Strategies to improve the physicochemical properties of peptide‑based drugs

Peptides are a rapid-growing class of therapeutics with unique and desirable physicochemical properties. Due to disadvantages such as low membrane permeability and susceptibility to proteolytic degradation, peptide-based drugs have limited bioavailability, a short half-life, and rapid in vivo elimin...

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Main Authors: Lee, Michelle Felicia *, Poh, Chit Laa *
Format: Article
Published: Springer 2023
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Online Access:http://eprints.sunway.edu.my/2159/
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author Lee, Michelle Felicia *
Poh, Chit Laa *
author_facet Lee, Michelle Felicia *
Poh, Chit Laa *
author_sort Lee, Michelle Felicia *
building SU Institutional Repository
collection Online Access
description Peptides are a rapid-growing class of therapeutics with unique and desirable physicochemical properties. Due to disadvantages such as low membrane permeability and susceptibility to proteolytic degradation, peptide-based drugs have limited bioavailability, a short half-life, and rapid in vivo elimination. Various strategies can be applied to improve the physicochemical properties of peptide-based drugs to overcome limitations such as limited tissue residence time, metabolic instability, and low permeability. Applied strategies including backbone modifcations, side chain modifcations, conjugation with polymers, modifcation of peptide termini, fusion to albumin, conjugation with the Fc portion of antibodies, cyclization, stapled peptides, pseudopeptides, cell-penetrating peptide conjugates, conjugation with lipids, and encapsulation in nanocarriers are discussed.
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spelling sunway-21592023-03-20T03:56:46Z http://eprints.sunway.edu.my/2159/ Strategies to improve the physicochemical properties of peptide‑based drugs Lee, Michelle Felicia * Poh, Chit Laa * RM Therapeutics. Pharmacology Peptides are a rapid-growing class of therapeutics with unique and desirable physicochemical properties. Due to disadvantages such as low membrane permeability and susceptibility to proteolytic degradation, peptide-based drugs have limited bioavailability, a short half-life, and rapid in vivo elimination. Various strategies can be applied to improve the physicochemical properties of peptide-based drugs to overcome limitations such as limited tissue residence time, metabolic instability, and low permeability. Applied strategies including backbone modifcations, side chain modifcations, conjugation with polymers, modifcation of peptide termini, fusion to albumin, conjugation with the Fc portion of antibodies, cyclization, stapled peptides, pseudopeptides, cell-penetrating peptide conjugates, conjugation with lipids, and encapsulation in nanocarriers are discussed. Springer 2023 Article PeerReviewed Lee, Michelle Felicia * and Poh, Chit Laa * (2023) Strategies to improve the physicochemical properties of peptide‑based drugs. Pharmaceutical Research. ISSN 0724-8741 https://link.springer.com/article/10.1007/s11095-023-03486-0 10.1007/s11095-023-03486-0
spellingShingle RM Therapeutics. Pharmacology
Lee, Michelle Felicia *
Poh, Chit Laa *
Strategies to improve the physicochemical properties of peptide‑based drugs
title Strategies to improve the physicochemical properties of peptide‑based drugs
title_full Strategies to improve the physicochemical properties of peptide‑based drugs
title_fullStr Strategies to improve the physicochemical properties of peptide‑based drugs
title_full_unstemmed Strategies to improve the physicochemical properties of peptide‑based drugs
title_short Strategies to improve the physicochemical properties of peptide‑based drugs
title_sort strategies to improve the physicochemical properties of peptide‑based drugs
topic RM Therapeutics. Pharmacology
url http://eprints.sunway.edu.my/2159/
http://eprints.sunway.edu.my/2159/
http://eprints.sunway.edu.my/2159/