Results 31 to 40 of about 10,137 (233)

Development of peptidomimetic ligands of Pro-Leu-Gly-NH2 as allosteric modulators of the dopamine D2 receptor

open access: yesBeilstein 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

Design and Synthesis of Novel Peptidomimetics for Cancer Immunotherapy

open access: yes, 2020
Tumor cells benefit from some certain signals, which are referred to as “immune checkpoints”, to escape immune-mediated destruction. With that in mind, it is believed that the blockade of these points, such as programmed cell death Ligand-1 (PD-L1) and ...
Zeynep, Tuğay   +11 more
core   +1 more source

Exploitation of the Ugi 5-Center-4-Component Reaction (U-5C-4CR) for the Generation of Diverse Libraries of Polycyclic (Spiro)Compounds

open access: yesFrontiers 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

Well-Tempered MetaDynamics based method to evaluate universal peptidomimetics [PDF]

open access: yes, 2018
Peptidomimetics are a broad family of compounds designed to mimic the main structural features of peptides, avoiding their metabolic drawbacks. In particular, universal peptidomimetics use only peptide side-chain analogs to mimic different secondary ...
GANDINI, ENRICO   +4 more
core   +1 more source

Improvement on Permeability of Cyclic Peptide/Peptidomimetic: Backbone N-Methylation as A Useful Tool

open access: yesMarine 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]

open access: yesPLoS 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

open access: yesFrontiers 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

open access: yesBeilstein 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

Studies of Insulin Dicarba-Peptidomimetics

open access: yes, 2019
This thesis explores the chemical synthesis of novel insulin molecules. It identifies new synthetic strategies to afford molecules of this type, and evaluates the biological activity of the insulins synthesised.
ANDREW MAGNUS WRIGHT (6563372)
core   +1 more source

Regioselective Cyclic Iminium Formation of Ugi Advanced Intermediates: Rapid Access to 3,4-Dihydropyrazin-2(1H)-ones and Other Diverse Nitrogen-Containing Heterocycles

open access: yesMolecules, 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

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