Results 51 to 60 of about 6,642 (186)

Dynamic Control of Nucleic Acids Self‐Assembly and Expression Using Photoswitches

Chemistry – A European Journal, EarlyView.
We review here the recent progress made in the design of molecular photoswitches, and highlight their implementation for the dynamic control over nucleic acids self‐assembly and expression. ABSTRACT Synthetic nucleic acids have become readily available and now constitute versatile building blocks in materials science—where they can be used to engineer ...
Noemí Nogal, Hugo Laigle, Maxime Mansy, Sébastien Ulrich, Mathieu Surin   +4 more
wiley   +1 more source

De Novo Design of Multivalent α/β‐Peptides Mimicking Transcription Factors Targeting the CBP KIX Domain

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, Vencel L. Petrovicz, Edit Wéber, Tamás A. Martinek, Zsófia Hegedüs   +4 more
wiley   +1 more source

Synthesis of Biologically Active Arginine Derivatives Derived from Salicylamide

Chemistry Proceedings
Peptidomimetics represent a promising group of biologically active compounds with broad therapeutic potential that mimic naturally occurring peptides while overcoming their limitations. In this study, novel peptidomimetics derived from salicylic acid and
Martin Šanda, Aleš Imramovský
doaj   +1 more source

Extracellularly Activatable Conjugates of RGD Peptidomimetics and Cryptophycin for αVβ3‐Targeted Cancer Therapy

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, Henriette Hartung, Jonah Kammer, Norbert Sewald   +3 more
wiley   +1 more source

Hybrid Macrocyclic Peptides — Synthetic Strategies to Diversify and Cyclize Peptide Libraries in Phage Display Selections

Chemistry – A European Journal, EarlyView.
Hybrid macrocyclic peptides unite genetically encoded peptide libraries with the structural complexity of synthetic small molecules. This Review critically analyzes phage‐compatible cyclization and diversification chemistries, highlights emerging opportunities beyond traditional cysteine‐based approaches, and outlines how future advances may enable the
Titia Rixt Oppewal, Clemens Mayer
wiley   +1 more source

Cyclic Octamer Peptoids: Simplified Isosters of Bioactive Fungal Cyclodepsipeptides

Molecules, 2018
Cyclic peptoids have recently emerged as an important class of bioactive scaffolds with unique conformational properties and excellent metabolic stabilities.
Assunta D’Amato, Giorgio Della Sala, Irene Izzo, Chiara Costabile, Yuichi Masuda, Francesco De Riccardis   +5 more
doaj   +1 more source

Diarylethene‐Containing Photoswitchable Analogues of Tubulysins—Design, Synthesis, Biological, and Structural Evaluation

European Journal of Organic Chemistry, EarlyView.
Diarylethene‐containing cyclic tubulysin analogues were designed, synthesized, and evaluated as light‐responsive cytotoxic agents. One analogue showed reversible photoswitching, photoregulated tubulin polymerization inhibition, and photoform‐dependent cytotoxicity.
Anna Iampolska, Sergii Afonin, Oleg Babii, Mahri Park, Juan Estévez‐Gallego, Michel O. Steinmetz, Andrea E. Prota, Anne S. Ulrich, David R. Spring, Igor V. Komarov   +9 more
wiley   +1 more source

Therapeutic peptides and peptidomimetics

Current Opinion in Biotechnology, 1997
Peptidomimetics are one set of probes used in the transition pathway of small molecule drug design. Cyclization of the peptide backbone and its modification with aromatic residues constitutes an effective approach to mimetic drug design and circumvents obstacles associated with delivery and formulation of peptides and peptidomimetics. In the past year,
T, Kieber-Emmons, R, Murali, M I, Greene
openaire   +2 more sources

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

Dimethyl‐, Diethyl‐, and Propylene Carbonates: An Emerging Class of Green Solvents for Organic Synthesis

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, Livia C. L. Valente, Thiago Barcellos, Daniela Hartwig, Laura Abenante, Eder J. Lenardão   +5 more
wiley   +1 more source