Mitochondria-Targeting Peptoids

Nam, Ho Yeon; Hong, Jong‐Ah; Choi, Jieun; Shin, Seung‐Heon; Cho, Steve K.; Seo, Jiwon; Lee, Jiyoun

doi:10.1021/acs.bioconjchem.8b00148

Cited by 29 publications

(28 citation statements)

References 41 publications

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“…After concluding that their compounds inhibited oxidative phosphorylation, the next step of this series of experiments was to use sterile technique to isolate mitochondria from PANC‐1 cells and determine which complex of the ETC was being inhibited using a previously published protocol to study the oxidation and reduction of Cytochrome c 5 . Alternative methods include assessing cellular respiration using a Seahorse XF from Agilent 9,10 or other polarographic and spectrophotometric methods 3 . Students gained valuable experience using mammalian cell culture and learned how it can be used in a “real‐world” drug‐discovery scenario.…”

Section: Resultsmentioning

confidence: 99%

A simple colorimetric experiment using mammalian cell culture to study metabolism

Sharma

Fizet

Montgomery

et al. 2020

Biochem Molecular Bio Educ

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The goal of this laboratory exercise is to give upper‐level undergraduate students an introduction to sterile technique in mammalian cell culture and metabolism. The experiment can be completed within a 3‐h lab period and can be performed either in conjunction with other biochemistry/metabolism experiments or used as a stand‐alone experiment. In this experiment, students are tasked with relating the acidification of cell culture medium to metabolism in order to elucidate the mechanism of action for a compound. Students can relate their experimental results to topics covered on glycolysis and oxidative phosphorylation in upper‐level biochemistry classes as well as gain valuable experience relating metabolism to drug discovery.

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Section: Resultsmentioning

confidence: 99%

A simple colorimetric experiment using mammalian cell culture to study metabolism

Sharma

Fizet

Montgomery

et al. 2020

Biochem Molecular Bio Educ

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“…Mitochrondria targeting delivery systems are widely sought after for the study of mitochrondrial diseases and for the provision of therapeutic developments. Although it is known that triphenylphosphonium cations are selective for mitochrondrial membrane association, Nam et al . followed a more traditional route using standard amine and guanidine side‐chains.…”

Section: Cellular Transportersmentioning

confidence: 99%

Peptoids as tools and sensors

Culf¹

2019

Biopolymers

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A review of molecular tools and sensors assembled on N‐substituted glycine, or α‐peptoid, oligomers between 2013 and November 2018 with the following sections: (a) Peptoids as crystal growth modifiers, (b) Peptoids as catalysts, (c) Ion and molecule sequestration and transport, (d) Peptoid sensors, (e) Macromolecule recognition, (f) Cellular transporters, (g) Medical imaging, (h) Future direction and (i) Summary and outlook. Peptoids are a promising class of peptide mimic making them an excellent platform for functional molecule preparation. Attributes of peptoid oligomers include: (a) the ease of precise sequence definition and mono‐dispersity; (b) access to a vast chemical space within simple and repeating chemical preparative steps and (c) thermal, chemical and biological stability all lending support for their application in a number of areas, with some that have been realised to date. The peptoid tool and sensor examples selected have realised practical utility. They serve to illustrate the rapidity of new insight that can generate in many disparate areas of science and technology, enabling the quick assembly of design criteria for efficient peptoid molecular tools and sensors.

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“…There are several mechanisms of membrane disruption in bacteria described for AMPs including barrel‐stave, carpet‐like, and formation of toroidal pores, yet none of them have been confirmed for peptoid substituents. Membrane damaging effect is suggested to be the primary mode of action by peptoids, while the potential intracellular targeting of ATP efflux, ribosome aggregation, enzymatic and mitochondrial activity, as well as nucleic acid synthesis, might be also involved. Peptoid amphipathic topology allows for electrostatic binding toward the lipid phosphate groups, implicated in membrane depolarization .…”

Section: Membrane‐active Peptoids: Advanced Peptide Biomimicrymentioning

confidence: 99%

Peptoid drug discovery and optimization via surface X‐ray scattering

2019

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Synthetic polymers mimicking antimicrobial peptides have drawn considerable interest as potential therapeutics. N‐substituted glycines, or peptoids, are recognized by their in vivo stability and ease of synthesis. Peptoids are thought to act primarily on the negatively charged lipids that are abundant in bacterial cell membranes. A mechanistic understanding of lipid–peptoid interaction at the molecular level will provide insights for rational design and optimization of peptoids. Here, we highlight recent studies that utilize synchrotron liquid surface X‐ray scattering to characterize the underlying peptoid interactions with bacterial and eukaryotic membranes. Cellular membranes are highly complex, and difficult to characterize at the molecular level. Model systems including Langmuir monolayers, are used in these studies to reduce system complexity. The general workflow of these systems and the corresponding data analysis techniques are presented alongside recent findings. These studies investigate the role of peptoid physicochemical characteristics on membrane activity. Specifically, the roles of cationic charge, conformational constraint via macrocyclization, and hydrophobicity are shown to correlate their membrane interactions to biological activities in vitro. These structure–activity relationships have led to new insights into the mechanism of action by peptoid antimicrobials, and suggest optimization strategies for future therapeutics based on peptoids.

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Mitochondria-Targeting Peptoids

Cited by 29 publications

References 41 publications

A simple colorimetric experiment using mammalian cell culture to study metabolism

A simple colorimetric experiment using mammalian cell culture to study metabolism

Peptoids as tools and sensors

Peptoid drug discovery and optimization via surface X‐ray scattering

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