Results 231 to 240 of about 14,786 (290)

The therapeutic potential of PROTACs

Expert Opinion on Therapeutic Patents, 2021
PROTACs represent a novel class of heterobifunctional molecules that simultaneously bind to a target protein and to an E3 ligase complex, resulting in the transfer of ubiquitin and initiating a process ultimately causing the proteasomal degradation of the target protein.
Andrew B, Benowitz, Katherine L, Jones, John D, Harling   +2 more
openaire   +2 more sources

The application of PROTAC in HDAC

European Journal of Medicinal Chemistry, 2023
Inducing protein degradation by proteolysis targeting chimera (PROTAC) has provided great opportunities for scientific research and industrial applications. Histone deacetylase (HDAC)-PROTAC has been widely developed since the first report of its ability to induce the degradation of SIRT2 in 2017.
Shaoting Chen, Yuxiang Zheng, Benji Liang, Yudong Yin, Jian Yao, Quande Wang, Yanghan Liu, Nouri Neamati   +7 more
openaire   +2 more sources

Controlling PROTACs with Light

ChemMedChem, 2020
AbstractProteolysis targeting chimeras, PROTACs, are emerging as a powerful strategy for exerting exogenous control over protein levels, allowing small molecules to exploit the ubiquitin–proteasome pathway for targeted protein degradation. This highlight focuses on the fusion of photochemistry with these bifunctional compounds, which has provided a ...
Shreya Verma, Debasish Manna
openaire   +2 more sources

PROTACs in Treatment of Cancer: A Review

Mini-Reviews in Medicinal Chemistry, 2021
Cancer treatment has become a major challenge amidst the resistance and relapse caused by the various treatments available. The PROteolysis TAargeting Chimera (PROTAC) technology involves the degradation of target protein against the inhibition by small drug molecules. The PROTACs with high potency and activity have been frequently reported; however,
Poonam Arora, Manjinder Singh, Varinder Singh, Shiveena Bhatia, Sandeep Arora   +4 more
openaire   +2 more sources

Advancements in delivery Systems for Proteolysis-Targeting Chimeras (PROTACs): Overcoming challenges and expanding biomedical applications.

Journal of Controlled Release
PROTAC (Proteolysis-Targeting Chimera), an emerging drug development strategy based on small molecule technology, has garnered widespread attention due to its high efficiency, broad applicability, low resistance, and dosage advantages.
Yawei Yu, Weitong Hu, Yihua Xu, Hong-Bin Xu, Jianqing Gao   +4 more
semanticscholar   +1 more source

Integrating Proteolysis‐Targeting Chimeras (PROTACs) with Delivery Systems for More Efficient and Precise Targeted Protein Degradation

Macromolecular rapid communications
Targeted protein degradation (TPD) using the proteolysis‐targeting chimeras (PROTACs) is emerging as a revolutionary technology, offering a potential strategy for cancer treatment by inducing the degradation of overexpressed oncogenic proteins in tumors.
Jiachan Lin, Zirui Chen, Dan Zhang, Nan Zhang, Hongzhong Chen, Dongsheng Guo   +5 more
semanticscholar   +1 more source

Optimization of a Series of RIPK2 PROTACs

Journal of Medicinal Chemistry, 2021
Receptor-interacting serine/threonine protein kinase 2 (RIPK2) is an important kinase of the innate immune system. Herein, we describe the optimization of a series of RIPK2 PROTACs which recruit members of the inhibitor of apoptosis (IAP) family of E3 ligases.
Afjal H. Miah, Ian E. D. Smith, Mark Rackham, Alina Mares, Aditya R. Thawani, Rakesh Nagilla, Pamela A. Haile, Bartholomew J. Votta, Laurie J. Gordon, Gillian Watt, Jane Denyer, Don T. Fisher, Phoebe Dace, Paul Giffen, Andrea Goncalves, Ian Churcher, Paul Scott-Stevens, John D. Harling   +17 more
openaire   +2 more sources

In Vitro ADME Profiling of PROTACs: Successes, Challenges, and Lessons Learned from Analysis of Clinical PROTACs from a Diverse Physicochemical Space.

Journal of Medicinal Chemistry
Established in vitro assays for ADME properties often struggle with compounds outside of the rule-of-5 space such as PROTACs. These bifunctional molecules, due to high lipophilicity and molecular weight, frequently exhibit low solubility, high ...
Abhishek Srivastava, A. Pike, Magda Swedrowska, Samuel Nash, Ken Grime   +4 more
semanticscholar   +1 more source

Unconventional PROTACs for cancer therapy.

Angewandte Chemie
Targeted protein degradation, which aims to eliminate dysregulated proteins, has emerged as a promising strategy for conquering challenging therapeutic targets.
Xu Zhang, Z. Song, X. Zhang, Jianhua Zou, Guocan Yu, Xiaoyuan Chen, Sheng Wang   +6 more
semanticscholar   +1 more source

PROTAC-ing tuberculosis

Nature Chemical Biology
Targeted protein degradation has emerged as a promising approach in drug discovery, harnessing a cell's intrinsic machinery to eliminate disease-related proteins. Now, a study paves the way to translating this technology into potential anti-mycobacterial therapies, by exploiting the bacterial protein-degradation complex.
Preti, Delia, Albanese, Valentina, Marconi, Peggy Carla Raffaella   +2 more
openaire   +3 more sources