Rational discovery of molecular glue degraders via scalable chemical profiling
C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
[HTML][HTML] Expanding the landscape of E3 ligases for targeted protein degradation
Targeted protein degradation (TPD) is a rapidly developing field in chemical biology and
drug discovery. Various TPD modalities have emerged, with proteolysis-targeting chimeras …
drug discovery. Various TPD modalities have emerged, with proteolysis-targeting chimeras …
Unifying catalysis framework to dissect proteasomal degradation paradigms
FP Rodriguez-Rivera, SM Levi - ACS Central Science, 2021 - ACS Publications
Diverging from traditional target inhibition, proteasomal protein degradation approaches
have emerged as novel therapeutic modalities that embody distinct pharmacological profiles …
have emerged as novel therapeutic modalities that embody distinct pharmacological profiles …
Prey for the proteasome: targeted protein degradation—a medicinal chemist's perspective
LM Luh, U Scheib, K Juenemann… - Angewandte Chemie …, 2020 - Wiley Online Library
Targeted protein degradation (TPD), the ability to control a proteins fate by triggering its
degradation in a highly selective and effective manner, has created tremendous excitement …
degradation in a highly selective and effective manner, has created tremendous excitement …
Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase
K Hoegenauer, S An, J Axford… - ACS Medicinal …, 2023 - ACS Publications
Redirecting E3 ligases to neo-substrates, leading to their proteasomal disassembly, known
as targeted protein degradation (TPD), has emerged as a promising alternative to traditional …
as targeted protein degradation (TPD), has emerged as a promising alternative to traditional …
Molecular glue concept solidifies
K Baek, BA Schulman - Nature chemical biology, 2020 - nature.com
Molecular-glue-mediated proximity-induced degradation now allows unprecedented
therapeutic targeting of previously undruggable proteins. Structures showing how aryl …
therapeutic targeting of previously undruggable proteins. Structures showing how aryl …
Beyond proteolysis-targeting chimeric molecules: designing heterobifunctional molecules based on functional effectors
L Hua, Q Zhang, X Zhu, R Wang, Q You… - Journal of Medicinal …, 2022 - ACS Publications
In recent years, with the successful development of proteolysis-targeting chimeric molecules
(PROTACs), the potential of heterobifunctional molecules to contribute to reenvisioning drug …
(PROTACs), the potential of heterobifunctional molecules to contribute to reenvisioning drug …
A “click chemistry platform” for the rapid synthesis of bispecific molecules for inducing protein degradation
RP Wurz, K Dellamaggiore, H Dou… - Journal of medicinal …, 2018 - ACS Publications
Proteolysis targeting chimeras (PROTACs) are bispecific molecules containing a target
protein binder and an ubiquitin ligase binder connected by a linker. By recruiting an …
protein binder and an ubiquitin ligase binder connected by a linker. By recruiting an …
Induced protein degradation: an emerging drug discovery paradigm
Small-molecule drug discovery has traditionally focused on occupancy of a binding site that
directly affects protein function, and this approach typically precludes targeting proteins that …
directly affects protein function, and this approach typically precludes targeting proteins that …
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 …