What question did this study set out to answer?

To identify the structural determinants of HIV-1 Tat(49-57) cell entry and engineer synthetic molecular transporters with improved cellular uptake and stability.

November 21, 2000Proceedings of the National Academy of SciencesOpen Access

The design, synthesis, and evaluation of molecules that enable or enhance cellular uptake: Peptoid molecular transporters

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Authors

PWPaul A. WenderUtah State University DMDennis J. MitchellMerck & Co., Inc., Rahway, NJ, USA (United States)KPKanaka PattabiramanAmgen (United States)

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Implication

In vitro study reveals polyguanidine peptoids enhance cellular uptake over native peptide sequences in Jurkat cells, indicating a protease-resistant drug delivery platform.

Key Points

To identify the structural determinants of HIV-1 Tat(49-57) cell entry and engineer synthetic molecular transporters with improved cellular uptake and stability.
Synthesized alanine-substituted, truncated, and homooligomeric analogues of Tat(49-57), alongside novel polyguanidine peptoid derivatives.
Measured cellular uptake efficiency and kinetics in Jurkat cells using flow cytometry and Michaelis-Menten kinetic analyses.
Alanine substitutions and truncations diminished uptake, while L-arginine nonamers (R9) and D-arginine nonamers (r9) enhanced uptake rates by 20-fold and >100-fold compared to Tat(49-57), respectively.
Polyguanidine peptoids possessing a six-methylene spacer (N-hxg) between the backbone and guanidine group showed uptake superior to both Tat(49-57) and r9, while providing protease resistance.

Cite This Study

Wender et al. (2000) studied this question.

synapsesocial.com/papers/69d727c73f906f6a06bef773 https://doi.org/10.1073/pnas.97.24.13003

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Implication

In vitro study reveals polyguanidine peptoids enhance cellular uptake over native peptide sequences in Jurkat cells, indicating a protease-resistant drug delivery platform.

The design, synthesis, and evaluation of molecules that enable or enhance cellular uptake: Peptoid molecular transporters

Discussion

Member takes

Implication

Key Points

Cite This Study

The design, synthesis, and evaluation of molecules that enable or enhance cellular uptake: Peptoid molecular transporters

Discussion

Member takes

Implication

Key Points

Cite This Study

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