Results 71 to 80 of about 17,763 (235)

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

Design of Peptidomimetic Functionalized Cholesterol Based Lipid Nanoparticles for Efficient Delivery of Therapeutic Nucleic Acids

Molecules, 2019
Lipid nanoparticles (LNP) are the most potent carriers for the delivery of nucleic acid-based therapeutics. The first FDA approved a short interfering RNA (siRNA) drug that uses a cationic LNP system for the delivery of siRNA against human transthyretin (
Ehexige Ehexige, Tsogzolmaa Ganbold, Xiang Yu, Shuqin Han, Huricha Baigude   +4 more
doaj   +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

Peptidomimetic blockade of MYB in acute myeloid leukemia

Nature Communications, 2017
Aberrant gene expression is a hallmark of acute leukemias. MYB-driven transcriptional coactivation with CREB-binding protein (CBP)/P300 is required for acute lymphoblastic and myeloid leukemias, including refractory MLL-rearranged leukemias.
Kavitha Ramaswamy, L. Forbes, Gerard Minuesa, T. Gindin, Fiona C. Brown, M. Kharas, A. Krivtsov, S. Armstrong, Eric R. Still, E. de Stanchina, B. Knoechel, R. Koche, A. Kentsis   +12 more
semanticscholar   +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

Novel Furanoid α-Substitued α-Amino Acid as a Potent Turn Mimic in Peptide Synthesis

Molecules, 2006
A stereoselective approach has been developed to the new sugar amino acid and potential potent turn mimic 5-O-(tert-butyldimethylsilyl)-3-deoxy-1,2-O- isopropylidene-3-methoxycarbonylamino-α-D-xylofuranose 3-C-carboxylic acid (12), via the [3,3 ...
Jana Raschmanová, Jozef Gonda, Miroslava Martinková   +2 more
doaj   +1 more source

New Morphiceptin Peptidomimetic Incorporating (1S,2R,3S,4S,5R)-2-Amino-3,4,5-trihydroxycyclopen-tane-1-carboxylic acid: Synthesis and Structural Study

Molecules, 2020
We present the synthesis and structural study of a new peptidomimetic of morphiceptin, which can formally be considered as the result of the replacement of the central proline residue of this natural analgesic drug with a subunit of (1S,2R,3S,4S,5R)-2 ...
Raquel Soengas, Marcos Lorca, Begoña Pampín, Víctor M. Sánchez-Pedregal, Ramón J. Estévez, Juan C. Estévez   +5 more
doaj   +1 more source

Structures of Zika virus NS2B‐NS3 protease in complex with peptidomimetic inhibitors

Antiviral Research, 2018
Zika virus NS2B‐NS3 protease plays an essential role in viral replication by processing the viral polyprotein into individual proteins. The viral protease is therefore considered as an ideal antiviral drug target.
W. W. Phoo, Zhenzhen Zhang, M. Wirawan, E. Chew, Alvin Bing Liang Chew, Jenny Kouretova, T. Steinmetzer, D. Luo   +7 more
semanticscholar   +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

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