Results 31 to 40 of about 17,763 (235)

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

Efficacy of natural antimicrobial peptides versus peptidomimetic analogues: a systematic review.

Future Medicinal Chemistry, 2022
Aims: This systematic review was carried out to determine whether synthetic peptidomimetics exhibit significant advantages over antimicrobial peptides (AMPs) in terms of in vitro potency.
Lauren Hellewell, Nakisa Malek Gilani, Christopher J. Stanton, L. Pelligand, H. Franzyk, L. Guardabassi, L. Good   +6 more
semanticscholar   +1 more source

Conjugates of 1'-Aminoferrocene-1-carboxylic Acid and Proline: Synthesis, Conformational Analysis and Biological Evaluation

Molecules, 2014
Our previous studies showed that alteration of dipeptides Y-Fca-Ala-OMe (III) into Y-Ala-Fca-OMe (IV) (Y = Ac, Boc; Fca = 1'-aminoferrocene-1-carboxylic acid) significantly influenced their conformational space.
Monika Kovačević, Krešimir Molčanov, Kristina Radošević, Višnja Gaurina Srček, Sunčica Roca, Alan Čače, Lidija Barišić   +6 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

Repurposing Azithromycin and Rifampicin Against Gram-Negative Pathogens by Combination With Peptidomimetics

Frontiers in Cellular and Infection Microbiology, 2019
Synthetic peptidomimetics may be designed to mimic functions of antimicrobial peptides, including potentiation of antibiotics, yet possessing improved pharmacological properties.
Kristin R. Baker, Kristin R. Baker, Bimal Jana, Bimal Jana, Anna Mette Hansen, Hanne Mørck Nielsen, Henrik Franzyk, Luca Guardabassi, Luca Guardabassi   +8 more
doaj   +1 more source

Cationic Peptidomimetic Amphiphiles Having a N-Aryl- or N-Naphthyl-1,2,3-Triazole Core Structure Targeting Clostridioides (Clostridium) difficile: Synthesis, Antibacterial Evaluation, and an In Vivo C. difficile Infection Model

Antibiotics, 2021
Clostridioides (also known as Clostridium) difficile is a Gram-positive anaerobic, spore producing bacterial pathogen that causes severe gastrointestinal infection in humans.
Muni Kumar Mahadari, Sreenu Jennepalli, Andrew J. Tague, Papanin Putsathit, Melanie L. Hutton, Katherine A. Hammer, Daniel R. Knight, Thomas V. Riley, Dena Lyras, Paul A. Keller, Stephen G. Pyne   +10 more
doaj   +1 more source

Quinazolinone-Peptido-Nitrophenyl-Derivatives as Potential Inhibitors of SARS-CoV-2 Main Protease

Viruses, 2023
The severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2-Mpro) plays an essential role in viral replication, transcription, maturation, and entry into host cells.
Huynh-Nguyet-Huong Giang, Feng-Pai Chou, Ching-Yun Chen, Shen-Chieh Chou, Sheng-Cih Huang, Tuoh Wu, Bui-Thi-Buu Hue, Hong-Cheu Lin, Tung-Kung Wu   +8 more
doaj   +1 more source

Bicyclic Pyrrolidine-Isoxazoline γ Amino Acid: A Constrained Scaffold for Stabilizing α-Turn Conformation in Isolated Peptides

Frontiers in Chemistry, 2019
Unnatural amino acids have tremendously expanded the folding possibilities of peptides and peptide mimics. While α,α-disubstituted and β-amino acids are widely studied, γ-derivatives have been less exploited.
Francesco Oliva, Raffaella Bucci, Lucia Tamborini, Stefano Pieraccini, Andrea Pinto, Sara Pellegrino   +5 more
doaj   +1 more source

Dioctanoyl Ultrashort Tetrabasic β-Peptides Sensitize Multidrug-Resistant Gram-Negative Bacteria to Novobiocin and Rifampicin

Frontiers in Microbiology, 2021
Recently reported peptidomimetics with increased resistance to trypsin were shown to sensitize priority multidrug-resistant (MDR) Gram-negative bacteria to novobiocin and rifampicin.
Danyel Ramirez, Liam Berry, Ronald Domalaon, Yanqi Li, Gilbert Arthur, Ayush Kumar, Frank Schweizer, Frank Schweizer   +7 more
doaj   +1 more source