Results 221 to 230 of about 827,025 (271)

Exploring Orodispersible Films Containing the Proteolysis Targeting Chimera ARV-110 in Hot Melt Extrusion and Solvent Casting Using Polyvinyl Alcohol. [PDF]

Pharmaceutics
Meloni V, Halstenberg L, Mareczek L, Lu J, Liang B, Gottschalk N, Mueller LK.   +6 more
europepmc   +1 more source

Generalizable Strategies for the Synthesis of Cereblon‐Recruiting PROTAC Prodrugs

Angewandte Chemie, Volume 138, Issue 40, 28 September 2026.
Cereblon‐recruiting PROTACs remain challenging to derivatize for prodrug‐based delivery. In this study, three complementary conjugation strategies enabled the efficient synthesis of cleavable PROTAC prodrugs with tunable release kinetics that can be incorporated into a library of PEGylated constructs and bottlebrush prodrugs.
Aiden X. Wang, Bin Liu, Elise M. Ackerman, Yichen Xiang, Hung V.‐T. Nguyen, Yivan Jiang, Angela N. Koehler, Jeremiah A. Johnson   +7 more
wiley   +1 more source

Structurally Specific Z-DNA Proteolysis Targeting Chimera Enables Targeted Degradation of Adenosine Deaminase Acting on RNA 1. [PDF]

J Am Chem Soc
Wang Z, Zhang D, Qiu X, Inuzuka H, Xiong Y, Liu J, Chen L, Chen H, Xie L, Kaniskan HÜ, Chen X, Jin J, Wei W.   +12 more
europepmc   +1 more source

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Proteolysis-targeting Chimeras for Targeting Protein for Degradation

Future Medicinal Chemistry, 2019
Proteolysis-targeting chimeras (PROTACs) are an emerging tool for therapeutic intervention by reducing or eliminating disease-causing proteins. PROTACs are bifunctional molecules that consist of a target protein ligand, a linker and an E3 ligase ligand, which mediate the polyubiquitination of the target protein, ultimately leading to the target protein
Gang Zhang, Jianguo Qi
exaly   +3 more sources

Reversible Assembly of Proteolysis Targeting Chimeras

ACS Chemical Biology, 2023
PROteolysis TArgeting Chimeras (PROTACs) are of significant current interest for the development of probe molecules and drug leads. However, they suffer from certain limitations. PROTACs are rule-breaking molecules with sub-optimal cellular permeability, solubility, and other drug-like properties.
Weijun Gui, Sarah F. Giardina, Madeline Balzarini, Francis Barany, Thomas Kodadek   +4 more
openaire   +2 more sources

The rise of covalent proteolysis targeting chimeras

Current Opinion in Chemical Biology, 2021
Targeted protein degradation offers several advantages over direct inhibition of protein activity and is gaining increasing interest in chemical biology and drug discovery. Proteolysis targeting chimeras (PROTACs) in particular are enjoying widespread application.
Ronen Gabizon, Nir London
openaire   +2 more sources

Proteolysis-Targeting Chimera Molecules Targeting SHP2

Future Medicinal Chemistry, 2022
SHP2 is a member of the non-receptor protein tyrosine phosphatases, encoded by PTPN11, and exhibits oncogenic activities. The close association between SHP2 and human cancer has made SHP2 a promising target for clinical therapy. Proteolysis-targeting chimera (PROTAC) technology utilizes the degradation mechanism of the ubiquitin proteasome system to ...
Dandan Yu, Mengzhu Zheng, Yang Liu, Lixia Chen, Hua Li   +4 more
openaire   +2 more sources

Advancing Strategies for Proteolysis-Targeting Chimera Design

Journal of Medicinal Chemistry, 2023
Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by degrading various disease-causing proteins, particularly those related to tumors. Therefore, the introduction of PROTACs has ushered in a new chapter of antitumor drug development, marked by significant advances over recent years.
Minglei Li, Ying Zhi, Bo Liu, Qingqiang Yao   +3 more
openaire   +2 more sources

Discovery of a Potent Proteolysis Targeting Chimera Enables Targeting the Scaffolding Functions of FK506-Binding Protein 51 (FKBP51) [PDF]

Angewandte Chemie - International Edition
The FK506‐binding protein 51 (FKBP51) is a promising target in a variety of disorders including depression, chronic pain, and obesity. Previous FKBP51‐targeting strategies were restricted to occupation of the FK506‐binding site, which does not affect ...
Frederik Lermyte, Christian Meyners, Felix Hausch   +2 more
exaly   +3 more sources

PROTAC (PROteolysis TArgeting Chimera)

La Chimica e l'Industria, 2022
PROTAC technology represents the spearhead of Targeted Protein Degradation, a new paradigm that in the past recent years has become increasingly used in pharmacology. Characterized by a profoundly different mechanism of action compared to classic approaches, it can be useful in tackling elusive molecular targets and hopefully help dealing with ...
openaire   +1 more source