Publications by authors named "Palash Jain"
Article Synopsis
- Peptides that target specific protein interactions present a promising therapy option, bridging the gap between small molecules and therapeutic proteins, but they face challenges like poor stability and low permeability.
- Cyclization of peptides, including techniques like "stapling," helps to create more stable and permeable cyclic peptides by enhancing their structure and resistance to metabolism.
- Through a detailed analysis of various cyclization methods, the study identifies effective cyclic peptides that target Mint2, with all-hydrocarbon stapling significantly boosting their stability and cell permeability.
Article Synopsis
- - There is a critical need for new treatments for Alzheimer's disease (AD) that can relieve symptoms and slow progression, particularly targeting the harmful accumulation of amyloid-β (Aβ) peptides, which arise from the amyloid precursor protein (APP).
- - Previous research on Mint2, a protein that interacts with APP and the enzyme complex responsible for Aβ production, has shown mixed results on whether it promotes or inhibits Aβ generation.
- - This study clarifies that Mint2 facilitates Aβ formation and highlights a promising therapeutic strategy by using a stable peptide inhibitor to target the APP-Mint2 interaction, which could significantly lower Aβ levels in neuronal models of AD.
An increased appreciation of the importance of optimizing drug-binding kinetics has lead to the development of various techniques for measuring the kinetics of unlabeled compounds. One approach is the competition-association kinetic binding method first described in the 1980s. The kinetic characteristics of the tracer employed greatly affects the reliability of estimated kinetic parameters, a barrier to successfully introducing these kinetic assays earlier in the drug discovery process.
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