Results 31 to 40 of about 26,717 (273)

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

open access: yesMolecules, 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   +6 more
doaj   +1 more source

In Search of Small Molecules That Selectively Inhibit MBOAT4

open access: yesMolecules, 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   +7 more
doaj   +1 more source

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

open access: yesFrontiers 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   +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

open access: yesAntibiotics, 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   +10 more
doaj   +1 more source

Designing Peptidomimetics [PDF]

open access: yesCurrent Topics in Medicinal Chemistry, 2018
The concept of a peptidomimetic was coined about forty years ago. Since then, enormous effort and interest have been devoted to mimic the properties of peptides with small molecules or pseudopeptides. The present report aims to review different approaches described in the past to succeed in this goal.
openaire   +4 more sources

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

open access: yesViruses, 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   +8 more
doaj   +1 more source

Repurposing cancer drugs, batimastat and marimastat, to inhibit the activity of a group I metalloprotease from the venom of the Western Diamondback rattlesnake, Crotalus atrox [PDF]

open access: yes, 2020
Snakebite envenomation causes over 140,000 deaths every year predominantly in developing countries. As a result, it is one of the most lethal neglected tropical diseases.
Bicknell, Andrew B.   +12 more
core   +1 more source

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

open access: yesFrontiers 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   +5 more
doaj   +1 more source

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

open access: yesFrontiers 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   +7 more
doaj   +1 more source

A New Multi-Objective Approach for Molecular Docking Based on RMSD and Binding Energy [PDF]

open access: yes, 2016
Ligand-protein docking is an optimization problem based on predicting the position of a ligand with the lowest binding energy in the active site of the receptor.
Aldana-Montes, Jose Francisco   +4 more
core   +1 more source

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