Linear Peptides in Intracellular Applications.

Abstract:

:To this point, efforts to develop therapeutic peptides for intracellular applications were guided by the perception that unmodified linear peptides are highly unstable and therefore structural modifications are required to reduce proteolytic breakdown. Largely, this concept is a consequence of the fact that most research on intracellular peptides hitherto has focused on peptide degradation in the context of antigen processing, rather than on peptide stability. Interestingly, inside cells, endogenous peptides lacking any chemical modifications to enhance stability escape degradation to the point that they may even modulate intracellular signaling pathways. In addition, many unmodified synthetic peptides designed to interfere with intracellular signaling, following introduction into cells, have the expected activity demonstrating that biologically relevant concentrations can be reached. This review provides an overview of results and techniques relating to the exploration and application of linear, unmodified peptides. After an introduction to intracellular peptide turnover, the review mentions examples for synthetic peptides as modulators of intracellular signaling, introduces endogenous peptides with bioactivity, techniques to measure peptide stability, and peptide delivery. Future experiments should elucidate the rules needed to predict promising peptide candidates.

journal_name

Curr Med Chem

authors

Zuconelli CR,Brock R,Adjobo-Hermans MJW

doi

10.2174/0929867324666170508143523

subject

Has Abstract

pub_date

2017-01-01 00:00:00

pages

1862-1873

issue

17

eissn

0929-8673

issn

1875-533X

pii

CMC-EPUB-83335

journal_volume

24

pub_type

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