Contents
Special Issue Topic

Bioactive Peptides discovery and development

Submission Deadline: November 30, 2024

Guest Editor

Prof. Xuechen Li E-Mail

Professor of Department of Chemistry, The University of Hong Kong, Hong Kong, China

Research Keywords: synthetic protein; antibiotics; glycoconjugates; drug conjugates

About the Special lssue

Peptides have emerged as an exciting therapeutic modality with middle-sized molecular weights and pharmacological properties in between traditional small molecule drugs and therapeutic proteins. Many peptide drugs have been clinically used for various diseases, including antimicrobial peptides, supplementary peptide hormones, peptide-drug conjugates and so on. In addition, peptides hold great promise for disrupting protein-protein interactions (PPIs) and drug delivery.

The past decades have witnesses great advances in bioactive peptides discovery and development. For instance,  genome mining has led to many new ribosomally synthesized and post-translationally modified peptides (RiPPs), various chemical methods have been developed to effectively cyclize peptides, peptide ligation allows for efficient synthesis of long peptides, super diverse peptide libraries provide powerful tools for high throughput screening and new knowledges have been gained for peptide intracellular delivery. 

This special issue calls for the submission in all aspect in peptides, including, but not limited to, new bioactive peptide discovery, biosynthesis, peptide synthesis, peptide delivery, cyclic peptides, peptide-drug conjugates, medicinal chemistry, etc.

Keywords: bioactive peptide, peptide synthesis, ribosomally synthesized and post-translationally modified peptides, peptide conjugates, peptide delivery, peptide high throughput screening

Published Articles

Open Access Commentary
Recent exploration of γ-AApeptide based antimicrobial peptide mimics as potential therapeutics towards drug-resistant bacteria
Over the last 60 years, only four new classes of antibiotics have been introduced, while the prevalence of antibiotic-resistant Gram-positive and Gram-negative bacteria has risen. This underscores the urgent need for new antibacterial therapeutics. This commentary leverages the recent exploration of γ-substituted-N-acylated-N-aminoethyl amino acid peptides (γ-AApeptides) to mimic the structures and function of natural antimicrobial peptides (AMPs), highlighting the promise and limitations for developing a new, effective treatment for antibiotic-resistant bacteria.
Published: February 19, 2025 Explor Drug Sci. 2025;3:100888
374 18 0
Open Access Original Article
Bicyclic peptide-enhanced covalent inhibitor of SARS-CoV-2 3CL protease
Aim: Develop technology to apply bicyclic peptides for discovering covalent inhibitors of proteases and use this technology to create bicyclic peptide—warhead conjugates for targeting the sever
Published: October 17, 2024 Explor Drug Sci. 2024;2:719–733
1154 39 1
Open Access Review
Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates
Chemo-select modification of peptides, targeting a handful of the most reactive proteinogenic amino acids (AAs), is gradually utilized to address the medical needs of peptide drugs and biopharmaceut
Published: September 06, 2024 Explor Drug Sci. 2024;2:540–554
1596 78 1
Open Access Review
Lipopeptide adjuvants for antibiotics and vaccines: the future step in the fight against multidrug-resistant and extensively drug-resistant pathogens
With the surge of antibiotic resistance in bacteria, the need for a larger arsenal of effective antibiotics and vaccines has drastically increased in the past decades. Antibiotics like vaccines can
Published: April 29, 2024 Explor Drug Sci. 2024;2:203–233
2322 45 3
Open Access Perspective
Daropeptide natural products
Cyclophane-containing peptides comprise an important group of macrocyclic peptides with unique structural properties and pharmaceutical relevance. Darobactin A is a ribosomally synthesized and post-
Published: April 19, 2024 Explor Drug Sci. 2024;2:190–202
1681 66 2
Open Access Review
Stapled peptides: targeting protein-protein interactions in drug development
Protein-protein interactions (PPIs) impersonate a significant role in many biological processes and are potential therapeutic targets in numerous human diseases. Stapled peptides, as the most promis
Published: April 18, 2024 Explor Drug Sci. 2024;2:154–189
4417 146 1
Open Access Review
Therapeutic proteins immunogenicity: a peptide point of view
Protein therapeutics are extensively used in the treatment of autoimmune diseases, but a subset of patients appears to be refractory to these treatments, mainly due to the development of an immune r
Published: October 26, 2023 Explor Drug Sci. 2023;1:377–387
3717 119 6
Open Access Original Article
Late-stage diversification strategy for the synthesis of peptide acids and amides using hydrazides
Aim: Modification of the C-terminus of a peptide to improve its properties, particularly after constructing the peptide chain, has great promise in the development of peptide therapeutics. This s
Published: October 09, 2023 Explor Drug Sci. 2023;1:322–335
2341 77 4
Open Access Original Article
A dextrorotatory residues-incorporated bioactive dodecapeptide against enterohemorrhagic Escherichia coli
Aim: This study aims to report an engineered peptide zp39 with favorable bioactivity against enterohemorrhagic Escherichia coli (E. coli, EHEC). Its antibacterial mechanisms and application in a
Published: June 30, 2023 Explor Drug Sci. 2023;1:210–220
1360 28 1
Open Access Review
Essential functions, syntheses and detection of sialyl Lewis X on glycoproteins
It is widely acknowledged that sialyl Lewis X (sLeX), the composition and linkage of which are N-acetylneuraminic acid (Neu5Ac) α2-3 galactose (Gal) β1-4 [fucose (Fuc) α1-3] N-acetylglucosamine, is usually attached to the cell surface. It presents as a terminal structure on either glycoproteins or glycolipids and has been demonstrated to be related to various biological processes, such as fertilization and selectin binding. Due to the vital role of sLeX, its synthesis as well as its determination approaches have attracted considerable attention from many researchers. In this review, the focus is sLeX on glycoproteins. The biological importance of sLeX in fertilization and development, immunity, cancers, and other aspects will be first introduced. Then the chemical and enzymatic synthesis of sLeX including the contributions from more than 15 international research groups will be described, followed by a brief view of the sLeX detection focusing on monosaccharides and linkages. This review is valuable for those readers who are interested in the chemistry and biology of sLeX.
Published: February 28, 2023 Explor Drug Sci. 2023;1:31–54
5320 128 2