
Pharmacological Research, Год журнала: 2024, Номер unknown, С. 107461 - 107461
Опубликована: Окт. 1, 2024
Язык: Английский
Pharmacological Research, Год журнала: 2024, Номер unknown, С. 107461 - 107461
Опубликована: Окт. 1, 2024
Язык: Английский
Translational Oncology, Год журнала: 2025, Номер 54, С. 102331 - 102331
Опубликована: Фев. 28, 2025
Язык: Английский
Процитировано
0Phytochemistry Reviews, Год журнала: 2025, Номер unknown
Опубликована: Март 19, 2025
Язык: Английский
Процитировано
0Chinese Medicine, Год журнала: 2025, Номер 20(1)
Опубликована: Март 24, 2025
Abstract In the past, drug research and development has predominantly followed a "single target, single disease" model. However, clinical data show that single-target drugs are difficult to interfere with complete disease network, prone develop resistance low safety in use. The proposal of multi-target therapy (also known as "cocktail therapy") provides new approach for discovery, which can affect reduce adverse reactions by regulating multiple targets. Natural products an important source innovative development, more than half approved small molecule related natural products. there many challenges process products, such active screening, target identification preclinical dosage optimization. Therefore, how good from always been challenge. This article summarizes applications shortcomings technologies product bioactivity clarify mode action (direct/indirect target), dose Moreover, response faced trend interdisciplinary multi-technology integration, strategy "active substances — optimization" is proposed solve key dimensions levels.
Язык: Английский
Процитировано
0Expert Opinion on Drug Discovery, Год журнала: 2025, Номер unknown
Опубликована: Апрель 5, 2025
Targeted protein degradation (TPD) is a cutting-edge technology that provides new avenues for drug discovery and development. PROteolysis TArgeting Chimeras (PROTACs) are the most established advanced TPD strategy, enabling selective of disease-associated 'undruggable' proteins interest (POIs) by leveraging cell's natural machinery. To confirm PROTAC-induced proximity drives degradation, target validation ternary complex formation must be thoroughly assessed. In this perspective, authors detail some widely used in silico, structural, vitro, cellulo methods to validate PROTAC engagement formation. Additionally, they discuss growing use PROTACs as chemical probes novel identification validation. Target essential approach, ongoing studies should prioritize confirming using assays conducted under physiologically relevant cellular conditions. The believe proteomics analyses among valuable tools elucidating mechanism, selectivity, outcomes PROTACs. They also remain optimistic about future development their engagement. While rapidly advancing, it still holds vast opportunities exploration, offering significant potential further both biological research drive drugs.
Язык: Английский
Процитировано
0Pharmacological Research, Год журнала: 2024, Номер unknown, С. 107461 - 107461
Опубликована: Окт. 1, 2024
Язык: Английский
Процитировано
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