Aza-Amino Acids Disrupt β-Sheet Secondary Structures [PDF]
Molecules, 2019 Cα to N substitution in aza-amino acids imposes local conformational constraints, changes in hydrogen bonding properties, and leads to adaptive chirality at the nitrogen atom. These properties can be exploited in mimicry and stabilization of peptide
Michael A. McMechen +3 more
doaj +2 more sources
Azasulfurylpeptide Modulation of CD36-Mediated Inflammation Without Effect on Neovascularization [PDF]
Biomedicines, 2018 Modulation of the cluster of differentiation-36 receptor (CD36) has proven promising for dampening pro-inflammatory macrophage signaling. For example, azapeptides (e.g., 1 and 2) bind CD36 selectively with high affinity, mitigate Toll-like receptor (TLR)
Stéphane Turcotte +8 more
doaj +2 more sources
From Covalent Traps to Fluorescent Beacons: The Expanding Arsenal of Chemical Probes for Studying Ubiquitin and Ubiquitin-Like Proteins. [PDF]
Angew Chem Int Ed EnglA large variety of chemistry‐based ubiquitin probes have been developed. ABSTRACT Ubiquitin (Ub) and ubiquitin‐like proteins (Ubls) orchestrate diverse cellular processes through reversible post‐translational modification of target proteins. Their conjugation is governed by a cascade of E1 activating, E2 conjugating, and E3 ligating enzymes, while ...
Chanda S, Liu WR.
europepmc +3 more sources
Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors. [PDF]
Angew Chem Int Ed Engl, 2021 The main protease (Mpro) of SARS‐CoV‐2 has been recognized as a significant drug target to treat COVID‐19. The design of a new fluorogenic substrate, the recombinant expression of Mpro and the development of an HTS assay were combined with a structure‐based rational approach leading to the discovery of tailored azanitriles and indole pyridyl esters as ...
Breidenbach J +20 more
europepmc +2 more sources
Sequential Optimization Approach Toward an Azapeptide-Based SARS-CoV-2 Main Protease Inhibitor. [PDF]
Arch Pharm (Weinheim)A series of small‐molecule azapeptides with various cysteine‐reactive electrophilic groups was designed, synthesized, and investigated for Mpro inhibition. Particularly suitable warheads were identified, and their linkage to a structurally expanded peptidomimetic scaffold afforded the potent lead compound 12, with kinac/Ki = 78,900 M–1s–1 and an ...
Voget R +9 more
europepmc +2 more sources
The CD36 Ligand-Promoted Autophagy Protects Retinal Pigment Epithelial Cells from Oxidative Stress. [PDF]
Oxid Med Cell Longev, 2021 The retinal pigment epithelium (RPE) performs many functions that maintain photoreceptor health. Oxidative damage to the RPE is a critical component in the pathogenesis of eye diseases such as age‐related macular degeneration (AMD). Ligands of the cluster of differentiation 36 (CD36) have previously preserved photoreceptor integrity in mouse models of ...
Dorion MF +5 more
europepmc +2 more sources
Targeting CD36 With EP 80317 Reduces Remote Inflammatory Response to Hind Limb Ischemia-Reperfusion in Mice. [PDF]
J Biochem Mol ToxicolProposed mechanism by which CD36 participates in generation of ROS and activation of leukocytes in the circulation and microvascular endothelium of lung tissue after reperfusion of an ischemic limb. Treatment with EP 80317, the CD36 modulator, decreased remote leukocyte recruitment, lipid mediators, cytokines, and lung tissue damage.
Elimam H +9 more
europepmc +2 more sources
Synthesis of new, rigid and conformation stabilizing spin labels for analysis of the orientation of transmembrane domains [PDF]
, 2021 Lipid-peptide interactions are involved in many essential processes of living organisms, such as cell fusion or transport processes and are therefore, in the center of research interest.
Portnova, Iryna
core +1 more source
Azapeptides as an Efficient Tool to Improve the Activity of Biologically Effective Peptides
Future Pharmacology, 2022 Peptides are highly potent biological active compounds with excellent selectivity and binding, but they have some drawbacks (e.g., low stability in vivo because of the enzymatic degradation, and fast elimination).
Karima Tarchoun +2 more
doaj +1 more source
The Impact of Activity‐Based Protein Profiling in Malaria Drug Discovery
ChemMedChem, Volume 17, Issue 14, July 19, 2022., 2022 Activity‐based protein profiling has impacted several biological research areas by providing functional fingerprints of enzymatic activity in complex proteomes. We discuss the main achievements of ABPP in the field of malaria research, including characterization of pathologically‐relevant enzymes, target and mechanism deconvolution of antimalarials ...
Luís A. R. Carvalho +1 more
wiley +1 more source