PROTAC Technology as a New Tool for Modern Pharmacotherapy DOI Creative Commons

Natalia Kubryń,

Łukasz Fijałkowski, Jacek Nowaczyk

и другие.

Molecules, Год журнала: 2025, Номер 30(10), С. 2123 - 2123

Опубликована: Май 11, 2025

The publication focuses on the innovative applications of PROTAC (proteolysis-targeting chimera) technology in modern pharmacotherapy, with particular emphasis cancer treatment. PROTACs represent an advanced therapeutic strategy that enables selective protein degradation, opening new possibilities drug design. This shows potential treatment cancers, viral infections (such as HIV and COVID-19), chronic diseases including atherosclerosis, Alzheimer’s disease, atopic dermatitis, Huntington’s disease. Promising results from clinical studies compound ARV-471 confirm effectiveness this approach. New types PROTACs, like TF-PROTAC PhosphoTAC, are designed to enhance effectiveness, stability, absorption drugs. conclusions review highlight broad various their relevance for future therapies, particularly oncology.

Язык: Английский

Medicinal Chemistry: A Key Driver in Achieving the Global Sustainable Development Goals DOI Creative Commons
Bianca Martinengo, Eleonora Diamanti, Elisa Uliassi

и другие.

Journal of Medicinal Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Март 20, 2025

In 2015, the United Nations officially launched Sustainable Development Goals (SDGs) as "the blueprint to achieve a better and more sustainable future for all. They address global challenges we face, including those related poverty, inequality, climate change, environmental degradation, peace justice. The 17 are all interconnected, in order leave no one behind, it is important that them by 2030". Here, have embedded medicinal chemistry key player SDGs. We firmly believe can must contribute world with an improved quality of life taken critical look at each SDGs, dividing into Priority Foundational, analyzed how has impact on them. Although much been done, determined make progress this area.

Язык: Английский

Процитировано

0

TogoPhosTAC: A Ready-To-Go and Adaptable Targeted Protein Dephosphorylation System DOI Creative Commons
Po‐Han Chen,

Yu-Yu Chen,

Dong-Ting Ke

и другие.

Research Square (Research Square), Год журнала: 2025, Номер unknown

Опубликована: Март 25, 2025

Abstract Phosphorylation targeting chimeras (PhosTACs) recruit phosphatases to dephosphorylate target proteins by proximity-induced protein interactions. However, recruiting a phosphatase subunit or holoenzyme using small molecules without compromising its activity adversely disturbing cellular function remains challenging. In addition, many do not have favorable activator binder currently. To overcome these limitations, here, we report an adapted mode of action, named togoPhosTAC, based on the molecule PhosTAC, engineered fusion FKBP12(F36V)-phosphatase, and lipid-based delivery system for targeted dephosphorylation. Through nanoparticles, delivered pre-fused complex PhosTACs FKBP12(F36V)-phosphatases in mRNA format directly rapid efficient intracellular The togoPhosTAC was able epidermal growth factor receptor (EGFR), tau, α-synuclein. Furthermore, togoPhosTAC-mediated tau dephosphorylation also correlates with reduced aggregation. sum, our hybrid biologic adaptor strategy bypassed challenges ligand development provided alternative generalizable solution precise modulation in cellulo.

Язык: Английский

Процитировано

0

PROTAC Technology as a New Tool for Modern Pharmacotherapy DOI Creative Commons

Natalia Kubryń,

Łukasz Fijałkowski, Jacek Nowaczyk

и другие.

Molecules, Год журнала: 2025, Номер 30(10), С. 2123 - 2123

Опубликована: Май 11, 2025

The publication focuses on the innovative applications of PROTAC (proteolysis-targeting chimera) technology in modern pharmacotherapy, with particular emphasis cancer treatment. PROTACs represent an advanced therapeutic strategy that enables selective protein degradation, opening new possibilities drug design. This shows potential treatment cancers, viral infections (such as HIV and COVID-19), chronic diseases including atherosclerosis, Alzheimer’s disease, atopic dermatitis, Huntington’s disease. Promising results from clinical studies compound ARV-471 confirm effectiveness this approach. New types PROTACs, like TF-PROTAC PhosphoTAC, are designed to enhance effectiveness, stability, absorption drugs. conclusions review highlight broad various their relevance for future therapies, particularly oncology.

Язык: Английский

Процитировано

0