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Carmaphycin B-Based Proteasome Inhibitors to Treat Human African Trypanosomiasis: Structure-Activity Relationship and Efficacy.
ACS Infect Dis
December 2024
Center for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, 9500 Gilman Drive, La Jolla, California 92093, United States.
The proteasome is essential for eukaryotic cell proteostasis, and inhibitors of the 20S proteasome are progressing preclinically and clinically as antiparasitics. We screened, the causative agent of human and animal African trypanosomiasis, with a set of 27 carmaphycin B analogs, irreversible epoxyketone inhibitors that were originally developed to inhibit the20S (Pf20S). The structure-activity relationship was distinct from that of the human c20S antitarget by the acceptance of d-amino acids at the P3 position of the peptidyl backbone to yield compounds with greatly decreased toxicity to human cells.
View Article and Find Full Text PDFSulfamoylated Estradiol Analogs Targeting the Actin and Microtubule Cytoskeletons Demonstrate Anti-Cancer Properties In Vitro and In Ovo.
Cancers (Basel)
August 2024
Department of Physiology, School of Medicine, Faculty of Health Sciences, University of Pretoria, Pretoria 0028, South Africa.
The microtubule-disrupting agent 2-methoxyestradiol (2-ME) displays anti-tumor and anti-angiogenic properties, but its clinical development is halted due to poor pharmacokinetics. We therefore designed two 2-ME analogs in silico-an ESE-15-one and an ESE-16 one-with improved pharmacological properties. We investigated the effects of these compounds on the cytoskeleton in vitro, and their anti-angiogenic and anti-metastatic properties in ovo.
View Article and Find Full Text PDFHandle with Care: Transformative Learning as Pedagogy in an Under-Resourced Health Care Context.
Teach Learn Med
April 2024
Ukwanda Centre for Rural Health, Department of Global Health, Faculty of Medicine and Health Sciences, Stellenbosch University, Cape Town, South Africa.
A significant component of health professions education is focussed on students' exposure to the social determinants of health and the challenges that patients within the health care system face. An appropriate way to provide such exposure is through distributed clinical training. This usually entails students training in smaller groups along the continuum of care, away from tertiary academic hospitals.
View Article and Find Full Text PDFInvestigating the 2016 surge in firearm violence in Illinois, USA, through community-based organisations: a qualitative study.
Inj Prev
November 2024
Department of Surgery, Northwestern University Feinberg School of Medicine, Chicago, Illinois, USA
Background: Illinois experienced a historic firearm violence surge in 2016 with a decline to baseline rates in 2018. This study aimed to understand this 2016 surge through the direct accounts of violence prevention community-based organisations (CBOs) in Illinois.
Methods: We conducted semistructured interviews with 20 representatives from 13 CBOs from the south and west sides of greater Chicago metropolitan area.
Roles of the Red List of Ecosystems in the Kunming-Montreal Global Biodiversity Framework.
Nat Ecol Evol
April 2024
CORDIO East Africa, Mombasa, Kenya.
The Kunming-Montreal Global Biodiversity Framework (GBF) of the UN Convention on Biological Diversity set the agenda for global aspirations and action to reverse biodiversity loss. The GBF includes an explicit goal for maintaining and restoring biodiversity, encompassing ecosystems, species and genetic diversity (goal A), targets for ecosystem protection and restoration and headline indicators to track progress and guide action. One of the headline indicators is the Red List of Ecosystems, the global standard for ecosystem risk assessment.
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