Results 61 to 70 of about 6,190 (152)

Hydroxamic Acid as a Potent Metal-Binding Group for Inhibiting Tyrosinase

Antioxidants, 2022
Tyrosinase, a metalloenzyme containing a dicopper cofactor, plays a central role in synthesizing melanin from tyrosine. Many studies have aimed to identify small-molecule inhibitors of tyrosinase for pharmaceutical, cosmetic, and agricultural purposes ...
Joonhyeok Choi, Trilok Neupane, Rishiram Baral, Jun-Goo Jee   +3 more
doaj   +1 more source

Synthesis and Activity‐Based Protein Profiling Identifies Aldo‐Keto Reductase 1C3 as Target Protein of Myxoglucamides

Angewandte Chemie International Edition, EarlyView.
Myxoglucamide A—a novel glycolipopeptide isolated from myxobacteria—was synthesized, and activity‐based protein profiling identified aldo‐keto reductase 1C3 (AKR1C3) as its main target in human cells. Structure‐activity relationship studies, together with biophysical characterization and X‐ray crystallography, elucidated the structural basis of AKR1C3 ...
Thomas Siemon, Vivek K. Mishra, Mingming Zhao, Konrad Büssow, Alexander Popoff, Chengzhang Fu, Rolf Müller, Lothar Jänsch, Wulf Blankenfeldt, Mark Brönstrup   +9 more
wiley   +1 more source

Preparation data of the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B and crystallization of BRD4(1)-inhibitor complexes

Data in Brief, 2016
This article presents detailed purification procedures for the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B. In addition we provide crystallization protocols for apo BRD4(1) and BRD4(1) in complex with numerous inhibitors.
Martin Hügle, Xavier Lucas, Gerhard Weitzel, Dmytro Ostrovskyi, Bernhard Breit, Stefan Gerhardt, Karin Schmidtkunz, Manfred Jung, Roland Schüle, Oliver Einsle, Stefan Günther, Daniel Wohlwend   +11 more
doaj   +1 more source

From anthelmintic to neuro‐oncology: A systematic review of mebendazole repurposing for brain tumour therapy

British Journal of Clinical Pharmacology, EarlyView.
Abstract Aim Mebendazole (MBZ), a benzimidazole anthelmintic with established clinical use, has emerged as a repurposing candidate for primary brain tumours due to its multimodal anticancer actions and central nervous system penetrance. This systematic review synthesizes preclinical and clinical evidence evaluating MBZ's efficacy, mechanisms of action ...
Ciara B. Blum, Milli McMenamin, Tessa Khoo, John M. Edwin, Prathibha Jose, Liam A. O’Callaghan   +5 more
wiley   +1 more source

“Personalized mechanisms of Lafora disease using Differential Scanning Fluorimetry”

The FASEB Journal, 2019
Lafora disease is an autosomal recessive neurodegenerative disease. Patients grow up normally for their first decade of life, then develop severe epilepsy, and die in their 20s or 30s from massive neurodegeneration. The field has demonstrated that the pathogenic agent of the disease are aberrant glycogen molecules.
Kit Donohue, M. Katherine Brewer, Craig W Vander Kooi, Matthew S Gentry   +3 more
openaire   +1 more source

Bacterial Expression of Human Butyrylcholinesterase as a Tool for Nerve Agent Bioscavengers Development

Molecules, 2017
Human butyrylcholinesterase is a performant stoichiometric bioscavenger of organophosphorous nerve agents. It is either isolated from outdated plasma or functionally expressed in eukaryotic systems.
Xavier Brazzolotto, Alexandre Igert, Virginia Guillon, Gianluca Santoni, Florian Nachon   +4 more
doaj   +1 more source

Polycationic Peptide Engineering of Phage Endolysins Expands Host Range and Enhances Antibacterial and Antibiofilm Activities Against Bacillus Species

Biotechnology and Bioengineering, EarlyView.
ABSTRACT The exponential rise in antimicrobial resistance has highlighted the urgent need for the development of alternative antibacterial strategies, including phage‐derived and engineered protein agents such as endolysins and artilysins. In this study, we report the rational design, expression, and functional characterization of novel artilysins ...
Farhat Ansari, Tarushi, Vandan Nagar
wiley   +1 more source

Parental Exposure to Nanoplastics and Graphene Oxide Induces Transgenerational Toxicity in Caenorhabditis elegans

Journal of Applied Toxicology, EarlyView.
ABSTRACT Environmental pollution by emerging contaminants such as nanoplastics (NPs) and graphene oxide (GO) represents a growing threat to global health and ecosystems. This study investigated the effects of parental exposure, both isolated and combined, to 100 μg/L NPs (polystyrene, spherical, 100 nm) and 100 mg/L GO, using Caenorhabditis elegans as ...
Gabriela Corrêa Soares, Larissa Müller, Suamy Machado Cruz, Andy Taipe Huisa, Danilo Roberto Carvalho Ferreira, Clascídia Aparecida Furtado, Juliane Ventura‐Lima   +6 more
wiley   +1 more source

Structural and Biochemical Characterization of the Diaminopimelate Epimerase DapF From Pseudomonas aeruginosa PA14

Proteins: Structure, Function, and Bioinformatics, EarlyView.
ABSTRACT The emergence of antibiotic resistance in bacteria is a major threat to global public health. To combat increasingly drug‐resistant bacteria like Pseudomonas aeruginosa, new targets for pharmaceuticals need to be explored. One such potential target for P.
Philipp Schneider, Claudia Hanko, Konrad Büssow, Stefan Schmelz, Wulf Blankenfeldt   +4 more
wiley   +1 more source

FoldAffinity: binding affinities from nDSF experiments

Scientific Reports, 2021
Differential scanning fluorimetry (DSF) using the inherent fluorescence of proteins (nDSF) is a popular technique to evaluate thermal protein stability in different conditions (e.g. buffer, pH).
Stephan Niebling, Osvaldo Burastero, Jérôme Bürgi, Christian Günther, Lucas A. Defelipe, Simon Sander, Ellen Gattkowski, Raghavendra Anjanappa, Matthias Wilmanns, Sebastian Springer, Henning Tidow, María García-Alai   +11 more
doaj   +1 more source