Targeting breast cancer: An overlook on current strategies

D Iacopetta, J Ceramella, N Baldino… - International Journal of …, 2023 - mdpi.com
Breast cancer (BC) is one of the most widely diagnosed cancers and a leading cause of
cancer death among women worldwide. Globally, BC is the second most frequent cancer …

Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications

Q Li, L Zhou, S Qin, Z Huang, B Li, R Liu… - European Journal of …, 2023 - Elsevier
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …

Insulin-like growth factor 2 (IGF2)-fused lysosomal targeting chimeras for degradation of extracellular and membrane proteins

B Zhang, RK Brahma, L Zhu, J Feng, S Hu… - Journal of the …, 2023 - ACS Publications
Targeted degradation of the cell-surface and extracellular proteins via the endogenous
lysosomal degradation pathways, such as lysosome-targeting chimeras (LYTACs), has …

ARE-PROTACs enable co-degradation of an Nrf2–MafG heterodimer

J Ji, S Ma, Y Zhu, J Zhao, Y Tong, Q You… - Journal of Medicinal …, 2023 - ACS Publications
Proteolysis-targeting chimera (PROTAC) technology has emerged as a potential strategy to
degrade “undruggable” proteins in recent years. Nrf2, an aberrantly activated transcription …

Sequential azidation/azolation of prenylated derivatives and a click reaction enable selective labeling and degradation of RAS protein

Y Gan, X Chen, Y Li, Y Guo… - The Journal of Organic …, 2023 - ACS Publications
We propose the introduction of the azido and azo-functionalities into prenylated derivatives
under mild conditions in a selective and efficient way. Upon protocol establishment and …

Discovery of effective dual Protac degraders for neurodegenerative disease-associated aggregates

W Zhu, W Zhang, J Chen, Y Tong, F Xu… - Journal of Medicinal …, 2024 - ACS Publications
The aggregation of specific proteins is a histopathological hallmark in various
neurodegenerative diseases (NDs), among which Alpha-synuclein (α-Syn) and tau have …

The new direction of drug development: Degradation of undruggable targets through targeting chimera technology

X Liang, H Ren, F Han, R Liang… - Medicinal Research …, 2024 - Wiley Online Library
Imbalances in protein and noncoding RNA levels in vivo lead to the occurrence of many
diseases. In addition to the use of small molecule inhibitors and agonists to restore these …

Journey of von hippel-lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders

N Setia, HTA Almuqdadi, M Abid - European Journal of Medicinal Chemistry, 2023 - Elsevier
The scientific community has shown considerable interest in proteolysis-targeting chimeras
(PROTACs) in the last decade, indicating their remarkable potential as a means of achieving …

Recent Advances in Bioconjugated Transition Metal Complexes for Cancer Therapy

E Bortolamiol, F Visentin, T Scattolin - Applied Sciences, 2023 - mdpi.com
The introduction of biologically relevant organic moieties in the coordination sphere of
transition metal complexes has recently become a well-established strategy to increase the …

A cocktail therapeutic strategy based on clofarabine-containing aptamer-PROTAC for enhanced cancer therapy

Z Chen, M Chen, R Liu, H Fan, J Zhang - Chemical Communications, 2023 - pubs.rsc.org
By introducing a therapeutic nucleoside analogue tail to the parent Aptamer-PROTACs, a
PROTAC-cocktail system (ApTCs-3X) was designed and evaluated. ApTCs-3X exhibited …