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 has created tremendous excitement in chemical biology and
… targeted protein degradation and discusses them from a medicinal chemist's perspective. …
… targeted protein degradation and discusses them from a medicinal chemist's perspective. …
Targeted protein degradation: mechanisms, strategies and application
L Zhao, J Zhao, K Zhong, A Tong, D Jia - … transduction and targeted …, 2022 - nature.com
… Targeted protein degradation (TPD), via the proteasomal and lysosomal pathways,
represent a novel tool to explore cellular pathways and a promising therapeutic approach. The …
represent a novel tool to explore cellular pathways and a promising therapeutic approach. The …
[PDF][PDF] Targeted protein degradation: A promise for undruggable proteins
KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
… However, recent advancements in the medicinal chemistry and chemical biology fields have
contributed significantly to change the traditional view of targeting such proteins. Since 2012…
contributed significantly to change the traditional view of targeting such proteins. Since 2012…
Selectivity through Targeted Protein Degradation (TPD) Miniperspective
A Gopalsamy - Journal of Medicinal Chemistry, 2022 - ACS Publications
… of degradation of one or more member proteins can lead to a … targeted protein degradation
field with respect to selectivity. … From our perspective, some of the key biological attributes to …
field with respect to selectivity. … From our perspective, some of the key biological attributes to …
Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry
E Génin, M Reboud-Ravaux… - Current topics in medicinal …, 2010 - ingentaconnect.com
… There are many opportunities for pharmacological intervention with protein degradation
catalyzed by proteasomes. Proteasome inhibitors are potential drugs for treating several …
catalyzed by proteasomes. Proteasome inhibitors are potential drugs for treating several …
Monomeric targeted protein degraders
EJ Hanan, J Liang, X Wang, RA Blake… - Journal of Medicinal …, 2020 - ACS Publications
… Perspective we first seek to provide an overview of methods for measuring protein degradation
… We will then highlight examples of protein degradation by monomeric small molecules, …
… We will then highlight examples of protein degradation by monomeric small molecules, …
The new direction of drug development: Degradation of undruggable targets through targeting chimera technology
X Liang, H Ren, F Han, R Liang… - Medicinal Research …, 2024 - Wiley Online Library
… glue technology are the hotspot applied to targeted protein degradation (TPD) using UPS in
recent … have taken a different approach, using the UPS to prevent target proteins from being …
recent … have taken a different approach, using the UPS to prevent target proteins from being …
PROTAC targeted protein degraders: the past is prologue
… foundational modalities for targeted protein degradation. Left-… perspective offers the first
comprehensive assessment of future potential targets with an eye towards protein degradation …
comprehensive assessment of future potential targets with an eye towards protein degradation …
Next-generation drugs and probes for chromatin biology: from targeted protein degradation to phase separation
K Cermakova, HC Hodges - Molecules, 2018 - mdpi.com
… However, this approach does not allow degradation of a specific target … for rapid protein
degradation in research settings (Figure 4). One such targeted protein degradation system is the …
degradation in research settings (Figure 4). One such targeted protein degradation system is the …
Rational multitargeted drug design strategy from the perspective of a medicinal chemist
X Li, X Li, F Liu, S Li, D Shi - Journal of Medicinal Chemistry, 2021 - ACS Publications
… If the two lead compounds do not have similar structures or the binding regions of the two
target proteins are not similar, the merged-pharmacophore strategy is difficult to implement. …
target proteins are not similar, the merged-pharmacophore strategy is difficult to implement. …
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