[HTML][HTML] Targeted protein degradation tools: overview and future perspectives

Y Prozzillo, G Fattorini, MV Santopietro, L Suglia… - Biology, 2020 - mdpi.com
Simple Summary Gene inactivation is a powerful strategy to study the function of specific
proteins in the context of cellular physiology that can be applied for only non-essential …

Transmembrane dislocases: a second chance for protein targeting

V Dederer, MK Lemberg - Trends in Cell Biology, 2021 - cell.com
Precise distribution of proteins is essential to sustain the viability of cells. A complex network
of protein synthesis and targeting factors cooperate with protein quality control systems to …

Molecular glues: the adhesive connecting targeted protein degradation to the clinic

JM Sasso, R Tenchov, DS Wang, LS Johnson… - Biochemistry, 2022 - ACS Publications
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …

Targeted protein degradation at the host–pathogen interface

C Grohmann, DS Marapana, G Ebert - Molecular Microbiology, 2022 - Wiley Online Library
Infectious diseases remain a major burden to global health. Despite the implementation of
successful vaccination campaigns and efficient drugs, the increasing emergence of …

Targeted protein degradation

P Zhou - Current opinion in chemical biology, 2005 - Elsevier
The ubiquitin-proteasome pathway plays a major role in cellular protein destruction and
regulates fundamental cellular processes such as the cell cycle, cell signaling, and …

[HTML][HTML] Protein degradation technology: a strategic paradigm shift in drug discovery

H Li, J Dong, M Cai, Z Xu, XD Cheng, JJ Qin - Journal of Hematology & …, 2021 - Springer
Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely
used strategy for treating malignant tumors. However, most intracellular proteins have been …

Targeted protein degradation: elements of PROTAC design

SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …

Ligand-induced genetic degradation as a tool for target validation

A Yesbolatova, Y Tominari, MT Kanemaki - Drug Discovery Today …, 2019 - Elsevier
Targeted protein degraders, known as proteolysis targeting chimeras (PROTACs), are
drawing more attention as next-generation drugs to target currently undruggable proteins …

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

TH Pillow, P Adhikari, RA Blake, J Chen… - …, 2020 - Wiley Online Library
The ability to selectively degrade proteins with bifunctional small molecules has the potential
to fundamentally alter therapy in a variety of diseases. However, the relatively large size of …

MERIT, a cellular system coordinating lysosomal repair, removal and replacement

J Jia, A Claude-Taupin, Y Gu, SW Choi, R Peters… - Autophagy, 2020 - Taylor & Francis
Membrane integrity is essential for cellular survival and function. The spectrum of
mechanisms protecting cellular and intracellular membranes is not fully known. Our recent …