A series of α7 nicotinic acetylcholine receptor full-agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Systematic exploration of the structure-activity relationships for both α7 potency and selectivity with respect to interaction with the hERG channel are described. Further profiling led to the identification of compound 22, a potent full agonist showing efficacy in the novel object recognition model of cognition enhancement.
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http://dx.doi.org/10.1016/j.bmcl.2012.03.040 | DOI Listing |
Invest Ophthalmol Vis Sci
January 2025
Eye Institute, Affiliated Hospital of Nantong University, Medical School of Nantong University, Nantong, Jiangsu, China.
Purpose: To investigate potential modes of programmed cell death in the lens epithelial cells (LECs) of patients with early age-related cortical cataract (ARCC) and to explore early-stage intervention strategies.
Methods: Anterior lens capsules were collected from early ARCC patients for comprehensive analysis. Ultrastructural examination of LECs was performed using transmission electron microscopy.
Ann Hematol
January 2025
Department of Medicine, School of Clinical Medicine, LKS Faculty of Medicine, the University of Hong Kong, Hong Kong, China.
Polycythemia vera (PV) is characterized by clonal hematopoietic stem or progenitor cells with constitutively active somatic mutation(s) in the Janus kinase 2 gene. Phlebotomy (Phl) and aspirin are often used alone for low-risk PV patients. However, data from the Low-PV study demonstrated that Phl and aspirin may not be adequate for patients.
View Article and Find Full Text PDFBiomater Sci
January 2025
Department of Biological Sciences and Engineering Indian Institute of Technology, Palaj, Gandhinagar 382355, India.
The application of nanotechnology in medical biology has seen a significant rise in recent years because of the introduction of novel tools that include supramolecular systems, complexes, and composites. Dendrimers are one of the remarkable examples of such tools. These spherical, regularly branching structures with enhanced cell compatibility and bioavailability have shown to be an excellent option for gene or drug administration.
View Article and Find Full Text PDFCancer Biother Radiopharm
January 2025
Advanced Innovative Partners, Inc. (AIP), Miami, Florida, USA.
Integrin antagonist complex (IAC), a novel αvβ3 integrin antagonist peptidomimetic, has emerged as a promising agent for molecular imaging of tumor angiogenesis. This study evaluates the biodistribution and clinical efficacy of [Ga]Ga-DOTAGA-IAC PET/CT in detecting radioiodine-refractory differentiated thyroid carcinoma (RAIR-DTC), comparing its diagnostic performance with [F]F-FDG PET/CT. In this prospective pilot study, RAIR-DTC patients underwent whole-body imaging with [F] F-FDG PET/CT, followed by [Ga]Ga-DOTAGA-IAC PET/CT.
View Article and Find Full Text PDFDalton Trans
January 2025
Institute of Biopharmaceutical Research, Liaocheng University, Liaocheng 252059, P. R. China.
Pt(IV) complexes as prodrugs of Pt(II) drugs exhibit numerous advantages such as enhanced stability, reduced toxicity, increased oral bioavailability, and efficacy in overcoming the drug resistance of Pt(II) compounds, which underscore their significant potential in the advancement of novel Pt anticancer agents. Furthermore, protective autophagy is pivotal in sustaining tumor cell homeostasis and modulating the tumor microenvironment (TME), thereby representing a critical target for the development of antitumor drugs. Specific inhibition or activation of autophagy during chemotherapy would break the internal homeostasis in the TME and increase antitumor activities.
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