This article summarizes molecular properties of the high-affinity choline transporter (CHT1) with reference to the historical background focusing studies performed in laboratories of the author. CHT1 is present on the presynaptic terminal of cholinergic neurons, and takes up choline which is the precursor of acetylcholine. The Na(+)-dependent uptake of choline by CHT1 is the rate-limiting step for synthesis of acetylcholine. CHT1 is the integral membrane protein with 13 transmembrane segments, belongs to the Na(+)/glucose co-transporter family (SLC5), and has 20-25% homology with members of this family. A single nucleotide polymorphism (SNP) for human CHT1 has been identified, which has a replacement from isoleucine to valine in the third transmembrane segment and shows the choline uptake activity of 50-60% as much as that of wild-type CHT1. The proportion of this SNP is high among Asians. Possible importance of choline diet for those with this SNP was discussed.
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http://dx.doi.org/10.1093/jb/mvu047 | DOI Listing |
Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi
January 2025
Department of Integrated Traditional Chinese and Western Medicine, Shandong First Medical University Affiliated Cancer Hospital, Jinan 250117, China. *Corresponding author, E-mail:
It has been popular and challenging to undertake researches on the delay of acquired resistance of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI). As key cells for tumor initiation, cancer stem cells (CSC) play an important role in the process of resistance to EGFR-TKI. Although preliminary studies found that traditional Chinese medicine (TCM) could inhibit CSC properties and delay EGFR-TKI resistance, the specific molecular mechanism remains unclear.
View Article and Find Full Text PDFMol Divers
January 2025
School of Sciences, China Pharmaceutical University, 639 Longmian Avenue, Nanjing, 211198, People's Republic of China.
The p53 protein is regarded as the "Guardian of the Genome," but its mutation is tumor progression and present in more than half of malignant tumors. The pro-metastatic property of mutant p53 makes a strong argument for targeting mutant p53 with new therapeutic strategies. However, mutant p53 was considered as a challenging target for drug discovery due to the lack of small molecular binding pockets.
View Article and Find Full Text PDFSci Rep
January 2025
Chemistry Department, School of Advanced Sciences, Vellore Institute of Technology-Chennai campus, Chennai, 600127, India.
Nickel complexes are a potential candidate for antibacterial and antifungal activity. A new Ni (II) complex, bis(2-methoxy-6-{[(2-methylpropyl)imino]methyl}phenolato)nickel (II) (2), was synthesised by reacting, bis(3-methoxy-salicylaldehyde)nickel (II) (1) with isobutylamine. It was characterised by single crystal X-ray diffraction (ScXRD), UV-Vis, NMR, IR, mass spectrometry, and thermogravimetry (TG) to study its structure and physico-chemical properties.
View Article and Find Full Text PDFNat Commun
January 2025
State Key Laboratory of Integrated Optoelectronics, College of Electronic Science and Engineering, Jilin University, Changchun, P. R. China.
Photoluminescence is one of the most intriguing properties of metal nanoclusters derived from their molecular-like electronic structure, however, achieving high photoluminescence quantum yield (PLQY) of metal core-dictated fluorescence remains a formidable challenge. Here, we report efficient suppression of the total structural vibrations and rotations, and management of the pathways and rates of the electron transfer dynamics to boost a near-unity absolute PLQY, by decorating progressive addition of cations. Specifically, with the sequential addition of Zn, Ag, and Tb into the 3-mercaptopropionic acids capped Au nanoclusters (NCs), the low-frequency vibration of the metal core progressively decreases from 144.
View Article and Find Full Text PDFEur J Pharmacol
January 2025
Department of Pharmacy, Abdul Wali Khan University Mardan, Mardan-23200, Pakistan; Department of Pharmacy, Korea University, Sejong 20019, South Korea. Electronic address:
The study investigated the anxiolytic, antidepressant, sedative/hypnotic and in silico molecular docking properties of the synthetic ephedrine-based derivative of thiourea, 3-benzothioyl-1-(3-hydroxy-3-phenyl-3-propyl)-1-methylthiourea. Safety profile of the compound at various doses was determined in an acute toxicity test. Results showed significant anti-anxiety effects of the compound in all mice studies.
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