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 …
PROTACs: Novel tools for improving immunotherapy in cancer
S Li, T Chen, J Liu, H Zhang, J Li, Z Wang, G Shang - Cancer Letters, 2023 - Elsevier
Posttranslational modifications (PTMs), such as phosphorylation, methylation, ubiquitination,
and acetylation, are important in governing protein expression levels. Proteolysis targeting …
and acetylation, are important in governing protein expression levels. Proteolysis targeting …
[HTML][HTML] PROTAC derivatization of natural products for target identification and drug discovery: Design of evodiamine-based PROTACs as novel REXO4 degraders
S Chen, K Bi, H Liang, Z Wu, M Huang, X Chen… - Journal of advanced …, 2024 - Elsevier
Abstract Introduction Natural products (NPs) play a crucial role in the development of
therapeutic drugs. However, it is still highly challenging to identify the targets of NPs …
therapeutic drugs. However, it is still highly challenging to identify the targets of NPs …
Cobalt-Catalyzed Carbon–Heteroatom Transfer Enables Regioselective Tricomponent 1, 4-Carboamination
K Zhuang, GC Haug, Y Wang, S Yin… - Journal of the …, 2024 - ACS Publications
Tricomponent cobalt (salen)-catalyzed carbofunctionalization of unsaturated substrates by
radical–polar crossover has the potential to streamline access to broad classes of …
radical–polar crossover has the potential to streamline access to broad classes of …
How many kinases are druggable? A review of our current understanding
There are over 500 human kinases ranging from very well-studied to almost completely
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …
Application of novel degraders employing autophagy for expediting medicinal research
X Li, Q Liu, X Xie, C Peng, Q Pang, B Liu… - Journal of Medicinal …, 2023 - ACS Publications
Targeted protein degradation (TPD) technology is based on a unique pharmacological
mechanism that has profoundly revolutionized medicinal research by overcoming limitations …
mechanism that has profoundly revolutionized medicinal research by overcoming limitations …
Research in the field of drug design and development
G Biala, E Kedzierska, M Kruk-Slomka… - Pharmaceuticals, 2023 - mdpi.com
The processes used by academic and industrial scientists to discover new drugs have
recently experienced a true renaissance, with many new and exciting techniques being …
recently experienced a true renaissance, with many new and exciting techniques being …
RAS degraders: The new frontier for RAS-driven cancers
TE Escher, KJF Satchell - Molecular Therapy, 2023 - cell.com
The function and significance of RAS proteins in cancer have been widely studied for
decades. In 2013, the National Cancer Institute established the RAS Initiative to explore …
decades. In 2013, the National Cancer Institute established the RAS Initiative to explore …
Sulfur-containing marine natural products as leads for drug discovery and development
Among the large series of marine natural products (MNPs), sulfur-containing MNPs have
emerged as potential therapeutic agents for the treatment of a range of diseases. Herein, we …
emerged as potential therapeutic agents for the treatment of a range of diseases. Herein, we …
Anticancer small-molecule agents targeting eukaryotic elongation factor 1A: State of the art
H Zhang, J Cai, S Yu, B Sun, W Zhang - International Journal of …, 2023 - mdpi.com
Eukaryotic elongation factor 1A (eEF1A) canonically delivers amino acyl tRNA to the
ribosomal A site during the elongation stage of protein biosynthesis. Yet paradoxically, the …
ribosomal A site during the elongation stage of protein biosynthesis. Yet paradoxically, the …