Results 1 to 10 of about 9,122 (118)

Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry
Peptidomimetic inhibitors mimic natural peptide substrates, employing electrophilic warheads to covalently interact with the catalytic Cys145 of Mpro.
Noor Atatreh, Radwa E. Mahgoub, Mohammad A. Ghattas   +2 more
doaj   +2 more sources

Conjugation of Antibiotics to Peptidomimetics Enhances Antimicrobial Spectrum of Activity [PDF]

Antibiotics
Background/Objectives: Antimicrobial conjugates have attracted considerable interest in addressing the threat of antimicrobial resistance by minimising the likelihood of resistance onset.
Joshua Fleming, Nathan James Carey, Yao Cheng, Hao Luo, Tsz Tin Yu, Mark D. P. Willcox, David StC Black, Edgar H. H. Wong, Naresh Kumar   +8 more
doaj   +2 more sources

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, Anna Meschkov, Anna Meschkov, Ute Schepers, Ute Schepers, Stefan Bräse, Stefan Bräse   +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, Henrik Franzyk, Anne Holch, Lone Gram   +3 more
doaj   +1 more source

The Antimicrobial, Antibiofilm and Anti-Inflammatory Activities of P13#1, a Cathelicidin-like Achiral Peptoid

Pharmaceuticals, 2023
Cationic antimicrobial peptides (CAMPs) are powerful molecules with antimicrobial, antibiofilm and endotoxin-scavenging activities. These properties make CAMPs very attractive drugs in the face of the rapid increase in multidrug-resistant (MDR) pathogens,
Valeria Cafaro, Andrea Bosso, Ilaria Di Nardo, Assunta D’Amato, Irene Izzo, Francesco De Riccardis, Marialuisa Siepi, Rosanna Culurciello, Nunzia D’Urzo, Emiliano Chiarot, Antonina Torre, Elio Pizzo, Marcello Merola, Eugenio Notomista   +13 more
doaj   +1 more source

Identification and Application of Two Promising Peptide Ligands for the Immunodetection of Imidacloprid Residue

Foods, 2022
As the most widely used neonicotinoid insecticide, it is of great significance to explore the immunoreagents and immunoassays for imidacloprid (IMI) residue.
Tianyang You, Yuan Ding, Yue Huang, Yang Lu, Minghua Wang, Xiude Hua   +5 more
doaj   +1 more source

Peptide–Protein Interactions: From Drug Design to Supramolecular Biomaterials

Molecules, 2021
The self-recognition and self-assembly of biomolecules are spontaneous processes that occur in Nature and allow the formation of ordered structures, at the nanoscale or even at the macroscale, under thermodynamic and kinetic equilibrium as a consequence ...
Andrea Caporale, Simone Adorinni, Doriano Lamba, Michele Saviano   +3 more
doaj   +1 more source

Discovery of novel spike/ACE2 inhibitory macrocycles using in silico reinforcement learning

Frontiers in Drug Discovery, 2022
Introduction: The COVID-19 pandemic has cast a heavy toll in human lives and global economics. COVID-19 is caused by the SARS-CoV-2 virus, which infects cells via its spike protein binding human ACE2.Methods: To discover potential inhibitory ...
Lev Shapira, Shaul Lerner, Guila Assayag, Alexandra Vardi, Dikla Haham, Gideon Bar, Vicky Fidelsky Kozokaro, Maayan Elias Robicsek, Immanuel Lerner, Amit Michaeli   +9 more
doaj   +1 more source

Peptoids with Antibiofilm Activity against the Gram Negative Obligate Anaerobe, Fusobacterium nucleatum

Molecules, 2021
Peptoids (oligo N-substituted glycines) are peptide analogues, which can be designed to mimic host antimicrobial peptides, with the advantage that they are resistant to proteolytic degradation.
Jamie Toole, Hannah L. Bolt, John J. Marley, Sheila Patrick, Steven L. Cobb, Fionnuala T. Lundy   +5 more
doaj   +1 more source

In Search of Small Molecules That Selectively Inhibit MBOAT4

Molecules, 2021
Ghrelin is a 28-residue peptide hormone produced by stomach P/D1 cells located in oxyntic glands of the fundus mucosa. Post-translational octanoylation of its Ser-3 residue, catalyzed by MBOAT4 (aka ghrelin O-acyl transferase (GOAT)), is essential for ...
Emily S. Murzinski, Ishika Saha, Hui Ding, David Strugatsky, Ryan A. Hollibaugh, Haixia Liu, Peter Tontonoz, Patrick G. Harran   +7 more
doaj   +1 more source