PROTAC targeted protein degraders: the past is prologue
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 …
tackle disease-causing proteins that have historically been highly challenging to target with …
Targeted protein degradation: mechanisms, strategies and application
L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …
development and application of protein activity modulators, particularly inhibitors, has been …
E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …
Therapeutic potential of pyrrole and pyrrolidine analogs: an update
N Jeelan Basha, SM Basavarajaiah, K Shyamsunder - Molecular Diversity, 2022 - Springer
The chemistry of nitrogen-containing heterocyclic compound pyrrole and pyrrolidine has
been a versatile field of study for a long time for its diverse biological and medicinal …
been a versatile field of study for a long time for its diverse biological and medicinal …
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 …
Exploring the target scope of KEAP1 E3 ligase-based PROTACs
Targeted protein degradation (TPD) uses small molecules to recruit E3 ubiquitin ligases into
the proximity of proteins of interest, inducing ubiquitination-dependent degradation. A major …
the proximity of proteins of interest, inducing ubiquitination-dependent degradation. A major …
Progress and challenges in targeted protein degradation for neurodegenerative disease therapy
Y Fang, J Wang, M Zhao, Q Zheng, C Ren… - Journal of Medicinal …, 2022 - ACS Publications
Neurodegenerative diseases (NDs) are currently incurable diseases that cause progressive
degeneration of nerve cells. Many of the disease-causing proteins of NDs are “undruggable” …
degeneration of nerve cells. Many of the disease-causing proteins of NDs are “undruggable” …
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 …
targeting chimera (PROTAC) was first reported. Various of distinctive degradation …
Regulation of host-pathogen interactions via the ubiquitin system
R Mukherjee, I Dikic - Annual Review of Microbiology, 2022 - annualreviews.org
Ubiquitination is a posttranslational modification that regulates a multitude of cellular
functions. Pathogens, such as bacteria and viruses, have evolved sophisticated …
functions. Pathogens, such as bacteria and viruses, have evolved sophisticated …