Tumor biomarkers for diagnosis, prognosis and targeted therapy

Y Zhou, L Tao, J Qiu, J Xu, X Yang, Y Zhang… - Signal transduction and …, 2024 - nature.com
Tumor biomarkers, the substances which are produced by tumors or the body's responses to
tumors during tumorigenesis and progression, have been demonstrated to possess critical …

Combinatorial strategies to target RAS-driven cancers

N Perurena, L Situ, K Cichowski - Nature Reviews Cancer, 2024 - nature.com
Although RAS was formerly considered undruggable, various agents that inhibit RAS or
specific RAS oncoproteins have now been developed. Indeed, the importance of directly …

Current advances and development strategies of orally bioavailable PROTACs

S Zeng, Y Ye, H **a, J Min, J Xu, Z Wang, Y Pan… - European Journal of …, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …

From bench to bedside: current development and emerging trend of KRAS-targeted therapy

Y Chen, Q Liu, H **e, J Ding - Acta Pharmacologica Sinica, 2024 - nature.com
Kirsten rat sarcoma 2 viral oncogene homolog (KRAS) is the most frequently mutated
oncogene in human cancers with mutations predominantly occurring in codon 12. These …

[HTML][HTML] Characteristic roadmap of linker governs the rational design of PROTACs

Y Dong, T Ma, T Xu, Z Feng, Y Li, L Song, X Yao… - … Pharmaceutica Sinica B, 2024 - Elsevier
Proteolysis targeting chimera (PROTAC) technology represents a groundbreaking
development in drug discovery, leveraging the ubiquitin‒proteasome system to specifically …

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 …

Discovery of a first-in-class degrader for the lipid kinase PIKfyve

C Li, Y Qiao, X Jiang, L Liu, Y Zheng… - Journal of Medicinal …, 2023 - ACS Publications
The phosphoinositide kinase PIKfyve has emerged as a new potential therapeutic target in
various cancers. However, limited clinical progress has been achieved with PIKfyve …

Discovery of novel BCL6-Targeting PROTACs with effective antitumor activities against DLBCL in vitro and in vivo

D Mi, C Li, Y Li, M Yao, Y Li, K Hong, C **e… - European journal of …, 2024 - Elsevier
The transcriptional repressor B cell lymphoma 6 (BCL6) plays a critical role in driving
tumorigenesis of diffuse large B-cell lymphoma (DLBCL). However, the therapeutic potential …

Inhibition of son of sevenless homologue 1 (SOS1): promising therapeutic treatment for KRAS-mutant cancers

T Chen, X Tang, Z Wang, F Feng, C Xu, Q Zhao… - European Journal of …, 2023 - Elsevier
Kristen rat sarcoma (KRAS) is one of the most common oncogenes in human cancers. As a
guanine nucleotide exchange factor, Son of Sevenless Homologue 1 (SOS1) represents a …

Current advances and development strategies of targeting son of sevenless 1 (SOS1) in drug discovery

J Wu, X Li, C Wu, Y Wang, J Zhang - European Journal of Medicinal …, 2024 - Elsevier
Abstract The Son of Sevenless 1 (SOS1) guanine nucleotide exchange factor, prevalent
across eukaryotic species, plays a pivotal role in facilitating the attachment of RAS protein to …