Blocking non-enzymatic functions by PROTAC-mediated targeted protein degradation

D Sun, J Zhang, G Dong, S He… - Journal of Medicinal …, 2022 - ACS Publications
The non-enzymatic functions of target proteins play key roles in the regulation of various cell
signaling pathways and are closely related to numerous human diseases. However …

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 …

[HTML][HTML] Emerging Strategies in Proteolysis-Targeting Chimeras (PROTACs): Highlights from 2022

R Tamatam, D Shin - International Journal of Molecular Sciences, 2023 - mdpi.com
Targeted protein degradation (TPD) is a promising therapeutic modality that has garnered
attention in academic, industrial, and pharmaceutical research for treating diseases such as …

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 …

[HTML][HTML] PROTAC targeted protein degraders: the past is prologue

M Békés, DR Langley, CM Crews - Nature Reviews Drug Discovery, 2022 - nature.com
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

[PDF][PDF] Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …

The state of the art of PROTAC technologies for drug discovery

C Wang, C Zheng, H Wang, L Zhang, Z Liu… - European Journal of …, 2022 - Elsevier
Protein degradation technology has progressed dramatically since 2001 when proteolysis
targeting chimera (PROTAC) was first reported. Various of distinctive degradation …

[HTML][HTML] PROTACs: emerging targeted protein degradation approaches for advanced druggable strategies

NI Sincere, K Anand, S Ashique, J Yang, C You - Molecules, 2023 - mdpi.com
A potential therapeutic strategy to treat conditions brought on by the aberrant production of a
disease-causing protein is emerging for targeted protein breakdown using the PROTACs …

[PDF][PDF] PROTACs: an emerging therapeutic modality in precision medicine

DA Nalawansha, CM Crews - Cell chemical biology, 2020 - cell.com
Targeted protein degradation (TPD) has emerged as an exciting new era in chemical
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …

PROTACS: A technology with a gold rush-like atmosphere

YW Wang, L Lan, M Wang, JY Zhang, YH Gao… - European Journal of …, 2023 - Elsevier
Abnormally expressed or malfunctioning proteins may affect or even damage cells, leading
to the onset of diseases. Proteolysis targeting chimera (PROTAC) technology has been …