Hesperadin, an established human Aurora B inhibitor, was tested against cultures of and and was identified to be a potent proliferation inhibitor. A series of analogs was designed and tested to establish the initial structure-activity relationships for each parasite. In this study, we identified multiple non-toxic compounds with high potency against and with good selectivity. These compounds may represent an opportunity for continued optimization.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4045489PMC
http://dx.doi.org/10.1039/C4MD00045EDOI Listing

Publication Analysis

Top Keywords

human aurora
8
repurposing human
4
aurora kinase
4
kinase inhibitors
4
inhibitors leads
4
leads anti-protozoan
4
anti-protozoan drug
4
drug discovery
4
discovery hesperadin
4
hesperadin established
4

Similar Publications

Long-Term Impact of an Online Physician Group-Coaching Program to Improve Burnout and Self-Compassion in Trainees.

J Healthc Manag

January 2025

Division of Hospital Medicine, Department of Medicine, University of Colorado Anschutz Medical Campus, Aurora, Colorado, and Rocky Mountain Regional VA Medical Center, Aurora, Colorado.

Goal: To evaluate long-term outcomes of Better Together Physician Coaching, a digital life-coaching program to improve resident well-being.

Methods: We performed a secondary analysis of survey data from the pilot program implementation between January 2021 and June 2022. An intention-to-treat analysis was completed for baseline versus post-6 months and baseline versus post-12 months for all outcome measures.

View Article and Find Full Text PDF

Human recombination-activating gene (RAG) deficiency can manifest with distinct clinical and immunological phenotypes. By applying a multiomics approach to a large group of -mutated patients, we aimed at characterizing the immunopathology associated with each phenotype. Although defective T and B cell development is common to all phenotypes, patients with hypomorphic variants can generate T and B cells with signatures of immune dysregulation and produce autoantibodies to a broad range of self-antigens, including type I interferons.

View Article and Find Full Text PDF

Background And Objectives: Salivary glands proteins but not glycoconjugates have been previously studied in mosquito vectors of human diseases. Glycoconjugates from salivary gland-derived proteins from human-feeding tick vectors can elicit hypersensitivity reactions which may also occur with mosquito bites. Protein glycoconjugate in salivary glands of the principal arboviral vector Aedes aegypti and the rapidly spreading malaria vector Anopheles stephensi were therefore investigated.

View Article and Find Full Text PDF

Importance: Medicare Advantage (MA) plans are designed to incentivize the use of less expensive drugs through capitated payments, formulary control, and preauthorizations for certain drugs. These conditions may reduce spending on high-cost therapies for conditions such as cancer, a condition that is among the most expensive to treat.

Objective: To determine whether patients insured by MA plans receive less high-cost drugs than those insured by traditional Medicare (TM).

View Article and Find Full Text PDF

Purpose: Uncorrected visual impairment (VI) significantly impacts life quality and exacerbates age-related health issues. Social determinants of health (SDOH) are associated with uncorrected VI, but quantitative evidence is limited. This study investigated the link between SDOH and uncorrected VI among aging adults to identify disparities and improve vision care.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!