Results 71 to 80 of about 10,137 (233)
Chemistry – A European Journal, EarlyView.A modular, de novo α/β‐peptide design strategy allows fine‐tuning of ligand properties, resulting in multivalent ligands that simultaneously target separate binding sites on the protein surface. ABSTRACT Protein‐protein interactions that regulate gene expression in the nucleus are increasingly recognized as potential therapeutic targets but present ...
Márk V. Tresztián +4 more
wiley +1 more source
Development of Antiviral Peptidomimetics
, 2023 Protein-protein interactions (PPIs) are essential for biological processes and are associated with a number of diseases, including cancer, infectious diseases, and neurodegenerative diseases.
Xue, Songyi
core
European Journal of Medicinal Chemistry ReportsThe design of pharmaceutically relevant compounds that mimic bioactive peptides or secondary structure elements in proteins is an important task in medicinal chemistry. Over time, various chemical strategies have been developed to convert natural peptide
Atsushi Yoshimori, Jürgen Bajorath
doaj +1 more source
Molecules, 2016 A solid-phase procedure is used to synthesize racemic peptidomimetics based on the fundamental peptide unit. The peptidomimetics are constructed around proline or proline homologues variably substituted at the amine and carbonyl sites.
Ziniu Zhou +2 more
doaj +1 more source
Chemistry – A European Journal, EarlyView.Integrin αVβ3‐targeting small‐molecule drug conjugates (SMDCs) were synthesized by conjugating a cryptophycin payload through a neutrophil elastase‐cleavable NPV‐PABC linker. RGD peptidomimetic and linker epimers served as controls for targeting and enzymatic cleavage, and the resulting conjugates displayed subnanomolar cytotoxicity in vitro.
Dominic Seißenschmidt +3 more
wiley +1 more source
Synthesis of thioureido peptidomimetics employing alkyl azides and dithiocarbamates
, 2018 An unprecedented approach for the assembly of thioureido peptidomimetics is developed employing alkyl azides and dithiocarbamates. Dithiocarbamates react with alkyl azides with the liberation of N2 and elemental sulfur thereby leading to thiourea in a ...
Vishwanatha, T.M. +4 more
core +1 more source
Plasmepsins as Antimalarial Drug Targets—Then, Now, and the Future
Medicinal Research Reviews, EarlyView.ABSTRACT Malaria is a devastating disease caused by Plasmodium parasites. Plasmodium parasites express ten cathepsin D‐like aspartyl proteases, called plasmepsins (PMs). These PMs have diverse roles fulfill diverse functions throughout the parasite's lifecycle, though several exhibit functional redundancies. Among them, PMV, PMIV, and PMX are essential
Brad E. Sleebs
wiley +1 more source
In Silico Structure‐Guided Design of Peptide Candidates Targeting γ‐Secretase Subunit Assembly
Proteins: Structure, Function, and Bioinformatics, EarlyView.ABSTRACT The γ‐secretase complex is a membrane‐embedded protease essential for intramembrane cleavage of substrates such as Notch receptors and the amyloid precursor protein (APP), processes central to cancer progression and Alzheimer's disease (AD) pathology.
Selcen Arı Yuka +2 more
wiley +1 more source
The Chemical Record, EarlyView.This review highlights recent advances in the use of organic carbonates, dimethyl carbonate (DMC), diethyl carbonate (DEC), and propylene carbonate (PC), as solvents in organic synthesis. Based on over seventy studies from the past 6 years, it shows their application in different organic reaction types, emphasizing their role in safer and more ...
Gabriela T. Quadros +5 more
wiley +1 more source
Cell adhesive PET membranes by surface grafting of RGD peptidomimetics.
, 2005 A non-peptide mimic of the Arg-Gly Asp (RGD) active sequence of adhesive proteins (such as vitronectin) has been equipped with two different spacer-arms for surface anchorage.
Biltresse, Stéphane +2 more
core +1 more source