD) technology is based on a unique pharmacological
mechanism that has profoundly revolutionized medicinal research by overcoming limitations …

Research in the field of drug design and development

G Biala, E Kedzierska, M Kruk-Slomka… - Pharmaceuticals, 2023 - mdpi.com
The processes used by academic and industrial scientists to discover new drugs have
recently experienced a true renaissance, with many new and exciting techniques being …

Targeting the epidermal growth factor receptor with molecular degraders: State-of-the-art and future opportunities

P Maity, J Chatterjee, KT Patil, S Arora… - Journal of Medicinal …, 2023 - ACS Publications
Epidermal growth factor receptor (EGFR) is an oncogenic drug target and plays a critical role
in several cellular functions including cancer cell growth, survival, proliferation …

Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease

Y Li, S Lin, Z Gu, L Chen, B He - Bioorganic & Medicinal Chemistry Letters, 2022 - Elsevier
Alzheimer's disease (AD) as the most prevalent dementia type has become one of the
greatest threats to the health and life of the elder people worldwide. Although there has …

A comprehensive review of BET-targeting PROTACs for cancer therapy

XL Zhou, F Zhao, YT Xu, YY Guan, T Yu… - Bioorganic & Medicinal …, 2022 - Elsevier
Targeted protein degradation using proteolysis-targeting chimeras (PROTACs) has
emerged as an effective strategy for drug discovery, given their unique advantages over …