Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/s00280-008-0764-0 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties.
Eur J Med Chem
December 2024
School of Pharmacy and Food Engineering, Wuyi University, 529020, Jiangmen, China; Department of Chemistry, University of Liverpool, L69 7ZD, Liverpool, UK. Electronic address:
Aryl quinolone derivatives can target the cytochrome bc complex of Plasmodium falciparum, exhibiting excellent in vitro and in vivo antimalarial activity. However, their clinical development has been hindered due to their poor aqueous solubility profiles. In this study, a series of bioisosteres containing saturated heterocycles fused to a 4-pyridone ring were designed to replace the inherently poorly soluble quinolone core in antimalarial quinolones with the aim to reduce π-π stacking interactions in the crystal packing solid state, and a synthetic route was developed to prepare these alternative core derivatives.
View Article and Find Full Text PDFComparative immunogenicity assessment of biosimilar natalizumab to its reference medicine: a matching immunogenicity profile.
Front Immunol
January 2025
Polpharma Biologics S.A., Gdansk, Poland.
Background: Biosimilar natalizumab (biosim-NTZ) is the first biosimilar monoclonal antibody of reference natalizumab (ref-NTZ) for treatment of relapsing forms of multiple sclerosis (MS). Within the totality of evidence for demonstration of biosimilarity, immunogenicity assessments were performed in healthy subjects and patients with relapsing-remitting MS (RRMS) to confirm a matching immunogenicity profile between biosim-NTZ and ref-NTZ.
Methods: Immunogenicity of biosim-NTZ versus ref-NTZ was evaluated in two pivotal clinical studies.
Discovery and clinical translation of ceperognastat, an O-GlcNAcase (OGA) inhibitor, for the treatment of Alzheimer's disease.
Alzheimers Dement (N Y)
December 2024
Eli Lilly and Company Indianapolis Indiana USA.
Introduction: The aggregation and spread of hyperphosphorylated, pathological tau in the human brain is hypothesized to play a key role in Alzheimer's disease (AD) as well as other neurogenerative tauopathies. O-GlcNAcylation, an important post-translational modification of tau and many other proteins, is significantly decreased in brain tissue of AD patients relative to healthy controls. Increased tau O-GlcNAcylation has been shown to reduce tau pathology in mouse in vivo tauopathy models.
View Article and Find Full Text PDFPiperine-loaded mesoporous silica nanoparticles as a promising strategy for targeting Echinococcus granulosus protoscoleces.
Sci Rep
January 2025
Department of Parasitology and Mycology, School of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran.
Medical and surgical treatments for cystic echinococcosis (CE) are challenged by various complications. This study evaluates in vitro protoscolicidal activity of piperine-loaded mesoporous silica nanoparticles (PIP-MSNs) against protoscoleces of Echinococcus granulosus. MSNs were prepared by adding tetraethyl orthosilicate to cetyltrimethylammonium bromide and NaOH, and then loaded with PIP.
View Article and Find Full Text PDFComplement factor H targeting antibody GT103 in refractory non-small cell lung cancer: a phase 1b dose escalation trial.
Nat Commun
January 2025
Grid Therapeutics, Durham, NC, USA.
GT103 is a first-in-class, fully human, IgG3 monoclonal antibody targeting complement factor H that kills tumor cells and promotes anti-cancer immunity in preclinical models. We conducted a first-in-human phase 1b study dose escalation trial of GT103 in refractory non-small cell lung cancer to assess the safety of GT103 (NCT04314089). Dose escalation was performed using a "3 + 3" schema with primary objectives of determining safety, tolerability, PK profile and maximum tolerated dose (MTD) of GT103.
View Article and Find Full Text PDFWant 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!