Targeted protein degradation directly engaging lysosomes or proteasomes

J Kim, I Byun, H Joh, HJ Kim, MJ Lee - Chemical Society Reviews, 2024 - pubs.rsc.org
Targeted protein degradation (TPD) has been established as a viable alternative to
attenuate the function of a specific protein of interest in both biological and clinical contexts …

Triazole-fused pyrimidines in target-based anticancer drug discovery

XJ Dai, LP Xue, SK Ji, Y Zhou, Y Gao, YC Zheng… - European Journal of …, 2023 - Elsevier
In recent decades, the development of targeted drugs has featured prominently in the
treatment of cancer, which is among the major causes of mortality globally. Triazole-fused …

Epigenetic Reader Bromodomain-Containing Protein 4 in Aging-Related Vascular Pathologies and Diseases: Molecular Basis, Functional Relevance, and Clinical …

X Zheng, K Diktonaite, H Qiu - Biomolecules, 2023 - mdpi.com
Aging is a key independent risk factor of various vascular diseases, for which the regulatory
mechanisms remain largely unknown. Bromodomain-containing protein 4 (BRD4) is a …

Lysine-specific demethylase 7A (KDM7A): A potential target for disease therapy

CY Li, YJ Liu, F Tao, RY Chen, JJ Shi, JF Lu… - Biochemical …, 2023 - Elsevier
Histone demethylation is a kind of epigenetic modification mediated by a variety of enzymes
and participates in regulating multiple physiological and pathological events. Lysine-specific …

Targeted Protein O-GlcNAcylation Using Bifunctional Small Molecules

B Ma, KS Khan, T Xu, J Xeque Amada… - Journal of the …, 2024 - ACS Publications
Protein O-linked β-N-acetylglucosamine modification (O-GlcNAcylation) plays a crucial role
in regulating essential cellular processes. The disruption of the homeostasis of O …

Targeting BRD4: Potential therapeutic strategy for head and neck squamous cell carcinoma

V Yongprayoon, N Wattanakul… - Oncology …, 2024 - spandidos-publications.com
As a member of BET (bromodomain and extra-terminal) protein family, BRD4 (bromodomain-
containing protein 4) is a chromatin-associated protein that interacts with acetylated histones …

Lysine deserts and cullin-RING ligase receptors: Navigating untrodden paths in proteostasis

NA Szulc, M Piechota, L Biriczová, P Thapa… - Iscience, 2023 - cell.com
The ubiquitin-proteasome system (UPS) governs the degradation of proteins by
ubiquitinating their lysine residues. Our study focuses on lysine deserts-regions in proteins …

Elevating PLK1 overcomes BETi resistance in prostate cancer via triggering BRD4 phosphorylation-dependent degradation in mitosis

Y Zhang, KW Fong, F Mao, R Wang, DB Allison… - Cell Reports, 2024 - cell.com
Summary Bromodomain-containing protein 4 (BRD4) has emerged as a promising
therapeutic target in prostate cancer (PCa). Understanding the mechanisms of BRD4 …

Emerging role of plant-based dietary components in post-translational modifications associated with colorectal cancer

C Rodríguez-García, F Gutiérrez-Santiago - Life, 2023 - mdpi.com
Colorectal cancer (CRC) is one of the most common cancers worldwide. Its main modifiable
risk factors are diet, alcohol consumption, and smoking. Thus, the right approach through …

AP-2δ is the most relevant target of AP-2 family-focused cancer therapy and affects genome organization

D Kołat, LY Zhao, M Kciuk, E Płuciennik… - Cells, 2022 - mdpi.com
Formerly hailed as “undruggable” proteins, transcription factors (TFs) are now under
investigation for targeted therapy. In cancer, this may alter, inter alia, immune evasion or …