Results 51 to 60 of about 29,245 (221)

Identification of a Nonribosomal Peptide Analog With Activity Against Multiple Gram‐Positive Bacteria via a Synthetic Bioinformatic Natural Product Discovery Approach

open access: yesAdvanced Science, EarlyView.
The genome of Rhodococcus erythropolis D‐1 was analyzed by bioinformatic tools to mine a novel nonribosomal peptide synthetase (NRPS) gene cluster. A nonribosomal peptide analog ZURJC5 associated with the NRPS was chemically synthesized. Through structure‐activity relationship studies, ZURJC28 was ultimately obtained and showed antibacterial activity ...
Keyi Chen   +9 more
wiley   +1 more source

Review and Current Perspectives on DNA Topoisomerase I and II Enzymes of Fungi as Study Models for the Development of New Antifungal Drugs

open access: yesJournal of Fungi
Fungal infections represent a growing public health problem, mainly stemming from two phenomena. Firstly, certain diseases (e.g., AIDS and COVID-19) have emerged that weaken the immune system, leaving patients susceptible to opportunistic pathogens ...
Dulce Andrade-Pavón   +2 more
doaj   +1 more source

Computational screening of chalcones acting against topoisomerase IIα and their cytotoxicity towards cancer cell lines

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2019
Targeted cancer therapy has become one of the high potential cancer treatments. Human topoisomerase II (hTopoII), which catalyzes the cleavage and rejoining of double-stranded DNA, is an important molecular target for the development of novel cancer ...
Kanyani Sangpheak   +11 more
doaj   +1 more source

Accelerating Primary Screening of USP8 Inhibitors from Drug Repurposing Databases with Tree‐Based Machine Learning

open access: yesAdvanced Intelligent Discovery, EarlyView.
This study introduces a tree‐based machine learning approach to accelerate USP8 inhibitor discovery. The best‐performing model identified 100 high‐confidence repurposable compounds, half already approved or in clinical trials, and uncovered novel scaffolds not previously studied. These findings offer a solid foundation for rapid experimental follow‐up,
Yik Kwong Ng   +4 more
wiley   +1 more source

Antibacterial activity of a DNA topoisomerase I inhibitor versus fluoroquinolones in Streptococcus pneumoniae.

open access: yesPLoS ONE, 2020
The DNA topoisomerase complement of Streptococcus pneumoniae is constituted by two type II enzymes (topoisomerase IV and gyrase), and a single type I enzyme (topoisomerase I).
Myriam V Valenzuela   +5 more
doaj   +1 more source

Integrated Clinical and Proteomic Profiling of CD19 Chimeric Antigen Receptor T Cell Therapy in Progressive Systemic Sclerosis

open access: yesArthritis &Rheumatology, EarlyView.
Objective To characterize the clinical, immunologic, and proteomic changes associated with CD19 chimeric antigen receptor T cell therapy in patients with progressive systemic sclerosis (SSc). Methods Patients with progressive SSc received CD19 chimeric antigen receptor (CAR)‐T cell therapy and were observed longitudinally for safety, clinical efficacy,
Chenhan Jia   +16 more
wiley   +1 more source

Expert Perspectives: Defining and Managing Progressive Pulmonary Fibrosis in Systemic Sclerosis

open access: yesArthritis &Rheumatology, EarlyView.
Systemic sclerosis–associated interstitial lung disease (SSc‐ILD) is one of the leading causes of morbidity and mortality in SSc, affecting up to three‐quarters of patients. The disease course is highly heterogeneous, ranging from indolent, nonprogressive forms to rapidly progressive pulmonary fibrosis (PPF).
Devis Benfaremo   +7 more
wiley   +1 more source

Structural and functional insights into the T-even type bacteriophage topoisomerase II

open access: yesNature Communications
T-even type bacteriophages are virulent phages commonly used as model organisms, playing a crucial role in understanding various biological processes. One such process involves the regulation of DNA topology during phage replication upon host infection ...
Yuhui Xin   +6 more
doaj   +1 more source

DNA-PK inhibitor peposertib enhances p53-dependent cytotoxicity of DNA double-strand break inducing therapy in acute leukemia

open access: yesScientific Reports, 2021
Peposertib (M3814) is a potent and selective DNA-PK inhibitor in early clinical development. It effectively blocks non-homologous end-joining repair of DNA double-strand breaks (DSB) and strongly potentiates the antitumor effect of ionizing radiation (IR)
Eric Haines   +9 more
doaj   +1 more source

Effect of developmental changes on pharmacokinetics of drugs used in the treatment of infant acute lymphoblastic leukaemia—A comprehensive review

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
While the event‐free survival (EFS) of children treated for acute lymphoblastic leukaemia (ALL) has improved greatly in the last decades, the EFS for patients diagnosed with ALL before the age of one is still under 50%. This outcome further decreases when infants have a rearrangement in the gene encoding histone‐lysine N‐methyltransferase 2A (KMT2A ...
Tirsa de Kluis   +5 more
wiley   +1 more source

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