An overview of PROTACs: a promising drug discovery paradigm

Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
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 …

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 …

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 …

Advances in targeted degradation of endogenous proteins

S Röth, LJ Fulcher, GP Sapkota - Cellular and Molecular Life Sciences, 2019 - Springer
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 …

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 …

PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs

M Maneiro, E De Vita, D Conole, CS Kounde… - Progress in medicinal …, 2021 - Elsevier
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 …

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 …

PROTAC: a novel drug delivery technology for targeting proteins in cancer cells

R Bala, RK Sindhu, R Madaan… - Current Drug Discovery …, 2023 - benthamdirect.com
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 …

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 …