Results 91 to 100 of about 10,137 (233)

GPE Analogs and Peptidomimetics

open access: yes, 2002
This invention relates to analogs and peptidomimetics of glycyl-L-prolyl-L-glutamic acid (GPE). In particular, this invention relates to GPE analogs and peptidomimetics that are anti-apoptotic and anti-necrotic, to methods of making them, to ...
Abood, NA, Brimble, Margaret
core  

Statine-based peptidomimetic compounds as inhibitors for SARS-CoV-2 main protease (SARS-CoV‑2 Mpro)

open access: yesScientific Reports
COVID-19 is a multisystemic disease caused by the SARS-CoV-2 airborne virus, a member of the Coronaviridae family. It has a positive sense single-stranded RNA genome and encodes two non-structural proteins through viral cysteine-proteases processing ...
Pedro Henrique R. de A. Azevedo   +18 more
doaj   +1 more source

Phenylalanine-derived β-lactam TRPM8 antagonists: revisiting configuration and new benzoyl derivatives [PDF]

open access: yesExploration of Drug Science
Aim: To expand the understanding of the structure-activity relationship within a family of amino acid-derived β-lactam TRPM8 (transient receptor potential melastatin channel, subtype 8) antagonists, this work investigated both the configuration ...
Cristina Martín-Escura   +6 more
doaj   +1 more source

Targeting the noncatalytic activity of GSK3β modulates neuronal excitability in medium spiny neurons via Nav1.6 interactions

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Kinases phosphorylate ion channels, but their noncatalytic roles via protein–protein interactions (PPI) are less understood. Here, we identified the peptidomimetic ZL141 to characterize the PPI between GSK3β and Nav1.6, revealing a noncatalytic role for GSK3β in regulating Nav1.6 currents and neuronal excitability ...
Aditya K. Singh   +19 more
wiley   +1 more source

Venom peptides and peptidomimetics as therapeutics

open access: yes, 2022
In the last 10 years, antimicrobial resistance (AMR) has become a huge public health concern with an estimated 10 million deaths per year and a projected $100 trillion impact on global the economy.
Ahmad, Zulfiqar, Akhtar, Suhail
core   +1 more source

A guide to the types, structures, and multifaceted functions of matrix metalloproteinases in cancer

open access: yesThe FEBS Journal, EarlyView.
Matrix metalloproteinases (MMPs) orchestrate cancer progression and metastasis through proteolytic and non‐proteolytic actions. By remodeling the tumor microenvironment, enhancing growth factor availability, and modulating cell behavior, MMPs promote proliferation, migration or invasion, and epithelial‐to‐mesenchymal transition. Alongside extracellular
Zoi Piperigkou   +4 more
wiley   +1 more source

Peptidomimetics to mimic protein-protein interactions [PDF]

open access: yes, 2005
Quenched Molecular Dynamics (QMD) used to explore molecular conformations was developed to operate in Insight II platform for two simulation engines: CHARMm and Discover.
Xia, Zebin
core  

ADAM17 and its proteolytic targets in disease pathogenesis

open access: yesThe FEBS Journal, EarlyView.
ADAM17 as a multifunctional sheddase with contrasting roles across inflammatory, metabolic, cardiovascular, and neoplastic diseases. Through regulated activation by iRhom, iTAP/FRMD8, and tetraspanins, ADAM17 cleaves diverse membrane ligands and receptors, thereby promoting inflammation, fibrosis, obesity, insulin resistance, and tumor progression ...
Abdulbasit Amin, Marina Badenes
wiley   +1 more source

Development of Bioactive Peptidomimetics

open access: yes, 2018
Peptidomimetics are synthetic foldamers that expected more resistant to proteolytic degradation and enormous chemodiversity when compared with peptides.
She, Fengyu
core  

One-Pot High-Throughput Synthesis of β-Turn Cyclic Peptidomimetics via “Volatilizable” Supports

open access: yes, 2016
A promising method for the high-throughput synthesis of linear C-hydroxyalkylamido peptidomimetics and β-turn cyclic peptidomimetics via “volatilizable” aminoalkyl functionalized silica gels is presented. Boc amino acids and carboxylic acids were coupled
Yangmei Li (322348)   +3 more
core   +1 more source

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