Drug delivery challenges and formulation aspects of proteolysis targeting chimera (PROTACs)

Saraswat A.L.; Vartak R.; Hegazy R.Patel A.Patel K.

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Drug delivery challenges and formulation aspects of proteolysis targeting chimera (PROTACs)

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? 2022 Elsevier LtdProteolysis targeting chimeras (PROTACs) have been extensively explored for targeted proteasomal degradation of disease-related proteins with enormous potential in the treatment of intractable diseases. However, PROTACs are poorly soluble and permeable bulky molecules facing several bioavailability challenges irrespective of the route of administration. Our review lays out crucial challenges in the delivery of target protein degraders and nanoformulation approaches to overcome physicochemical and biological hurdles that can aid in transporting these target-protein degraders to the disease site. We have elaborated on the current formulation approaches and further highlighted the prospective delivery strategies that could be probed for disease-specific targeted delivery of PROTACs.

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《Drug discovery today》 |2023年第1期|103387-103387|共6页
作者
Saraswat A.L.; Vartak R.; Hegazy R.Patel A.Patel K.;
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College of Pharmacy and Health Sciences St John's University;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Drug permeation; Nanoformulation; PROTAC; Protein degradation; Solubility enhancement; Targeted therapy;

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1. Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective [J] . Pike Andy, Williamson Beth, Harlfinger StephanieMartin ScottMcGinnity Dermot F. Drug discovery today . 2020,第10期

机译：Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective
2. Rational Design for Nitroreductase (NTR)-Responsive Proteolysis Targeting Chimeras (PROTACs) Selectively Targeting Tumor Tissues [J] . Shi Shi, Du Yu, Zou YiNiu JingCai ZeyuWang XiaonanQiu FeihuangDing YiYang GengchenWu YunzeXu YungenZhu Qihua Journal of Medicinal Chemistry . 2022,第6期

机译：Rational Design for Nitroreductase (NTR)-Responsive Proteolysis Targeting Chimeras (PROTACs) Selectively Targeting Tumor Tissues
3. Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets [J] . Xiong Yan, Zhong Yue, Yim HyerinYang XiaobaoPark Kwang-SuXie LingPoulikakos Poulikos I.Han XiaoranXiong YueChen XianLiu JingJin Jian Journal of the American Chemical Society . 2022,第49期

机译：Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets
4. Targeted drug delivery with focus ultrasound-induced blood-brain barrier opening Using acoustically-activated nanodroplets [C] . Chen C.C., Sheeran P.S., Shih-Ying Wu, IEEE International Ultrasonics Symposium . 2013

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Drug delivery challenges and formulation aspects of proteolysis targeting chimera (PROTACs)

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