Results 1 to 10 of about 17,763 (235)
International Journal of Molecular Sciences, 2023 Covalent peptidomimetic protease inhibitors have gained a lot of attention in drug development in recent years. They are designed to covalently bind the catalytically active amino acids through electrophilic groups called warheads.
Florenci Gonzalez +2 more
exaly +2 more sources
Human defensin-inspired discovery of peptidomimetic antibiotics
Proceedings of the National Academy of Sciences of the United States of America, 2022 Significance We report the development of peptidomimetic antibiotics derived from a natural antimicrobial peptide, human α-defensin 5. By engaging multiple bacterial targets, the lead compound is efficacious in vitro and in vivo against bacteria with ...
Jue Zhang +2 more
exaly +2 more sources
Marine Drugs, 2021 Peptides have a three-dimensional configuration that can adopt particular conformations for binding to proteins, which are well suited to interact with larger contact surface areas on target proteins.
Zhengshuang Xu
exaly +2 more sources
Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds [PDF]
Journal of Enzyme Inhibition and Medicinal ChemistryPeptidomimetic inhibitors mimic natural peptide substrates, employing electrophilic warheads to covalently interact with the catalytic Cys145 of Mpro.
Noor Atatreh +2 more
doaj +2 more sources
Development of Peptidomimetic Inhibitors of the ERG Gene Fusion Product in Prostate Cancer
Cancer Cell, 2017 SUMMARY Transcription factors play a key role in the development of diverse cancers, and therapeutically targeting them has remained a challenge. In prostate cancer, the gene encoding the transcription factor ERG is recurrently rearranged and plays a ...
Irfan Asangani +2 more
exaly +2 more sources
Conjugation of Antibiotics to Peptidomimetics Enhances Antimicrobial Spectrum of Activity [PDF]
AntibioticsBackground/Objectives: Antimicrobial conjugates have attracted considerable interest in addressing the threat of antimicrobial resistance by minimising the likelihood of resistance onset.
Joshua Fleming +8 more
doaj +2 more sources
Short Cationic Peptidomimetic Antimicrobials
Antibiotics, 2019 The rapid growth of antimicrobial resistance against several frontline antibiotics has encouraged scientists worldwide to develop new alternatives with unique mechanisms of action. Antimicrobial peptides (AMPs) have attracted considerable interest due to
Rajesh Kuppusamy +3 more
doaj +2 more sources
A peptidomimetic modulator of the CaV2.2 N-type calcium channel for chronic pain
Proceedings of the National Academy of Sciences of the United States of America, 2023 Significance Transmembrane Cav2.2 voltage-gated calcium channels play a central role in pain through providing the Ca2+ for sustained neuronal firing and neurotransmitter release.
Kimberly Gomez +36 more
semanticscholar +1 more source
Cyclic Peptoid-Peptide Hybrids as Versatile Molecular Transporters
Frontiers in Chemistry, 2021 Addressing intracellular targets is a challenging task that requires potent molecular transporters capable to deliver various cargos. Herein, we report the synthesis of hydrophobic macrocycles composed of both amino acids and peptoid monomers. The cyclic
Claudine Nicole Herlan +6 more
doaj +1 more source
Adaptive evolution of Escherichia coli to an α-peptide/β-peptoid peptidomimetic induces stable resistance. [PDF]
PLoS ONE, 2013 Antimicrobial peptides (AMPs) and synthetic analogues thereof target conserved structures of bacterial cell envelopes and hence, development of resistance has been considered an unlikely event.
Line Hein-Kristensen +3 more
doaj +1 more source