Results 91 to 100 of about 33,100 (295)

Engineering Rapid Payload Release Rate in 1,6‐Elimination Processes of Self‐Immolative Linkers

Angewandte Chemie, EarlyView.
The payload release rate of self‐immolative linkers was greatly improved through stabilization of an intermediate carbocation, thereby achieving an up to 10 000‐fold improvement in rate constant. Furthermore, lipophilicity was identified as another factor that affects the release rate. This new strategy is applicable to different payloads and different
Albert Marten Schulte, Gülbahar Bozan, Francesca Amoroso, Bart Cornelissen, Wiktor Szymanski   +4 more
wiley   +2 more sources

Prodrugs of Reverse Fosmidomycin Analogues

, 2015
Fosmidomycin inhibits IspC (Dxr, 1-deoxy-d-xylulose 5-phosphate reductoisomerase), a key enzyme in nonmevalonate isoprenoid biosynthesis that is essential in Plasmodium falciparum. The drug has been used successfully to treat malaria patients in clinical
Graewert, Tobias, Claudia Lienau (1648396), Adelbert Bacher (1304808), Held, Jana, Karin Brücher (1648393), Kurz, Thomas, Benjamin Mordmüller (1648387), Behrendt, Christoph, Fischer, Markus, Bruecher, Karin, Boris Illarionov (1304811), Maes, Louis, Tobias Gräwert (1648402), Christoph Behrendt (1648390), Jana Held (224956), Sergio Wittlin (181945), Konzuch, Sarah, Thomas Kurz (1648405), Wittlin, Sergio, Lienau, Claudia, Sarah Konzuch (1648399), Louis Maes (191127), Markus Fischer (111964), Illarionov, Boris, Bacher, Adelbert, Mordmueller, Benjamin, Mordmüller, Benjamin Gottlieb   +26 more
core   +1 more source

Spatiotemporally Precise Rheumatoid Arthritis Therapy via a Triple‐Locked Cascaded Nanoplatform With Dual‐Channel Self‐Reporting

Advanced Science, EarlyView.
An orthogonally programmable nanotheranostic (MB@YW NPs) enables precision therapy for rheumatoid arthritis. A triple‐locked (pH, HOCl/ONOO−, light) independently drives the release of methotrexate and sulfasalazine. Trackable by dual‐channel fluorescence, this coordinated drug delivery remodels the inflammatory microenvironment to markedly suppress ...
Jihong Liu, Wendi Zhu, Shiyun Xu, Shichang Liu, Wenjun Tang, Xiaoyu Ma, Ting Yang, Haojian Yang, Hongtong Wang, Lu Cao, Lijie Tan, Qi Wang   +11 more
wiley   +1 more source

BRCA1 Mutation‐Recognizing Tetrahedral Framework Nucleic Acid Nanoplatform Enables Coordinated PARP/WEE1 Inhibition and STING‐Associated Antitumor Immunity in Ovarian Cancer

Advanced Science, EarlyView.
BRCA1 mutation‐responsive FBOA‐tFNA selectively recognizes mutant transcripts and coordinates reduction‐responsive intracellular delivery of olaparib and adavosertib, amplifying DNA damage and weakening G2/M checkpoint protection. These effects are accompanied by STING‐associated immune activation and stronger antitumor immunity, while sequential anti ...
Chenyi Wang, Mengying Yao, Jinhui Xie, Dingjie Wang, Yashi Shi, Xiaodan Mao, Chunhua Lu, Pengming Sun   +7 more
wiley   +1 more source

Advanced Prodrug Strategies in Nucleoside and Non-Nucleoside Antiviral Agents: A Review of the Recent Five Years

Molecules, 2017
Background: Poor pharmacokinetic profiles and resistance are the main two drawbacks from which currently used antiviral agents suffer, thus make them excellent targets for research, especially in the presence of viral pandemics such as HIV and hepatitis ...
Hanadi Sinokrot, Tasneem Smerat, Anas Najjar, Rafik Karaman   +3 more
doaj   +1 more source

Phase‐Programmed Microneedles Enable Sequential Hydrogen and Quercetin Release for Scar‐Reduced Regeneration of Burn Wounds

Advanced Science, EarlyView.
A phase‐programmed microneedle patch, comprising a poly (lactic‐co‐glycolic acid) (PLGA) shell and a sulfobutylether‐β‐cyclodextrin (SBECD) core, is designed for sequential hydrogen and quercetin release for scar‐reduced regeneration of burn wounds. ABSTRACT Burn wounds complicated by bacterial infection and fibrotic scarring remain a major clinical ...
Yongnian Zeng, Zhigang Chu, Huiyuan Yang, Wen Zhang, Peng Jiang, Jiapeng Lei, Siyu Zhang, Qiongfang Ruan, Shuhua Liu, Wei Li   +9 more
wiley   +1 more source

Protease-Activated Drug Development

Theranostics, 2012
In this extensive review, we elucidate the importance of proteases and their role in drug development in various diseases with an emphasis on cancer. First, key proteases are introduced along with their function in disease progression.
Ki Young Choi, Magdalena Swierczewska, Seulki Lee, Xiaoyuan Chen
doaj  

Clickable prodrugs bearing potent and hydrolytically cleavable nicotinamide phosphoribosyltransferase inhibitors

, 2018
Keivan Sadrerafi, Emilia O Mason, Mark W Lee Jr Department of Chemistry, University of Missouri, Columbia, MO, USA Purpose: Our previous study indicated that carborane containing small-molecule 1-(hydroxymethyl)-7-(4′-(trans-3″-(3‴-pyridyl ...
Lee Jr MW, Sadrerafi K, Mason EO
core  

Glutaredoxine reduzieren schnell Glutathionhydroper‐ und Glutathionpolysulfide

Angewandte Chemie, EarlyView.
Glutaredoxine (Grx) reduzieren Glutathionpolysulfide (GSSnSG) schnell zu Glutathionhydroper/polysulfiden (GSSnH) oder GSSnH zu Wasserstoff(poly)sulfiden (H2Sn). Die Reduktion glutathionylierter Grx durch reduziertes Glutathion (GSH) liefert Glutathiondisulfid (GSSG).
Philipp Reinert, Seiryo Ogata, Laura Leiskau, Sernur Sena Yildiz, Takaaki Akaike, Uladzimir Barayeu, Marcel Deponte   +6 more
wiley   +1 more source

Aktivierung von Metallkomplexen durch Ultraschallwellen für eine gezielte Krebstherapie

Angewandte Chemie, EarlyView.
Ultrasound enables non‐invasive activation of metal‐based therapeutics deep within tumors. Acoustic cavitation can drive sonodynamic reactive oxygen species generation or mechanochemical metal–ligand bond dissociation, enabling controlled release of bioactive payloads.
Félix Grosjean, Nicolás Montesdeoca, Gilles Berger, Johannes Karges   +3 more
wiley   +1 more source