Results 21 to 30 of about 26,717 (273)

Brilacidin Demonstrates Inhibition of SARS-CoV-2 in Cell Culture

open access: yesViruses, 2021
Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the newly emergent causative agent of coronavirus disease-19 (COVID-19), has resulted in more than two million deaths worldwide since it was first detected in 2019.
Allison Bakovic   +7 more
doaj   +1 more source

Synthesis of imidazo[1,2-a]pyridine-containing peptidomimetics by tandem of Groebke–Blackburn–Bienaymé and Ugi reactions

open access: yesBeilstein Journal of Organic Chemistry, 2023
Peptidomimetics with a substituted imidazo[1,2-a]pyridine fragment were synthesized by a tandem of Groebke–Blackburn–Bienaymé and Ugi reactions. The target products contain substituted imidazo[1,2-a]pyridine and peptidomimetic moieties as pharmacophores ...
Oleksandr V. Kolomiiets   +5 more
doaj   +1 more source

QSAR Modelling of Peptidomimetic Derivatives towards HKU4-CoV 3CLpro Inhibitors against MERS-CoV

open access: yesChemistry, 2021
In this paper, we report the relationship between the anti-MERS-CoV activities of the HKU4 derived peptides for some peptidomimetic compounds and various descriptors using the quantitative structure activity relationships (QSAR) methods.
Imad Hammoudan   +4 more
doaj   +1 more source

1,2,3-Triazoles as Biomimetics in Peptide Science

open access: yesMolecules, 2021
Natural peptides are an important class of chemical mediators, essential for most vital processes. What limits the potential of the use of peptides as drugs is their low bioavailability and enzymatic degradation in vivo.
Naima Agouram   +2 more
doaj   +1 more source

A SPLUNC1 Peptidomimetic Inhibits Orai1 and Reduces Inflammation in a Murine Allergic Asthma Model.

open access: yesAmerican Journal of Respiratory Cell and Molecular Biology, 2021
Orai1 is a plasma membrane Ca2+ channel that mediates store operated Ca2+ entry (SOCE) and regulates inflammation. Short palate lung and nasal epithelial clone 1 (SPLUNC1) is an asthma gene modifier which inhibits Orai1/SOCE via its C-terminal α6 region.
J. Wrennall   +12 more
semanticscholar   +1 more source

A VEGFB-Based Peptidomimetic Inhibits VEGFR2-Mediated PI3K/Akt/mTOR and PLCγ/ERK Signaling and Elicits Apoptotic, Antiangiogenic, and Antitumor Activities

open access: yesPharmaceuticals, 2023
Vascular endothelial growth factor receptor 2 (VEGFR2) mediates VEGFA signaling mainly through the PI3K/AKT/mTOR and PLCγ/ERK1/2 pathways. Here we unveil a peptidomimetic (VGB3) based on the interaction between VEGFB and VEGFR1 that unexpectedly binds ...
Mohadeseh Namjoo   +8 more
doaj   +1 more source

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

open access: yesFrontiers 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   +9 more
doaj   +1 more source

Heterocycles as a Peptidomimetic Scaffold: Solid-Phase Synthesis Strategies

open access: yesPharmaceuticals, 2021
Peptidomimetics are a privileged class of pharmacophores that exhibit improved physicochemical and biological properties. Solid-phase synthesis is a powerful tool for gaining rapid access to libraries of molecules from small molecules to biopolymers and ...
Aizhan Abdildinova, M. Kurth, Y. Gong
semanticscholar   +1 more source

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

open access: yesMolecules, 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   +5 more
doaj   +1 more source

In vitro and in vivo screening for novel essential cell-envelope proteins in Pseudomonas aeruginosa [PDF]

open access: yes, 2015
The Gram-negative bacterium Pseudomonas aeruginosa represents a prototype of multi-drug resistant opportunistic pathogens for which novel therapeutic options are urgently required.
Bragonzi, Alessandra   +5 more
core   +1 more source

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