Results 21 to 30 of about 6,386 (165)
Covalent Peptide‐Based N‐Myc/Aurora‐A Inhibitors Bearing Sulfonyl Fluoride Warheads [PDF]
J Pept SciN‐Myc‐derived peptidomimetics bearing aryl sulfonyl fluoride warheads were shown to act as effective N‐Myc/Aurora‐A PPI inhibitors, selectively labelling Aurora‐A in a recognition‐directed manner. ABSTRACT Orthosteric inhibition of the N‐Myc/Aurora‐A protein–protein interaction (PPI) represents a potential mechanism by which degradation of N‐Myc can be
Dawber R +6 more
europepmc +2 more sources
Combinatorial assembly of small molecules into bivalent antagonists of TrkC or TrkA receptors.
PLoS ONE, 2014 A library of peptidomimetics was assembled combinatorially into dimers on a triazine-based core. The pharmacophore corresponds to β-turns of the neurotrophin polypeptides neurotrophin-3 (NT-3), nerve growth factor (NGF), or brain-derived neurotrophic ...
Fouad Brahimi +4 more
doaj +1 more source
Beilstein Journal of Organic Chemistry, 2013 A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH2 (PLG) modulates dopaminergic neurotransmission.
Swapna Bhagwanth +2 more
doaj +1 more source
Frontiers in Chemistry, 2018 An Ugi multicomponent reaction with chiral cyclic amino acids, benzyl isocyanide and cyclic ketones (or acetone) has been exploited as key step for the generation of peptidomimetics.
Lisa Moni +5 more
doaj +1 more source
Marine Drugs, 2021 Peptides have a three-dimensional configuration that can adopt particular conformations for binding to proteins, which are well suited to interact with larger contact surface areas on target proteins.
Yang Li, Wang Li, Zhengshuang Xu
doaj +1 more source
A readily applicable strategy to convert peptides to peptoid-based therapeutics. [PDF]
PLoS ONE, 2013 Incorporation of unnatural amino acids and peptidomimetic residues into therapeutic peptides is highly efficacious and commonly employed, but generally requires laborious trial-and-error approaches.
Minyoung Park +3 more
doaj +1 more source
The Use of Peptides in the Treatment of Fragile X Syndrome: Challenges and Opportunities
Frontiers in Psychiatry, 2021 Fragile X Syndrome (FXS) is the most frequent cause of inherited intellectual disabilities and autism spectrum disorders, characterized by cognitive deficits and autistic behaviors.
Alice Romagnoli, Daniele Di Marino
doaj +1 more source
Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics
Beilstein Journal of Organic Chemistry, 2014 In the recent past, the design and synthesis of peptide mimics (peptidomimetics) has received much attention. This because they have shown in many cases enhanced pharmacological properties over their natural peptide analogues.
Gijs Koopmanschap +2 more
doaj +1 more source
Molecules, 2023 Herein, advanced intermediates were synthesized through Ugi four-component reactions of isocyanides, aldehydes, masked amino aldehyde, and carboxylic acids, including N-protected amino acids.
Naděžda Cankařová, Viktor Krchňák
doaj +1 more source
Peptidomimetic Thrombin Inhibitors [PDF]
Pathophysiology of Haemostasis and Thrombosis, 2003 The central position of thrombin in the coagulation cascade has made it a popular target for discovery of novel antithrombotic agents. Starting with hirudin, a natural peptide isolated from the medicinal leech, its shorter synthetic analogue hirulog, and argatroban,the first therapeutically used synthetic small-molecule thrombin active site inhibitor ...
openaire +2 more sources