48 documents found, page 1 of 5
Proximity-Induced Nucleic Acid Degrader (PINAD) approach to targeted RNA degrad...
Mikutis, Sigitas; Rebelo, Maria; Yankova, Eliza; Gu, Muxin; Tang, Cong; Coelho, Ana R; Yang, Mo; Hazemi, Madoka E.; Pires de Miranda, MartaCopyright © 2023 The Authors. Published by American Chemical Society; Nature has evolved intricate machinery to target and degrade RNA, and some of these molecular mechanisms can be adapted for therapeutic use. Small interfering RNAs and RNase H-inducing oligonucleotides have yielded therapeutic agents against diseases that cannot be tackled using protein-centered approaches. Because these therapeutic agents ar...
De novo human angiotensin-converting enzyme 2 decoy NL-CVX1 protects mice from ...
Rebelo, Maria; Tang, Cong; Coelho, Ana R; Labão-Almeida, Carlos; Schneider, Matthias M.; Tatalick, Laurie; Ruivo, Pedro; Pires de Miranda, Marta© The Author(s) 2023. Published by Oxford University Press on behalf of Infectious Diseases Society of America. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (https://creativecommons.org/licenses/by/4.0/), which permits unrestricted reuse, distribution, and reproduction in any medium, provided the original work is properly cited.; The emergence of novel v...
Merging the Isonitrile‐Tetrazine (4+1) cycloaddition and the Ugi four‐component...
Méndez, Yanira; Vasco, Aldrin V.; Ivey, Galway; Dias, Ana Laura; Gierth, Peter; Sousa, Bárbara B.; Navo, Claudio D.; Torres‐Mozas, Angel© 2023 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.; Multicomponent reactions are of utmost importance at generating a unique, wide, and complex chemical space. Herein we desc...
De novo human angiotensin - converting enzyme 2 Decoy NL-CVX1 protects mice fro...
Rebelo, Maria; Tang, Cong; Coelho, Ana R.; Labão-Almeida, Carlos; Schneider, Matthias M.; Tatalick, Laurie; Ruivo, Pedro; de Miranda, Marta PiresThe emergence of novel variants of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) underscores the need to investigate alternative approaches to prevent infection and treat patients with coronavirus disease 2019. Here, we report the preclinical efficacy of NL-CVX1, a de novo decoy that blocks virus entry into cells by binding with nanomolar affinity and high specificity to the receptor-binding doma...
Ibrutinib inhibits BMX-dependent endothelial VCAM-1 expression in vitro and pro...
Kohs, Tia C. L.; Olson, Sven R.; Pang, Jiaqing; Jordan, Kelley R.; Zheng, Tony J.; Xie, Aris; Hodovan, James; Muller, Matthew; McArthur, Carrie© 2022 The Author(s) under exclusive licence to Biomedical Engineering Society.; Introduction: Inflammatory activation of the vascular endothelium leads to overexpression of adhesion molecules such as vascular cell adhesion molecule-1 (VCAM-1), contributing to the pro-thrombotic state underpinning atherogenesis. While the role of TEC family kinases (TFKs) in mediating inflammatory cell and platelet activation i...
Controlled in‐cell generation of active Palladium(0) species for bioorthogonal ...
Konč, Juraj; Sabatino, Valerio; Jiménez‐Moreno, Ester; Latocheski, Eloah; Pérez, Laura Rodríguez; Day, Jason; Domingos, Josiel B.© 2021 Wiley-VCH GmbH; Owing to their bioorthogonality, transition metals have become very popular in the development of biocompatible bond-cleavage reactions. However, many approaches require design and synthesis of complex ligands or formulation of nanoparticles which often perform poorly in living cells. This work reports on a method for the generation of an active palladium species that triggers bond-cleavi...
Single mutation on Trastuzumab modulates the stability of antibody–drug conjuga...
Ferhati, Xhenti; Jiménez-Moreno, Ester; Hoyt, Emily A.; Salluce, Giulia; Cabeza-Cabrerizo, Mar; Navo, Claudio D.; Compañón, Ismael; Akkapeddi, PadmaCopyright © 2022 The Authors. Published by American Chemical Society; Antibody-drug conjugates (ADCs) are a class of targeted therapeutics used to selectively kill cancer cells. It is important that they remain intact in the bloodstream and release their payload in the target cancer cell for maximum efficacy and minimum toxicity. The development of effective ADCs requires the study of factors that can alter the...
Structural insights into TRPV2 activation by small molecules
Pumroy, Ruth A.; Protopopova, Anna D.; Fricke, Tabea C.; Lange, Iris U.; Haug, Ferdinand M.; Nguyen, Phuong T.; Gallo, Pamela N.; Sousa, Bárbara B.© The Author(s) 2022. Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party ...
Dichloro Butenediamides as irreversible site‐selective protein conjugation reagent
Laserna, Victor; Abegg, Daniel; Afonso, Cláudia F.; Martin, Esther M.; Adibekian, Alexander; Ravn, Peter; Corzana, Francisco; Bernardes, Gonçalo J. L.© 2021 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.; We describe maleic-acid derivatives as robust cysteine-selective reagents for protein labelling with comparable kinetics a...
A structural ensemble of a tau-microtubule complex reveals regulatory tau phosp...
Brotzakis, Z. Faidon; Lindstedt, Philip R.; Taylor, Ross J.; Rinauro, Dillon J.; Gallagher, Nicholas C. T.; Bernardes, Gonçalo J. L.© 2021 The Authors. Published by American Chemical Society.; Tau is a microtubule-associated protein that regulates the stability of microtubules. We use metainference cryoelectron microscopy, an integrative structural biology approach, to determine an ensemble of conformations representing the structure and dynamics of a tau-microtubule complex comprising the entire microtubule-binding region of tau (residues ...