We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the alpha4beta2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was found to have a very similar agonist activity profile to that of cytisine.
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http://dx.doi.org/10.1021/jm051196m | DOI Listing |
Parasit Vectors
January 2025
Department of Veterinary Biosciences, Melbourne Veterinary School, Faculty of Science, The University of Melbourne, Parkville, VIC, 3010, Australia.
Background: Nippostrongylus brasiliensis-a nematode of rodents-is commonly used as a model to study the immunobiology of parasitic nematodes. It is a member of the Strongylida-a large order of socioeconomically important parasitic nematodes of animals. Lipids are known to play essential roles in nematode biology, influencing cellular membranes, energy storage and/or signalling.
View Article and Find Full Text PDFCell Commun Signal
January 2025
Department of Obstetrics and Gynecology, Peking University Third Hospital, Beijing, 100191, China.
Background: Ovarian cancer (OC), particularly high-grade serous ovarian carcinoma (HGSOC), is the leading cause of mortality from gynecological malignancies worldwide. Despite the initial effectiveness of treatment, acquired resistance to poly(ADP-ribose) polymerase inhibitors (PARPis) represents a major challenge for the clinical management of HGSOC, highlighting the necessity for the development of novel therapeutic strategies. This study investigated the role of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3), a pivotal regulator of glycolysis, in PARPi resistance and explored its potential as a therapeutic target to overcome PARPi resistance.
View Article and Find Full Text PDFReprod Biol Endocrinol
January 2025
Department of Molecular and Developmental Medicine, Siena University, Siena, 53100, Italy.
Background: Endocrine-disrupting chemicals (EDCs) interfere with the endocrine system and negatively impact reproductive health. Biochanin A (BCA), an isoflavone with anti-inflammatory and estrogen-like properties, has been identified as one such EDC. This study investigates the effects of BCA on transcription, metabolism, and hormone regulation in primary human granulosa cells (GCs), with a specific focus on the activation of bitter taste receptors (TAS2Rs).
View Article and Find Full Text PDFJ Transl Med
January 2025
Medical School of Nanjing University, Nanjing, 210093, China.
Background: Clear cell renal cell carcinoma (ccRCC) has a high incidence rate and poor prognosis, and currently lacks effective therapies. Recently, peptide-based drugs have shown promise in cancer treatment. In this research, a new endogenous peptide called CBDP1 was discovered in ccRCC and its potential anti-cancer properties were examined.
View Article and Find Full Text PDFBMC Plant Biol
January 2025
Department of Integrative Agriculture, College of Agriculture and Veterinary Medicine, United Arab Emirates University, P.O. Box 15551, Al Ain, Abu Dhabi, United Arab Emirates.
This study investigated the effects of non-thermal atmospheric plasma (NTAP) treatment on the growth, chemical composition, and biological activity of geranium (Pelargonium graveolens L'Herit) leaves. NTAP was applied at a frequency of 13.56 MHz, exposure time of 15 s, discharge temperature of 25 °C, and power levels (T1 = 50, T2 = 80, and T3 = 120 W).
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