Recent Advances in Peptide Drug Discovery: Novel Strategies and Targeted Protein Degradation DOI Creative Commons
Katarina Vrbnjak, Raj Nayan Sewduth

Pharmaceutics, Год журнала: 2024, Номер 16(11), С. 1486 - 1486

Опубликована: Ноя. 20, 2024

Recent technological advancements, including computer-assisted drug discovery, gene-editing techniques, and high-throughput screening approaches, have greatly expanded the palette of methods for discovery peptides available to researchers. These emerging strategies, driven by recent advances in bioinformatics multi-omics, significantly improved efficiency peptide when compared with traditional vitro vivo methods, cutting costs improving their reliability. An added benefit peptide-based drugs is ability precisely target protein-protein interactions, which are normally a particularly challenging aspect discovery. Another breakthrough this field targeted protein degradation through proteolysis-targeting chimeras. revolutionary compounds represent noteworthy advancement over small-molecule inhibitors due unique mechanism action, allows specific proteins unprecedented specificity. The inclusion as protein-of-interest-targeting moiety versatility possibility targeting otherwise undruggable proteins. In review, we discuss various novel wet-lab computational multi-omic provide an overview therapeutic agents discovered these cutting-edge potential delivery drugs.

Язык: Английский

Designing a Novel Ultrashort Cyclic [R3W4V] Antimicrobial Peptide with Superior Antimicrobial Potential Based on the Transmembrane Structure to Facilitate Pore Formation DOI
Lei Liu, Zhihong Shi, Mingqiong Tong

и другие.

Journal of Chemical Information and Modeling, Год журнала: 2025, Номер unknown

Опубликована: Фев. 20, 2025

The clinical application of antimicrobial peptides (AMPs) is frequently hindered by the inherent limitations linear peptides. Previous studies have primarily focused on physicochemical properties AMPs, and there a scarcity information regarding transmembrane structure interactions AMPs with cell membranes their activity. present study first to propose that backbone cyclization R3W4V (l(R3W4V)) into cyclic (c[R3W4V]) form can enhance stability its consequently improve antibacterial results bacterial inhibition assays performed herein demonstrated activity c[R3W4V] against Staphylococcus aureus Bacillus subtilis was approximately 17-fold 19-fold higher than l(R3W4V). effect bilayer membrane further assessed via well-tempered bias-exchange metadynamics simulations long-time conventional unbiased molecular dynamics simulations. This single peptide assumes stable configuration. Consequently, as number accumulating in core increases at peptide-lipid ratios, phospholipid headgroups embedded hydrophobic lipid core, leading fusion, permeabilization, deformation upper lower leaflets bilayer. provides novel computational perspective enhancing efficacy highlights importance peptide-membrane structures, dynamics, promoting membrane-disruptive potential

Язык: Английский

Процитировано

0
A highly active angiotensin I-converting enzyme inhibitory peptide KAKW designed based on the role of C-terminal residue, and its antihypertensive effects on spontaneously hypertensive rats DOI

Yangting Hu,

Dewei Xie,

Xujun Chen

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер unknown, С. 117564 - 117564

Опубликована: Март 1, 2025

Язык: Английский

Процитировано

0
Recent Advances in Peptide Drug Discovery: Novel Strategies and Targeted Protein Degradation DOI Creative Commons
Katarina Vrbnjak, Raj Nayan Sewduth

Pharmaceutics, Год журнала: 2024, Номер 16(11), С. 1486 - 1486

Опубликована: Ноя. 20, 2024

Recent technological advancements, including computer-assisted drug discovery, gene-editing techniques, and high-throughput screening approaches, have greatly expanded the palette of methods for discovery peptides available to researchers. These emerging strategies, driven by recent advances in bioinformatics multi-omics, significantly improved efficiency peptide when compared with traditional vitro vivo methods, cutting costs improving their reliability. An added benefit peptide-based drugs is ability precisely target protein-protein interactions, which are normally a particularly challenging aspect discovery. Another breakthrough this field targeted protein degradation through proteolysis-targeting chimeras. revolutionary compounds represent noteworthy advancement over small-molecule inhibitors due unique mechanism action, allows specific proteins unprecedented specificity. The inclusion as protein-of-interest-targeting moiety versatility possibility targeting otherwise undruggable proteins. In review, we discuss various novel wet-lab computational multi-omic provide an overview therapeutic agents discovered these cutting-edge potential delivery drugs.

Язык: Английский

Процитировано

0