Cargando…

The tale of proteolysis targeting chimeras (PROTACs) for Leucine‐Rich Repeat Kinase 2 (LRRK2)

Here we present the rational design and synthetic methodologies towards proteolysis‐targeting chimeras (PROTACs) for the recently‐emerged target leucine‐rich repeat kinase 2 (LRRK2). Two highly potent, selective, brain‐penetrating kinase inhibitors were selected, and their structure was appropriatel...

Descripción completa

Detalles Bibliográficos
Autores principales:	Konstantinidou, Markella, Oun, Asmaa, Pathak, Pragya, Zhang, Bidong, Wang, Zefeng, ter Brake, Frans, Dolga, Amalia M., Kortholt, Arjan, Dömling, Alexander
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	John Wiley and Sons Inc. 2020
Materias:	Communications
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8048960/ https://www.ncbi.nlm.nih.gov/pubmed/33278061 http://dx.doi.org/10.1002/cmdc.202000872

Ejemplares similares

PROTACs– a game-changing technology
por: Konstantinidou, Markella, et al.
Publicado: (2019)

Proteolysis targeting chimeras (PROTACs) in cancer therapy
por: Ocaña, Alberto, et al.
Publicado: (2020)

Proteolysis-targeting chimeras (PROTACs) in cancer therapy
por: Li, Xinyi, et al.
Publicado: (2022)

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics
por: Khan, Sajid, et al.
Publicado: (2020)

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies
por: He, Yonghan, et al.
Publicado: (2020)

Proteolysis-Targeting Chimeras (PROTACs) in Cancer Therapy: Present and Future
por: Li, Rui, et al.
Publicado: (2022)

Characterization of Lipopolysaccharide Effects on LRRK2 Signaling in RAW Macrophages
por: Oun, Asmaa, et al.
Publicado: (2023)

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
por: Li, Xin, et al.
Publicado: (2020)

Proteolysis-Targeting Chimera (PROTAC): Is the Technology Looking at the Treatment of Brain Tumors?
por: Lospinoso Severini, Ludovica, et al.
Publicado: (2022)

Emerging Strategies in Proteolysis-Targeting Chimeras (PROTACs): Highlights from 2022
por: Tamatam, Rekha, et al.
Publicado: (2023)

A Conserved Role for LRRK2 and Roco Proteins in the Regulation of Mitochondrial Activity
por: Rosenbusch, Katharina E., et al.
Publicado: (2021)

Cancer-Specific Delivery of Proteolysis-Targeting Chimeras (PROTACs) and Their Application to Cancer Immunotherapy
por: Moon, Yujeong, et al.
Publicado: (2023)

Proteolysis Targeting Chimeras (PROTACs): A Perspective on Integral Membrane Protein Degradation
por: Ruffilli, Camilla, et al.
Publicado: (2022)

Proteolysis-Targeting Chimera (PROTAC) Delivery into the Brain across the Blood-Brain Barrier
por: Tashima, Toshihiko
Publicado: (2023)

Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications
por: Goracci, Laura, et al.
Publicado: (2020)

A Mechanistic Pharmacodynamic Modeling Framework for the Assessment and Optimization of Proteolysis Targeting Chimeras (PROTACs)
por: Haid, Robin Thomas Ulrich, et al.
Publicado: (2023)

Comprehensive Transcriptomic Analysis of Novel Class I HDAC Proteolysis Targeting Chimeras (PROTACs)
por: Baker, India M., et al.
Publicado: (2022)

Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
por: Bond, Michael J., et al.
Publicado: (2021)

MDM2-Based Proteolysis-Targeting Chimeras (PROTACs): An Innovative Drug Strategy for Cancer Treatment
por: Vicente, André T. S., et al.
Publicado: (2022)

Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1
por: Hu, Mingxing, et al.
Publicado: (2020)

Cell Morphological Profiling Enables High-Throughput Screening for PROteolysis TArgeting Chimera (PROTAC) Phenotypic Signature
por: Trapotsi, Maria-Anna, et al.
Publicado: (2022)

Design, Synthesis, and Biological Evaluation of Proteolysis Targeting Chimeras (PROTACs) for the Dual Degradation of IGF-1R and Src
por: Manda, Sudhakar, et al.
Publicado: (2020)

Targeting Oncoproteins for Degradation by Small Molecule-Based Proteolysis-Targeting Chimeras (PROTACs) in Sex Hormone-Dependent Cancers
por: Liu, Li, et al.
Publicado: (2022)

Proteolysis Targeting Chimera (PROTAC) for Macrophage Migration Inhibitory Factor (MIF) Has Anti‐Proliferative Activity in Lung Cancer Cells
por: Xiao, Zhangping, et al.
Publicado: (2021)

Design, Synthesis and Biological Characterization of Histone Deacetylase 8 (HDAC8) Proteolysis Targeting Chimeras (PROTACs) with Anti-Neuroblastoma Activity
por: Darwish, Salma, et al.
Publicado: (2022)

LRRK2 Structure-Based Activation Mechanism and Pathogenesis
por: Zhang, Xiaojuan, et al.
Publicado: (2023)

LRRK2 Targeting Strategies as Potential Treatment of Parkinson’s Disease
por: Wojewska, Dominika Natalia, et al.
Publicado: (2021)

Allosteric inhibition of LRRK2, where are we now
por: Soliman, Ahmed, et al.
Publicado: (2020)

Structural biology of the LRRK2 GTPase and kinase domains: implications for regulation
por: Gilsbach, Bernd K., et al.
Publicado: (2014)

Activation Mechanism of LRRK2 and Its Cellular Functions in Parkinson's Disease
por: Rosenbusch, Katharina E., et al.
Publicado: (2016)

Doubly Constrained C-terminal of Roc (COR) Domain-Derived Peptides Inhibit Leucine-Rich Repeat Kinase 2 (LRRK2) Dimerization
por: Pathak, Pragya, et al.
Publicado: (2023)

Shining a Light on Proteolysis Targeting Chimeras
por: Teichmann, Ellen, et al.
Publicado: (2019)

Proteolysis-targeting chimeras and their implications in breast cancer
por: Tecalco-Cruz, Angeles C., et al.
Publicado: (2021)

The clinical advances of proteolysis targeting chimeras in oncology
por: Xie, Hao, et al.
Publicado: (2021)

Covalent inhibitors: a rational approach to drug discovery
por: Sutanto, Fandi, et al.
Publicado: (2020)

Editorial: LRRK2—Fifteen Years From Cloning to the Clinic
por: Rideout, Hardy, et al.
Publicado: (2022)

HaloTag‐Targeted Sirtuin‐Rearranging Ligand (SirReal) for the Development of Proteolysis‐Targeting Chimeras (PROTACs) against the Lysine Deacetylase Sirtuin 2 (Sirt2)
por: Schiedel, Matthias, et al.
Publicado: (2020)

Assays and technologies for developing proteolysis targeting chimera degraders
por: Liu, Xingui, et al.
Publicado: (2020)

Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras
por: Lebraud, Honorine, et al.
Publicado: (2016)

Novel Design Strategies to Enhance the Efficiency of Proteolysis Targeting Chimeras
por: Zhao, Chunlong, et al.
Publicado: (2022)

Cannot write session to /tmp/vufind_sessions/sess_8n395v5eq64mpfbgc783u5grme