A cyclic azapeptide ligand of the scavenger receptor CD36/SR-B2 reduces the atherosclerotic lesion progression and enhances plaque stability in apolipoprotein E-deficient mice [PDF]
Frontiers in Pharmacology, 2023 Atherosclerosis is a chronic inflammatory disease of the arterial walls that develops at predisposed sites. As a major risk factor for adverse cardiovascular pathology, atherosclerosis can progress to myocardial infarction and stroke, due to the rupture ...
Jade Gauvin +12 more
doaj +2 more sources
Computational Investigation of Conformational Properties of Short Azapeptides: Insights from DFT Study and NBO Analysis [PDF]
Molecules, 2023 Azapeptides have gained much attention due to their ability to enhance the stability and bioavailability of peptide drugs. Their structural preferences, essential to understanding their function and potential application in the peptide drug design ...
Mouna El Khabchi +7 more
doaj +2 more sources
Azapeptide activity-based probes for the SARS-CoV-2 main protease enable visualization of inhibition in infected cells. [PDF]
Chem Sci, 2023 The COVID-19 pandemic has revealed the vulnerability of the modern, global society. With expected waves of future infections by SARS-CoV-2, treatment options for infected individuals will be crucial in order to decrease mortality and hospitalizations ...
Vanhoutte R +10 more
europepmc +3 more sources
Synthesis and Biomedical Potential of Azapeptide Modulators of the Cluster of Differentiation 36 Receptor (CD36) [PDF]
Biomedicines, 2020 The innovative development of azapeptide analogues of growth hormone releasing peptide-6 (GHRP-6) has produced selective modulators of the cluster of differentiation 36 receptor (CD36).
Caroline Proulx +5 more
doaj +2 more sources
Transmembrane Fluoride Transport by a Cyclic Azapeptide With Two β-Turns [PDF]
Frontiers in Chemistry, 2021 Diverse classes of anion transporters have been developed, most of which focus on the transmembrane chloride transport due to its significance in living systems.
Zhixing Zhao +7 more
doaj +2 more sources
Ubiquitin Azapeptide Esters as Next-Generation Activity-Based Probes for Cysteine Enzymes in the Ubiquitin Signal Pathway. [PDF]
J Am Chem SocUbiquitination is a pivotal cellular process that controls protein homeostasis and regulates numerous biological functions. Its pathway operates through a cascade of enzyme reactions involving ubiquitin-activating (E1), ubiquitin-conjugating (E2), and ...
Chanda S +11 more
europepmc +3 more sources
Cyst Reduction in a Polycystic Kidney Disease Drosophila Model Using Smac Mimics [PDF]
Biomedicines, 2019 Autosomal dominant polycystic kidney disease (ADPKD) is an inherited malady affecting 12.5 million people worldwide. Therapeutic options to treat PKD are limited, due in part to lack of precise knowledge of underlying pathological mechanisms.
Cassandra Millet-Boureima +3 more
doaj +3 more sources
Neighbor effect on conformational spaces of alanine residue in azapeptides [PDF]
HeliyonThe conformational properties of Alanine (Ala) residue have been investigated to understand protein folding and develop force fields. In this work, we examined the neighbor effect on the conformational spaces of Ala residue using model azapeptides, Ac ...
Ho-Jin Lee +9 more
doaj +2 more sources
Selective Azapeptide CD36 Ligand MPE-298 Regulates oxLDL-LOX-1-Mediated Inflammation and Mitochondrial Oxidative Stress in Macrophages [PDF]
CellsMacrophage mitochondrial dysfunction, caused by oxidative stress, has been proposed as an essential event in the progression of chronic inflammation diseases, such as atherosclerosis.
Mukandila Mulumba +10 more
doaj +2 more sources
Heterochiral coupling to bilateral β-turn structured azapeptides bearing two remote chiral centers [PDF]
Nature CommunicationsEnantioselective synthesis governed by chiral catalysts has been extensively developed, but that without any chiral auxiliaries or chiral catalysts is rare, particularly when remote stereogenic centers are involved.
Xiaosheng Yan +6 more
doaj +2 more sources