[HTML][HTML] Degradation of proteins by PROTACs and other strategies

Y Wang, X Jiang, F Feng, W Liu, H Sun - Acta Pharmaceutica Sinica B, 2020 - Elsevier
Blocking the biological functions of scaffold proteins and aggregated proteins is a
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …

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, 2024 - 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 …

E3 ligases: a potential multi-drug target for different types of cancers and neurological disorders

KM Saravanan, M Kannan, P Meera… - Future Medicinal …, 2022 - Taylor & Francis
Ubiquitylation is a posttranslational modification of proteins that is necessary for a variety of
cellular processes. E1 ubiquitin activating enzyme, E2 ubiquitin conjugating enzyme, and E3 …

Discovery of neddylation E2s inhibitors with therapeutic activity

MAA Mamun, Y Liu, YP Geng, YC Zheng, Y Gao… - Oncogenesis, 2023 - nature.com
Neddylation is the writing of monomers or polymers of neural precursor cells expressed
developmentally down-regulated 8 (NEDD8) to substrate. For neddylation to occur, three …

Therapeutic Editing of the TP53 Gene: Is CRISPR/Cas9 an Option?

R Mirgayazova, R Khadiullina, V Chasov… - Genes, 2020 - mdpi.com
The TP53 gene encodes the transcription factor and oncosuppressor p53 protein that
regulates a multitude of intracellular metabolic pathways involved in DNA damage repair …

The tripartite nexus: autophagy, cancer, and tripartite motif-containing protein family members

MA Mandell, B Saha, TA Thompson - Frontiers in pharmacology, 2020 - frontiersin.org
Autophagy is a cellular degradative process that has multiple important actions in cancer.
Autophagy modulation is under consideration as a promising new approach to cancer …

Key players in the mutant p53 team: Small molecules, gene editing, immunotherapy

V Chasov, R Mirgayazova, E Zmievskaya… - Frontiers in …, 2020 - frontiersin.org
The transcription factor p53 is a key tumor suppressor that is inactivated in almost all
cancers due to either point mutations in the TP53 gene or overexpression of its negative …

Isatin-Schiff base-copper (II) complex induces cell death in p53-positive tumors

E Bulatov, R Sayarova, R Mingaleeva… - Cell Death …, 2018 - nature.com
Medicinal bioinorganic chemistry is a thriving field of drug research for cancer treatment.
Transition metal complexes coordinated to essential biological scaffolds represent a highly …

[HTML][HTML] Novel approaches for the rational design of PROTAC linkers

A Zagidullin, V Milyukov, A Rizvanov… - Exploration of Targeted …, 2020 - ncbi.nlm.nih.gov
Proteolysis targeting chimeras (PROTACs) represent a promising class of hetero-bivalent
molecules that facilitate ubiquitination of a target protein by simultaneously binding and …

Discovery of a Natural Ent-Kaurene Diterpenoid Oridonin as an E3 Ligase Recruiter for PROTACs

J Huang, X Fu, F Qiu, Z Liang, C Cao… - Journal of the …, 2024 - ACS Publications
PROTACs have emerged as a therapeutic modality for the targeted degradation of proteins
of interest (POIs). Central to PROTAC technology are the E3 ligase recruiters, yet only a few …