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An overview of PROTACs: a promising drug discovery paradigm
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
[HTML][HTML] Bivalent ligands for protein degradation in drug discovery
M Scheepstra, KFW Hekking, L van Hijfte… - Computational and …, 2019 - Elsevier
Targeting the “undruggable” proteome remains one of the big challenges in drug discovery.
Recent innovations in the field of targeted protein degradation and manipulation of the …
Recent innovations in the field of targeted protein degradation and manipulation of the …
Clp-targeting BacPROTACs impair mycobacterial proteostasis and survival
DM Hoi, S Junker, L Junk, K Schwechel, K Fischel… - Cell, 2023 - cell.com
Summary The ClpC1: ClpP1P2 protease is a core component of the proteostasis system in
mycobacteria. To improve the efficacy of antitubercular agents targeting the Clp protease …
mycobacteria. To improve the efficacy of antitubercular agents targeting the Clp protease …
Mechanistic and structural features of PROTAC ternary complexes
R Casement, A Bond, C Craigon, A Ciulli - Targeted protein degradation …, 2021 - Springer
The rapid and ever-growing advancements from within the field of proteolysis-targeting
chimeras (PROTAC)-induced protein degradation have driven considerable development to …
chimeras (PROTAC)-induced protein degradation have driven considerable development to …
Advances in targeted degradation of endogenous proteins
Protein silencing is often employed as a means to aid investigations in protein function and
is increasingly desired as a therapeutic approach. Several types of protein silencing …
is increasingly desired as a therapeutic approach. Several types of protein silencing …
Recent advances in targeted protein degraders as potential therapeutic agents
N Yang, B Kong, Z Zhu, F Huang, L Zhang, T Lu… - Molecular Diversity, 2024 - Springer
Targeted protein degradation (TPD) technology has gradually become widespread in the
past 20 years, which greatly boosts the development of disease treatment. Contrary to small …
past 20 years, which greatly boosts the development of disease treatment. Contrary to small …
PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs
The vast majority of currently marketed drugs rely on small molecules with an 'occupancy-
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …
Targeted protein degradation mechanisms
Y Zhang, C Loh, J Chen, N Mainolfi - Drug Discovery Today: Technologies, 2019 - Elsevier
Targeted protein degradation mediated by small molecule degraders represents an exciting
new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit …
new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit …
PROTAC: a novel drug delivery technology for targeting proteins in cancer cells
The treatment measures of malignant carcinomas are most important for human health. In
recent years the use of targeted therapy based on small molecule compounds and identical …
recent years the use of targeted therapy based on small molecule compounds and identical …
Exploring the Role of PROTACs for the Treatment of Breast Cancer
A Pannu, RK Goyal, S Goswami - … Protein Degradation: A Paradigm Shift in …, 2024 - Springer
The emergence of PROTACs as a transformative class of therapeutic agents has prompted
an intense investigation into their potential role in breast cancer. This chapter consolidates …
an intense investigation into their potential role in breast cancer. This chapter consolidates …