Insight into Recent Advances in Degrading Androgen Receptor for Castration-Resistant Prostate Cancer

QH Chen, E Munoz, D Ashong - Cancers, 2024 - mdpi.com
Simple Summary A promising approach to combat aggressive prostate cancer involves
androgen receptor degraders, which break down the crucial protein driving cancer …

Revolutionizing drug targeting strategies: integrating artificial intelligence and structure-based methods in PROTAC development

Danishuddin, MS Jamal, KS Song, KW Lee, JJ Kim… - Pharmaceuticals, 2023 - mdpi.com
PROteolysis TArgeting Chimera (PROTAC) is an emerging technology in chemical biology
and drug discovery. This technique facilitates the complete removal of the target proteins …

Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders

C Bouvier, R Lawrence, F Cavallo, W Xolalpa… - Cells, 2024 - mdpi.com
Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …

Small-Molecule Approaches to Target Transcription Factors

H Cui, M Stilgenbauer… - Annual Review of Cancer …, 2024 - annualreviews.org
Dysregulated transcription factor activity is a defining feature of various cancer types. As
such, targeting oncogenic transcriptional dependency has long been pursued as a potential …

Novel Acyl Thiourea-Based Hydrophobic Tagging Degraders Exert Potent Anti-Influenza Activity through Two Distinct Endonuclease Polymerase Acidic-Targeted …

X Ma, X Wang, F Chen, W Zou, J Ren… - Journal of Medicinal …, 2024 - ACS Publications
The spread of the influenza virus has caused devastating pandemics and huge economic
losses worldwide. Antiviral drugs with diverse action modes are urgently required to …

Targeted Protein Degradation: Current and Emerging Approaches for E3 Ligase Deconvolution

Y Xiao, Y Yuan, Y Liu, Z Lin, G Zheng… - Journal of Medicinal …, 2024 - ACS Publications
Targeted protein degradation (TPD), including the use of proteolysis-targeting chimeras
(PROTACs) and molecular glue degraders (MGDs) to degrade proteins, is an emerging …

Targeted protein degradation in CNS disorders: a promising route to novel therapeutics?

S Kuemper, AG Cairns, K Birchall, Z Yao… - Frontiers in Molecular …, 2024 - frontiersin.org
Targeted protein degradation (TPD) is a rapidly expanding field, with various PROTACs
(proteolysis-targeting chimeras) in clinical trials and molecular glues such as …

Targeted Protein Degradation (TPD) for Immunotherapy: Understanding Proteolysis Targeting Chimera-Driven Ubiquitin-Proteasome Interactions

R Kamaraj, S Ghosh, S Das, S Sen, P Kumar… - Bioconjugate …, 2024 - ACS Publications
Targeted protein degradation or TPD, is rapidly emerging as a treatment that utilizes small
molecules to degrade proteins that cause diseases. TPD allows for the selective removal of …

Targeting kelch-like (KLHL) proteins: Achievements, challenges and perspectives

Y Zhou, Q Zhang, Z Zhao, X Hu, Q You… - European Journal of …, 2024 - Elsevier
Kelch-like proteins (KLHLs) are a large family of BTB-containing proteins. KLHLs function as
the substrate adaptor of Cullin 3-RING ligases (CRL3) to recognize substrates. KLHLs play …

Targeting the Undruggables----the Power of Protein Degraders

C Zhang, Y Liu, G Li, Z Yang, C Han, X Sun, C Sheng… - Science Bulletin, 2024 - Elsevier
Undruggable targets typically refer to a class of therapeutic targets that are difficult to target
through conventional methods or have not yet been targeted, but are of great clinical …