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 …
Chemistries of bifunctional PROTAC degraders
C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
Discovery of XL01126: a potent, fast, cooperative, selective, orally bioavailable, and blood–brain barrier penetrant PROTAC degrader of leucine-rich repeat kinase 2
X Liu, AF Kalogeropulou, S Domingos… - Journal of the …, 2022 - ACS Publications
Leucine-rich repeat kinase 2 (LRRK2) is one of the most promising targets for Parkinson's
disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors …
disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors …
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 …
environment within the cell. However, when natural proteostasis mechanisms are …
Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation
RP Wurz, H Rui, K Dellamaggiore… - Nature …, 2023 - nature.com
Targeted protein degradation via “hijacking” of the ubiquitin-proteasome system using
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …
durability of their effectiveness can be limited. Resistance to these therapies is often related …
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 …
Recent developments in epigenetic cancer therapeutics: clinical advancement and emerging trends
K Nepali, JP Liou - Journal of Biomedical Science, 2021 - Springer
Epigenetic drug discovery field has evidenced significant advancement in the recent times.
A plethora of small molecule inhibitors have progressed to clinical stage investigations and …
A plethora of small molecule inhibitors have progressed to clinical stage investigations and …
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 …
Direct-to-biology accelerates PROTAC synthesis and the evaluation of linker effects on permeability and degradation
CE Hendrick, JR Jorgensen, C Chaudhry… - ACS medicinal …, 2022 - ACS Publications
A platform to accelerate optimization of proteolysis targeting chimeras (PROTACs) has been
developed using a direct-to-biology (D2B) approach with a focus on linker effects. A large …
developed using a direct-to-biology (D2B) approach with a focus on linker effects. A large …