Results 31 to 40 of about 12,487 (241)

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

Design, Synthesis, and Antitumor Activities Study of Stapled A4K14-Citropin 1.1 Peptides

open access: yesFrontiers in Chemistry, 2020
A4K14-citropin 1.1 is a structurally optimized derivative derived from amphibians' skin secreta peptide Citropin, which exhibits broad biological activities.
Nan Wang   +7 more
doaj   +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

Peptidomimetic Polyurethanes Disrupt Surface Established Bacterial Biofilms and Prevent Biofilm Formation

open access: yes, 2021
Over 80% of all chronic bacterial infections in humans are associated with biofilms, which are surface-associated bacterial communities encased within a secreted exopolysaccharide matrix that can provide resistance to environmental and chemical insults ...
Abraham, Joy   +4 more
core   +1 more source

Multicomponent synthesis of artificial nucleases and their RNase and DNase activity

open access: yesBeilstein Journal of Organic Chemistry, 2011
The synthesis of new, artificial ribonucleases containing two amino acid residues connected by an aliphatic linker has been developed. Target molecules were synthesized via a catalytic three-component Ugi reaction from aliphatic diisocyanides ...
Anton V. Gulevich   +5 more
doaj   +1 more source

Sequence Changes Modulate Peptoid Self-Association in Water

open access: yesFrontiers in Chemistry, 2020
Peptoids, N-substituted glycine oligomers, are a class of diverse and sequence-specific peptidomimetics with wide-ranging applications. Advancing the functional repertoire of peptoids to emulate native peptide and protein functions requires engineering ...
Amelia A. Fuller   +8 more
doaj   +1 more source

Survey of Dipeptidyl Peptidase III Inhibitors: From Small Molecules of Microbial or Synthetic Origin to Aprotinin

open access: yesMolecules, 2022
Dipeptidyl peptidase III (DPP III) was originally thought to be a housekeeping enzyme that contributes to intracellular peptide catabolism. More specific roles for this cytosolic metallopeptidase, in the renin-angiotensin system and oxidative stress ...
Marija Abramić, Dejan Agić
doaj   +1 more source

Nano-G<sub>s</sub> Protein Peptidomimetics: Rational Design of Gα C-Terminus-Derived Peptides Mimicking Key Components of G<sub>s</sub>-β<sub>2</sub>AR Interactions. [PDF]

open access: yesAngew Chem Int Ed Engl
G protein‐coupled receptors (GPCRs) are major therapeutic targets. Modulating GPCR activity through intracellular sites is evolving. A structure‐ and computation‐assisted approach generated small G protein‐derived peptidomimetics targeting the intracellular binding crevice of the β2 adrenergic receptor mimicking features of the full G protein.
Tran PT   +11 more
europepmc   +2 more sources

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