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 …
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 …
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. …
[HTML][HTML] Multi-target pharmacology: possibilities and limitations of the “skeleton key approach” from a medicinal chemist perspective
A Talevi - Frontiers in pharmacology, 2015 - frontiersin.org
… selectivity, eg, the drug target must be exclusively or preferentially expressed … , targeted
proteins in a pathogen should not have homologous proteins in the host or homologous proteins …
proteins in a pathogen should not have homologous proteins in the host or homologous proteins …
Overview of recent strategic advances in medicinal chemistry
G Wu, T Zhao, D Kang, J Zhang, Y Song… - Journal of medicinal …, 2019 - ACS Publications
… target identification methods have been used to successfully elucidate the target proteins
of … that display weak affinity to the target (the KTGS approach) is considered a robust way to …
of … that display weak affinity to the target (the KTGS approach) is considered a robust way to …
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